Ntshav qab zib mellitus qhia

Hauv tsab xov xwm, peb xav txog cov lus qhia rau kev siv, tus nqi thiab cov qauv ntawm Sitagliptin.

Nws ua raws li phosphate monohydrate. Daim ntawv tso tawm yog cov ntsiav tshuaj nyias zaj duab xis.

Cov tshuaj muaj qhov sib txawv tseem ceeb ntawm pharmacological kev txiav txim siab thiab cov qauv hauv tshuaj lom neeg los ntawm cov tshuaj analogues, nrog rau cov derivatives ntawm alpha-glycosidase inhibitors, biguanides thiab sulfonylureas.

Kev txwv tsis pub DPP 4 los ntawm txhais tau tias "Sitagliptin" ua rau muaj kev nce siab ntawm cov tshuaj hormones HIP thiab GLP-1. Cov tshuaj hormones no yog nyob ntawm incretins. Lawv qhov zais cia ua nyob rau hauv cov hnyuv.

Raws li kev noj mov, qhov siab ntawm cov tshuaj hormones no nce ntxiv. Tus incretins yog ib feem ntawm cov kev tsim hluav taws xob uas tswj cov piam thaj hauv tsev hauv tib neeg lub cev. Cov lus piv txwv ntawm Sitagliptin yuav tsum raug xaiv los ntawm kws kho mob.

Cov yam ntxwv ntawm pharmacokinetics

Cov tshuaj yog nqus ntawm tus nqi siab tom qab nws siv los ntawm tus neeg mob. Cov cuab yeej no muaj kev ntsuas zoo ntawm kev paub txog ntawm 87%. Kev noj ntawm cov rog rog tsis cuam tshuam loj heev ntawm pharmacological kinetics ntawm cov tshuaj.

Cov tshuaj hloov tawm yog ib feem ntawm cov zis tsis hloov pauv. Tom qab kev txais tos nres, nws tawm hauv cov zis thaum lub limtiam nrog zis (87%) thiab quav (13%).

Qhov no tau lees paub los ntawm cov lus qhia rau kev siv nrog Sitagliptin. Cov tshuaj ntawm cov tshuaj yog qhov zoo rau ntau.

Kev qhia rau kev siv tshuaj

Cov tshuaj yog siv rau hauv kev siv ntawm monotherapy, yog tias tus neeg mob kuaj mob nrog tus mob ntshav qab zib hom 2 mellitus. Cov tshuaj no raug pom zoo rau kev siv tsis hais txog ntawm cov zaub mov noj. Kev sib xyaw ntawm Sitagliptin thiab Metformin tuaj yeem siv los ua cov kev kho mob nyuaj nyob rau hauv qhov muaj ntawm hom II mob ntshav qab zib mellitus.

Hauv kev sib xyaw nrog Metformin, kev pom zoo ntawm kev siv tshuaj yog 100 mg ib hnub ib zaug.

Yog tias koj plam lub sijhawm ntawm nws txoj kev tswj hwm, koj yuav tsum haus Sitagliptin sai li sai tau. Qhov no vim yog qhov tseeb tias kev siv tshuaj ntawm ob zaug ntawm cov tshuaj tsis tso cai.

Txwv tsis pub haus ib yam tshuaj ntau dua li kev pom zoo hauv cov lus qhia yog txwv tsis pub.

Cov tshuaj ua rau nws tuaj yeem tswj hwm theem ntawm cov suab thaj hauv lub cev, txawm li cas los xij, cov tshuaj no tsis kho ntshav qab zib.

Kev siv cov tshuaj yuav tsum tau ua thaum tus neeg mob zoo, nres kev kho mob tsuas yog tom qab kev pom zoo thiab sab laj ntawm tus kws kho mob uas tuaj koom.

Puas yog Citagliptin puas muaj qee yam analogues? Hais txog nws hauv qab no.

Cov lus qhia rau kev siv tshuaj

"Sitagliptin" yog cov tshuaj uas thev taus zoo heev thaum noj los ntawm tus neeg mob, tsis yog zoo li kev kho mob monotherapy, tab sis raws li ib feem ntawm kev kho mob nrog lwm tus neeg sawv cev nrog hypoglycemic zog.

Qhov txhaj tshuaj tseem ceeb ntawm cov tshuaj tawm tom qab ob lub raum. Txoj kev no ntawm kev tshem tawm cov kev ua si nquag los ntawm tib neeg lub cev xav tau tus kws tshaj lij los saib xyuas kev noj qab haus huv ntawm lub cev no yog tias tus neeg mob tau mob raum tsis ua ntej siv cov tshuaj. Yog tias tsim nyog, cov koob tshuaj tau muab hloov kho. Yog tias muaj daim ntawv me me hauv lub raum tsis ua hauj lwm, kev kho qhov hloov tshuaj tsis raug ua.

Yog tias tus neeg mob tau mob raum tsawg, kev noj tshuaj ntau dua yuav tsum tsis pub ntau tshaj 50 milligram ib hnub.Cov tshuaj tuaj yeem siv tau txhua lub sijhawm, tsis hais txog qhov txheej txheem, xws li lim ntshav.

Thaum cov tshuaj no yog siv los ua ib txoj hauv kev kho mob nyuaj, kom tiv thaiv qhov tshwm sim ntawm cov tshuaj sulfon nyob rau hauv tus neeg mob lub cev, ntau npaum li cas ntawm sulfonylurea derivatives yuav tsum tau ua yuav tsum tau txo.

Kev noj cov tshuaj uas siv yog txiav txim los ntawm tus kws kho mob koom nrog sai li sai tau ua tiav kev soj ntsuam ntawm tus neeg mob lub cev raug mob los ntawm hom mob ntshav qab zib thib ob.

Yog tias muaj kev ua xyem xyav ntawm kev loj hlob ntawm pancreatitis nyob rau hauv tus neeg mob lub cev, nws yog qhov yuav tsum tau tsum tsis txhob siv cov Sitagliptin thiab lwm yam tshuaj uas tuaj yeem tsim kev cuam tshuam ntawm pathology.

Ua ntej siv cov tshuaj, cov kws kho mob tshwj xeeb yuav tsum qhia tus neeg mob txog thawj cov tsos mob tshwm sim ntawm tus mob pancreatitis.

Yog li nws tau hais nyob rau hauv cov lus qhia rau kev siv rau "Sitagliptin." Nqe, xyuas thiab analogues yuav muab rau hauv qab no.

Cov Yuav Tsum Muaj

Kev siv cov tshuaj no tuaj yeem ua rau muaj kev phom sij txog txoj sia, ua mob hnyav rau ntawm daim tawv nqaij ntawm lub cev.

Yog tias cov tshuaj siv tsis raug, nws tuaj yeem ua rau ntau yam kev mob tshwm sim hauv lub cev. Yog tias thawj cov tsos mob ntawm kev ua txhaum cai tshwm sim, koj yuav tsum sab laj nrog tus kws kho mob tshwj xeeb.

Siv cov tshuaj kom nruj raws li cov lus qhia thiab hauv tus nqi raug txiav txim los ntawm tus kws kho mob tuaj koom.

Thaum siv tshuaj yeeb, nws yuav tsum raug coj mus rau hauv tus account tias muaj tag nrho ntau yam ntawm ntau yam contraindications:

• muaj thawj hom mob ntshav qab zib,
• kev tiv thaiv tsis haum
• tus menyuam cov menyuam lub sijhawm,
• mob ketoacidosis,
• pub niam mis
• tus neeg mob lub hnub nyoog qis dua kaum yim xyoo.

Tus nqi thiab cov duab tsis tau qhia nyob rau hauv cov lus qhia rau kev siv nrog Sitagliptin.

Muaj kev phiv ntau

Thaum lub sij hawm siv cov tshuaj nyob rau hauv tib neeg, heev ob peb phiv tuaj yeem tshwm sim. Ntawm lawv yog sau tseg:

• angioedema,
• khaus
• anaphylaxis,
• tes taw mob
• ua pob
• rov qab mob
• daim tawv nqaij vasculitis
• arthralgia
• urticaria
• myalgia
• exfoliative kab mob ntawm daim tawv nqaij, Stevens-Johnson mob,
• mob taub hau
• mob leeg txhaj,
• kev ua haujlwm tsis zoo rau lub raum, qhov tsis muaj txhij txhua ntawm cov khoom hloov hauv no, uas xav tau lim ntshav,
• cem quav
• nasopharyngitis,
• ntuav
• kis ntawm tus kab mob ua pa.

Thaum siv tshuaj, nws yog ib qho tsim nyog kom ua raws nraim li cov lus pom zoo hauv cov lus qhia, koj tsis tuaj yeem noj nws yog tias koj muaj tsawg kawg ib ntawm kev tsis sib haum. Yog tias muaj tshuaj lom lossis noj ntau dhau tshwm sim los ntawm kev siv tshuaj, koj yuav tsum hu rau lub tsheb thauj neeg mob tam sim ntawd, vim tias cov xwm txheej tsis zoo no tuaj yeem ua rau muaj mob muaj mob loj uas tuaj yeem ua rau tuag taus.

Cov hauv paus ntsiab lus thiab cov hau kev rau kev kuaj ntshav qab zib

Txog kev kho mob pob qij txha, peb cov neeg nyeem tau siv DiabeNot siv tau zoo. Pom qhov nrov ntawm cov khoom no, peb tau txiav txim siab muab nws rau koj kom txaus siab.

Kev kuaj mob ntshav qab zib mellitus muaj nyob rau hauv kev ua tiav kev soj ntsuam, dhau qhov kev kuaj mob uas tsim nyog thiab kuaj los ntawm kws kho mob los ntawm tus kws kho mob endocrinologist. Nws feem ntau tsis yooj yim los ua qhov kev kuaj mob no, vim tias ntau tus neeg mob mus rau hauv lub tsev kho mob twb muaj tus kab mob khiav lawm.

Tab sis cov kev tshawb fawb niaj hnub no tuaj yeem paub tsis tsuas yog thaum pib, zais cov theem ntawm cov ntshav qab zib, tab sis kuj tseem muaj qhov mob ua ntej qhov mob no, uas yog hu ua mob ntshav qab zib lossis ua txhaum cai ntawm kev zam rau cov carbohydrates.

Cov chaw soj ntsuam kuaj mob txoj kev

Tus kws kho mob sib sau ua ke, qhia txog cov xwm txheej phom sij, raws roj ntsha, mloog lus tsis txaus siab, tshuaj xyuas tus neeg mob, txiav txim siab nws qhov hnyav.

Cov tsos mob uas tau coj mus rau hauv tus account thaum kuaj ntshav qab zib:

• muaj zog nqhis dej tas mus li - polydipsia,
• ntev li ntawm zis muaj ntau - polyuria,
• yuag yuag nrog kev qab los ntxiv rau - hom mob ntshav qab zib hom 1,
• ceev, qhov hnyav nce - hom rau cov ntshav qab zib hom 2,
• tawm hws, tshwj xeeb yog tom qab noj mov tag,
• kev ua kom tsis muaj zog, nkees,
• khaus heev ntawm daim tawv nqaij uas tsis tuaj yeem txaus siab rau ib qho twg,
• xeev siab, ntuav,
• cov kab mob sib kis, xws li ua mob rau daim tawv, ua pob ntau zaus tawm ntawm qhov ncauj lossis lub paum, thiab lwm yam.

Nws tsis tsim nyog tias ib tus neeg muaj tag nrho cov tsos mob tshwm sim, tab sis yog tias tsawg 2-3 pom tau nyob rau tib lub sijhawm, ces nws tsim nyog mus soj ntsuam ntxiv.

Nws yuav tsum raug sau tseg tias nrog mob ntshav qab zib hom 1, txhua qhov tsos mob tshwm sim sai thiab tus neeg mob tuaj yeem nco lub hnub tim ntawm qhov pib ntawm cov tsos mob, thiab qee tus neeg mob tau dhau los ua tsis xav txog tias lawv xaus rau kev saib xyuas hauv lub xeev muaj ntshav qab zib tsis xeev. Cov neeg mob uas muaj ntshav qab zib hom no feem ntau yog cov neeg muaj hnub nyoog 40-45 xyoo lossis menyuam yaus.

Lub latent chav kawm yog tus yam ntxwv ntau ntawm hom 2 mob ntshav qab zib mellitus, yog li peb yuav sib tham ntxiv txog kev kuaj mob ntawm daim ntawv tshwj xeeb no ntawm kev noj haus uas tsis hnov ​​mob carbohydrate metabolism.

Qhov tseem ceeb rau kev txheeb xyuas tus mob ntshav qab zib hom 2 yog cov muaj pheej hmoo, uas suav nrog:

• hnub nyoog tshaj 40-45 xyoo,
• Mob ntshav qab zib lossis tsis hnov ​​qab cov ntshav qabzib,
• rog dhau, rog dhau (BMI tshaj 25),
• nce ntshav lipid profile,
• ntshav siab, ntshav siab tshaj 140/90 hli RT. Kos duab.
• qoj ib ce tsis muaj dag zog
• Cov poj niam uas lub sijhawm yav dhau los muaj kev paub txog qee cov kev zom cov carbohydrate thaum cev xeeb tub lossis yug tau menyuam yaus uas hnyav dua 4.5 kg,
• polycystic lub zes qe menyuam.

Txhua tus neeg uas muaj hnub nyoog 40-45 xyoos yuav tsum tau kuaj ntshav qab zib ib zaug hauv txhua 3 lub xyoos, thiab cov neeg muaj rog thiab muaj tsawg kawg ntawm cov kev pheej hmoo - ib xyoos ib zaug.

Hauv kev tshwm sim ntawm tus mob ntshav qab zib hom 2, keeb kwm muaj txoj haujlwm tseem ceeb. Qhov muaj los ntawm tus kab mob no hauv cov neeg txheeb ze yuav muaj feem ntau tsim cov ntshav qab zib hom 2. Txheeb cais hais tias ib tus neeg uas muaj niam txiv uas mob ntshav qab zib yuav tau mob ntxiv rau 40% tus neeg.

Dosage daim ntawv

Zaj duab xis-cov ntsiav tshuaj 25 mg, 50 mg lossis 100 mg

Ib ntsiav tshuaj muaj

cov tshuaj heev - sitagliptin phosphate monohydrate 32.13 mg, 64.25 mg lossis 128.5 mg (sib npaug rau 25 mg, 50 mg lossis 100 mg ntawm sitagliptin),

zam txim: microcrystalline cellulose, calcium hydrogen phosphate (anhydrous), tsis tuaj yeem, croscarmellose sodium, magnesium stearate, sodium stearyl fumarate,

zaj duab xis txheej muaj pes tsawg leeg Opadray® II Paj Yeeb 85F97191 (rau qhov tau txais koob tshuaj 25 mg), Opadray® II Lub teeb beige 85F17498 (rau qhov ntsuas ntau npaum li 50 mg), Opadray® II Beige 85F17438 (rau qhov tau txais 100 mg): polyvinyl cawv, titanium dioxide E171, macrogol / polyethylene glycol 3350, talc, hlau (III) oxide daj E172, hlau (III) oxide liab E172.

25 mg ntsiav tshuaj - Cov ntsiav tshuaj yog puag ncig, biconvex, them nrog xaum zaj duab xis sheath, sau nrog "221" ntawm ib sab thiab du ntawm lwm yam.

50 mg ntsiav tshuaj - Cov ntsiav tshuaj yog puag ncig, biconvex, coated nrog ib zaj duab xis membrane ntawm lub teeb beige xim, nrog engraving "112" ntawm ib sab thiab du ntawm lwm yam.

100 mg ntsiav tshuaj - Cov ntsiav tshuaj zoo li tus kheej, biconvex, npog nrog lub plhaub zaj duab xis plhaub, nrog lub ntsej muag "277" ntawm ib sab thiab du rau lwm yam.

Kev sim tshawb fawb txoj kev

Rau kev txheeb xyuas tus kab mob ntshav qab zib hom 2, ntau hom kev kuaj tau siv. Qee qhov kev siv yog siv los ua kev soj ntsuam. Kev kuaj mob yog ib txoj kev kawm tshawb nrhiav qhov tseeb ntawm tus mob thaum ntxov, ua los ntawm coob tus neeg uas feem ntau tsis muaj cov tsos mob tshwm sim ntawm tus kab mob. Cov qauv kev ntseeg siab tshaj plaws rau kev kuaj ntshav qab zib yog kev txiav txim siab ntawm glycosylated hemoglobin.

Glycosylated hemoglobin yog erythrocyte hemoglobin uas tau txuas cov suab thaj hauv ib lub cev.Qhov qib ntawm glycosylation nyob ntawm kev mloog ntawm cov piam thaj hauv cov ntshav, uas nyob hauv erythrocytes tseem tsis tau hloov pauv thaum lawv lub neej peb lub hlis. Cov peev xwm ntawm glycosylated hemoglobin yog 4.5-6.5% ntawm tag nrho cov nyiaj ntawm hemoglobin.

Hauv qhov no, txhua lub sijhawm, feem pua ​​ntawm cov hemoglobin qhia txog thaj tsam cov ntshav qab zib hauv nruab nrab ntawm tus neeg mob rau 120 hnub ua ntej kev tshawb fawb. Qhov no pab tsis tsuas qhia tawm cov mob ntshav qab zib hom 2 mob ntshav qab zib mellitus, tab sis kuj tseem txiav txim siab txog kev tiv thaiv kab mob thiab ntsuas qhov tsis txaus ntawm kev kho.

Cov hau kev rau kuaj ntshav qab zib tau muab faib ua cov theem pib thiab ntxiv.

Cov hau kev tseem ceeb muaj li hauv qab no:

1. kev txiav txim siab ntawm cov ntshav qab zib theem, nqa tawm: ntawm lub plab khoob, 2 teev tom qab noj mov, ua ntej yuav mus pw,
2. kev tshawb fawb txog qhov nyiaj glycosylated hemoglobin,
3. kuaj ntshav qabzib - thaum kawm, tus neeg mob haus ib qho txiaj ntsig ntawm cov piam thaj thiab pub ntshav los ntawm tus ntiv tes ua ntej thiab 2 teev tom qab kev kuaj mob cocktail. Qhov kev ntsuam xyuas no tau pab qhia meej txog hom kev mob uas tsis txaus siab ntawm cov carbohydrate metabolism, tso cai rau koj paub qhov txawv cov ntshav qab zib los ntawm ntshav qab zib muaj tseeb,
4. kev txiav txim siab ntawm kev muaj suab thaj hauv cov zis - cov piam thaj nkag hauv cov zis thaum nws cov concentration ntau dua 8-9 kev txiav txim siab,
5. kev tsom xam ntawm theem ntawm fructosamine - tso cai rau koj kom pom cov qib qab zib hauv 3 lub lis piam dhau los,
6. cov kev kawm txog kev saib xyuas ntawm ketones hauv cov zis lossis ntshav - txiav txim siab qhov pib mob ntshav qab zib lossis nws cov kev mob tshwm sim.

Cov hau kev txuas ntxiv tau raug hu ua uas txiav txim rau cov ntsuas hauv qab no:

1. ntshav insulin - los txiav txim qhov rhiab ntawm lub cev nqaij mus rau insulin,
2. autoantibodies rau hlwb pancreatic thiab insulin - nthuav tawm lub autoimmune ua rau ntshav qab zib,
3. proinsulin - qhia txog kev ua haujlwm ntawm lub txiav,
4. ghrelin, adiponectin, leptin, resistin - qhov ntsuas ntawm keeb kwm ntawm keeb kwm adipose ntaub so ntswg, kev txheeb xyuas ntawm cov ua rau kev rog,
5. C-peptide - tso cai rau koj kom paub qhov ntsuas kev noj tshuaj insulin los ntawm cov hlwb,
6. HLA kev ntaus - siv los txheeb xyuas cov kab mob pathologies.

Cov hau kev no tau muab rau thaum muaj kev nyuaj thaum kuaj tus kab mob hauv qee cov neeg mob, ntxiv rau xaiv txoj kev kho. Kev teem sij hawm ntawm cov hau kev ntxiv yog txiav txim siab tsuas yog los ntawm tus kws kho mob.

Cov chaw muag tshuaj

Cov Tshuaj Pharmacokinetics

Tom qab qhov ncauj tswj hwm ntawm 100 mg ntawm sitagliptin, qhov siab tshaj plaws (Cmax) yog ua tiav nyob rau hauv thaj tsam li 1 mus rau 4 teev txij li lub sijhawm saib xyuas. Thaj chaw hauv qab cov phiaj xwm concentration-sijhawm (AUC) nce ntxiv rau qhov sib npaug ntawm cov koob tshuaj thiab qhov ntau thiab tsawg rau 8.52 μmol · teev thaum noj 100 mg ntawm qhov ncauj, Cmax yog 950 nmol, ib nrab-lub neej (T1 / 2) yog 12.4 teev. Lub plasma AUC ntawm sitagliptin nce ntxiv kwv yees li 14% tom qab kev noj tshuaj ntxiv 100 mg ntawm cov tshuaj thaum nce mus txog rau lub xeev qhov sib luag tom qab txhaj thawj zaug. Qhov sib txuam ntawm cov leeg- thiab ib leeg ntawm AUC ua haujlwm sib txawv ntawm sitagliptin yog qhov tseem ceeb (5.8% thiab 15.1%). Cov tshuaj pharmacokinetics ntawm sitagliptin feem ntau hauv cov tib neeg muaj kev noj qab haus huv thiab cov neeg mob ntshav qab zib hom 2 zoo sib xws. Kev Tsis Txaus Siab Qhov tsis ncaj ncees ntawm bioavailability ntawm sitagliptin yog kwv yees li 87%. Txij li thaum ua kev sib xyaw ua ke ntawm sitagliptin thiab cov zaub mov muaj roj tsis muaj kev cuam tshuam rau cov pharmacokinetics, cov tshuaj yuav raug kho tsis hais cov pluas noj.

Kev xa Khoom. Qhov ntim nruab nrab ntawm kev faib tawm hauv qhov sib npaug tom qab noj ib koob ntawm 100 mg ntawm sitagliptin yog kwv yees li 198 L. Qhov feem ntawm sitagliptin uas khi rau cov ntshav muaj protein ntau yog qhov qis, ntawm 38%.

Kev zom zaub mov. Tsuas yog ib feem me me ntawm cov tshuaj tau txais hauv lub cev yog metabolized. Kwv yees li 79% ntawm cov sitagliptin yog cov tsis hloov pauv hauv cov zis. Kwv yees li ntawm 16% ntawm cov tshuaj tau tawm hauv cov qauv ntawm nws cov metabolites.Ib co kua nplaum ntawm rau (6) metabolites tau pom tias tej zaum tsis cuam tshuam rau cov kev ua ntawm inhibitory nyhuv ntawm sitagliptin DPP-4 hauv ntshav. Thawj qhov enzyme uas tau koom nrog qhov kev siv metabolism tsawg ntawm sitagliptin tau pom tias CYP3A4 muaj feem cuam tshuam nrog CYP2C8.

Chaw Sau Ntawv. Tom qab qhov ncauj tswj hwm ntawm 14C-daim ntawv qhia sitagliptin los ntawm cov neeg ua haujlwm pab noj qab haus huv, 100% cov tshuaj tau tawm hauv 1 lub lis piam nrog quav thiab tso zis ntawm 13% thiab 87%, feem. Qhov kev tshem tawm hauv nruab nrab ib nrab ntawm lub neej rau kev tswj hwm qhov ncauj ntawm ib koob ntawm 100 mg ntawm sitagliptin yog kwv yees li 12.4 teev; kev tshem lub raum yog kwv yees li 350 ml / min.

Kev nthuav dav ntawm sitagliptin yog nqa tawm feem ntau los ntawm kev tawm los ntawm lub raum los ntawm kev ua haujlwm ntawm cov tubular muaj kev zais cia. Sitagliptin yog cov txheej txheem rau cov thauj ntawm hom III organic human anions (hOAT-3), uas tej zaum yuav koom nrog kev zam ntawm sitagliptin los ntawm lub raum. Kev koom tes ntawm hOAT-3 hauv kev thauj khoom ntawm sitagliptin tseem tsis tau muaj kev tshawb nrhiav qhov chaw kuaj mob. Sitagliptin tseem yog ib lub zog p-glycoprotein, uas kuj yuav koom nrog kev tshem tawm ntawm sitagliptin. Txawm li cas los xij, cyclosporin, ib qho inhibitor ntawm p-glycoprotein, tsis txo qis kev tshem tawm ntawm sitagliptin. Sitagliptin tsis yog lub cev rau cov organic cationic transporter (OCT2), cov organic anionic transporter (OAT1), lossis cov thauj cov protein (PEPT1 / 2).

Hauv kev tshawb fawb hauvvitro, sitagliptin tsis inhibit OAT3 (IC50 = 160 μM) lossis p-glycoprotein (txog 250 μM) kev sib kho hloov chaw ntawm kev kho mob ntshav muaj ntau. Hauv cov kev tshawb fawb soj ntsuam, sitagliptin muaj cov nyhuv me rau plasma qhov ntau ntawm digoxin, txawm li cas los xij, sitagliptin tej zaum yuav yog qhov tsis haum p-glycoprotein.

Cov neeg mob lub raum tsis ua hauj lwm. Hauv cov neeg mob uas lub raum tsis ua haujlwm me me (creatinine tshem tawm KK 50-80 ml / min) tsis muaj qhov chaw kho mob nce siab ntawm cov concentration ntawm sitagliptin hauv ntshav plasma piv nrog pawg tswj hwm ntawm cov neeg ua haujlwm noj qab haus huv. Kev kwv yees nce li 2 npaug ntawm AUC rau sitagliptin tau pom nyob hauv cov neeg mob uas mob raum tsis txaus (CC 30-50 ml / min), 4 npaug ntawm AUC raug pom nyob hauv cov neeg mob uas lub raum tsis ua haujlwm loj (CC tsawg dua 30 ml / min) thiab cov neeg mob mob raum tsis ua haujlwm uas yog lub siab mob hlwb, piv nrog cov pab pawg tswj hwm. Yog li, txhawm rau kom ua tiav txoj kev kho tshuaj ntawm cov tshuaj hauv cov ntshav ntshav hauv cov neeg mob uas mob raum mus rau lub raum tsis ua haujlwm, yuav tsum tau txhaj tshuaj kho. Sitagliptin rau qee qhov me me yog tawm thaum lub sij hawm hemodialysis (13.5% ntawm koob tshuaj nyob rau hauv 3-4 teev lim ntshav, uas pib 4 teev tom qab noj tshuaj).

Cov neeg mob mob siab tsis ua haujlwm. Hauv cov neeg mob uas muaj mob me ntsis tsis txaus siab (7-9 cov ntsiab lus ntawm Child-Pugh nplai), tsis tas yuav hloov kho koob tshuaj. Tsis muaj cov ntaub ntawv tshawb fawb txog kev siv cov sitagliptin hauv cov neeg mob uas tsis muaj peev xwm rau hepatic txaus (ntau dua li 9 ntsiab lus ntawm Cov Ntawv Qhia Me-Pugh). Txawm li cas los xij, vim tias qhov tseeb tias sitagliptin feem ntau ua rau lub raum ua haujlwm, ib qho yuav tsum tsis txhob cia siab tias muaj kev hloov pauv tseem ceeb ntawm pharmacokinetics ntawm sitagliptin hauv cov neeg mob uas muaj qhov ua rau mob hepatic hnyav.

Laus lub caij nyoog. Tsis tas yuav mus txhaj qhov tshuaj hloov raws qhov muaj hnub nyoog. Hauv cov neeg mob laus (65-80 xyoo), ntshav ntau ntawm sitagliptin yog 19% siab dua hauv cov neeg mob hluas.

Cov menyuam. Kev tshawb fawb txog kev siv cov sitagliptin hauv cov menyuam yaus tsis tau ua.

Tus tub los ntxhais, haiv neeg, lub cev nyhavCov. Tsis tas yuav hloov qhov tshuaj ntau ntxiv nyob ntawm poj niam txiv neej, haiv neeg lossis BMI. Cov yam ntxwv no tsis muaj kev cuam tshuam loj hauv lub tsev tshuaj pharmacokinetics ntawm sitagliptin.

Mob ntshav qab zib Hom 2. Cov tshuaj pharmacokinetics ntawm sitagliptin feem ntau zoo tib yam rau cov neeg noj qab haus huv thiab cov neeg mob ntshav qab zib hom 2. Cov kev tshawb fawb soj ntsuam pom tau tias poj niam txiv neej, haiv neeg thiab lub cev hnyav tsis muaj qhov cuam tshuam loj hauv cov chaw muag tshuaj ntawm sitagliptin.

Cov Tshuaj Hauv Tshuaj

Januvia yog tus tswvcuab ntawm cov tshuaj tiv thaiv kab mob hauv lub qhov ncauj hu ua dipeptidyl peptidase 4 (DPP-4) inhibitors, uas txhim kho glycemic tswj hauv cov neeg mob uas muaj ntshav qab zib hom 2 los ntawm kev nce qib ntawm cov tshuaj hormones nquag ntawm tsev neeg muaj zog. Cov tshuaj hormones ntawm tsev neeg incretin, suav nrog glucagon-zoo li peptide-1 (GLP-1) thiab glucose-dependant insulinotropic peptide (HIP), yog zais hauv cov hnyuv nruab hnub, lawv qib nce ntxiv hauv kev teb rau kev noj zaub mov. Tus incretins yog ib feem ntawm cov txheej txheem kho mob sab hauv lub zog rau kev tswj hwm cov ntshav qabzib homeostasis. Nrog cov ntshav khov ntshav lossis ntshav qabzib, cov tshuaj hormones ntawm tsev neeg muaj ntau ntxiv los ua rau muaj insulin synthesis ntau ntxiv, nrog rau nws qhov zais cia los ntawm pancreatic beta hlwb vim ua rau cov cim intracellular cuam tshuam nrog cyclic AMP (adenosine monophosphate).

Cov kev tshawb fawb ntawm GLP-1 lossis DPP-4 cov tshuaj tiv thaiv nyob hauv cov tsiaj qauv nrog tus mob ntshav qab zib hom 2 tau pom tias muaj cov ntshav qabzib zoo dua β cov hlwb thiab kev ua kom muaj zog ntawm cov tshuaj insulin. Muaj kev nce ntxiv hauv cov piam thaj nrog kev nce hauv insulin ntau lawm. GLP-1 kuj tseem pab txhawb ntxiv kom muaj kev zais ntawm glucagon los ntawm alpha cell. Qhov kev txo qis hauv glucagon qhov siab tshaj tawm txog keeb kwm yav dhau los ntawm kev nce qib hauv insulin ua rau muaj kev txo qis ntshav qabzib ntau los ntawm lub siab, uas thaum kawg ua rau txo qis glycemia.

Thaum lub siab tsis zoo ntawm cov piam thaj hauv ntshav, cov txiaj ntsig tau teev ntawm incretins ntawm kev tso tawm insulin thiab ib qho kev txo qis hauv glucagon tso pa tsis pom. Qhov txiaj ntsig ntawm kev tsim tawm ntawm GLP-1 thiab GUI nyob ntawm theem ntawm cov piam thaj hauv cov ntshav. Tsis muaj kev tsim tawm ntawm cov kua dej los yog kev tawm tsam cov khoom ntawm glucagon GLP-1 nrog cov ntshav qabzib tsawg hauv cov ntshav. GLP-1 thiab HIP txhawb kev tsim tawm ntawm cov tshuaj insulin tsuas yog thaum cov ntshav qabzib hauv lub ntsej muag pib dhau ntawm qhov tsis suav. GLP-1 thiab HIP tsis cuam tshuam rau qhov glucagon tso tawm rau hauv kev teb rau hauv lub ntsej muag hypoglycemia. Nyob rau hauv cov kev mob tshwm sim hauv lub cev, kev ua si ntawm incretins raug txwv los ntawm enzyme DPP-4, uas tau nrawm hydrolyzes nce nrog kev tsim cov khoom tsis muaj zog.

Januvia tiv thaiv cov hydrolysis ntawm incretins los ntawm enzyme DPP-4, yog li ua kom cov ntshav ntau ntawm cov nquag cov ntaub ntawv ntawm GLP-1 thiab HIP. Los ntawm kev nce qib ntawm incretins, Januvia nce cov piam thaj hauv kev tso tawm ntawm cov kua dej thiab pab txo qis lub ntsej muag ntawm glucagon. Hauv cov neeg mob uas muaj hom 2 mob ntshav qab zib mellitus nrog hyperglycemia, cov kev hloov pauv hauv kev zais ntawm insulin thiab glucagon ua rau qhov txo qis ntawm glycosylated hemoglobin НbА1С thiab txo qis hauv plasma concentration ntawm cov piam thaj, txiav txim siab ntawm lub plab tsis muaj zog thiab tom qab kev ntsuam xyuas mob. Cov piam thaj ntawm sitagliptin txawv ntawm cov teebmeem ntawm sulfonylureas, uas ua rau cov insulin tso tawm txawm tias muaj cov ntshav qabzib tsawg dua thiab tuaj yeem ua rau cov ntshav qabzib hauv cov neeg mob ntshav qab zib hom 2 thiab cov ntsiab lus noj qab nyob zoo. Sitagliptin yog qhov muaj kev xaiv tshwj xeeb rau qhov enzyme DPP-4, thiab ntawm kev siv tshuaj ntau tsis yog nws cuam tshuam txog cov enzymes DPP-8 lossis DPP-9.

Abstract ntawm cov ntawv sau txog kev tshawb fawb txog tshuaj thiab kev kho mob, tus kws sau haujlwm ua haujlwm - Kim S.S., Kim Yin Zhuo, Lee K.D., Park C.H., Kim Y.I., Lee Y.S., Chung S.Ch. ., Lee S.Ch.

Txog kev kho mob ntawm hom 2 mob ntshav qab zib mellitus (T2DM), thaum pib ua ke ntawm kev kho nrog hypoglycemic tshuaj yog qhov pom zoo. Hauv kev ua haujlwm ntau, ob-dig muag, kev sim kev sib tw hauv cov pab pawg sib luag, cov kev ua tau zoo thiab kev nyab xeeb ntawm sitagliptin thiab metformin tau muab los ua cov tshuaj sib xyaw ua ke (Sit / Met) tau muab piv nrog glimepiride raws li kev kho mob thawj zaug rau cov neeg mob ntshav qab zib hom 2. Txoj kev Cov neeg mob nrog T2DM (hnub nyoog> 18 xyoo) muaj kev pheej hmoo kom tau txais Sith / Met lossis glimepiride tsis pub dhau 30 lub lis piam tom qab thawj zaug ntxuav tawm.Lub hom phiaj xaus yog qhov hloov HbA1 qib los ntawm qhov pib. Cov theem ob kawg suav nrog cov ntaub ntawv los ntawm cov neeg mob uas ua tiav kev kho mob nrog glimepiride HbA1c (n = 145). Tom qab 30 lub hlis ntawm kev kho mob, zaum / Met sib xyaw ua ke ntau dua glimepiride hauv kev txo qis HbA1c (1.49 thiab 0.71%, feem, qhov cuam tshuam sib txawv ntawm 0.78%, p ntawm glimepiride (40.1%, p ntawm glimepiride (qhov sib txawv ntawm qhov nruab nrab ntawm 23.5 mg / dl, p ntawm hypoglycemia thiab qhov hnyav nce tau cov lus tsawg tsawg hauv pawg Sit / Met piv nrog glimepiride (5.5% piv rau 20.1%, 0.83 kg piv rau +0.90 kg, ntsig txog, rau ntawm ob qho kev sib piv, tus nqi ntawm p nrog glimepiride, kev teem caij Sit / Met ua kev kho mob thawj zaug 30 lub lis piam tom qab pib ntawm kev kawm tau muab ntau cim txhim kho hauv glycemic tswj thiab lub cev hnyav, thaum muaj kev txo qis ntawm qhov tshwm sim ntawm kev mob ntshav qab zib.

Cov ntawv sau ntawm cov ntawv pov thawj scientific ntawm lub ncauj lus "Qhov ua tau zoo thiab kev nyab xeeb ntawm kev sib xyaw ua ke ntawm sitagliptin / metformin piv nrog glimepiride rau cov neeg mob uas muaj ntshav qab zib hom 2: cov neeg ua haujlwm ntau qhov kev tshawb pom ob leeg dig muag"

Kev ua tau zoo thiab kev nyab xeeb ntawm kev sib koom ua ke ntawm sitagliptin / metformin piv nrog glimepiride hauv cov neeg mob uas muaj hom 2 mob ntshav qab zib mellitus: multicenter randomized ob npaug

Kim S. SL 2, Kim I. CHL 2, Lee C.D. 3, Park C.H. 4, Kim Y.I. 5, Lee YE. 7, Chung S.Ch. 6, Lee S. Feem 8

1 Lub Chaw Haujlwm ntawm Endocrinology thiab Metabolism, Chav Haujlwm Kho Mob, Tsev Kho Mob Hauv Tsev Kawm Ntawv Busan State University, Kaus Lim Qab Teb

2 Lub koom haum rau Kev Tshawb Fawb Txog Kev Tshawb Fawb Txog Kev Tshawb Fawb, Busan State University Cov Chaw Kho Mob, Kaus Lim Qab Teb

3 Lub Chaw Haujlwm ntawm Endocrinology thiab Metabolism, Chav Haujlwm Kho Mob, Tsev Kho Mob Daedong, Kaus Lim Qab Teb

4 Lub Chaw Haujlwm ntawm Endocrinology thiab Metabolism, Lub Tsev Haujlwm Saib Xyuas Kev Kho Mob, Tsev Kho Mob Pean Peck, Tsev Kawm Ntawv ntawm Inje, Tsev Kawm Qib Siab Tshuaj, Tsev Kawm Ntawv ntawm Inje, Busan, Sab Qab Teb Kauslim

5 Lub Chaw Haujlwm ntawm Endocrinology thiab Metabolism, Lub Tsev Haujlwm Saib Xyuas Kev Kho, Ulsan University Tsev Kho Mob, Kaus Lim Qab Teb

6 Lub Chaw Haujlwm ntawm Endocrinology thiab Metabolism, Lub Tsev Haujlwm Kho Mob, Dongkang Medical Center, Kaus Lim Qab Teb

7 Lub Chaw Haujlwm ntawm Endocrinology thiab Metabolism, Lub Tsev Haujlwm Kho Mob, Dongguk University College ntawm Tshuaj, Gyeongju, Kaus Lim Qab Teb

8 MSD Kauslim Teb Ltd, Seoul, Kaus Lim Qab Teb

Txog kev kho mob ntawm hom 2 mob ntshav qab zib mellitus (T2DM), thaum pib ua ke ntawm kev kho nrog hypoglycemic tshuaj yog qhov pom zoo. Hauv kev ua haujlwm ntau, ob-dig muag, kev sim kev sib tw hauv cov pab pawg sib luag, cov kev ua tau zoo thiab kev nyab xeeb ntawm sitagliptin thiab metformin tau muab los ua cov tshuaj sib xyaw ua ke (Sit / Met) tau muab piv nrog glimepiride raws li kev kho mob thawj zaug rau cov neeg mob ntshav qab zib hom 2.

Txoj kev Cov neeg mob nrog T2DM (hnub nyoog> 18 xyoo) muaj kev pheej hmoo kom tau txais Sith / Met lossis glimepiride rau 30 lub lis piam tom qab thawj zaug ntxuav tawm. Lub hom phiaj xaus yog qhov hloov HbA1 qib los ntawm qhov pib. Thib ob xaus cov ntaub ntawv suav nrog cov neeg mob cov ntaub ntawv

* Cov ntawv no tau nthuav tawm rau pej xeem raws li Cov Lus Cog Tseg ntawm Kev Tsim Kho Ib Ntus tsis muaj daim ntawv tso cai, uas tso cai rau koj siv, faib thiab luam tawm cov ntaub ntawv nyob rau hauv txhua txoj kev, muab hais tias qhov kev ua haujlwm qub tau raug txheeb xyuas kom raug.

HbA1c Cov chaw muab kev kho mob Kuv nrhiav tsis tau dab tsi koj xav tau? Sim cov ntawv nyeem kev pabcuam xaiv.

8 MSD Kaus Lim Kauslim Ltd, Seoul, Kaus Lim Qab Teb, Kaus Lim Qab Teb

Pib thaum ntxov ntawm kev sib xyaw ua ke siv cov tshuaj tiv thaiv kab mob antihyperglycemic pom zoo rau kev kho mob ntshav qab zib hom 2 (T2D). Tam sim no multicenter ob lub qhov muag dig muag randomized ib pawg-kev kawm tshawb xyuas qhov ua tau zoo thiab kev nyab xeeb ntawm sitagliptin thiab metformin tsau-koob tshuaj sib xyaw (Sita / Met) piv nrog glimepiride hauv T2D cov neeg mob thaum pib kho.

Txoj kev Cov neeg mob ntshav qab zib hom 2 (hnub nyoog> 18 xyoos) tau xaiv rau Sita / Met lossis glimepiride rau 30 lub lis piam tom qab ntxuav lub sijhawm. Qhov pib xaus yog hloov los ntawm lub hauv paus (CFB) hauv HbA1c. Cov theem ob yog cov kev faib ua feem ntawm cov neeg mob uas ua tiav lub hom phiaj HbA1c

Cov lus xaus. Piv nrog gLimepiride, Sita / Met raws li kev kho thaum xub thawj coj Los txhim kho ntau dua glycemic tswj thiab lub cev hnyav hloov, nrog tsawg dua qhov kev mob ntshav qab zib, dhau 30 lub lis piam.

glimepiride, hypoglycemia, metformin, sitagliptin phosphate

J Ntshav Qab Zib. 2017, 9: 412-422. doi: 10.1111 / 1753-0407.12432

Kev soj ntsuam thiab kev mob ntshav qab zib ntawm cov ntshav qab zib thiab nws cov kev kho mob txuas ntxiv yog qhov teeb meem tseem ceeb rau zej zog kev kho mob 1, 2. Feem ntau ntawm cov kabmob ntshav qab zib hauv 2014 ntawm cov neeg laus yog 9%, 90% ntawm cov neeg no yog hom ntshav qab zib hom 2 (T2DM) ) Hauv Kaus Lim Qab Teb, raws li Lub Tebchaws Txoj Haujlwm Kev Noj Qab Haus Huv thiab Khoom Noj Khoom Noj, xyoo 2011.kev kwv yees kwv yees li ntawm cov ntshav qab zib mellitus hauv cov neeg mob hnub nyoog> 30 xyoo yog 10.5% raws li cov ntaub ntawv ntawm kev yoo plasma ntshav qab zib (yoo ntshav) thiab 12.4% raws li cov ntaub ntawv ntawm qib ntawm kev yoo ntshav ntshav thiab HbA1c.

Rau cov ntshav qab zib mellitus, muaj qhov sib txuam ntawm kev muaj tus kab mob nrog kev txhim kho micro - thiab macro-vascular qhov teeb meem ua rau kev puas tsuaj rau cov plab hnyuv siab raum thiab cov ntaub so ntswg, cov kev mob no tau sau tseg hauv 30-50% ntawm cov neeg mob, thiab lawv qhov kev pheej hmoo yog feem ntau cuam tshuam nrog yav dhau los pom tias muaj ntshav qab zib tsawg. Txij li thaum glycemic txoj kev kho yog tsuas yog tsom rau kev tiv thaiv ntawm microvascular cov teeb meem, kev sib raug zoo ntawm glycemic tswj thiab macrovascular cov teeb meem me ntsis tsis muaj zog 7-9. Txawm li cas los xij, qhov zoo dua ntawm kev ua tiav kev tswj hwm glycemic nyob rau theem thaum ntxov ntawm kev kho mob ntshav qab zib yog qhov tseem ua tau los tswj kev tswj kav rau ib xyoo lossis ntau dua txawm tias tsis tshua muaj kev kho ntxiv 10, 11. Cov kev tshawb pom tsis ntev los no txhawb kev hloov pauv hauv cov ntsiab lus ntawm kev ua tiav ua ntej ntawm glycemic cov hom phiaj hauv cov neeg mob ntshav qab zib hom 2.

Cov txheej txheem kev kho mob tau tsim los ntawm American Association of Clinical Endocrinologist (AACE) pom zoo thaum pib ntawm kev sib xyaw metformin nrog kev pib HbA1c qib> 7.5% (58 mmol / mol), txij li ua tiav HbA1c theem ntawm 9.0% (75 mmol / mol), txij li cov neeg mob no tsis zoo li yuav ua tiav qib theem ntawm HbA1c nrog metformin monotherapy. Yog li, qhov pib ntawm kev sib xyaw ua ke

kev kho nrog hypoglycemic tshuaj nrog ntau cov txheej txheem ntawm kev ua yuav yog qhov kev xaiv tshwj xeeb zoo rau cov neeg mob ntshav qab zib hom 2.

Hauv kev soj ntsuam tam sim no, sulfonyl-urea derivatives 17-19 feem ntau yog siv los ua thawj zaug kev kho mob los txhawb cov kua dej hauv cov neeg mob ntshav qab zib hom 2. Vim nws lub peev xwm los txhim kho cov tshuaj insulin zais ntshis (uas yog qhov teeb meem muaj txiaj ntsig hauv T2DM), glimepiride tau siv ua thawj kab kev kho mob hauv ntau lub teb chaws, suav nrog Kauslim. Txawm li cas los xij, vim muaj ntau dua ntawm kev tuag tag nrho piv nrog metformin, kev txhawj xeeb txog kev nyab xeeb ntawm sulfonylurea derivatives 20, 21 tshwm sim ntxiv, Tsis tas li ntawd, kev txhim kho hypoglycemia thiab qhov nce hauv lub cev hnyav tau sau tseg nrog kev siv glimepiride. Sitagliptin, yog ib qho muaj zog ntau ntawm dipeptidyl peptidase (DPP) tshuaj tiv thaiv, yog thawj cov tshuaj siv rau hauv chav kawm no los kho cov neeg mob ntshav qab zib hom 2. Sitagliptin txhim kho insulin secretion thiab txo qis glucagon qhov kev xav ntawm cov tshuaj tiv thaiv kev ua yeeb yam-tshiab, qhov kev ua haujlwm ntawm cov tshuaj no yog nyob ntawm cov piam thaj hauv qib 23, 24. Cov kab mob siab, siab ua tau zoo thiab ua siab ntev zoo rau kev sib xyaw ntawm sitagliptin thiab metformin (Sit / Met) hauv cov neeg mob tau ua pov thawj. nrog T2DM 25, 26. Txawm li cas los xij, yav dhau los tsis muaj kev tshawb fawb txog kev sib txuam ruaj ruaj Sit / Met tau ua hauv Kauslim.

Lub hom phiaj ntawm kev kawm nthuav tawm hauv Kaus Lim Kauslim yog kawm txog kev ua tau zoo thiab kev nyab xeeb ntawm kev kho mob thaum pib ntawm Sit / Met FDC piv nrog glimepiride hauv cov neeg mob ntshav qab zib hom 2.

Kev nthuav qhia multicenter randomized ob lub qhov muag pom kev tshawb pom hauv cov pawg sib txuas tau ua txij thaum Lub Tsib Hlis 6, 2010 txog Lub Kaum Hlis 29, 2013 hauv 21 lub chaw saib xyuas ntawm Kaus Lim Qab Teb rau 39 lub limtiam (kev cim tus lej CLinicaLtriaLs.gov Ш: NCT00993187, raws tu qauv ntawm lub tuam txhab Merk MK-0431A -202). Cov neeg mob tau kho nyob rau ntawm 1: 1 piv rau 30 lub lis piam kev kho tom qab kev xaiv 6 lub lis piam induction lub sijhawm / lub sijhawm ntxuav thiab lub luag haujlwm 2 lub lis piam rau kev kho qhov muag tsis pom tseeb (Daim Duab 1, A). Txoj kev kawm no tau tshawb nrhiav raws li

Daim duab. 1. Tshawb Fawb Tsim thiab Kev faib Tawm rau Cov Mob

A - cov ncauj lus kom ntxaws qhia txog kev faib tawm ntawm cov neeg mob, B - Sit / Met EyO - sitagliptin thiab metformin hauv kev sib koom ua ke, AE - qhov tshwm sim tsis txaus siab, SNA - ib qho xwm txheej tsis txaus ntseeg.

* Lub chaw kuaj mob hauv tsev kho mob tau raug kaw vim tias tus kws tshawb fawb raug lawb tawm ntawm nws tus kheej qhov kev ywj pheej thiab nws tsis tuaj yeem hloov tus neeg mob mus rau lwm lub chaw kuaj mob. Tus neeg pab txhawb nqa tau txiav txim siab kaw qhov chaw soj ntsuam thiab tsis suav tus neeg mob thaum lub sijhawm xaiv rau kev kawm tawm.

nrog rau cov qauv ntawm Cov Cai Kav rau kev ua qhov zoo sim soj ntsuam, cov cai ntawm Helsinki tshaj tawm thiab siv rau lub xeev thiab / lossis cov cai hauv zos. Ua ntej txoj kev tshawb fawb no, kev pom zoo tau txais los ntawm pawg neeg saib xyuas kev coj ncaj ncees nyob hauv txhua lub chaw tshawb fawb, nrog rau kev sau ntawv tso cai ntawm txhua tus neeg mob.

raws li cov kev tshawb xav tau lossis nthuav tawm tus neeg mob ua rau muaj kev pheej hmoo raws li tus kws tshawb fawb lossis kev soj ntsuam kev kho mob. Cov neeg mob tau raug cais tawm ntawm txoj kev tshawb nrhiav thaum lub sijhawm pib ntawm cov placebo lossis thaum lub sijhawm randomization yog tias theem ntawm GPN lossis cov txiaj ntsig ntawm kev sojntsuam cov ntshav capillary ntshav qabzib hauv lub chaw soj ntsuam tau tsawg dua 110 mg / dl lossis siab dua 300 mg / dl, feem.

Lub sijhawm pib ua haujlwm suav nrog cov neeg mob laus (> 18 xyoo) nrog T2DM uas tsis tau xeeb tub, tsis pub niam mis, thiab rau tus neeg muaj qhov tshwm sim tsis tshua muaj menyuam thaum lub sijhawm kawm lossis lub sijhawm kuaj pom. Kev xaiv cov qauv ntawm qhov kev tshuaj ntsuam xyuas tau muaj qib HbA1c los ntawm> 7.0 (53 mmol / mol) txog 6.5 (48 mmol / mol) txog 7.0 (53 mmol / mol) txog 14 hnub, tshuaj tiv thaiv tshuaj tiv thaiv, phais mob rau cov tshuaj loog (tsis pub dhau 30 hnub ua ntej pib kawm lossis npaj kev cuam tshuam), thiab cov kev xaiv ua kev sim tshuaj (tsis pub dhau 8 lub lis piam ua ntej pib kawm).

Lwm qhov kev cais tawm muaj xws li hypersensitivity los yog contraindications rau kev siv ntawm tej sulfonylurea derivatives, DPP-4 inhibitors los yog biguanides, ntshiab creatinine> 1.5 mg / dl hauv cov txiv neej thiab> 1.4 mg / dl hauv cov poj niam, triglycerides saum 500 mg / dl, tsis txaus ntawm cov thyroid-stimulating hormone, kab mob siab hauv lub sijhawm nquag (tshwj tsis yog rau cov roj ntsha tiv thaiv kab mob), cov kab mob plawv, qhov tshwm sim zoo ntawm kev tshuaj ntsuam ntawm tib neeg cov tshuaj tiv thaiv kab mob, kev cuam tshuam ntawm cov ntshav hematopoietic, keeb kwm ntawm malignant neoplasms, kuaj ntsuas zis zoo, ntsuas lub cev (BMI)> 35 kg / m2, lossis cov xwm txheej uas tuaj yeem ua rau tsis ua raws

Thoob plaws lub sijhawm pib / ntxuav tawm, cov neeg mob tau qhia txog kev noj haus thiab kev tawm dag zog, thiab qhia txog kev siv ntshav cov ntshav ntsuas. Lub sijhawm placebo, cov neeg mob tau noj cov tshuaj placebo kom haum rau Sit / Met hauv cov tshuaj sib tov sib xyaw (FDC) 50/500 mg (1 ntsiav tshuaj thaum sawv ntxov thiab noj hmo), ua ke nrog cov tshuaj placebo sib xyaw rau 1 mg glimepiride (1 lub sijhawm ib hnub mus txog rau thaum yav sawv ntxov noj mov).

Thaum lub sijhawm kev kho mob, pab pawg sim tau coj Sit / Met hauv kev sib koom ua ke (Yanumet, Merck & Co., Inc., West Point, PA, USA) 50/500 mg 2 zaug hauv ib hnub ntawm qhov ncauj thaum noj mov nrog ib feem feem ntawm 50 txog / 1000 mg 2 zaug hauv ib hnub rau 4 lub sijhawm. Txog rau lub 8 thij tom qab thawj lub sijhawm 4 lub lis piam, kev tso cai tau pom zoo nrog kev txo qis ntawm Sit / Met FDC thaum tsis pom zoo, ces tsis muaj kev hloov pauv ntau ntxiv. Cov tshuaj Placebo sib xyaw rau glimepiride (Merck & Co., Inc., InvaGen Pharmaceuticals, Happodge, New York, Tebchaws Asmeskas) tau yuam kom noj ib hnub ib zaug. Cov neeg mob los ntawm pawg tswj hwm tau txais glimepiride hauv thawj koob tshuaj 1 mg / hnub nrog ib feem nce txog li 6 mg / hnub rau thawj 8 lub lim tiam ntawm kev txiav txim siab los ntawm kev tshawb fawb, raws li cov lus pom zoo ntawm ADA (American Diabetes Association, American Association of Diabetologist). Cov tshuaj placebo sib thooj rau Sit / Met FDC yuav tsum tau noj 2 zaug nyob rau ib hnub.Txhawm rau kom pom tseeb qhov muag tsis pom kev, ib txoj hauv kev nrog ob hom tshuaj placebo tau siv: (1) cov neeg mob los ntawm pawg Cit / Met FDC tau txais Cit / Met FDC 50/500 mg ntsiav tshuaj thiab / lossis Sit / Met FDC 50/1000 mg thiab cov tshuaj placebo sib xyaw rau glimepiride, ( 2) cov neeg mob los ntawm cov pab pawg glimepiride tau txais 2 cov tshuaj placebo kom haum rau Sit / Met FDC 50/500 mg thiab / lossis Sit / Met FDC 50/1000 mg thiab glimepiride ntsiav tshuaj (qhov koob tau txiav txim siab raws li kev txiav txim siab) 1 lossis 2 mg.

Ua raws li kev kho mob

Yuav kom ua tau raws li cov qauv xaiv thaum lub sijhawm qhia, kev qhia txog 85% ntawm kev ua raws li kev kho yuav tsum tau (suav raws li kev txiav txim siab ntawm cov tshuaj placebo ua rau hauv kev kho qhov muag tsis pom tseeb). Thoob plaws lub sijhawm kev kho mob, kev ua raws li kev kho tau raug soj ntsuam los ntawm kev siv cov qauv hauv qab no: feem pua ​​kev ua raws = (pes tsawg hnub kho / cov hnub xav tau ntawm kev kho mob) x 100

Randomization / Distribution / Dig Muag Hom

Randomization schemes tau npaj los ntawm tus qauv ntsuas ntaub ntawv uas tsis koom nrog txoj kev tshawb no. Tom kawg ntawm cov placebo cov lus qhia ua ntej (mus saib 5), txhua tus neeg mob uas cov ntaub ntawv tau xaiv cov qauv raug xaiv tau tus lej ze ntawm cov khoom siv tau los ntawm DreamCIS (Seoul, Kauslim Teb). Qhov muag tsis pom hom kev npaj thiab hnab ntawv kaw nrog cov lej tau muab los ntawm Merck Sharp & Dohme (West Point, PA, USA). Txoj kev tshawb no yog ob chav dig muag, i.e. Cov kws tshawb nrhiav, neeg saib mob neeg mob, kws tshuaj thiab cov neeg mob tsis muaj ntaub ntawv qhia txog kev kho mob li cas.

Kev ntsuas thiab qhov ua tau zoo

Kev ntsuas kev ntsuas ntawm lub qog ntshav qab zib lub zog ntawm kev kho tau raws li qib HbA1c, GPN thiab qib kev kam rau ntawm cov tshuaj kawm. Qhov ua tau zoo ntawm qhov xaus yog qhov hloov HbAlc qib los ntawm lub hauv paus ntawm lub lim tiam 30 ntawm kev kho. Cov kev ua tiav theem ob suav nrog kev hloov pauv hauv GPN qib txij li pib mus rau theem pib nyob rau lub lim tiam 30 thiab qhov feem pua ​​ntawm cov neeg mob uas tau ncav cuag lub hom phiaj HbA1c qib qis dua 7% (53 mmol / mol) ntawm lub lim tiam 30.

Kev nyab xeeb cov ntsiab lus suav nrog qhov tshwm sim ntawm ntu ntawm hypoglycemia thiab hloov hauv lub cev qhov hnyav los ntawm lub hauv paus. Txhua qhov kev nyab xeeb thiab kev ua siab ntev tau raug ntsuas los ntawm tus lej ntawm cov kev kho mob ntsig txog qhov tsis zoo (AEs), cov txiaj ntsig ntawm kev kuaj ntshav biochemical (suav nrog cov theem ntawm alanine aminotransferase, aspartate minotransferase, tag nrho bilirubin thiab alkaline phosphatase), hem ntshav ntawm ntshav (nrog rau suav cov ntshav feem ntau, leukocyte cov tshuaj loog thiab tus naj npawb tsis muaj tseeb ntawm neutrophils), cov cim tseem ceeb ntawm lub xeev ntawm lub cev thiab cov zis tawm kev soj ntsuam.

Txog 139 cov neeg mob hauv txhua pawg kho mob (tag nrho ntawm 278 tus neeg mob) yuav tsum txiav txim siab qhov tseeb nruab nrab qhov sib txawv ntawm 0.4% ntawm qhov hloov HbA1c qib los ntawm lub hauv paus mus rau 30 lub lim tiam ntawm kev kho mob nruab nrab ntawm Sit / Met FDC thiab glimepiride pawg nrog ob qho tseem ceeb sib txawv. thiab 0.05. Qhov kev xam no tau ua raws li qhov kwv yees ntawm qhov txawv ntawm qhov txawv (SD) ntawm 1% los ntsuas qhov kev hloov hauv HbA1c qib los ntawm lub hauv paus mus rau 30 lub lim tiam ntawm kev kho mob, suav txog qhov kev xav ntawm 90% zog thiab 5% ntawm cov neeg mob uas cov ntaub ntawv tsis tuaj yeem ntsuas.

Thawj qhov kawg ntawm kev soj ntsuam los sib piv pawg kho mob kom paub meej txog qhov zoo tshaj ntawm ib txoj kev kho mob tau ua tiav siv covariance tsom xam (ANCOVA) rau qhov ua tiav cov qauv ntawm cov neeg mob rau kev tsom xam (FAS) nrog tus nqi p Kuv tsis pom qhov koj xav tau? Sim cov ntawv nyeem kev pabcuam xaiv.

Ntawm 628 cov neeg mob uas muaj ntshav qab zib hom 2 uas tau txheeb xyuas qhov kev koom nrog txoj kev tshawb fawb no, cov ntaub ntawv tsis suav nrog; tshuav 292 leej raug xaiv (147 rau Pawg / Met FDC pawg thiab 145 rau glimepiride pawg). 229 cov neeg mob ua tiav txoj kev tshawb no (saib Daim Duab 1, B). Tus nqi tawm tsis tiav yog 17.7% hauv pawg Sit / Met FDC thiab 25.5% hauv pawg neeg glimepiride.

Cov cwj pwm hauv paus feem ntau piv tau ntawm ob pab pawg (saib Cov Lus 1), tshwj tsis yog lub sijhawm ntev dua ntawm T2DM hauv pawg Sit / Met FDC (4.6 thiab 3.9 xyoo).Lub hnub nyoog nruab nrab ntawm cov neeg mob yog 54.8 thiab 53.1 xyoo hauv Sith / MetFDC thiab glimepiride pawg, feem; qhov nruab nrab HbA1c qib yog 8.0% (64 mmol / mol) hauv pawg Sith / Met FDC thiab 8.1% (64 mmol / mol) nyob rau hauv pawg glimepiride. Thaum pib, 38.8 thiab 43.3% ntawm cov neeg mob tsis tau txais kev kho mob ntshav qab zib yav dhau los hauv pawg Sit / Met FDC thiab glimepiride, feem. Cov ntaub ntawv hais txog kev noj tshuaj

Rooj 1. Lub hom phaj ntawm cov pejxeem thiab cov chaw khomob

Qhov Taw Qhia Kuv Zaum / Ntsib FDC (n = 147) 1 Glimepiride (n = 145) 1 Tag Nrho (n = 292) 1

Hnub nyoog, xyoo 54.8 ± 8.5 53.1 ± 9.2 53.9 ± 8.9

Cov Tub Ntxhais Txiv Neej Poj Niam 81 (55.1) 66 (44.9) 84 (57.9) 61 (42.1) 165 (56.5) 127 (43.5)

Lub cev hnyav, kg 67.3 ± 8.8 67.7 ± 10.4 67.5 ± 9.6

BMI, kg / m2 25.2 ± 2.7 25.0 ± 2.8 25.1 ± 2.7

Ntev ntawm hom 2 mob ntshav qab zib mellitus, xyoo 4.6 ± 4.6 3.9 ± 3.7 4.2 ± 4.2

HbA1c% mmol / mol 8.0 ± 0.9 64.0 ± 9.8 8.1 ± 0.9 65.0 ± 9.8 8.0 ± 0.8 64.0 ± 8.7

GPN, mg / dl 171.5 ± 41.2 168.3 ± 39.4 169.9 ± 40.3

GFR 75.9 ± 11.7 76.7 ± 16.2 76.2 ± 13.3

Cov roj (cholesterol) tag nrho, mg / dl 176.1 ± 34.9 171.0 ± 32.4 173.5 ± 33.7

LDL roj cholesterol, mg / dl 97.3 ± 33.0 95.0 ± 28.1 96.2 ± 30.6

HDL roj, mg / dL 48.2 ± 11.0 48.8 ± 10.1 48.5 ± 10.5

Kev ua kom puas tsuaj, mg / dl 150.5 ± 88.2 134.1 ± 72.1 142.3 ± 80.8

VAJ, mmHg 125.3 ± 11.2 126.3 ± 13.2 125.8 ± 12.2

DBP, mmHg 76.7 ± 8.1 77.7 ± 8.5 77.2 ± 8.3

Cov kev kho mob ntshav qab zib dhau los Yog Tsis Yog 90 (61.2) 57 (38.8) 82 (56.6) 63 (43.4) 172 (58.9) 120 (41.1)

Kev kho yav dhau los 118 (80.3) 123 (84.8) 241 (82.5)

Cov Tshuaj Hypolipidemic 65 (44.2) 66 (45.5) 131 (44.9)

PAC inhibitors 43 (29.3) 43 (29.7) 86 (29.5)

Antiplatelet tshuaj 57 (38.8) 53 (36.6) 110 (37.7)

Lus khaws xav Tshwj tsis yog muaj lwm qhov tau qhia, cov ntaub ntawv tau nthuav tawm raws li tus qauv iation kev sib txawv (Los ntawm) lossis n (%). Sit / Met EyO - sitagliptin thiab metformin hauv kev sib koom ua ke, DBP - ntshav tshuaj tiv thaiv kab mob hauv ntshav siab, GPN - yoo ntshav qabzib ntshav, RAS - renin-angiotensin system, CAD - systolic ntshav siab, BMI - lub cev huab hwm coj qhov ntsuas, GFR - glomerular pom kev sib luag, cov roj (cholesterol) LDL roj yog cov lipoprotein tsawg-cov roj, HDL cov cholesterol yog cov roj lipoprotein ntau heev.

Cov Lus 2. Cov ntsiab lus ntawm qhov siab tshaj plaws, zaum kawg thiab nruab nrab qhov kawg ntawm glimepiride

Tus naj npawb ntawm cov neeg mob uas muaj 141

Txhais D Koob ± RMS

kev txawv txav (hav zoov) 2.0 ± 1.3

Tus naj npawb ntawm cov neeg mob (%) nrog qhov siab tshaj plaws

Tus naj npawb ntawm cov neeg mob (%) nrog rau tag nrho cov koob tshuaj

80.3% ntawm cov neeg mob hauv pawg Sit / Met FDC thiab 84.8% ntawm cov neeg mob hauv cov pab pawg neeg glimepiride qhia txog keeb kwm ntawm cov tshuaj, cov feem ntau hais lipid-txo cov tshuaj, tom qab los ntawm cov zaus ntawm tshuaj antithrombotic thiab tshuaj uas cuam tshuam rau renin-angiotensin system.

Hauv ob pawg neeg, ntawm cov neeg mob muaj qib siab ntawm kev ua raws li kev kho mob (> 90%). Feem ntau ntawm cov neeg mob siv cov tshuaj tshawb rau ntau tshaj 24 lub lis piam. Qhov nruab nrab lub sijhawm ntawm cov tshuaj ntawm ib koob twg zoo sib xws hauv ob pawg kho mob (175.6 hnub hauv pawg Sit / Met FDC thiab 166.6 hnub hauv pawg glimepiride).

Koob kos txoj cai ib feem hauv qhov pab pawg glimepiride

Cov tshuaj nruab nrab cov tshuaj ntawm glimepiride yog 2.0 mg (thaj tsam: 1.0-6.0 mg). Qhov siab tshaj plaws ntawm 1 mg tau muab rau 46.1% (65/141) ntawm cov neeg mob, thiab tsuas yog 17.7% (25/141) ntawm cov neeg mob tau txais qhov siab tshaj plaws ntawm 6 mg (Cov Lus 2). Qhov tshuaj txhaj kawg ntawm glimepiride yog 1 mg hauv 49.6% (70/141) thiab 6 mg hauv 17.0% (24/141) ntawm tus neeg mob.

Kev Ntsuam Xyuas Kev Ntsuam Xyuas (FAS)

Thawj qhov kawg

Hauv lub lis piam 30, tus nqi nruab nrab HbA1c txo los ntawm tus nqi pib: 8% (64 mmol / mol) rau 6.5%

Sitagliptin / Metformin FDC A

90 80 70 60 50 40 30 20 10

p Kuv nrhiav tsis tau yam koj xav tau? Sim cov ntawv nyeem kev pabcuam xaiv.

- Sitagliptin / Metformin FDC - Glimepiride

5 6 7 8 (0W) (2W) (4W) (8W)

- Sitagliptin / Metformin FDC - Glimepiride

Daim duab. 2. Qhov ntsuas pom ntawm kev ua tau zoo thiab kev nyab xeeb thaum lub sijhawm kho mob hauv cov pab pawg ntawm sitagliptin thiab metformin hauv kev sib xyaw ua ke (FDC) lossis glimepiride (A, B, G)

Kev hloov pauv hauv kev sib piv nrog thawj qhov tseem ceeb ntawm (A) HbA1c ntawm cov tshuaj ntsuam xyuas tiav (FAS), (B) yoo plasma ntshav qab zib (GPN) hauv FAS, thiab (D) lub cev qhov hnyav hauv cov neeg ntawm cov neeg mob uas tau txais tsawg kawg ib koob ntawm cov tshuaj kawm (APaT). Qhov feem ntawm cov neeg mob uas ncav cuag lub hom phiaj HbA1c ntawm 7 thiab 6.5% nyob rau lub lim tiam 30 (FAS) (B). Tus naj npawb ntawm cov neeg mob uas muaj tsawg kawg yog 1 ntu kev muaj qog ntshav qab zib (APaT pejxeem) (D). Cov ntaub ntawv txhais tau tias ± tus qauv yuam kev ntawm qhov phem (SEM) (B, D, D) lossis txhais tau tias ± SEM (A, C).

Qhov txawv = -14.7% p Kuv nrhiav tsis pom qhov koj xav tau? Sim cov ntawv nyeem kev pabcuam xaiv.

Lub lim tiam 30, lub hom phiaj HbA1 ^ qib qis dua 7.0% (53 mmol / mol) tau ua tiav hauv qhov kev ntsuas ntawm cov neeg mob loj nyob hauv pawg Sit / Met FDC.

piv nrog pawg glimepiride (81.2 thiab 40.1%, p nruab nrab (36.5 lub hlis)

Lub sijhawm siv los kuaj ntshav qab zib: medians (24.8 kg / m2) BMI: 65 xyoo: medians (56 xyoo) hnub nyoog: nruab nrab (7.8%)

Value Tus nqi pib HbA1c (%): Kuv nrhiav tsis tau yam koj xav tau? Sim cov ntawv nyeem kev pabcuam xaiv.

Rat Stratum: tsis tas yuav siv cov tshuaj hypoglycemic

Rat Stratum: noj tshuaj hypoglycemic

Daim duab. 3. Kev tsom xam pawg

Daim duab piav qhia qhov sib txawv ntawm cov kev xaiv kev kho mob (glimepiride minus sitagliptin nrog metagin hauv kev sib txuas ua ke) piv rau theem ntawm HbA1c hauv pawg sib txawv, txiav txim siab los ntawm thawj qhov kev sib piv thiab tib neeg yam ntxwv. Ib qho tseem ceeb txo piv nrog thawj tus nqi tau pom nyob hauv txhua pawg neeg ntawm ob pawg kho mob. Hauv ob pawg kho mob, nrog rau qhov pib siab tshaj HbA1c qhov tseem ceeb, qhov ntau dua qhov txo qis hauv qhov ntsuas no txij li qib pib tau sau tseg. Intergroup qhov sib txawv hauv kev hloov pauv ntawm qhov nruab nrab txwv ntawm qhov pib mus rau 30 lub lim tiam feem ntau zoo tib yam nyob hauv txhua pawg me tau txheeb xyuas raws lub hnub nyoog, poj niam txiv neej, lub cev nyhav (BMI) thiab ntev dua ntawm hom 2 mob ntshav qab zib mellitus.

Rooj ntawv 3. Nthuav txog cov xwm txheej tsis zoo

Sab Cib / Met FDC Glimepiride

(n = 146) (n = 144) glimepiride (95% CI +)

Qhov tshwm sim tuag taus 0 (0) 0 (0)

Cov xwm txheej tsis zoo 8 (5.5) 9 (6.3) -0.8 (-7.7, 5.0)

Cov xwm txheej tsis zoo uas cuam tshuam nrog kev siv tshuaj * 37 (25.3) 39 (27.1) -1.7 (-11.9.8.4)

Cov xwm txheej tsis zoo (cov neeg mob nrog> 1 qhov tshwm sim) 88 (60.3) 101 (70.1) -9.9 (-20.6, 1.1)

Cov xwm txheej phem tshwm sim thaum kho (> 5% ntawm cov neeg mob)

Kev mob plab hnyuv tsis zoo 51 (34.9) 27 (18.8) 16.2 (6.0, 26.0)

Kev Sib Tw 19 (13.0) 9 (6.3)

Zawv plab 15 (10.3) 4 (2.8)

Xeev Xav 10 (6.8) 4 (2.8)

Mob plab plab 4 (2.7) 0 (0.0)

Kab mob sib kis thiab cab tau 31 (21.2) 32 (22.2) -1.0 (-9.0, 11.0)

Nasopharyngitis 13 (8.9) 17 (11.8)

Cov mob ua pa sab saud 12 (8.2) 4 (2.8)

Kev zom zaub mov thiab kev noj haus 14 (9.6) 33 (22.9) -13.3 (5.0, 22.0)

Kev Ntshav Siab 8 (5.5) 29 (20.1)

Tsis tshua muaj qab los noj mov 6 (4.1) 0 (0.0)

Cov txiaj ntsig ntawm kev ntsuas thiab kev kawm 8 (5.5) 15 (10.4) -4.9 (-1.0, 12.0)

Nce cov ntshav qabzib 0 (0,0) 6 (4,2)

Kev ua txhaum ntawm cov kab mob hlwb 14 (9.6) 9 (6.3) 3.3 (-10.0, 3.0)

Kiv taub hau 5 (3.4) 2 (1.4)

Musculoskeletal thiab mob cov ntaub so ntswg mob 10 (6.8) 11 (7.6) 2.0 (-7.0, 2.0)

Ua txhaum ntawm daim tawv nqaij thiab cov nqaij mos subcutaneous 4 (2.7) 10 (6.9) -4.2 (-1.0, 10.0)

Discontinuation ntawm kev kho mob kom ua vim qhov xwm txheej tsis zoo 8 (5.5) 8 (5.6) -0.1 (-5.8, 5.6)

Kev txiav tawm ntawm kev kho vim tias muaj kev kho mob ntsig txog cov kev mob tshwm sim. 7 (4.8) 3 (2.1) 2.7 (-1.8, 7.8)

Kev txiav tawm txoj kev kho vim tias muaj kev phom sij loj 1 (0.7) 1 (0.7) 0

Lus khaws xav Tshwj tsis yog muaj lwm qhov tau qhia, pes tsawg tus neeg koom hauv txhua pab pawg tau nthuav tawm, feem pua ​​yog muab rau kev thaiv chaw. Txawm hais tias tus neeg mob tuaj yeem muaj 2 lossis ntau qhov xwm txheej tsis zoo, tus neeg mob cov ntaub ntawv hauv txhua pawg tau sau tseg tsuas yog 1 zaug. * Tau txhais los ntawm cov kws tshawb fawb yog qhov ua tau, tej zaum lossis muaj tseeb txog kev tswj hwm tshuaj. 95% kev ntseeg siab (CI) tau muab xam raws li tus qauv ntawm M1eSpep thiab IgtPep. Zaum / Met EyO, sitagliptin thiab metformin hauv kev sib txuam ua ke.

Rau lwm qhov ntsuas (tseem ceeb ua haujlwm, kev tshawb xyuas biochemical ntawm cov ntshav, ntshav lipids lossis lwm yam hematological), thaj chaw kho mob tau hloov pauv tseem ceeb los ntawm thawj theem lossis qhov sib txawv ntawm cov pab pawg tsis tau sau cia.

Qhov kev ua haujlwm ntau tshaj ob-qhov muag pom nyob rau hauv Kauslim cov neeg mob ntshav qab zib hom 2 qhia tau qhov zoo tshaj ntawm Sith / Met FDC dua glimepiride hais txog kev txo qis HbA1c thiab GPN qib tom qab 30 lub lis piam pib kho. Lub hom phiaj HbA1c qib qis dua 7.0% (53 mmol / mol) tau ua tiav hauv qhov kev ntsuas ntawm cov neeg mob hauv pawg Sit / Met FDC. Txawm hais tias ob qho kev xaiv kho kev ua tau zoo glycemic tswj, kev kho glimepiride ua rau qhov hnyav hauv lub cev, thaum nrog Sit / Met, qhov txo qis me ntsis tau pom nrog tsawg dua cov kev qhia hypoglycemia. Feem ntau, ob txoj kev xaiv kho tau zoo rau.

Rau kev kho ua ke nrog sitagliptin thiab metformin, cov hauj lwm zoo yav dhau los tau qhia txog kev ua tiav glycemic

tswj hwm, ua siab ntev zoo, muaj feem cuam tshuam rau lub cev qhov hnyav thiab tsis tshua muaj kev mob ntshav qab zib 25, 26, 28. Hauv kev tshawb nrhiav tam sim no, cov ntaub ntawv ntxiv tau txais ntawm kev siv Sit / Met hauv kev sib xyaw ua ke hauv cov neeg mob ntshav qab zib hom 2. Ua raws li kev kho mob tam sim no hauv Kaus Lim, glimepiride yog thawj cov tshuaj rau kab mob ntshav qab zib hom 2 tam sim no. Cov txiaj ntsig ntawm txoj kev tshawb nrhiav tam sim no qhia tias Sit / Met FDC muaj qhov ua tau zoo dua rau kev teem sijhawm kho mob rau cov neeg mob ntshav qab zib hom 2 ntau dua li kev kho mob monotherapy nrog glimepiride. Raws li cov lus pom zoo tam sim no ntawm kev siv tshuaj sib xyaw ua ke nyob rau theem pib ntawm kev kho mob hauv cov neeg mob uas tsis ua tiav cov hom phiaj ntawm HbA1c, cov txiaj ntsig no yog qhov tseem ceeb rau kev tswj hwm cov neeg mob ntshav qab zib hauv Kaus Lim Kauslim.

Hauv cov kev tshawb fawb dhau los ntsuas qhov ua tau zoo thiab kev nyab xeeb ntawm kev sib xyaw ua ke nrog sitagliptin thiab metformin hauv Kauslim neeg Asmeskas, qhov kev ua tau zoo thiab kev tiv thaiv zoo ntawm kev sib xyaw no tau lees paub. Kev tshawb nrhiav tsis ntev los no tau piv rau kev ua haujlwm ntawm glycemic tswj kev siv tshuaj tiv thaiv metformin-ua ke nrog kev kho nrog sitagliptin, sulfonylurea derivative (glimepiride lossis

nrog hloov kho gliclazide) lossis pioglitazone hauv 116 yav dhau los tsis muaj kev kho mob Kauslim, cov neeg mob zoo li glycemic tswj ntawm peb cov kev sib txuas ua ke tau pom nyob rau hauv ntau ntawm theem pib HbA1c qib. Hauv lwm txoj kev tshawb nrhiav, cov neeg mob Kauslim uas yav tas los tau txais kev kho ua ke (ob zaug lossis peb zaug sib xyaw nrog metformin) tau txais kev txhim kho zoo hauv glycemic thaum lub sijhawm kho nrog sitagliptin ntawm koob tshuaj 100 mg / hnub. Hauv cov pab pawg uas hloov tawm ntawm glimepiride mus rau sitagliptin, qhov ntau zaus ntawm cov ntshav qog ntshav qab zib tsawg zuj zus, yog li, hauv cov neeg mob uas rov qab ua dua sai sai hypoglycemia, kev xaiv kev kho mob zoo sib xws kuj yuav raug txiav txim siab. Txawm hais tias pom tau qhov ua tau zoo ntawm kev sib xyaw ua ke, tsis tau muaj ib qho kev tshawb fawb ntawm Sit / Met hauv kev sib koom ua ke nyob rau yav tas los hauv Kauslim, thiab qhov kev tshawb fawb nthuav tawm yog thawj zaug.

Cov txiaj ntsig tau zoo ntawm kev siv cov tshuaj sib xyaw ua ke ntawm cov tshuaj tiv thaiv tau siv yav dhau los tau qhia rau lwm qhov kev sib txuas ua ke ob qho tshuaj sib txuas rau kev kho T2DM. Hauv kev xaiv, qhib, ntau tus neeg tshawb pom hauv cov pab pawg sib luag, 209 Cov neeg mob Kauslim tsis tau ua tiav T2DM kev tswj hwm, txawm hais tias metformin monotherapy, glimepiride / metformin FDC tau siv rau hauv kev txhaj tshuaj qis lossis metformin koob tshuaj tiv thaiv (tsis pub dhau 24 lub lis piam), glimepiride / metformin FDC dhau ib feem kaum koob tshuaj metformin hauv kev sib raug zoo rau kev tswj hwm glycemic. Qhov kev tshawb xyuas lub suab nrov tau xaus tias metformin / pioglitazone FDC zoo rau cov neeg mob ntshav qabzib insulin-tiv thaiv, uas tsis ua tiav cov hom phiaj kev kho mob uas tau ua tiav cov qauv kev pom zoo ntawm kev kho mob thaum lub sij hawm monotherapy. Hauv kev txheeb xyuas qhov tseeb ntawm ib qho chaw khaws ntaub ntawv ntawm 16,928 tus neeg mob, tau pom tias nrog rosiglitazone / metformin FDC, muaj qhov kev nthuav dav tseem ceeb ntawm kev kho mob piv rau kev kho mob uas suav nrog 2 tshuaj. Feem ntau, kev siv FDC tsis tuaj yeem tsuas yog txhim kho kev ua raws li kev kho mob, tab sis kuj tseem muaj cov ntaub ntawv zam rau lub siab dua, muaj kev yooj yim dua rau cov neeg mob, thiab muaj peev xwm nce nqi ntau dua. Kev siv ntawm Sit / Met FDC hauv txoj kev tshawb fawb nthuav tawm tuaj yeem yog ib qho ntawm cov xwm txheej uas cuam tshuam rau qhov kev ua raws siab rau kev kho (

Yuav luag 40% ntawm cov neeg mob nyob hauv txoj kev tshawb no tsis tau txais kev kho mob ntshav qab zib yav dhau los. Qhov ua tau zoo ntawm kev kho mob thawj zaug nrog Sit / Met FDC hauv cov neeg mob tsis kho yav tas los tau raug ntsuas hauv ntau cov kev tshawb fawb yav dhau los 35-37.Qhov ua tau zoo thiab kev nyab xeeb ntawm Sit / Met FDC piv rau pioglitazone tsis ntev los no tau kawm nyob hauv ob txoj kev tshawb nrhiav dav dav uas muaj kwv yees li 500 tus neeg mob, txhua tus tau lees paub qhov tseeb ntawm kev txhim kho glycemic tswj nrog Sit / Met 35, 37. Ntxiv rau,

Ntawm cov neeg mob nyob hauv pawg Sit / Met, tau pom qhov txo qis hauv lub cev qhov hnyav, thaum nyob hauv cov neeg mob los ntawm pawg pioglitazone, lub cev hnyav dua qub. Hauv lwm qhov muag dig ob zaug, kev tshawb fawb txog 1250 uas yav tas los tsis tau txais kev kho mob, lawv coj Sith / Met FDC lossis metformin, raws li nws cov txiaj ntsig, kev pib Sith / Met FDC kev kho mob piv nrog metformin monotherapy tau txais txiaj ntsig ntau dua li cov kev tiv thaiv glycemic, thiab cov ntsuas zoo sib xws ntawm kev poob phaus raug kaw thiab qis dua kev mob plab thiab mob raws plab. Ob qhov ua ntej lawm cov kev kho mob hauv cov neeg mob uas tsis tau kho dua nrog T2DM tom qab 18 lossis 24 lub limtiam ntawm Sit / Met txoj kev kho tau pom tias muaj kev txhim kho ntau ntxiv ntawm kev tswj glycemic dua li cov kev kho mob nrog tshuaj thiab / lossis cov placebo. Thiab qhov txiaj ntsig zoo tau txuas ntxiv mus tas li thoob plaws hauv kev kho mob, uas tau kav ntev txog 2 xyoos. Raws li cov kev qhia txog kev ntxuav tawm lub sijhawm uas tsim los ntawm txoj kev tshawb fawb tsim, qhov muaj txiaj ntsig Sieve / Met FDC zoo tshaj plaws uas tau sau tseg hauv qhov kev tshawb fawb tam sim no yuav qee qhov cuam tshuam qhov tseeb tias ntau tus neeg mob tsis tau txais kev kho ua ntej.

Hauv cov pab pawg glimepiride, qhov tshwm sim ntau dua ntawm cov ntshav qog ntshav tau tshwm sim piv nrog pawg Sit / Met FDC (20.1 thiab 5.5%). Txij li nyob rau hauv ntau dua 46% ntawm cov neeg mob qhov siab tshaj plaws lossis zaum kawg ntawm cov tshuaj yog 1 mg thiab tsuas yog hais txog 17% ntawm cov neeg mob tau txais 6 mg raws li qhov ntau tshaj lossis tag nrho cov koob tshuaj, cov txiaj ntsig no tau xav tau. Txawm hais tias qhov kev tshawb nrhiav tam sim no tso cai feem pua ​​ntawm ib koob tshuaj glimepiride ntawm kev txiav txim siab ntawm cov kws kho mob, nws yuav tsum raug sau tseg tias vim qhov muag dig ob ntawm qhov kev tshawb fawb, cov kws kho mob tsis muaj ntaub ntawv hais txog kev kho mob tshwj xeeb. Yog li, txoj kev tshawb fawb no qhia txog kev coj ua tiag tiag ntawm qhov uas ua rau kom qhov koob tshuaj glimepiride nce ntxiv. Qhov tseeb tseem ceeb yog tias nyob hauv pawg glimepiride, thaum thov cov koob tshuaj uas tsis tshua muaj siab, tau pom tias muaj kev kub siab ntau dua ntawm qhov mob ntshav qab zib tsawg. Muab cov kev txhawj xeeb cuam tshuam nrog hypoglycemia, kev siv cov sulfonylurea derivative therapy tshuaj tuaj yeem ncua qhov ua tiav ntawm lub hom phiaj glycemic. Tsis tas li ntawd, rau qhov ua kom ntshav qab zib tshwm sim los ntawm sulfonyl-urea derivatives, qhov kev siv tshuaj tiv thaiv kab mob tau pom tseeb, nrog rau kev rov qab sib txuam nrog kev nce qib hauv BMI, uas tuaj yeem piav qhia ntxiv rau qhov nce hauv lub cev hnyav hauv cov pab pawg glimepiride hauv txoj kev tshawb fawb tam sim no.

Hauv pawg Sit / Met FDC, qhov ntsuas qis ntawm kev kho tsis tau raug pom tau muab piv nrog glimepiride pawg (17.7 thiab 25.5%). Txawm hais tias qhov tso kev kawm tawm ntawm ob pawg neeg zoo li siab, muab ncua sijhawm ntawm kev kawm (39 lub lis piam), tus nqi no yog nyob rau hauv ib qho chaw tau.

Kev tshawb fawb nthuav tawm piv rau kev ua tau zoo thiab kev nyab xeeb ntawm kev kho mob monotherapy (glimepiride) thiab kev tiv thaiv ob qho kev tiv thaiv (Sit / Met FDC). Ib tug xov tooj ntawm cov kev tshawb fawb yav dhau los kuj tau piv rau kev kho mob monotherapy thiab kev sib txuas ua ke 31, 36, 37, yog li

txhua qhov kev ua xyem xyav txog kev xaiv tshuaj nyob hauv txoj kev kawm no tsis muaj qhov tseeb. Ib qho ntxiv, qhov tseeb tias glimepiride tam sim no yog thawj cov tshuaj rau cov neeg mob ntshav qab zib hom 2 hauv Kauslim yog qhov laj thawj ntxiv rau nws siv hauv pawg sib piv hauv qhov kev tshawb nrhiav tam sim no.

Txawm hais tias 628 cov neeg mob tau kuaj xyuas rau txoj kev tshawb no, tsuas yog 292 tus neeg tau txais randomized rau ib pab pawg kho mob twg.Feem ntau cov neeg mob uas tsis nyob hauv qhov kev tshuaj ntsuam tau vim yog qhov HbA1c muaj nuj nqis heev lossis tsis tshua muaj nuj nqis, kev tsim muaj peev xwm tsis paub meej, thiab lwm yam ua tsis tau raws li cov qauv xaiv. Cov yam ntxwv ntawm ntau tus neeg mob tsis tau ua tiav raws li cov lus teev tseg nyob rau lub sijhawm qhia paub vim tias muaj HbA1c tsawg, uas tej zaum vim muaj kev hloov pauv hauv kev ua neej ntawm cov neeg mob thaum lub sijhawm 6-lub hlis qhia lub sijhawm. Qhov no qhia tau qhov txiaj ntsig zoo ntawm kev ua neej noj qab haus huv ntawm kev mob ntshav qab zib. Tsis tas li ntawd, raws li tau tham txog yav dhau los, kev pom zoo nrog kev nce ntxiv ntawm glimepiride tuaj yeem tsis txaus, uas yuav cuam tshuam cov txiaj ntsig ntawm txoj kev tshawb no.

Hauv kev xaus, nws yuav tsum raug sau tseg tias kev siv tshuaj sib xyaw ua ke nyob rau theem thaum ntxov ntawm kev kho mob ua raws li cov qauv niaj hnub ntawm kev kho mob rau ntshav qab zib. Txoj kev tshawb nrhiav tam sim no yog thawj zaug los ntsuas qhov kev nyab xeeb thiab ua tau zoo ntawm Sit / Met hauv kev sib xyaw ua ke piv rau glimepiride hauv Kauslim cov neeg mob T2DM yog kev kho thaum pib. Cov txiaj ntsig ntawm txoj kev kawm no qhia tias Sit / Met FDC tuaj yeem yog qhov kev xaiv kho mob zoo rau cov neeg mob ntshav qab zib hom 2 piv nrog glimepiride monotherapy. Cov kev tshawb fawb txuas ntxiv yog xav tau los soj ntsuam cov kev mob mus ntev ntawm Sit / Met FDC thiab cov txiaj ntsig ntawm kev sib xyaw no ntawm cov ntsiab lus kawg ntawm cov hlab plawv, nrog rau kev tuag ntawm cov neeg mob T2DM.

Combination Kev sib xyaw ntawm Sit / Met raws li thawj qhov kev pabcuam tau muab kev txhim kho ntau ntxiv hauv kev yoo glycemic tswj thiab yoo plasma ntshav qab zib (GPN) 30 lub lis piam tom qab pib piv nrog glimepiride. Tsis tas li ntawd, nrog kev siv Sit / Met, ib qho me ntsis ntawm lub cev qhov hnyav thiab tsis tshua pom lub qog hypoglycemia tau muab piv nrog kev kho glimepiride.

Qhov kev tshawb nrhiav tam sim no ntsuas thawj zaug rau kev nyab xeeb thiab ua haujlwm ntawm Sit / Met hauv ib qho chaw ruaj khov

kev sib xyaw ua ke piv nrog glimepiride hauv Kauslim cov neeg mob uas muaj hom 2 mob ntshav qab zib mellitus (T2DM) raws li kev pib kho.

■ Cov ntsiab lus tseem ceeb ntawm txoj kev tshawb no: kev sib xyaw ntawm Sit / Met raws li kev kho qhov pib tau muab kev txhim kho ntau ntxiv nyob rau hauv theem ntawm HbA1c thiab GPN 30 lub lis piam tom qab pib piv nrog glimepiride. Glimepiride txoj kev kho ua rau qhov hnyav hauv lub cev nce ntxiv, thaum siv Sit / Met tau ua rau me ntsis poob qis thiab tsis tshua muaj kev mob ntshav qab zib.

Qhov kev tshawb fawb no muab dab tsi: Qhov kev tshawb fawb no ua ntej ntsuas kev nyab xeeb thiab ua tau zoo ntawm kev sib xyaw ntawm Sit / Met piv nrog glimepiride monotherapy ua kev kho mob thawj zaug hauv cov neeg mob Kauslim ntshav qab zib hom 2.

Txoj kev kawm no tau pab nyiaj los ntawm MSD International GmbH, uas yog cov koom tes hauv Merck & Co., Inc. (Kenilworth, New Jersey, USA). Tus neeg pab txhawb nqa tau koom nrog tsim qhov kev tshawb fawb, sau, tshuaj xyuas thiab tshuaj xyuas cov ntaub ntawv, thiab ntxiv rau hauv kev sau ntawm daim ntawv tshaj tawm. Kev pab hauv kev sau cov ntawv kho mob tau muab los ntawm Tejas Tirodkar (Kev Sib Tham Cactus, Mumbai, Is Nrias teb). Txoj kev pabcuam no tau pab nyiaj los ntawm MSD Korea Ltd. Cov sau phau ntawv ua tsaug rau txhua tus kws tshawb fawb uas tau koom nrog txoj kev tshawb no: Young Sik Choi (Evangelical Clinic ntawm Kosin University), Jong Ryeal Hahm (Lub Tsev Kho Mob ntawm Gyeongsang State University), Mi Kyung Kim (Maryknoll Medical Center), Ja Young Park (St. Mary's Busan Clinic) ), Quav Rae

Cho (Fatima Clinic hauv Changwon), Kyung Mook Choi (Guro Clinic ntawm Kauslim University), Dae Jung Kim (Aju University Clinic), Ki Young Lee (Gil Medical Center ntawm Gachon University), Chong Hwa Kim (Ilsan Clinic, State Health Insurance Service) ), Dong Jun Kim (Ilsan Peck Clinic, University of Inje), Choon Hee Chung (Separate Christian Clinic rau Wongju), Ji Oh Mok (Tsev Kho Mob Phocong ntawm Sun-Chun-hyang University) thiab Sung Hee Choi (Bundang Clinic, State University of Seoul).

SJL yog ib tus neeg ua haujlwm ntawm MSD Korea Ltd, tag nrho lwm tus kws sau ntawv tsis muaj kev tsis sib haum xeeb los ntawm kev txaus siab yuav tsum tau nthuav tawm.

Txoj kev tshawb no yog teev npe hauv Cli-nicalTrials.gov cov ntaub ntawv (ID: NCT00993187).

COV NTAUB NTAWV QHIA TXOJ CAI

Kim Hauv Joo, Lub Chaw Haujlwm ntawm Endocrinology thiab Metabolism, Lub Chaw Haujlwm Tiv Thaiv, Lub Tsev Kho Mob Hauv Tsev Kawm Ntawv Busan State University, South Kauslim E-mail: [email protected]

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24. Herman G.A., Bergman A., Stevens C., li al. Qhov ntxim nyiam ntawm qhov ncauj ntawm qhov ncauj ntawm sitagliptin, dipeptidyl peptidase-4 inhibitor, ntawm kev nce qib thiab ntshav qabzib cov ntshav tom qab kev soj ntsuam qhov ncauj qab zib hauv cov neeg mob ntshav qab zib hom 2. J Clin Endocrinol Metab. 2006, 91: 4612-9.

25. Goldstein B.J., Feinglos M.N., Lunceford J.K. Johnson J., li al., Sitagliptin 036 Kev Kawm Pab Pawg. Cov txiaj ntsig ntawm kev pib ua ke nrog kev kho mob nrog sitagliptin, dipeptidyl peptidase-4 inhibitor, thiab metformin ntawm glycemic tswj hauv cov neeg mob uas muaj ntshav qab zib hom 2. Ntshav Qab Zib Kho Mob. 2007, 30: 1979-87.

26. Charbonnel B., Karasik A., Liu J., Wu M., li al., Sitagliptin Kawm 020 Pab Pawg. Kev ua tau zoo thiab kev nyab xeeb ntawm dipeptidyl peptidase-4 inhibitor sitagliptin ntxiv rau kev kho mob metformin txuas mus ntxiv rau cov neeg mob ntshav qab zib hom 2 tsis txaus tswj nrog metformin ib leeg. Ntshav Qab Zib Kho Mob. 2006, 29: 2638-43.

27. Miettinen O., Nurminen M. Kev sib piv ntawm ob qho nqi. Txoj Cai Med. Xyoo 1985, 4: 213-26.

28. Chwieduk C.M. Sitagliptin / metformin ua ke-koob tshuaj sib xyaw: Hauv cov neeg mob uas muaj ntshav qab zib hom 2 mellitus. Tshuaj Xyoo 2011, 71: 349-61.

29. Lee Y.K., Nkauj S.O., Kim K.J., et al. Cov hauj lwm zoo Glycemic ntawm metformin-based dual-ua ke nrog kev kho mob nrog sulphonylurea, pioglitazone, lossis DPP4-inhibitor hauv tshuaj-naas Korean hom 2 cov neeg mob ntshav qab zib. Ntshav Qab Zib Metab J. 2013, 37: 465-74.

30. Chung H.S., Lee M.K. Kev ua tau zoo ntawm sitagliptin thaum ntxiv rau cov kev kho mob txuas ntxiv hauv cov neeg kawm Kauslim nrog hom 2 mob ntshav qab zib mellitus. Ntshav Qab Zib Metab J. 2011, 35: 411-7.

31. Kim H.S., Kim D.M., Cha B.S., li al. Kev ua tau zoo ntawm glimepiride / metformin tsau-koob tshuaj sib xyaw vs metformin hloov pauv ntawm hom 2 mob ntshav qab zib cov neeg mob tsis txaus tswj ntawm qis tshuaj metformin monotherapy: ib qho kev tsim kho, qhib daim ntawv lo, cov pab pawg sib tw, cov kws tshaj lij kev kawm hauv Kaus Lim Kauslim. J Kev Tshawb Nrhiav Ntshav Qab Zib. Xyoo 2014, 5: 701-8.

32. Derosa G., Salvadeo S.A. Pioglitazone thiab metformin tsau-koob tshuaj sib xyaw ua ke hauv hom 2 mob ntshav qab zib mellitus: cov ntaub ntawv pov thawj-tshuaj xyuas los ntawm nws qhov chaw kho mob. Cov Ntawv Pov Thawj. Xyoo 2008, 2: 189-98.

33. Vanderpoel D.R., Hussein M.A., Watson-Heidari T., Perry A. Ua raws li cov koob tshuaj ntawm rosiglitazone maleate / metformin hydrochloride nyob rau hauv cov ncauj lus nrog hom 2 mob ntshav qab zib mellitus: kev tsom xam cov ntaub ntawv pov thawj rov qab. Clin Ther. 2004, 26: 2066-75.

34. Bain S.C. Kev kho mob ntawm hom 2 mob ntshav qab zib mellitus nrog cov tshuaj rau cov ncauj lus: kev kho kom zoo rau kev kho ua ke. Kev Ua Siab Phem. 2009, 15: 750-62.

35. Perez-Monteverde A., Seck T., Xu L., li al. Kev ua tau zoo thiab kev nyab xeeb ntawm sitagliptin thiab kev txhaj tshuaj tiv thaiv sib xyaw ua ke ntawm sitagliptin thiab metformin vs. pioglitazone hauv tshuaj yeeb na nave cov neeg mob ntshav qab zib hom 2. Int J Clin Kev Xyaum. Xyoo 2011, 65: 930-8.

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Pauv npe ntawm kev npaj: Amaril®. Lub npe txawv teb chaws tsis muaj npe: glimepiride. Dosage daim ntawv thiab muaj pes tsawg leeg: ntsiav tshuaj. Amaryl® 1.2.3.4 mg: 1 ntsiav tshuaj muaj 1.2.3.4 mg ntawm glimepiride, feem. Pharmacotherapeutic pawg: hypoglycemic tus neeg sawv cev rau kev tswj hwm qhov ncauj ntawm III tiam sulfonylurea pawg. Kev siv rau kev siv: hom 2 mob ntshav qab zib mellitus (hauv kev kho mob monotherapy lossis ua ib feem ntawm kev sib xyaw ua ke nrog metformin lossis insulin). Kev noj tshuaj thiab kev tswj hwm: Amaril® ntsiav tshuaj noj tag nrho yam tsis muaj ntxo, haus kua kom ntau about (li 0.5 khob). Thawj qhov tshuaj yog 1 mg ntawm glimepiride 1 zaug ib hnub. Nws raug nquahu kom nce lub koob tshuaj nyob rau hauv kev saib xyuas tsis tu ncua ntawm cov ntshav qabzib thiab nyob rau hauv raws li cov qib nce ntxiv hauv qab no: 1 mg-2 mg-Zmg-4 mg-6 mg-8 mg nrog ncua sijhawm ntawm 1-2 lub lis piam. Nws tau noj ua ntej noj tshais tag nrho lossis pluas mov tseem ceeb. Cov tshuaj tiv thaiv: hom 1 mob ntshav qab zib mellitus, mob ntshav qab zib ketoacidosis, mob ntshav qab zib thiab ua rau lub ntsej muag tsis hnov ​​qab, ua kom lub ntsej muag txhawm rau lub ntsej muag lossis ib qho ntawm cov tshuaj tiv thaiv kab mob, rau lwm yam sulfonylureas lossis sulfonamides, cev xeeb tub thiab lactation, mob hnyav rau lub cev, mob raum tsis zoo, cov menyuam yaus tsis zoo. hnub nyoog (tsis muaj cov ntaub ntawv tshawb fawb txog kev siv), muaj kab mob tsis tshua muaj keeb (galactose intolerance, lactase deficiency lossis glucose-galactose malabsor) btsiya). Nrog ceev faj: hauv thawj lub lis piam ntawm kev kho mob, nyob rau ntawm qhov muaj kev pheej hmoo txaus rau kev txhim kho ntshav qab zib (saib cov lus qhia ua tiav rau kev siv tshuaj kho mob), rau cov kab mob sib kis, hloov pauv hauv txoj kev ua neej ntawm cov neeg mob, glucose-6-phosphate dehydrogenase deficiency, thiab gastrointestinal malabsorption (plab hnyuv ob leeg, plab hnyuv paresis).Cov lus qhia tshwj xeeb: hauv thawj lub lis piam ntawm kev kho mob, qhov kev pheej hmoo ntawm ntshav siab tuaj yeem nce ntxiv - ua tib zoo saib xyuas glycemia. Yog tias muaj kev mob tshwj xeeb hauv kev ntxhov siab (kev mob, kev phais mob, kev kis tus kab mob febrile), yuav tsum tau hloov mus ib ntus rau kev kho tshuaj insulin. Kev cuam tshuam nrog lwm cov tshuaj: glimepiride yog metabolized los ntawm cytochrome P4502C9 (CYP2C9), uas yuav tsum tau coj mus rau hauv tus account thaum siv ib txhij nrog cov inducers (xws li rifampicin) lossis inhibitors (e.g. fluconazole) CYP2C9. Rau kev cuam tshuam nrog lwm cov tshuaj, saib cov lus qhia ua tiav rau kev siv tshuaj. Sab tshwm sim: hypoglycemia. Muaj qee zaus: xeev siab, ntuav, tsis xis nyob rau hauv epigastrium, mob plab zawv plab, muaj kev hloov pauv tsis tu ncua ntawm kev ua haujlwm ntawm daim siab enzymes thiab / lossis cholestasis, kab mob siab, ua rau pom kev tsis txaus siab vim muaj kev hloov pauv hauv cov ntshav ntxiv, thrombocytopenia, leukopenia, hemolytic anemia, erythrocytopenia, granulocyt , agranulocytosis, pancytopenia, pruritus, urticaria, tawv nqaij ua xua, ua xua vasculitis, ua xoo. Kev noj ntau dhau: mob siab rau noj ntau dhau, nrog rau kev kho ntev nrog cov tshuaj glimepiride ntau dhau tuaj yeem ua rau muaj kev txhim kho mob ntshav qab zib, ua rau lub neej muaj ntshav qab zib. Sai li sai tau dhau qhov kev siv tshuaj ntau dhau lawm, koj yuav tsum qhia koj tus kws kho mob sai. Kev mob ntshav siab ntshav qab zib tuaj yeem tso tseg sai sai los ntawm kev noj zaubmov sai sai. ATX Code: A10BB12. Hnub tas sij hawm: 3 xyoos. Ua ntej yuav teem caij, koj yuav tsum nyeem cov lus qhia rau kev siv tshuaj los ntawm cov tshuaj

1. Daim ntawv sau npe ntawm cov tshuaj Amaril® rau kev siv tshuaj medical 0 N015530 / 01. 2. Cov lus qhia rau kev siv tshuaj Amaril®, rau ib tus lej P N015530 / 01-131216.3. Ametov A.C. nrog eoavt. Muaj peev xwm ntawm kev siv glimepiride los pib kho kev kho suab thaj. Cov txiaj ntsig ntawm Amaril-MONO kev soj ntsuam kawm. Ntshav Qab Zib mellitus, 2013: No. 3. 4. Glinkina I.V. li al,, kev ua tau zoo thiab kev nyab xeeb ntawm kev sib xyaw dawb ntawm glimepiride thiab metformin hauv cov neeg mob uas muaj hom 2 mob ntshav qab zib mellitus hauv kev sim kho mob tiag tiag: ib qho kev soj ntsuam kev soj ntsuam // Siv Tshuaj Kho Kom Zoo. Endocrinology 2/2012: 16-20.5. Zaitseva N.V. li al., <Kev kho mob sib xyaw nrog glimepiride thiab metformin hauv cov neeg mob ntshav qab zib hom 2. Cov kev tshwm sim ntawm Lavxias teb sab kev soj ntsuam kawm // Farmateka. - 2014. - No. 16.6. www.apteka.ru, nkag mus rau lub xaib kawg - 07/06/2017. "Tus nqi ntawm ib ntsiav tshuaj nyob rau hauv ib pob No. 90 yog 25% qis dua tus nqi ntawm ib ntsiav tshuaj hauv pob 30 rau kev kho mob sib piv.

Sawv cev ntawm Sanofi-aventis lub cev tuag JSC (Fabkis) 125009, Moscow, ul. Tverskaya, d. 22. Xov tooj: (495) 721-14-00, fax mus: (495) 721-14-11, www.sanofi.ru.SARU.GLI.17.06.0953

36. Reasner C., Olansky L., Seck T. L., li al. Cov txiaj ntsig ntawm kev kho thaum pib nrog kev txhaj tshuaj tiv thaiv sib xyaw ua ke ntawm sitagliptin thiab metformin piv nrog metformin monotherapy rau cov neeg mob hom 2 mob ntshav qab zib mellitus. Ntshav Qab Zib Obib Metab. Xyoo 2011, 13: 644-52.

37. Wainstein J., Katz L., Engel S.S., li al. Kev pib kho nrog kev kho kom haum-sib xyaw ua ke ntawm sitagliptin thiab metformin ua rau muaj kev txhim kho ntau dua nyob rau hauv glycemic tswj piv nrog pioglitazone

tshuaj mob ntshav qab zib rau cov neeg mob ntshav qab zib hom 2. Ntshav Qab Zib Obib Metab. Xyoo 2012, 14: 409-18.

Kws Tshuaj

Metformin + sitagliptin yog kev sib koom ua ke ntawm ob yam tshuaj yeeb dej caw (DV) nrog kev sib txuam (sib ntxiv) cov tshuab ntawm kev nqis tes - sitagliptin, DPP-4 inhibitor, thiab metformin, tus sawv cev ntawm chav kawm biguanide. Nws siv los txhim kho glycemic tswj hauv cov neeg mob uas muaj ntshav qab zib hom 2.

Thaum tswj hwm qhov ncauj, sitagliptin yog cov nquag xaiv DPP-4 inhibitor, npaj rau kev kho mob hom 2 mob ntshav qab zib mellitus.Qhov teebmeem ntawm cov tshuaj ntawm cov chav kawm ntawm cov tshuaj - DPP-4 inhibitors yog kho kom haum xeeb los ntawm kev ua kom muaj zog ntawm incretins. Los ntawm inhibiting DPP-4, sitagliptin tsub kom qhov siab ntxiv ntawm ob qho kev paub ua kom muaj cov tshuaj hormones ntawm tsev neeg incretin: GLP-1 thiab HIP.Tus incretins yog ib feem ntawm cov txheej txheem kho mob sab hauv lub zog rau kev tswj hwm cov ntshav qabzib homeostasis. Thaum cov ntshav qabzib feem ntau yog nce siab ntshav qabzib, GLP-1 thiab GUIs nce cov khoom cua thiab tso kua ntshav tawm los ntawm cov roj ntsha pancreatic beta hlwb. GLP-1 tseem tseem ceeb kev tsis txaus siab ntawm glucagon los ntawm pancreatic alpha cells, yog li txo cov synthesis ntawm cov piam thaj hauv lub siab. Qhov kev ua haujlwm ntawm qhov kev sib txawv no txawv ntawm cov txheej txheem ntawm kev ua ntawm sulfonylurea derivatives, uas txhawb kev tso tawm ntawm insulin txawm tias muaj ntshav qabzib ntau ntau, uas yog fraught nrog txoj kev loj hlob ntawm sulfonylinduced hypoglycemia tsis yog hauv cov neeg mob uas muaj ntshav qab zib 2 mellitus, tab sis kuj rau cov neeg noj qab haus huv. Ua tus xaiv thiab muaj kev cuam tshuam zoo ntawm DPP-4 enzyme, sitagliptin hauv kev kho kom zoo ntau tsis cuam tshuam cov kev ua haujlwm ntawm cov enzymes DPP-8 lossis DPP-9. Sitagliptin sib txawv hauv cov qauv tshuaj thiab cov tshuaj pharmacological los ntawm cov qauv tshuaj tiv thaiv ntawm GLP-1, insulin, sulfonylurea derivatives lossis meglitinides, biguanides, gamma receptor agonists ua haujlwm los ntawm peroxis proliferator (PPARγ), alpha-glucosidase inhibitors thiab amylin analogues.

Metformin yog ib hom tshuaj hypoglycemic uas ua rau muaj cov ntshav qabzib ntau nyob rau hauv cov neeg mob ntshav qab zib hom 2, txo qis cov ntshav qabzib thiab postprandial ntshav qabzib. Nws cov tshuaj pharmacological ntawm kev ua txawv ntawm cov txheej txheem ntawm kev ua ntawm qhov ncauj hypoglycemic cov neeg sawv cev ntawm lwm cov chav kawm.

Metformin txo cov synthesis ntawm cov piam thaj hauv lub siab, kev nqus ntawm cov piam thaj hauv cov hnyuv thiab nce insulin rhiab heev los ntawm kev txhim kho kev nkag siab thiab siv cov suab thaj. Tsis zoo li sulfonylurea derivatives, metformin tsis ua rau cov ntshav qog ntshav qab zib hauv cov neeg mob uas muaj ntshav qab zib hom 2 lossis cov neeg muaj kev noj qab haus huv (tshwj tsis yog qee yam, saib "Kev Txwv rau kev siv", Metformin) thiab tsis ua rau hyperinsulinemia. Thaum kho nrog metformin, insulin secretion tsis hloov, thaum lub sij hawm qhov tseem ceeb ntawm cov tshuaj insulin rau ntawm lub plab khoob thiab tus nqi txhua hnub ntawm cov ntshav plasma concentration ntawm insulin yuav txo qis.

Kev tswj hwm qhov ncauj ntawm ib zaug xwb ntawm sitagliptin rau cov neeg mob uas muaj ntshav qab zib hom 2 ua rau muaj kev cuam tshuam ntawm cov kev ua si ntawm DPP-4 enzyme rau 24 teev, uas yog nrog los ntawm ob mus rau peb zaug ntau ntxiv nyob rau hauv kev ua kom muaj zog ntawm cov ntshav dhia ua ke GLP-1 thiab HIP, qhov nce ntawm ntshav plasma concentration ntawm insulin thiab C-peptide, txo qis hauv kev ua haujlwm ntawm cov ntshav gluculin. yoo plasma ntshav qabzib cov ntsiab lus, nrog rau txo qis ntawm glycemic kev hloov pauv tom qab cov piam thaj lossis zaub mov thau khoom.

Kev coj ntawm sitagliptin nyob rau hauv ib koob tshuaj txhua hnub ntawm 100 mg rau 4-6 lub hlis txhim kho txoj haujlwm ntawm pancreatic beta hlwb hauv cov neeg mob uas muaj hom 2 mob ntshav qab zib mellitus, raws li muaj pov thawj los ntawm cov kev hloov pauv hauv cov cim xws li HOMA-β (kev ntsuas ntawm homeostasis hauv qauv-β), qhov sib piv proinsulin / insulin, kev ntsuam xyuas ntawm kev tawm tsam ntawm pancreatic beta hlwb raws li lub vaj huam sib luag ntawm kev ntsuam xyuas kev rov qab ua siab rau cov zaub mov noj. Raws li kev tshawb fawb soj ntsuam ntawm qib II thiab III, qhov kev ua haujlwm ntawm glycemic tswj ntawm sitagliptin hauv kev tswj hwm ntawm 50 mg 2 zaug hauv ib hnub tau piv nrog cov txiaj ntsig ntawm kev tswj hwm ntawm 100 mg ib zaug ib hnub.

Hauv kev xaiv, muab cov placebo-tswj, ob lub qhov muag, ob zaug sim 4-lub sijhawm hla kev kawm hauv cov neeg ua haujlwm pab dawb noj qab haus huv, cov teebmeem ntawm sitagliptin hauv kev sib xyaw nrog metformin, lossis tsuas yog sitagliptin, lossis tsuas yog metformin, lossis placebo ntawm kev hloov pauv plasma ntau ntawm kev ua haujlwm thiab tag nrho GLP-1 thiab qabzib tom qab kev tswj hwm tau kawm cov khoom noj. Cov txiaj ntsig ntawm qhov hnyav nruab nrab ntawm kev saib xyuas ntawm nquag GLP-1 4 teev tom qab noj mov tau nce thaj tsam li 2 zaug tom qab noj xwb sitagliptin lossis tsuas yog metformin piv nrog cov placebo. Kev tswj hwm ua ke ntawm sitagliptin thiab metformin ua rau kom suav daws cov nyhuv nrog qhov nce 4 npaug ntawm qhov kev coj ua ntawm lub zog GLP-1 piv nrog qhov muaj zog hauv cov pab pawg placebo.

Txais tos ntawm sitagliptin ib leeg tau nrog los ntawm kev nce ntxiv hauv qhov kev xav ntawm tsuas yog ua haujlwm GLP-1 vim kev txwv tsis pub DPP-4 enzyme, thaum kev tswj hwm ntawm metformin ib leeg tau nrog los ntawm kev sib luag hauv qhov siab ntawm tag nrho thiab nquag GLP-1. Cov ntaub ntawv tau txais los cuam tshuam ntau cov txheej txheem hauv qab qhov nce hauv kev mloog zoo ntawm cov nquag GLP-1 tom qab noj ob lub tshuaj no. Cov txiaj ntsig ntawm txoj kev tshawb no kuj qhia tau tias nws yog sitagliptin, thiab tsis yog metformin, uas tau muab kev nce siab hauv kev ua kom muaj zog ntawm GLP-1.

Hauv cov kev tshawb fawb hauv cov neeg ua haujlwm noj qab haus huv, noj cov tshuaj sitagliptin tsis yog nrog lub suab thaj txo qis thiab tsis ua rau lub cev tsis muaj ntshav qab zib, uas tau lees tias cov piam thaj hauv thaj ua haujlwm ntawm insulinotropic nyhuv thiab kev cuam tshuam ntawm glucagon synthesis.

Hauv kev tshawb nrhiav, kev siv tshuaj placebo nrog cov neeg mob ntshav siab, ua ke siv cov tshuaj tiv thaiv kabmob (ib lossis ntau daim ntawv: ACE inhibitors, ARA II, BKK, beta-blockers, diuretics) nrog sitagliptin feem ntau pom zoo los ntawm cov neeg mob. Hauv pawg no ntawm cov neeg mob, sitagliptin qhia pom tias muaj qhov zoo me ntsis: nyob rau hauv ib koob tshuaj txhua hnub ntawm 100 mg, sitagliptin txo tus nqi nruab nrab niaj hnub mob tus nqi ntawm SBP los ntawm 2 hli Hg. piv rau pab pawg placebo. Hauv cov neeg mob uas muaj ntshav siab, tsis muaj kev tiv thaiv hypotensive.

Ntxim rau cov kab mob electrophysiology

Hauv kev tshawb nrhiav, kev siv cov placebo tshuaj tiv thaiv kab mob hauv cov neeg tuaj yeem noj qab haus huv, sitagliptin tau siv ib zaug ntawm 100 lossis 800 mg (8 npaug ntawm qhov ntau ntawm cov koob pom zoo) lossis placebo. Tom qab noj cov tshuaj pom zoo rau kev kho mob ntawm ib qho txiaj ntsig ntawm cov tshuaj ntawm lub sijhawm QT luv, zoo li thaum lub sijhawm nws cov ntshav C_max , thiab ntawm lwm yam ntsiab lus pov thawj thoob plaws hauv qhov kev tshawb fawb, tsis tau tshawb pom. Tom qab noj 800 mg, qhov siab tshaj plaws nyob rau hauv cov placebo-kho tau txhais tau hais tias hloov lub sijhawm ntawm QT sib piv rau thawj zaug tus nqi 3 teev tom qab noj cov tshuaj yog 8 ms. Ib qho kev nce zoo li ntawd tau raug ntaus nqi tseem ceeb. Tom qab noj 800 mg, lub plasma C tus nqi_max Sitagliptin yog kwv yees li 11 npaug ntau dua qhov muaj txiaj ntsig tom qab siv tshuaj kho 100 mg.

Cov txiaj ntsig ntawm kev tshawb nrhiav bioequivalence hauv cov neeg ua haujlwm pab dawb noj qab haus huv tau qhia tias kev sib xyaw ua ke (metformin + sitagliptin) 500/50 mg thiab 1000/50 mg yog zoo sib xws rau kev tswj hwm txawv ntawm cov koob tshuaj tsim nyog ntawm sitagliptin thiab metformin.

Muab pov thawj pom kev sib luag ntawm cov ntsiav tshuaj muaj qis tshaj plaws thiab siab tshaj plaws ntawm cov tshuaj metformin, cov ntsiav tshuaj nrog cov tshuaj nruab nrab ntawm cov tshuaj metformin (metformin + sitagliptin) 850/50 mg kuj tau muab rau bioequivalence, muab hais tias cov tshuaj tiv thaiv cov tshuaj tiv thaiv tau muab sib xyaw ua ke hauv cov ntsiav tshuaj.

Sitagliptin. Qhov tsis txaus ntseeg txog kev yooj yim ntawm sitagliptin yog kwv yees li 87%. Noj sitagliptin tib lub sijhawm ua cov rog rog tsis muaj kev cuam tshuam cov pharmacokinetics ntawm kev sib xyaw.

Metformin. Qhov peev xwm tsis txaus ntseeg ntawm metformin thaum noj ntawm lub plab khoob ntawm koob tshuaj 500 mg yog 50-60%. Cov txiaj ntsig ntawm kev tshawb fawb ntawm ib qho kev txhaj tshuaj ntawm metformin hauv koob tshuaj txij li 500 txog 1500 mg thiab los ntawm 850 txog 2550 mg qhia txog kev ua txhaum ntawm qhov koob tshuaj sib npaug nrog nce ntau dua, uas ntau dua vim txo qis dua li qhov cuam tshuam sai. Siv cov khoom noj tsis tshua txaus nrog txo tus nqi thiab tus nqi ntawm nqus metformin, raws li muaj pov thawj los ntawm kev txo ntshav ntshav C_max los ntawm kwv yees li 40%, ib qho kev txo qis hauv AUC ntawm 25%, thiab lub sijhawm 35-feeb kev ncav cuag C_max tom qab ib koob tshuaj metformin nyob rau hauv ib koob tshuaj 850 mg ib txhij nrog cov zaub mov piv nrog qhov muaj nuj nqis ntawm cov coj ua tom qab noj ib qho koob tshuaj sib xws ntawm cov tshuaj ntawm ib plab khoob. Cov kab mob tseem ceeb hauv kev txo qis ntawm qhov tsis muaj pharmacokinetic tsis tau tsim.

Sitagliptin. Nruab Nrab V_ss tom qab siv ib zaug txhaj, 100 mg ntawm sitagliptin hauv cov neeg tuaj yeem noj qab haus huv yog kwv yees li 198 l. Qhov feem ntawm sitagliptin thim rov qab khi rau cov protein ntau yog me me (38%).

Metformin. V_d metformin tom qab noj ib zaug xwb ntawm 850 mg ib koob (654 ± 358) l. Metformin tsuas yog rau qee qhov me me khi rau cov ntshav protein. Metformin yog ib feem thiab muab faib ua cov ntshav liab kom tsis tu ncua. Thaum siv cov metformin hauv koob tshuaj thiab cov qauv pom zoo, ntshav C_ss (feem ntau C_max tsis dhau 5 μg / ml txawm tias tom qab siv ntau tshaj plaws.

Sitagliptin. Kwv yees li 79% ntawm sitagliptin tsuas yog tsis hloov pauv los ntawm lub raum, kev hloov pauv hauv lub cev yog qhov tsawg heev.

Tom qab 14 C-daim ntawv lo sitagliptin raug muab ntawm qhov ncauj, kwv yees li 16% ntawm kev tswj hwm hauv radioactivity tau tawm nrog rau cov tshuaj sitagliptin metabolites. Ib co ntsiab lus ntau ntawm 6 sitagliptin metabolites tau pom tias tsis pab txhawb cov ntshav DPP-4 inhibitory kev ua si ntawm sitagliptin. Hauv kev tshawb fawb hauv vitro isoenzymes ntawm cytochrome system CYP3A4 thiab CYP2C8 tau pom tias yog cov neeg tseem ceeb uas cuam tshuam nrog cov kev siv metabolism ntawm sitagliptin.

Metformin. Tom qab ib qho kev tswj hwm iv rau metformin cov neeg ua haujlwm noj qab haus huv, yuav luag tag nrho cov koob tshuaj tau raug hloov tawm tsis hloov los ntawm lub raum. Kev hloov pauv ntawm daim siab thiab tawm nrog lub plab nrog tsis tshwm sim.

Sitagliptin. Tom qab 14 C-daim ntawv lo sitlliptin tau noj los ntawm cov neeg ua haujlwm noj qab haus huv, yuav luag txhua tus neeg tshaj tawm txoj haujlwm raug tshem tawm ntawm lub cev hauv ib lub lis piam, suav nrog 13% dhau los ntawm txoj hnyuv thiab 87% dhau los ntawm lub raum. Nruab Nrab T_1/2 sitagliptin nrog qhov ncauj tswj hwm ntawm 100 mg yog kwv yees li 12.4 teev, kev tshem lub raum yog kwv yees li 350 ml / min.

Kev zam ntawm sitagliptin yog nqa tawm feem ntau los ntawm kev ua haujlwm hauv lub raum los ntawm lub tshuab ntawm kev ua kom nquag plias. Sitagliptin yog cov txheej txheem ntawm kev hloov pauv ntawm cov tib neeg cov anions ntawm peb hom (hОAT-3), uas koom nrog kev tshem tawm ntawm sitagliptin los ntawm lub raum. Cov kab mob tseem ceeb ntawm kev koom tes ntawm hOAT-3 hauv kev thauj khoom ntawm sitagliptin tseem tsis tau tsim. P-gp tuaj yeem cuam tshuam txog kev tshem tawm cov teeb meem ntawm sitagliptin (raws li lub cev), tab sis P-gp inhibitor cyclosporin tsis txo qhov pom kev rov ua haujlwm ntawm sitagliptin.

Metformin. Kev tshem tawm ntawm cov metformin ntau dua li cov neeg uas muaj creatinine tshem tawm los ntawm 3.5 zaug, qhia txog lub raum ua kom zoo li qhov tseem ceeb ntawm kev nthuav tawm. Tom qab noj cov tshuaj metformin, kwv yees li 90% ntawm cov tshuaj nqus tau zoo yog tso tawm los ntawm lub raum thaum thawj 24 teev thaum muaj ntshav T_1/2 kwv yees li 6.2 teev, nyob rau hauv cov ntshav cov nqi no tau txuas ntxiv mus rau 17.6 teev, qhia txog kev tuaj yeem koom nrog cov qe ntshav liab ua qhov ua kom muaj qhov faib ntxiv.

Pharmacokinetics ntawm cov neeg mob ib leeg

Yam 2 Cov Neeg Mob Ntshav Qab Zib

Sitagliptin. Cov tshuaj pharmacokinetics ntawm sitagliptin hauv cov neeg mob ntshav qab zib hom 2 zoo ib yam li cov pharmacokinetics hauv cov neeg noj qab haus huv.

Metformin. Nrog rau cov kev ua kom lub raum ua haujlwm, cov chaw muag tshuaj tom qab ib zaug thiab rov ua dua ntawm cov tshuaj metformin hauv cov neeg mob uas muaj ntshav qab zib hom 2 thiab cov neeg noj qab nyob zoo yog qhov qub, cov tshuaj tsis nthuav tawm thaum noj tshuaj.

Kev sib xyaw ua ke ntawm metformin + sitagliptin yuav tsum tsis txhob raug rau cov neeg mob raum tsis ua haujlwm (saib "Contraindications").

Sitagliptin. Hauv cov neeg mob uas mob raum tsis txaus, kwv yees li 2 npaug ntawm ntshav AUC ntawm sitagliptin tau sau tseg, thiab rau cov neeg mob uas muaj mob loj thiab cov ntu (nyob ntawm hemodialysis), qhov nce hauv AUC yog 4-npaug piv nrog cov kev tswj hwm hauv cov neeg muaj kev noj qab haus huv.

Metformin. Hauv cov neeg mob uas lub raum txo qis kev ua haujlwm (creatinine tshem tawm) T_1/2 lengthens, thiab lub raum tshem tawm kom tsawg zuj zus hauv kev sib txig sib luag kom txo cov creatinine ntshiab.

Sitagliptin. Hauv cov neeg mob uas muaj mob me ntsis tsis txaus siab (7 points9 cov ntsiab lus ntawm Child-Pugh nplai), cov nqi nruab nrab ntawm AUC thiab C_max sitagliptin tom qab siv ib koob tshuaj 100 mg nce ntxiv txog 21 thiab 13%, feem, piv nrog cov tib neeg muaj kev noj qab haus huv. Qhov sib txawv no tsis yog qhov tseem ceeb. Tsis muaj cov ntaub ntawv tshawb fawb txog kev siv cov sitagliptin hauv cov neeg mob uas tsis muaj peev xwm rau hepatic txaus (ntau dua li 9 ntsiab lus ntawm Cov Ntawv Qhia Me-Pugh). Txawm li cas los xij, raws li kev txiav txim siab feem ntau ntawm lub raum ntawm kev nthuav dav, qhov kev hloov pauv tseem ceeb ntawm pharmacokinetics ntawm sitagliptin hauv cov neeg mob uas muaj mob hepatic tsis txaus ntseeg tsis tau kwv yees.

Metformin. Cov kev tshawb fawb ntawm cov tshuaj pharmacokinetic ntawm metformin hauv cov neeg mob uas lub siab tsis ua haujlwm tsis tau ua.

Sitagliptin. Raws li kev tsom xam cov ntaub ntawv ntawm pharmacokinetic ntawm kev soj ntsuam sim ua ntu I thiab II, poj niam txiv neej tsis muaj kev cuam tshuam loj hauv chaw kho mob ntawm pharmacokinetic cov kev cai ntawm sitagliptin.

Metformin. Qhov txwv tsis pub siv ntawm metformin tsis txawv ntau hauv cov tib neeg muaj kev noj qab haus huv thiab cov neeg mob uas muaj ntshav qab zib hom 2 raws li poj niam txiv neej. Raws li kev tswj xyuas cov kab mob kev soj ntsuam, qhov cuam tshuam hypoglycemic ntawm metformin hauv cov txiv neej thiab poj niam tau zoo sib xws.

Sitagliptin. Raws li cov pej xeem pharmacokinetic tsom xam ntawm cov ntaub ntawv los ntawm kev soj ntsuam hauv qib I thiab II, lub hnub nyoog ntawm cov neeg mob tsis muaj kev cuam tshuam los ntawm kev kho mob rau cov pharmacokinetic tsis muaj ntawm sitagliptin. Qhov kev cia siab ntawm sitagliptin hauv cov neeg mob laus (65-80 xyoo) yog kwv yees li 19% siab dua ntawm cov neeg mob hluas.

Metformin. Tsuas siv cov ntaub ntawv los ntawm cov chaw muag tshuaj tswj kev tshawb fawb ntawm metformin hauv cov neeg laus noj qab nyob zoo qhia tias lawv cov ntshav ua kom tag nrho tsawg, T_1/2 lengthens, thiab tus nqi ntawm C_max nce ntxiv piv rau cov tub ntxhais hluas noj qab nyob zoo. Cov ntaub ntawv no txhais tau hais tias muaj kev hloov pauv ntsig txog lub hnub nyoog hauv cov chaw muag tshuaj ntawm metformin yog vim muaj kev txo qis hauv kev ua haujlwm ntawm lub raum.

Kev kho mob nrog kev sib xyaw ua ke ntawm metformin + sitagliptin tsis yog qhia rau cov neeg laus thaum hnub nyoog ≥80 xyoo, tsuas yog cov neeg uas muaj creatinine tshem tawm tau qhia tias kev ua haujlwm hauv lub raum tsis raug txo qis (saib "Kev Ceeb Toom", Metformin).

Kev kawm txog kev sib xyaw ntawm metformin + sitagliptin hauv cov menyuam yaus tsis tau ua.

Sitagliptin. Raws li kev ntsuam xyuas ntawm cov ntaub ntawv pharmacokinetic los ntawm kev soj ntsuam sim ua ntu I thiab II, kev sib tw tsis muaj kev cuam tshuam los ntawm kev siv tshuaj rau cov txheej txheem pharmacokinetic ntawm sitagliptin, suav nrog cov sawv cev ntawm Caucasian thiab Mongoloid haiv neeg, cov neeg sawv cev ntawm Latin America lub teb chaws thiab lwm haiv neeg thiab pawg neeg.

Metformin. Cov kev tshawb fawb txog qhov muaj feem cuam tshuam txog kev sib tw ntawm cov haiv neeg pharmacokinetic cov metformin tsis tau ua. Raws li kev tshawb fawb tau soj ntsuam ntawm cov tshuaj metformin hauv cov neeg mob uas muaj hom 2 mob ntshav qab zib mellitus, qhov ua kom lub ntsej muag hypoglycemic piv tau rau cov neeg sawv cev ntawm Caucasian, Negroid haiv neeg thiab Latin America lub teb chaws.

Sitagliptin. Raws li kev soj ntsuam cov nyom thiab cov neeg ntawm pharmacokinetic cov tsis tau los ntawm kev soj ntsuam hauv qib I thiab II, BMI tsis muaj kev cuam tshuam loj hauv kev kho mob rau cov pharmacokinetic tsis haum ntawm sitagliptin.

Kev siv cov tshuaj Metformin + Sitagliptin

Kev sib xyaw ntawm metformin + sitagliptin yog qhia tias pib kev kho mob rau cov neeg mob ntshav qab zib hom 2 mob ntshav txhawm rau txhim kho glycemic tswj, yog tias kev noj zaub mov zoo thiab kev tawm dag zog tsis pub tswj tau zoo.

Kev sib xyaw ntawm metformin + sitagliptin yog qhia ua ib qho txuas rau kev noj haus thiab kev tawm dag zog kom txhim kho glycemic tswj nyob rau hauv cov neeg mob uas muaj ntshav qab zib hom 2 uas tsis ua tiav kev tswj hwm zoo rau cov keeb kwm yav dhau los ntawm monotherapy nrog metformin lossis sitagliptin, lossis tom qab tsis muaj kev sib xyaw ua ke nrog kev kho mob nrog ob DV.

Kev sib xyaw ntawm metformin + sitagliptin yog qhia rau cov neeg mob ntshav qab zib hom 2 ntshav qab zib kom txhim kho glycemic tswj nrog sulfonylurea derivatives (triple ua ke: metformin + sitagliptin + sulfonylurea derivative) thaum kev noj zaub mov zoo thiab kev tawm dag zog yog ua ke nrog ob ntawm peb yam tshuaj no: metformin, sitagliptin los yog sulfonylurea derivatives tsis ua rau muaj kev tswj hwm glycemic txaus.

Kev sib xyaw ntawm metformin + sitagliptin yog qhia rau cov neeg mob uas muaj ntshav qab zib hom 2 los txhim kho glycemic tswj nrog thiazolidinediones (PPARγ receptor agonists ua haujlwm los ntawm peroxisome proliferator), thaum kev noj zaub mov noj thiab kev tawm dag zog yog ua ke nrog ob ntawm peb yam tshuaj no: metformin, sitagliptin lossis thiazolidine tsis txhob ua rau kev tswj glycemic txaus.

Kev sib xyaw ntawm metformin + sitagliptin yog qhia rau cov neeg mob uas muaj ntshav qab zib hom 2 los txhim kho glycemic tswj nrog insulin, thaum noj thiab qoj ib ce sib xyaw nrog insulin tsis ua rau kev tswj glycemic txaus.

Ntawv thov kev txwv

Siv rau cov laus

Kev sib xyaw ua ke ntawm metformin + sitagliptin. Txij li txoj hauv kev tseem ceeb ntawm kev tshem tawm cov sitagliptin thiab metformin yog lub raum thiab qhov ua haujlwm tsis zoo ntawm lub raum tsawg zuj zus nrog lub hnub nyoog, qhov kev ntsuas ua ntej txiav txim thaum ua ke ntawm metformin + sitagliptin nce ntxiv hauv kev faib ua feem rau lub hnub nyoog. Cov neeg laus tau txais kev ceeb toom xaiv koob tshuaj thiab saib xyuas lub raum kev ua haujlwm zoo (saib "Kev Ceeb Toom", Kev kuaj xyuas lub raum).

Sitagliptin. Raws li kev tshawb fawb hauv chav kho mob, qhov ua tau zoo thiab kev nyab xeeb ntawm sitagliptin hauv cov neeg laus (> 65 xyoo) cov neeg mob tau piv rau kev ua tau zoo thiab kev nyab xeeb rau cov neeg mob hluas (PM, tsis pom zoo rau siv thaum cev xeeb tub.

Tsis muaj kev tshawb nrhiav kev sim ntawm kev sib xyaw ua ke ntawm metformin + sitagliptin txhawm rau tshuaj xyuas qhov cuam tshuam ntawm kev ua haujlwm yug me nyuam.

Sitagliptin. Sitagliptin tsis tau qhia txog teratogenicity thaum lub sijhawm organogenesis thaum muab qhov ncauj rau cov nas ntawm cov koob tshuaj txhua hnub txog 250 mg / kg lossis rau luav ntawm cov koob tshuaj ntau txog 125 mg / kg (uas ntau tshaj plasma kis hauv tib neeg los ntawm 32 thiab 22 zaug, feem, tom qab noj cov tshuaj pom zoo txhua hnub ntawm 100 mg) Cov. Kev nce me ntsis ntawm cov zaus ntawm malformation ntawm tav nyob rau hauv cov xeeb ntxwv tau sau tseg (tsis tuaj, hypoplasia, curvature) thaum muab qhov ncauj ntawm kev noj tshuaj txhua hnub ntawm 1000 mg / kg (uas ntau tshaj qhov kis rau tib neeg los ntawm 100 lub sijhawm tom qab noj cov tshuaj pom zoo txhua hnub ntawm 100 mg). Nws muaj qhov me me tawm ntawm lub cev qhov hnyav hauv cov xeeb ntxwv ntawm cov nas ntawm ob tus poj niam thaum pub niam mis thiab txo qhov hnyav ntawm qhov nce ntawm qhov kawg ntawm kev pub mis niam hauv cov txiv neej nrog kev tswj hwm ntawm 1000 mg / kg txhua hnub ntawm sitagliptin rau cov poj niam cev xeeb tub. Txawm li cas los xij, cov ntaub ntawv ntawm kev tshawb fawb kev ua me nyuam tsis yeej ib txwm cuam tshuam ncaj qha nrog cov nyhuv ntawm sitagliptin ntawm tib neeg kev ua me nyuam.

Metformin. Metformin tsis tau ua pov thawj teratogenicity thaum muab ntawm qhov ncauj rau cov nas nyob rau hauv cov koob tshuaj txhua hnub txog li 600 mg / kg. Qhov no ntau tshaj ntawm cov ntshav muaj feem rau hauv tib neeg los ntawm 2 thiab 6 zaug (hauv cov nas thiab luav, feem) tom qab noj qhov siab tshaj plaws pom zoo siv tshuaj kho mob txhua hnub ntawm 2000 mg. Qhov tseem ceeb ntawm lub plasma concentration hauv qhov me nyuam hauv plab qhia qhov hloov chaw ib nrab.

Kev tshawb nrhiav kev sim los txiav txim siab qhov kev zais cia ntawm cov sib xyaw ua ke ntawm kev sib xyaw ua ke ntawm metformin + sitagliptin hauv niam mis tsis tau ua. Raws li kev tshawb fawb ntawm cov khoom sib txawv ntawm ib leeg, ob leeg ntawm sitagliptin thiab metformin yog zais rau hauv cov kua mis ntawm cov nas. Tsis muaj ntaub ntawv qhia txog kev zais ntawm cov sitagliptin mus rau tib neeg cov kua mis. Yog li, kev sib xyaw ntawm cov tshuaj metformin + sitagliptin yuav tsum tsis txhob siv tshuaj thaum lactation.

Qhov tshwm sim ntawm Metformin + Sitagliptin

Hauv kev tshawb nrhiav cov tshuaj placebo, kev kho ua ke nrog sitagliptin thiab metformin feem ntau tau pom zoo los ntawm cov neeg mob ntshav qab zib hom 2 mob ntshav qab zib. Qhov tshwm sim ntawm kev mob tshwm sim nrog kev kho mob ua ke nrog sitagliptin thiab metformin tau sib piv rau zaus thaum noj metformin ua ke nrog placebo.

Ua ke kev kho mob nrog sitagliptin thiab metformin

Hauv 24-lub lim tiam placebo-tswj cov kev tshawb nrhiav qhov tseeb ntawm kev pib sib xyaw nrog kev kho mob nrog sitagliptin thiab metformin (sitagliptin 50 mg + metformin 500 lossis 1000 mg 2 zaug hauv ib hnub) hauv cov tshuaj sib xyaw ua ke piv nrog metformin monotherapy pawg (500 lossis 1000 mg 2 zaug hauv ib hnub) , sitagliptin (100 mg ib hnub ib zaug) lossis placebo, cov kev mob tshwm sim hauv qab no cuam tshuam nrog cov tshuaj tau pom, pom nrog ib qho zaus ntawm ≥1% hauv pawg kho mob sib xyaw thiab ntau dua hauv pawg placebo: raws plab (sitagliptin + metformin - 3.5%,) metformin - 3.3%, sitagliptin - 0%, tso placebo - 1.1%), xeev siab (1.6, 2.5, 0 thiab 0.6%), dyspepsia (1.3, 1.1, 0 thiab 0%), pom tsis meej (1.3, 0.5, 0 thiab 0%), ntuav (1.1, 0.3, 0 thiab 0%), mob taub hau (1.3, 1.1, 0.6 thiab 0%) thiab hypoglycemia (1.1, 0.5, 0.6 thiab 0%).

Ntxiv sitagliptin rau cov tshuaj metformin kho tam sim no

Hauv 24-lub lis piam, kev kawm tshuaj placebo, thaum sitagliptin tau ntxiv ntawm koob tshuaj 100 mg / hnub rau kev kho mob tam sim no nrog metformin, tsuas cuam tshuam nrog kev tswj hwm tau pom nrog ntau zaus ≥1% hauv pawg kho mob nrog sitagliptin thiab ntau dua li ntawm pawg placebo, muaj xeev siab (sitagliptin + metformin - 1.1%, placebo + metformin - 0.4%).

Kev mob ntshav qab zib thiab kev phiv tshuaj los ntawm lub plab zom mov

Hauv kev soj ntsuam cov tshuaj placebo ntawm kev kho mob ua ke nrog sitagliptin thiab metformin, qhov tshwm sim ntawm kev mob ntshav qab zib (tsis hais txog ntawm kev sib luag) hauv cov pab pawg sib koom ua ke tau muab piv rau qhov muaj ntau zaus hauv cov kev kho mob ntawm metformin ua ke nrog cov placebo (1.3-1.6 thiab 2.1% ntsig txog). Qhov ntau zaus ntawm kev saib xyuas qhov tshwm sim tsis zoo los ntawm lub plab zom zaws (tsis hais txog qhov ua rau kev sib raug zoo) hauv kev sib koom ua ke ntawm sitagliptin thiab metformin tau sib piv rau cov zaus hauv cov metformin monotherapy pawg: raws plab (sitagliptin + metformin - 7.5%, metformin - 7.7%), xeev siab (4.8, 5.5%), ntuav (2.1, 0.5%), mob plab (3, 3.8%). Hauv txhua qhov kev tshawb fawb, qhov tshwm sim tsis zoo nyob rau hauv daim ntawv ntawm cov ntshav khov (hypoglycemia) tau sau tseg los ntawm txhua daim ntawv tshaj tawm los ntawm cov kws kho mob pom tias muaj cov ntshav qog ntshav qab zib, kev ntsuas ntxiv ntawm cov ntshav qabzib tsis tau.

Ua ke nrog kev kho mob nrog sitagliptin, metformin thiab sulfonylurea derivative

Hauv 24-lub lis piam, kev kawm tshuaj placebo siv sitagliptin ntawm koob tshuaj 100 mg / hnub tiv thaiv keeb kwm ntawm kev kho mob tam sim no nrog glimepiride ntawm koob tshuaj ≥4 mg / hnub thiab metformin ntawm koob tshuaj ≥1500 mg / hnub, cov tshuaj tiv thaiv kab mob hauv qab no tau pom nrog ntau zaus ≥1% hauv pawg kho mob nrog sitagliptin thiab ntau dua li ntau dua hauv cov pawg placebo: hypoglycemia (sitagliptin - 13.8%, placebo - 0.9%), cem quav (1.7 thiab 0%).

Ua ke nrog kev kho mob nrog sitagliptin, metformin thiab PPARγ agonist

Raws li kev tshawb nrhiav tshuaj placebo siv sitagliptin ntawm koob tshuaj 100 mg / hnub tiv thaiv keeb kwm yav dhau los ntawm kev kho mob tam sim no nrog rosiglitazone thiab metformin, nyob rau 18 lub lim tiam ntawm kev kho mob cov kev mob tshwm sim tom qab tau pom tias cuam tshuam nrog kev noj, pom nrog ntau zaus ntawm ≥1% hauv pawg kho mob nrog sitagliptin thiab ntau dua dua li hauv cov pawg placebo: mob taub hau (sitagliptin - 2.4%, placebo - 0%), raws plab (1.8, 1.1%), xeev siab (1.2, 1.1%), mob ntshav qab zib (1 , 2, 0%), ntuav (1,2, 0%). Nyob rau ntawm lub lim tiam 54 ntawm kev kho ua ke, cov kev mob tshwm sim hauv qab no tau pom tias cuam tshuam nrog kev tswj hwm, pom nrog ntau zaus ntawm in1% hauv pawg kho mob nrog sitagliptin thiab ntau dua nyob hauv pawg placebo: mob taub hau (sitagliptin - 2.4%, placebo - 0%) , hypoglycemia (2.4, 0%), cov kab mob ua pa rau sab saud (1.8, 0%), xeev siab (1.2, 1.1%), hnoos (1.2, 0%), mob fungal ntawm daim tawv nqaij ( 1,2, 0%), ntu ntu (1,2, 0%), ntuav (1,2, 0%).

Ua ke kev kho mob nrog sitagliptin, metformin thiab insulin

Hauv 24-lub lis piam, kev kawm tshuaj placebo siv sitagliptin ntawm koob tshuaj 100 mg / hnub tiv thaiv keeb kwm yav dhau los ntawm kev kho mob tam sim no nrog metformin ntawm koob tshuaj 001500 mg / hnub thiab ib qho tshuaj insulin tas li, tsuas cuam tshuam qhov cuam tshuam nrog kev noj tshuaj thiab soj ntsuam nrog ntau zaus ntawm ≥1% pawg kho mob nrog sitagliptin thiab ntau zaus ntau dua li pab pawg nrog cov placebo muaj cov ntshav qog ntshav qis (sitagliptin - 10.9%, placebo - 5.2%). Lwm qhov kev tshawb nrhiav 24-lub lim tiam hauv cov neeg mob tau txais sitagliptin ua kev kho mob nrog kev kho mob nrog insulin (nrog lossis tsis muaj metformin), tsuas pom qhov tshwm sim tsis zoo uas tau pom nrog cov zaus ntawm ≥1% hauv pawg kho mob nrog sitagliptin thiab metformin, thiab ntau dua li ntawm pawg placebo thiab metformin yog ntuav (sitagliptin thiab metformin - 1.1%, cov placebo thiab metformin - 0.4%).

Hauv kev txheeb xyuas qhov dav dav ntawm 19 ob zaug qhov muag tsis pom, muaj kev soj ntsuam kev soj ntsuam ntawm kev siv cov sitagliptin (ntawm 100 mg / hnub) lossis kev tswj cov tshuaj (nquag lossis cov placebo), qhov tshwm sim ntawm tus mob pancreatitis yog 0.1 tus neeg rau 100 tus neeg mob-xyoo ntawm kev kho mob hauv txhua pawg (saib "Kev Ntsuas Cov kev ceev faj ").

Tsis muaj qhov sib txawv hauv tsev kho mob hauv cov cim tseem ceeb lossis ECG (suav nrog lub sijhawm QTc ntu nruab nrab) tau pom nrog kev kho ua ke nrog sitagliptin thiab metformin.

Kev phiv tshuaj tsis zoo vim kev siv cov sitagliptin

Cov neeg mob tsis tau ntsib kev phiv tshuaj vim tias sitagliptin, qhov ntau yog ≥1%.

Kev phiv tshuaj tiv thaiv vim yog siv cov metformin

Cov kev phiv tshuaj pom nyob rau hauv cov metformin pawg hauv> 5% ntawm cov neeg mob thiab ntau dua li ntau dua hauv cov pawg placebo yog zawv plab, xeev siab / ntuav, flatulence, asthenia, dyspepsia, mob plab, thiab mob taub hau.

Thaum lub sijhawm sau npe tom qab kev saib xyuas ntawm kev siv ntawm kev sib xyaw ntawm metformin + sitagliptin lossis sitagliptin, uas yog ib feem ntawm nws, hauv kev kho mob monotherapy thiab / lossis kev sib koom ua ke nrog kev kho mob nrog lwm cov tshuaj hypoglycemic, ntxiv cov xwm txheej tsis zoo tau tshwm sim. Vim tias cov ntaub ntawv no tau txais los ntawm cov neeg tsis paub meej txog qhov loj me, qhov kev paub ntau heev thiab qhov cuam tshuam ntawm cov xwm txheej tsis zoo no nrog kev kho tsis tuaj yeem txiav txim siab. Cov kev mob tshwm sim no suav nrog kev tiv thaiv tsis haum, suav nrog anaphylaxis, angioedema, tawv nqaij ua pob, urticaria, tawv nqaij vasculitis, ua mob rau daim tawv nqaij, nrog rau mob Stevens-Johnson syndrome, mob hlab ntsha hlwb, suav nrog hemorrhagic thiab necrotic nrog rau qhov ua rau tuag taus thiab tsis ua rau kom mob, ua rau lub raum tsis ua haujlwm, nrog rau lub raum tsis ua haujlwm (mob ntshav qis) ), mob ua pa rau sab nraub qaum, mob nasopharyngitis, cem quav, ntuav, mob taub hau, mob caj pas, mob pob txha, mob leeg, txha caj qaum, mob nraub qaum, khaus.

Kev hloov pauv hauv tsev kho mob

Sitagliptin. Qhov nquag ntawm qhov tsis zoo ntawm kev kuaj ntsuas hauv pawg kho mob nrog sitagliptin thiab metformin tau sib piv nrog cov zaus hauv cov pawg kho mob nrog cov placebo thiab metformin. Feem ntau, tab sis tsis yog txhua qhov kev sim pom tau nce me ntsis ntawm cov qe ntshav dawb (kwv yees li 200 / comparedl piv nrog cov placebo, cov ntsiab lus nruab nrab thaum pib kho 6600 / μl), vim tias nce neutrophils ntau ntxiv. Qhov kev hloov pauv no tsis yog qhov tseem ceeb hauv tsev kho mob.

Metformin. Hauv kev tswj xyuas cov kev tshawb fawb soj ntsuam cov tshuaj metformin kav ntev li 29 lub lim tiam, qhov txo qis hauv ib txwm muaj ntawm cyanocobalamin (vitamin B₁₂) rau cov nuj nqis tsis xws luag hauv cov ntshav ntshav kwv yees li 7% ntawm cov neeg mob, tsis muaj kev kuaj mob. Qhov zoo li txo qis vim kev xaiv malabsorption ntawm vitamin B₁₂ (piv txwv li, kev ua txhaum ntawm kev tsim ntawm ib txoj hauv kev nrog Lub Tsev Teev Ntuj sab hauv tsim nyog rau qhov nqus ntawm cov vitamin B₁₂), tsis tshua muaj neeg ua rau muaj kev txhim kho ntshav khov thiab kho tau yooj yim los ntawm kev tshem tawm cov tshuaj metformin lossis kev noj cov tshuaj vitamin B ntxiv.₁₂ (saib "Kev Ceeb Toom").

Kev sib txuam

Sitagliptin thiab metformin

Kev tswj hwm tib lub sij hawm ntau ntawm cov tshuaj sitagliptin (50 mg 2 zaug hauv ib hnub) thiab metformin (1000 mg 2 zaug hauv ib hnub) tsis nrog kev hloov pauv hauv pharmacokinetic ntau ntawm sitagliptin lossis metformin hauv cov neeg mob uas muaj ntshav qab zib hom 2 mellitus.

Cov kev tshawb fawb ntawm cov nyhuv interdrug rau pharmacokinetic cov kev txwv ntawm kev sib xyaw ntawm metformin + saxagliptin tseem tsis tau ua, txawm li cas los xij, muaj tsawg tus ntawm cov kev tshawb fawb zoo sib xws tau ua rau txhua qhov ntawm cov sib xyaw ua ke - sitagliptin thiab metformin.

Hauv kev tshawb fawb txog kev sib cuam tshuam nrog lwm cov tshuaj, sitagliptin tsis muaj kev cuam tshuam loj hauv lub chaw muag tshuaj ntawm metformin, rosiglitazone, glibenclamide, simvastatin, warfarin, lossis tshuaj tiv thaiv qhov ncauj. Raws li cov ntaub ntawv no, sitagliptin tsis inhibit isoenzymes ntawm CYP3A4, CYP2C 8 lossis CYP2C 9. Cov Ntaub Ntawv hauv vitro qhia tias sitagliptin tseem tsis tau txhawb CYP2D6, CYP1A 2, CYP2C 19 thiab CYP2B 6 isoenzymes thiab tsis ntxias CYP3A4.

Raws li cov pej xeem pharmacokinetic tsom xam hauv cov neeg mob uas muaj ntshav qab zib hom 2, kev kho mob concomitant tsis muaj kev cuam tshuam loj hauv kev kho mob ntawm pharmacokinetics ntawm sitagliptin. Txoj kev tshawb no tau tshuaj xyuas ntau cov tshuaj feem ntau siv los ntawm cov neeg mob uas mob ntshav qab zib hom 2, nrog rau hypocholesterolemic tshuaj (statins, fibrates, ezetimibe), cov tshuaj tiv thaiv kab mob (clopidogrel), cov tshuaj tiv thaiv kev tiv thaiv kab mob (ACE inhibitors, ARA II, beta-blockers, BKK, hydrochlorothiazide, analgesics thiab NSAIDs (naproxen, diclofenac, anticropressin, cantcopinin, celecoproxin, celecopine, celecopine, celecopine, celecopine, celecoprox, czycopine, celecoprox, celecoprox, celecoprox, celecoprox, celecoprox, thiab cwmcoproxin, cantcoproxin, cantcopin ), antihistamines (cetirizine), proton twj tso kua mis inhibitors (omeprazole, lansoprazole) thiab rau kev kho mob erectile kawg (sildenafil).

Kev nce hauv AUC (11%) raws li tau muaj qhov nruab nrab C tau sau tseg_max (18%) digoxin thaum sib xyaw nrog sitagliptin. Qhov nce no tsis yog pom tias tseem ceeb hauv tsev kho mob, txawm li cas los xij, kev saib xyuas ntawm tus neeg mob tau pom zoo thaum noj digoxin.

Kev nce hauv AUC thiab C tau sau tseg_max sitagliptin los ntawm 29 thiab 68%, feem, nrog kev sib xyaw ua ke ntawm qhov ncauj ntawm saxagliptin ntawm koob tshuaj 100 mg thiab cyclosporine (muaj zog P-gp inhibitor) ntawm ib koob ntawm 600 mg. Cov kev hloov pauv no hauv cov qauv pharmacokinetic ntawm sitagliptin tsis yog qhov tseem ceeb hauv kev kho mob.

Glibenclamide: hauv kev kawm txog kev sib txuas yeeb tshuaj-yeeb tshuaj ntawm kev siv ib zaug ntawm metformin thiab glibenclamide rau cov neeg mob uas muaj ntshav qab zib hom 2, tsis muaj kev hloov pauv hauv pharmacokinetic thiab pharmacodynamic tsis dhau ntawm metformin tau pom. Hloov pauv hauv AUC thiab C_max glibenclamide tau hloov zoo heev. Cov ntaub ntawv tsis txaus (ib qho tshuaj xwb) thiab qhov tsis sib xws ntawm lub plasma concentration ntawm glibenclamide nrog cov tshuaj muaj txiaj ntsig pom muaj nyob hauv nqe lus nug txog cov kab mob tseem ceeb ntawm qhov kev cuam tshuam no.

Furosemide: Hauv kev kawm txog kev sib cuam tshuam tshuaj ntawm ib qho tshuaj tiv thaiv ib zaug ntawm metformin thiab furosemide hauv cov neeg ua haujlwm pab dawb noj qab haus huv, kev hloov pauv ntawm pharmacokinetic cov tshuaj ntawm ob qho tshuaj tau raug pom. Furosemide nce tus nqi ntawm C_max metformin hauv plasma thiab ntshav tag nrho yog 22%, AUC tus nqi ntawm metformin nyob rau hauv tag nrho cov ntshav los ntawm 15%, yam tsis muaj kev hloov pauv lub plawv ntawm cov tshuaj. C qhov tseem ceeb_max thiab AUC ntawm furosemide, nyob rau hauv lem, txo los ntawm 31 thiab 12%, ntsig txog, thiab T_1/2 txo qis los ntawm 32% yam tsis muaj kev hloov pauv tseem ceeb hauv lub raum kev lim hiam ntawm furosemide. Tsis muaj xov xwm qhia txog txoj kev sib cuam tshuam tshuaj nruab nrab ntawm ob qho tshuaj yeeb nrog kev siv sib xyaw ntev.

Nkagedipine: thaum kawm txog kev sib txuas lus tshuaj-yeeb tshuaj ntawm nifedipine thiab metformin tom qab siv ib zaug tshuaj los ntawm cov neeg tuaj yeem noj qab haus huv, kev nce ntshav hauv C ntau dua_max thiab AUC ntawm metformin los ntawm 20 thiab 9%, feem, nrog rau kev nce ntxiv ntawm cov metformin uas tau ua tawm los ntawm lub raum. T_max thiab T_1/2 metformin tsis tau hloov pauv. Nws yog raws li kev nce rau hauv nqus ntawm metformin nyob rau hauv muaj nifedipine. Cov nyhuv ntawm metformin rau ntawm pharmacokinetics ntawm nifedipine yog qhov tsawg heev.

Npaj Cationic: cationic tshuaj (i.e., amiloride, digoxin, morphine, procainamide, quinidine, quinine, ranitidine, triamteren, trimethoprim lossis vancomycin) zais cia los ntawm tubular tso pa tuaj yeem tuaj yeem sib cuam tshuam nrog metformin, kev sib tw rau kev sib koom ua ke ntawm cov leeg tub thauj khoom. Cov kev sib tw zoo sib xws tau pom nrog kev tswj hwm tib lub sijhawm ntawm metformin thiab cimetidine los ntawm cov neeg tuaj yeem noj qab haus huv hauv kev tshawb fawb ntawm ib qho thiab ntau koob, nrog 60% nce ntxiv hauv concentration C_max metformin hauv plasma thiab tag nrho cov ntshav; thiab nce 40% ntawm AUC ntawm metformin hauv plasma thiab ntshav tag nrho. Hauv tib koob T T kawm_1/2 metformin tsis hloov pauv. Metformin tsis cuam tshuam dabtsi rau pharmacokinetics ntawm cimetidine. Thiab txawm hais tias kev sib cuam tshuam txog yeeb tshuaj no feem ntau yog qhov tseem ceeb theoretical (tshwj tsis yog cimetidine), ua tib zoo saib xyuas tus neeg mob thiab koob tshuaj hloov kho ntawm kev sib xyaw ntawm cov tshuaj metformin + sitagliptin thiab / lossis cov tshuaj cationic saum toj no los ntawm qhov sib luag rau lub raum feem menyuam yaus thaum raug coj los ua ke.

Lwm tus: qee cov tshuaj muaj hyperglycemic muaj peev xwm thiab tej zaum yuav cuam tshuam nrog tsim kev tswj ntawm glycemia. Cov no suav nrog thiazide thiab lwm yam tshuaj loog, corticosteroids, phenothiazines, cov thyroid hormones, estrogens, qhov ncauj tawm tsam, phenytoin, nicotinic acid, sympathomimetics, BKK thiab isoniazid. Thaum muab tshuaj rau cov neeg mob rau tus neeg mob tau txais kev sib xyaw ntawm metformin + sitagliptin, kev saib xyuas qhov tseeb ntawm glycemic tswj tsis pom zoo.

Thaum cov neeg ua haujlwm noj qab haus huv tau noj cov tshuaj metformin thiab propranolol lossis metformin thiab ibuprofen, tsis muaj kev txwv cov tshuaj pharmacokinetic ntawm cov tshuaj no.

Tsuas yog ib qho tsis tseem ceeb ntawm metformin khi rau cov ntshav plasma protein, yog li, kev sib cuam tshuam tshuaj sib xyaw ntawm metformin nrog cov tshuaj uas nquag khi rau cov ntshav plasma (salicylates, sulfanilamides, chloramphenicol thiab probenecid) tsis zoo li, tsis zoo li sulfonylureas, uas tseem khi rau ntshav protein.

Tsuas tshuaj thiab tswj hwm

Januvia tuaj yeem noj tau yam tsis xav txog noj mov.

Qhov tshuaj pom zoo thawj zaug yog 100 mg ib hnub ib zaug.

Yuav tsum tsis txhob txhaj tshuaj ntxiv thaum siv Januvia ua ke nrog metformin thiab / lossis PPARon agonist (thiazolidinediones). Cov tshuaj yuav tsum tau noj tib lub sijhawm.

Thaum siv Januvia ua ke nrog sulfonylurea lossis tshuaj insulin, qis dua ntawm sulfonylurea lossis insulin tuaj yeem raug txiav txim siab txo qis kev pheej hmoo ntawm hypoglycemia.

Thaum hla lub koob tshuaj Januvia, tus neeg mob yuav tsum noj sai sai thaum nws nco qab qhov no. Tsis txhob noj ob zaug koob tshuaj ntawm lub hnub ntawm kev txais neeg mob.

Cov neeg mob lub raum tsis ua hauj lwm. Cov neeg mob uas lub raum tsis ua haujlwm (CC ≥50 ml / min, kwv yees sib luag nrog qhov ntshav plasma creatinine theem ntawm ≤1.7 mg / dL hauv cov txiv neej, ≤1.5 mg / dL hauv cov poj niam) tsis tas yuav tsum kho tshuaj ntawm Januvia.

Rau cov neeg mob uas tsis tshua mob raum (CC ≥30 ml / min, tab sis 1.7 mg / dl, tab sis ≤3 mg / dl hauv cov txiv neej,> 1.5 mg / dl, tab sis ≤2.5 mg / dl hauv cov poj niam), Januvia koob tshuaj yog 50 mg ib ib hnub.

Rau cov neeg mob uas lub raum tsis ua haujlwm loj (CC 3 mg / dl hauv cov txiv neej,> 2.5 mg / dl hauv cov poj niam), nrog rau lub davhlau ya nyob twg ntawm cov kab mob raum, uas yuav tsum tau mob hemodialysis lossis peritoneal lim ntshav, koob tshuaj Januvia yog 25 mg ib hnub ib zaug. Januvia tuaj yeem siv tsis hais lub sijhawm lim ntshav.

Cov neeg mob mob siab tsis ua haujlwm. Tsis tas yuav kho ntau npaum li cas ntawm Januvia yog yuav tsum muaj hauv cov neeg mob uas tsis tshua mob me me mus rau mob rau daim siab tsis muaj zog. Cov tshuaj tsis tau kawm hauv cov neeg mob uas muaj lub siab ua haujlwm tsis zoo.

Cov neeg laus cov neeg mob. Cov neeg laus yuav tsum tsis muaj kev kho kom haum. Kev siv cov Januvia hauv cov neeg mob uas laus dua 75 xyoo tsis tau kawm.

Cov me nyuam lub hnub nyoog. Nws tsis pom zoo kom siv Januvia rau cov menyuam yaus thiab cov tub ntxhais hluas hnub nyoog qis dua 18 xyoo vim tsis muaj kev tshawb fawb soj ntsuam txog kev nyab xeeb thiab ua haujlwm hauv pawg hnub nyoog no.

Muaj peev xwm ntawm txoj thov

Sitagliptin tsis inhibit qhov kev ua ntawm Rosiglitazone, Simvastatin, Metformin, thiab Warfarin. Nws tuaj yeem siv los ntawm cov poj niam uas pheej siv tshuaj tiv thaiv qhov ncauj. Yog tias nws tau txiav txim siab nrog Dioxin, tom qab ntawv qhov tsim nyog ntawm tom kawg yuav txhim kho me ntsis, txawm li cas los xij, cov kev hloov pauv no tsis tas yuav siv tshuaj kho kom haum.

"Sitagliptin" raug tso cai siv ib txhij nrog cov tshuaj tiv thaiv kab mob (piv txwv, nrog "Ketoconazole") thiab nrog cyclosporine. Cov nyhuv ntawm cov tshuaj hauv cov xwm txheej zoo li no tsis yog qhov tseem ceeb thiab tsis hloov cov kev mob ntawm lawv txoj kev siv.

Txij li nyob rau hauv kev kho mob ntshav qab zib hom 2, ib qho kev thauj khoom ob zaug tau ua rau lub raum, xaiv cov tshuaj ntau dhau los, nws yog ib qho tsim nyog yuav tsum coj mus rau hauv lawv tus peev xwm thiab tus mob

"Sitagliptin" yog lub npe tshuaj thoob ntiaj teb, nws cov lus lag luam yog "Januvia."

Thaum lub sijhawm sim tshuaj, kev noj tshuaj raws li sitagliptin tsis muaj lub zog thiab lub zog tseem ceeb ntawm cov chaw muag tshuaj ntawm Rosiglitazon, Simvastatin, Metformin, qhov ncauj tawm tsam, Warfarin thiab Glibenclamide.

Thaum siv kev npaj ua raws li sitagliptin, kev txwv tsis pub isoenzymes CYP2C9, CYP3A4 thiab CYP2C8 tsis tshwm sim. Ib qho ntxiv, cov tshuaj no tsis tiv thaiv cov enzymes hauv qab no: CYP2C19, CYP1A2, CYP2B6 thiab CYP2D6. "

Kev siv tib lub sijhawm "Metformin" thiab "Sitagliptin" tsis coj cov kev hloov pauv tseem ceeb hauv cov khw muag tshuaj ntawm cov tshuaj nquag ntawm cov tom kawg hauv cov ntshav qab zib mellitus.

Lub zog Yanumet tuaj yeem suav tau tias yog ib qho piv txwv ntawm Sitagliptinum Sitagliptin, nws suav nrog metformin thiab sitagliptin.

Muaj ib cov tshuaj nrog tib cov tshuaj nquag - metformin thiab sitagliptin - qhov no "Velmetia." Lwm cov analogues ntawm "Yanumet" muaj qhov zoo sib xws thiab ATC code:

• Avandamet
• Glibomet,
• Douglimax
• Choj.

Ua raws li kev tshuaj xyuas ntawm cov neeg mob siv cov tshuaj no rau kev kho mob, lawv muaj kev cuam tshuam zoo rau cov piam thaj hauv tib neeg lub cev, txawm li cas los xij, lawv yuav tsum tswj hwm tus mob kom zoo vim yog qhov pom tshwm sim ntawm ntau cov kev mob tshwm sim.

Tus nqi ntawm cov tshuaj yog nyob ntawm ntim thiab thaj av ntawm lub tebchaws. Sib txawv li ntawm 1596-1724 rubles. Tus nqi ntawm cov ntsuas ntawm "Sitagliptin" "Yanumet" yog los ntawm 1680 rubles.

Raws li cov lus ceeb toom ntawm ntau cov chaw sib tham, cov tshuaj no feem ntau kho rau cov neeg mob ntshav qab zib nyob rau theem pib ntawm pathology. Kev tshuaj xyuas ntawm cov kws tshaj lij thiab cov neeg mob pom tias muaj ntau ntau ntawm subtleties hauv kev siv incretinomimetic.

"Sitagliptin" yog cov tshuaj tshiab tshiab, tsis yog txhua tus kws kho mob muaj kev paub ntau yam hauv kev siv. Txog thaum tsis ntev los no, Metformin tau siv dav, tab sis tam sim no Januvia raug kho raws li kev kho mob monotherapy. Nrog cov naj npawb txaus ntawm qhov muaj peev xwm, nws tsis tsim nyog los muab nws ntxiv nrog cov tshuaj xws li Metformin.

Cov lus sib piv ntawm "Sitagliptin" "Yanumet" yog qhia ntxiv rau cov kev tswj hwm kev tawm dag zog thiab kev noj zaub mov, ua rau muaj kev tswjhwm zoo ntawm cov ntshav qab zib hom 2. Kev txheeb xyuas txog nws feem ntau yog qhov zoo.Txawm li cas los xij, cov ntshav qab zib tau hais tias cov tshuaj thiab nws cov analogues ib txwm tsis tau raws li txhua qhov kev xav tau, nws cov kev ua haujlwm tsawg dua sijhawm. Cov ntsiab lus ntawm no tsis yog kev quav, tab sis cov yam ntxwv ntawm tus kab mob: hom mob ntshav qab zib thib ob yog hom mob ntev ntev uas tau nce zuj zus.

Peb tau tshuaj xyuas cov tshuaj "Sitagliptin" tus nqi, tshuaj xyuas thiab cov qauv duab.

Noj ntau dhau

Thaum qhov kev sim tshuaj, ib koob tshuaj sitagliptin ib koob txog li 800 mg feem ntau tau pom zoo los ntawm cov neeg tuaj yeem noj qab haus huv. Tsawg hloov me me hauv QT ntu, tsis suav tias yog kev kho mob tseem ceeb, tau pom nyob hauv ib txoj kev tshawb fawb ntawm sitagliptin hauv ib koob tshuaj txhua hnub ntawm 800 mg (saib "Pharmacodynamics", Ntxim rau cov kab mob electrophysiology) Koob tshuaj ntau dua 800 mg / hnub hauv tib neeg tsis tau kawm.

Hauv kev sim tshuaj rau kev rov ua dua ntawm kev tswj hwm ntawm sitagliptin (theem I), tsis muaj qhov tshwm sim tsis zoo uas cuam tshuam nrog kev kho nrog sitagliptin tau pom nrog ib koob tshuaj ib hnub txog li 400 mg rau 28 hnub.

Yog tias muaj kev noj ntau dhau, nws yog ib qho tsim nyog yuav tsum pib ua tus qauv txhawb kev ntsuas: tshem tawm tseem tsis tau nqus sitagliptin los ntawm lub plab zom mov, saib xyuas cov cim tseem ceeb, suav nrog ECG, nrog rau kev teem sijhawm kho mob yog tias tsim nyog.

Sitagliptin yog lub cev tsis zoo: raws li kev tshawb fawb soj ntsuam, tsuas yog 13.5% ntawm cov koob tshuaj tau tawm hauv lub sijhawm 3-4 teev ntawm kev lim ntshav. Yog tias xav tau kev kho mob, kev kho mob ntev mus ntev yog kho tau. Tsis muaj ntaub ntawv hais txog cov hauj lwm zoo ntawm peritoneal lim ntshav tawm.

Tau muaj qee zaum muaj kev noj tshuaj ntau tshaj ntawm metformin, suav nrog kev tswj hauv ntau tshaj 50 g (50,000 mg). Hypoglycemia tau pom nyob hauv kwv yees li 10% ntawm tag nrho cov neeg mob ntawm kev noj tshuaj tshaj plaws, txawm li cas los xij, qhov txuas meej nrog kev siv ntau tshaj ntawm metformin tsis tau tsim. Kev tsim cov kab mob lactic acidosis nrog kwv yees li 32% ntawm tag nrho cov mob ntawm kev noj tshuaj ntau tshaj metformin (saib "Kev Ceeb Toom", Metformin) Qhov mob ceev ceev yog qhov ua tau (metformin raug lim ntshav ntawm lub nrawm txog ntawm 170 ml / min ntawm cov ntshav liab zoo) txhawm rau txhawm rau tshem tawm cov tshuaj metformin ntau dhau nyob tsam ho muaj neeg siv ntau tshaj.

Kev ceev faj Metformin + Sitagliptin

Metformin + Sitagliptin Kev Sib Tham

Hauv lub sijhawm sau npe tom qab ntawm kev soj ntsuam, cov lus ceeb toom tau txais ntawm kev txhim kho ntawm tus mob ua paug, nrog rau hemorrhagic lossis necrotic nrog rau kev ua rau tuag taus thiab tsis mob, rau cov neeg mob noj sitagliptin (saib "Phiv Rau Sab", Kev soj ntsuam tom qab cuv npe tas).

Txij li cov xov no tau txais kev yeem los ntawm cov pejxeem uas tsis paub tseeb, nws tsis tuaj yeem ntseeg tau kwv yees ntau npaum li cas ntawm cov xov xwm no lossis tsim kom muaj kev sib raug zoo nrog lub sijhawm siv tshuaj. Cov neeg mob yuav tsum tau qhia paub txog cov yam ntxwv ntawm tus yam ntxwv ntawm tus mob pancreatitis: mob hnyav plab heev. Soj ntsuam qhov tseeb ntawm pancreatitis ploj tom qab tsis mus kev ntawm sitagliptin. Thaum xav tias tsam muaj tus mob ua rau pancreatitis, nws yuav tsum tsum tsis txhob noj tshuaj ua ke ntawm metformin + sitagliptin thiab lwm yam tshuaj muaj feem phom sij.

Kev kuaj xyuas lub raum

Txoj kev xaiv zoo tshaj plaws rau kev tshem tawm metformin thiab sitagliptin yog mob raum. Txoj kev pheej hmoo ntawm kev txuam nrog metformin thiab kev txhim kho ntawm cov kab mob lactic acidosis nce ntxiv hauv kev faib ua feem ntawm qhov tsis ua haujlwm ntawm lub raum, vim li no, kev sib xyaw ntawm metformin + sitagliptin yuav tsum tsis txhob raug rau cov neeg mob uas muaj cov ntshav tsim muaj cov ntsiab lus siab dua qhov muaj hnub nyoog ntsig txog VGN. Hauv cov neeg mob laus, vim tias lub hnub nyoog ntsig txog txo kev ua haujlwm ntawm lub raum, ib qho yuav tsum siv zog ua kom tau txais kev tswj glycemic txaus nyob rau cov koob tshuaj tsawg kawg ntawm metformin + sitagliptin ua ke. Hauv cov neeg mob laus, tshwj xeeb tshaj yog cov laus tshaj 80 xyoo, lawv niaj hnub soj ntsuam raum ua haujlwm. Ua ntej pib kev kho mob nrog kev sib xyaw ua ke ntawm metformin + sitagliptin, thiab tseem tsawg kawg ib xyoos ib zaug tom qab pib kev kho mob, nrog kev pab los ntawm kev ntsuam xyuas uas tsim nyog, lawv pom tseeb kev ua haujlwm zoo li qub.Nrog txoj kev muaj peev xwm ntxiv ntawm kev txhim kho lub raum ua haujlwm, lub raum kev ua haujlwm soj ntsuam tau nqa tawm ntau dua, thiab thaum nws kuaj pom, kev sib xyaw ntawm metformin + sitagliptin yog lawb tawm.

Kev tsim cov ntshav qog ntshav nrog kev siv ua ke nrog sulfonylureas lossis insulin

Ib yam li lwm yam kab mob hypoglycemic, hypoglycemia tau pom nrog kev siv sitagliptin thiab metformin nrog rau cov tshuaj insulin lossis sulfonylurea derivatives (saib "Phiv"). Txhawm rau txo cov kev pheej hmoo ntawm sulfonylinduced lossis insulin-induced hypoglycemia, qhov koob tshuaj sulfonylurea lossis insulin derivative yuav tsum tau txo.

Kev tsim cov ntshav qog ntshav nrog kev siv ua ke nrog sulfonylureas lossis insulin

Hauv kev tshawb nrhiav kev soj ntsuam ntawm sitagliptin, ob qho tib si hauv kev kho mob monotherapy thiab hauv kev sib xyaw nrog cov tshuaj uas tsis ua rau kev txhim kho hypoglycemia (i.e. metformin lossis PPARγ agonists - thiazolidinediones), qhov tshwm sim ntawm hypoglycemia hauv cov pab pawg ntawm cov neeg mob noj sitagliptin tau nyob ze rau ntau zaus hauv cov pab pawg ntawm cov neeg mob noj tshuaj. Ib yam li lwm yam kab mob hypoglycemic, hypoglycemia tau pom nrog kev siv sitagliptin tib lub sijhawm sib xyaw nrog insulin lossis sulfonylurea derivatives (saib "Phiv Los Ntawm Sab"). Txhawm rau txo cov kev pheej hmoo ntawm sulfonylinduced lossis insulin-induced hypoglycemia, qhov koob tshuaj sulfonylurea lossis insulin derivative yuav tsum tau txo.

Thaum lub sijhawm sau npe tom qab kuaj xyuas kev siv ntawm kev sib xyaw ntawm metformin + sitagliptin lossis sitagliptin, uas yog ib feem ntawm nws, hauv kev kho mob monotherapy thiab / lossis kev sib koom ua ke nrog kev kho mob nrog lwm tus neeg hypoglycemic, kev tiv thaiv hypersensitivity tau kuaj pom. Cov kev cuam tshuam no suav nrog anaphylaxis, angioedema, exfoliative kab mob ntawm daim tawv nqaij, suav nrog Stevens-Johnson syndrome. Vim tias cov ntaub ntawv no tau txais los ntawm cov neeg tsis paub meej txog qhov loj me, kev paub ntau zaus thiab kev sib raug zoo nrog txoj kev kho ntawm cov kev tsis zoo no tsis tuaj yeem txiav txim siab. Cov kev cuam tshuam no tau tshwm sim hauv thawj 3 lub hlis tom qab pib kho nrog sitagliptin, qee qhov tau pom tom qab noj thawj koob. Yog tias qhov kev txhim kho ntawm cov tshuaj tiv thaiv tsis haum lub cev tsis muaj qhov tsis zoo, xav tau kom tsis txhob noj tshuaj sib xyaw ua ke ntawm metformin + sitagliptin, soj ntsuam lwm qhov ua rau muaj kev txhim kho ntawm qhov tshwm sim tsis zoo thiab qhia lwm cov kev kho lipid-txo qis (saib "Contraindications" thiab "Side Effects"), Kev soj ntsuam tom qab cuv npe tas).

Cov kab mob lactic acidosis yog ib qho mob uas tsis tshua pom muaj tab sis mob hnyav hauv lub cev tab sis kev loj hlob vim yog cov tshuaj metformin thaum kho nrog kev sib xyaw ntawm metformin + sitagliptin. Kev tuag ntawm cov kab mob lactic acidosis mus txog kwv yees li 50%. Kev loj hlob ntawm cov kab mob lactic acid tuaj yeem tshwm sim tiv thaiv keeb kwm ntawm qee tus kab mob somatic, tshwj xeeb hauv kev mob ntshav qab zib mellitus lossis lwm yam kab mob pathological, nrog los ntawm mob ntshav qab zib thiab hypoxemia ntawm cov ntaub so ntswg thiab kabmob. Lactic acidosis yog tus cwj pwm los ntawm kev nce siab ntawm lactate hauv cov ntshav plasma (> 5 mmol / l), cov ntshav pH qis, hluav taws xob tsis sib xws nrog kev nce hauv anion interval, nce ntxiv ntawm qhov feem ntawm lactate / pyruvate. Yog tias cov metformin yog qhov ua rau acidosis, nws cov ntshav plasma feem ntau yog> 5 μg / ml. Raws li cov lus ceeb toom, cov kab mob lactic acidosis hauv kev kho cov tshuaj metformin tsim muaj qhov tsis tshua muaj heev (hauv thaj tsam li 0.03 rau ib tus neeg mob 1000 xyoo, muaj kev tuag ntawm kwv yees li 0.015 kis rau 1000 tus neeg mob xyoo). Txog 20,000 tus neeg mob-xyoo kev siv tshuaj metformin kho, tsis muaj cov mob ntawm cov kab mob lactic acidosis tau qhia hauv kev kuaj mob.Cov kab mob uas tau paub muaj feem ntau hauv cov neeg mob ntshav qab zib mellitus nrog rau lub raum tsis ua haujlwm, nrog rau cov kab mob loj thiab mob raum hypoperfusion, feem ntau ua ke nrog concomitant ntau somatic / phais kab mob thiab polypharmacy. Txoj kev pheej hmoo ntawm kev tsim mob lactic acidosis hauv cov neeg mob uas lub plawv tsis ua haujlwm yuav tsum tau hloov kho cov tshuaj tseem ceeb, tshwj xeeb tshaj yog nrog kev tsis txaus siab ntawm lub plawv tsis haum / lub plawv tsis ua haujlwm rau qhov mob siab, nrog rau kev mob ntshav siab thiab hypoxemia, yog nce ntau. Txoj kev pheej hmoo ntawm kev tsim cov kab mob lactic acid nce nyob rau hauv kev faib ua feem ntawm kev tsis ua haujlwm ntawm lub raum thiab cov neeg mob lub hnub nyoog, yog li ntawd, kev soj ntsuam kom zoo rau lub raum kev ua haujlwm, nrog rau kev siv tshuaj tsawg kawg ntawm metformin, tuaj yeem txo qhov kev pheej hmoo ntawm lactic acidosis. Kev ua tib zoo saib xyuas lub raum kev ua haujlwm yog qhov tshwj xeeb tshaj yog nyob rau hauv kev kho mob ntawm cov neeg laus, thiab rau cov neeg mob laus dua 80 xyoo, kev kho mob nrog metformin pib tsuas yog tom qab kev paub tseeb ntawm kev ua haujlwm raum txaus raws li cov ntsiab lus ntawm kev tsim cov tshuaj ntsuam xyuas, vim tias cov neeg mob no muaj kev pheej hmoo ntau dua ntawm kev mob lactic acidosis. Tsis tas li ntawd, nyob rau hauv ib qho xwm txheej twg los nrog kev txhim kho hypoxemia, lub cev qhuav dej lossis sepsis, metformin yuav tsum tau tshem tawm tam sim ntawd. Muab hais tias nrog lub siab ua haujlwm tsis zoo, kev ua haujlwm ntawm lactate yog qhov txo qis, metformin yuav tsum tsis txhob raug rau cov neeg mob uas kuaj mob lossis kuaj pom ntawm daim siab mob. Thaum kho nrog metformin, yuav tsum haus dej cawv ntau, txij li cawv cawv potentiates cov nyhuv ntawm metformin ntawm lactate metabolism. Ib qho ntxiv, kev kho mob nrog metformin ib pliag txuas mus ib ntus rau lub sijhawm ntawm kev tshawb nrhiav intravascular radiopaque thiab kev phais mob.

Qhov pib ntawm cov kab mob lactic acid feem ntau tsis yooj yim rau kev kuaj pom, thiab nws yog nrog cov tsos mob tshwj xeeb nkaus xwb xws li malaise, myalgia, mob ntsws ua pa nyuaj, ua rau tsaug zog ntau dua, thiab tsis qhia meej dyspeptic. Nrog kev mob siab rau ntawm chav kawm ntawm cov kab mob lactic acidosis, mob ntshav qab zib, mob ntshav qis, thiab tiv thaiv bradyarrhythmia tuaj yeem koom nrog cov tsos mob aforementioned. Tus kws kho mob thiab tus neeg mob yuav tsum paub txog qhov tseem ceeb ntawm cov tsos mob zoo li no, thiab tus neeg mob yuav tsum qhia tus kws kho mob tam sim ntawd ntawm lawv qhov tsos. Kev kho mob nrog metformin raug muab tso tseg kom txog thaum qhov xwm txheej ntshiab.

Plasma ntau ntawm electrolytes, ketones, ntshav qabzib tau txiav txim siab, ntxiv rau (raws li qhia) pH tus nqi ntawm cov ntshav, cov concentration ntawm lactate. Qee zaum cov ntshav ntsiab lus ntawm metformin kuj tseem yuav pab tau. Tom qab tus neeg mob tau siv los kho qhov zoo tshaj plaws ntawm cov tshuaj metformin, mob plab nyhuv cov yam ntxwv ntawm cov theem pib ntawm kev kho mob yuav tsum ploj mus. Yog tias cov tsos mob zoo li no tshwm sim, tom qab ntawd lawv feem ntau yuav yog lub cim ntawm kev tsim cov kab mob lactic acidosis lossis lwm tus mob hnyav.

Yog tias, thaum kho nrog metformin, qhov ua kom tsis haum ntawm lactate hauv cov ntshav muaj ntshav ntau dua VGN, tshuav tsis ntau dua 5 mmol / l, qhov no tsis yog pathognomonic rau lactic acidosis thiab vim yog kev mob tsis zoo xws li ntshav qab zib mellitus lossis rog rog, lossis kev ua haujlwm ntau dhau ntawm lub cev, lossis kev ntsuas lub cev yuam kev. Cov. Hauv txhua tus neeg mob uas muaj ntshav qab zib thiab metabolic acidosis thaum tsis muaj kev paub txog ketoacidosis (ketonuria thiab ketonemia), muaj kev pheej hmoo ntawm lactic acidosis.

Lactic acidosis yog ib tus mob uas yuav tsum tau siv tshuaj khomob xwm txheej nyob hauv tsev kho mob. Metformin kev kho mob raug tso tseg thiab qhov tsim nyog ntawm kev saib xyuas kev kho mob yog nqa tawm tam sim ntawd. Txij li metformin raug lim ntshav ntawm lub nrawm ntawm 170 ml / min nyob rau hauv kev mob ntawm hemodynamics zoo, hemodialysis sai tau pom zoo kom kho sai sai acidosis thiab tshem tawm cov tshuaj metformin.Cov kev ntsuas no feem ntau ua rau muaj kev ploj sai ntawm txhua qhov tsos mob ntawm cov kab mob lactic acidosis thiab kho kom rov zoo ntawm tus neeg mob (saib. "Contraindications").

Nyob rau hauv ib txwm mob, nrog metformin monotherapy, hypoglycemia tsis txhim kho, txawm li cas los xij, nws txoj kev loj hlob muaj peev xwm tiv thaiv keeb kwm ntawm kev tshaib plab, tom qab lub cev tseem ceeb tsis muaj kev cuam tshuam tom ntej ntawm cov calories noj, thaum siv lwm cov tshuaj tiv thaiv hypoglycemic (sulfonylurea derivatives thiab insulin) lossis dej cawv. Txhawm rau ntau dua, kev txhim kho hypoglycemia cuam tshuam rau cov laus, cov neeg ua haujlwm tsis muaj zog lossis ua rau cov neeg mob, cov neeg mob uas quav cawv, cov neeg mob adrenal lossis qias neeg tsis txaus. Kev mob ntshav qab zib yog ib qho nyuaj rau nco txog cov neeg laus thiab cov neeg mob uas siv cov beta-blockers.

Cov tshuaj kws kho mob ua rau muaj kev cuam tshuam tsis zoo rau lub raum kev ua haujlwm lossis kev faib tawm tshuaj metformin. Kev siv cov tshuaj ib txhij uas cuam tshuam rau lub raum kev ua haujlwm, hemodynamics lossis kev faib tawm cov tshuaj metformin (xws li cov tshuaj cationic uas tau tawm hauv lub cev los ntawm tubular cov pa) yuav tsum tau sau tseg nrog kev ceev faj (saib "Kev cuam tshuam", Metformin).

Kev tshawb nrhiav hluav taws xob nrog kev saib xyuas intravascular ntawm iodine-muaj cov tshuaj tiv thaiv kab mob piv txwv (piv txwv li urography, iv cholangiography, angiography, suav tomography nrog iv kev tswj hwm ntawm cov tshuaj tiv thaiv kev cuam tshuam)

Kev tswj fwm ntawm cov tshuaj iodine uas muaj cov tshuaj tiv thaiv kab mob cuam tshuam nrog kev loj hlob ntawm cov kab mob lactic acidosis hauv cov neeg mob noj cov tshuaj metformin, thiab tuaj yeem ua rau mob raum tsis zoo (saib "Contraindications"). Yog li, cov neeg mob uas tau teem sijhawm rau qhov kev kawm no yuav tsum tsum tsis txhob noj cov tshuaj metformin + sitagliptin 48 teev ua ke thiab ua ntej 48 teev tom qab kev tshawb fawb. Kev rov pib kho mob yog tso cai tau tsuas yog tom qab kuaj pom tseeb ntawm lub raum li qub.

Vascular kev sib tsoo (poob siab) ntawm txhua qhov kev mob ntshav siab, lub plawv tsis ua haujlwm, mob myocardial infarction thiab lwm yam mob nrog rau kev txhim kho hypoxemia tuaj yeem ua rau kev loj hlob ntawm lactic acidosis thiab lub raum azotemia. Yog tias cov xwm txheej tau sau tseg hauv tus neeg mob thaum kho nrog kev sib xyaw ntawm cov tshuaj metformin + sitagliptin, kev sib xyaw yuav tsum nres tam sim ntawd.

Kev siv ntawm kev sib xyaw ua ke ntawm metformin + sitagliptin yuav tsum tsis ua hauj lwm txuas ntxiv mus kom txog lub sijhawm ua kev phais mob (tshwj tsis yog muaj kev sib cais me me uas tsis tas yuav txwv txoj kev haus dej haus cawv thiab kev tshaib nqhis) thiab kom txog thaum noj mov li qub, tau txais kev kuaj pom tseeb ntawm lub raum kev ua haujlwm tau.

Cawv cawv potentiates cov nyhuv ntawm metformin ntawm lactic acid metabolism. Tus neeg mob yuav tsum tau ceeb toom txog kev phom sij ntawm kev haus cawv (ib qho tshuaj ntau npaum li cas lossis ib qho tshuaj me me ib zaug) rau lub sijhawm kho mob nrog kev sib xyaw ntawm metformin + sitagliptin.

Lub siab ua haujlwm tsis zoo

Txij li thaum muaj cov neeg paub txog kev loj hlob ntawm cov kab mob lactic acidosis hauv cov neeg mob uas lub siab tsis ua haujlwm, nws tsis pom zoo kom sau cov tshuaj sib xyaw ua ke ntawm metformin + sitagliptin hauv cov neeg mob uas kuaj mob lossis kuaj pom ntawm daim siab mob siab.

Qhov concentration ntawm cyanocobalamin (vitamin B₁₂) hauv ntshav ntshav

Hauv cov kev tshawb fawb soj ntsuam ntawm cov tshuaj metformin kav ntev li 29 lub lis piam, 7% ntawm cov neeg mob tau pom tias qhov qis ntawm kev pib ua rau muaj cyanocobalamin (vitamin B₁₂) nyob rau hauv cov ntshav plasma yam tsis muaj kev txhim kho kev soj ntsuam cov tsos mob ua kom tsis muaj zog. Kev txo qis zoo ib yam yog vim xaiv malabsorption ntawm vitamin B₁₂ (piv txwv li, kev ua txhaum ntawm kev tsim ntawm txoj kev nrog Lub Tsev Teev Ntuj nyob sab hauv tsim nyog rau kev nqus ntawm cov vitamins B₁₂), tsis tshua muaj neeg ua rau muaj kev txhim kho ntshav khov thiab kho tau yooj yim los ntawm kev tshem tawm cov tshuaj metformin lossis kev noj cov tshuaj vitamin B ntxiv.₁₂Cov. Thaum kho nrog kev sib xyaw ua ke ntawm metformin + sitagliptin, nws raug nquahu kom kuaj xyuas qhov hematological ntawm cov ntshav ib xyoos ib zaug, thiab txhua yam kev hloov pauv uas tshwm sim yuav tsum kawm thiab kho. Cov Neeg Mob Vitamin B Tsis Txaus₁₂ (vim tias txo qis kev nqus lossis nqus cov vitamin B₁₂ los yog calcium) nws raug nquahu kom txiav txim siab ntshav plasma cov vitamin B₁₂ ntawm cov sijhawm ntawm 2-3 xyoo.

Hloov pauv mus kawm qhov xwm txheej ntawm cov neeg mob uas tau txais hom tshuaj tiv thaiv ntshav qab zib mellitus tsawg kawg

Yog tias kuaj ntshav tsis haum lossis chaw kuaj mob tus kab mob (tshwj xeeb yog ib qho mob uas tsis tuaj yeem pom meej meej) tshwm sim hauv tus neeg mob uas muaj kev tiv thaiv tus mob ntshav qab zib hom ntshav qab zib thaum lub sijhawm kho nrog kev sib xyaw ntawm metformin + sitagliptin, ketoacidosis lossis lactic acidosis yuav tsum tau muab tshem tawm tam sim ntawd. Kev ntsuam xyuas ntawm tus neeg mob lub cev yuav tsum muaj kev kuaj ntshav rau electrolytes thiab ketones, cov ntsiab lus ntawm cov piam thaj hauv cov ntshav, nrog rau (yog tias qhia) ntshav pH, ntshav ntau ntawm lactate, pyruvate thiab metformin. Nrog rau kev loj hlob ntawm acidosis ntawm tej kev etiology, koj yuav tsum tam sim ntawd tsum tsis txhob noj ua ke ntawm metformin + sitagliptin thiab ntsuas kev tsim nyog los kho acidosis.

Poob ntawm glycemic tswj

Hauv qhov xwm txheej ntawm lub cev kev nyuaj siab (hyperthermia, mob, mob lossis phais) nyob rau hauv tus neeg mob nrog kev paub yav dhau los ua ntej glycemic tswj, ib ntus poob ntawm glycemic tswj yog ua tau. Nyob rau cov caij nyoog zoo li no, kev hloov ib ntus ntawm kev sib xyaw ua ke ntawm metformin + sitagliptin nrog kev kho tshuaj insulin yog qhov zoo, thiab tom qab daws qhov mob tshwm sim, tus neeg mob tuaj yeem rov pib kho dua.

Cuam Tshuam rau kev muaj peev xwm tsav tsheb thiab ua haujlwm nrog tshuab. Tsis muaj kev tshawb nrhiav tau ua tiav los kawm txog cov txiaj ntsig ntawm kev sib xyaw ntawm metformin + sitagliptin ntawm kev muaj peev xwm tsav tsheb thiab ua haujlwm nrog cov txheej txheem. Txawm li cas los xij, cov kev mob uas kiv taub hau thiab tsaug zog thaum sau cov tshuaj sitagliptin yuav tsum raug suav nrog.

Ib qho ntxiv, cov neeg mob yuav tsum paub txog kev pheej hmoo ntawm cov ntshav qog ntshav thaum siv tshuaj sib xyaw ua ke ntawm metformin + sitagliptin nrog sulfonylurea derivatives lossis insulin.

Cov qauv ntsuas cov cai thiab cov kua nplaum nyeem cov qabzib

Cov txiaj ntsig yoo ib txwm rau tag nrho cov ntshav - 3.3-5.5 mmol / L, rau ntshav - 4.0-6.1 mmol / L.

Tso ntshav ntsuas rau qhov kev soj ntsuam yooj yim no nws muaj nws cov subtleties. Ntshav, txawm tias venous lossis capillary, yuav tsum tau ua rau kev txheeb xyuas thaum sawv ntxov ntawm lub plab khoob. Koj tsis tuaj yeem noj rau 10 teev, koj tuaj yeem haus cov dej huv, tab sis ua ntej ntawd, cov zaub mov yuav tsum paub.

Tam sim ntawd ua ntej kev tswjfwm nws yog qhov tsim nyog kom tsis txhob muaj kev ntxhov siab, tsis txaus ntseeg, qoj ib ce, koj tsis tuaj yeem haus luam yeeb. Qhov tshwm sim tuaj yeem cuam tshuam los ntawm qee pawg tshuaj (salicylates, cov neeg sawv cev ntawm cov tshuaj tua kab mob), vitamin C, ntxiv rau lwm yam tshuaj, kab mob thiab mob uas yuav tsum ceeb toom rau tus kws kho mob uas tuaj koom.

Ib txoj kev tshawb fawb pom zoo rau kev soj ntsuam yog yoo cov piam thaj. Ib txoj kev ncaj thiab txoj kev yooj yim tso cai rau koj los soj ntsuam pawg neeg coob coob kom muaj cov metabolism hauv kev ua kom yuag. Qhov kev tsom xam no hais txog cov uas yuav ua tau yam tsis muaj kws kho mob sau ntawv. Nws yog ib qho tseem ceeb tshwj xeeb pub ntshav ntawm cov ntiv tes rau qab zib rau cov neeg uas yuav muaj ntshav qab zib hom 2.

Sitagliptin los tswj kev qab los noj mov thiab ntshav qab zib lub cev

Hauv pathogenesis ntawm ntshav qab zib hom 2, peb cov txheej txheem tseem ceeb yog qhov txawv:

1. Ntaub so ntswg insulin kuj,
2. Kev cuam tshuam hauv kev tsim cov tshuaj insulin endogenous,
3. Ntau cov synthesis ntawm qabzib los ntawm lub siab.

Lub luag haujlwm rau kev txhim kho ntawm cov kab mob insidious no nyob nrog b thiab c hlwb ntawm lub txiav. Qhov tom kawg kuj tsim cov tshuaj hormones uas txhawb kev hloov pauv ntawm cov piam thaj rau lub zog rau cov leeg thiab lub hlwb. Yog hais tias tus nqi ntawm nws cov khoom lag luam qis qis, qhov no provokes hyperglycemia.

B-cov hlwb yog lub luag haujlwm rau kev tsim cov khoom ntawm glucagon, nws dhau mus tsim kev tsim nyog ua ntej rau kev zais cia ntau dhau ntawm cov piam thaj los ntawm nplooj siab. Globins glucagon ntau dhau thiab tsis muaj cov tshuaj insulin muab cov kev mob rau kev txuam nrog cov piam thaj tsis ua haujlwm hauv cov ntshav.

Kev tswj tau zoo ntawm tus mob ntshav qab zib hom 2 tsis tuaj yeem ua tsis tau yam tsis muaj kev ruaj khov thiab lub sijhawm ntev (rau tag nrho lub sijhawm ntawm tus kabmob) tswj kev noj cov zaub mov carbohydrate. Ntau cov kev sim thoob ntiaj teb lees paub tias tsuas yog nyiaj qab zib thiaj li ua kom muaj kev tiv thaiv ntawm cov teeb meem thiab ua kom lub neej muaj hnub nyoog ntev dua ntawm tus mob ntshav qab zib.

Txawm hais tias tag nrho cov tshuaj muaj ntau yam tshuaj tiv thaiv kab mob, tsis yog txhua tus neeg mob tswj kom ua tiav kev them nyiaj ruaj khov ntawm carbohydrates nrog lawv pab. Raws li kev tshawb pom muaj tseeb UKPDS txoj kev tshawb nrhiav, 45% ntawm cov neeg mob ntshav qab zib tau txais 100% kev them nyiaj rau kev tiv thaiv microangiopathy tom qab 3 xyoos, thiab tsuas yog 30% tom qab 6 xyoo.

Cov teeb meem no sau qhov kev xav tau los tsim kho cov kev kawm tshiab ntawm cov tshuaj uas yuav tsis tsuas yog pab tshem tawm cov teeb meem metabolic, tab sis kuj tswj hwm tus txiav, txhawb lub cev muaj zog uas tso cai rau kev tswj cov tshuaj insulin thiab glycemia.

Cov tshuaj ntawm cov incretin koob, uas tuaj yeem tswj hwm tus mob ntshav qab zib hom 2 yam tsis muaj kev kho ntawm tus txiav, kev hloov pauv sai ntawm glycemia, qhov kev pheej hmoo ntawm hypoglycemia, yog qhov kev tsim kho tshiab los ntawm cov kws tshuaj.

Lub inhibitor ntawm GLP-4 enzyme, Sitagliptin, pab cov ntshav qab zib kom tswj tau lub siab thiab lub cev qhov hnyav, muab lub cev kom muaj peev xwm ntawm nws tus kheej ntawm kev daws teeb meem ntawm teeb meem piam thaj.

Tso tawm daim ntawv thiab muaj pes tsawg leeg

Cov tshuaj raws li sitagliptin nrog lub npe lag luam Januvia muaj nyob rau hauv daim ntawv ntawm cov ntsiav tshuaj puag ncig nrog cov xim liab lossis beige hue thiab cim "227" rau 100 mg, "112" rau 50 mg, "221" rau 25 mg. Cov ntsiav tshuaj yog ntim rau hauv lub thawv yas lossis tus cwj mem qhuav. Muaj peev xwm muaj ntau lub phaj ntim hauv ib lub thawv.

Cov kev ua yeeb yam tseem ceeb sitagliptin phosphate hydrate yog ntxiv nrog croscarmellose sodium, magnesium stearate, cellulose, sodium stearyl fumarate, tsis muaj tshuaj calcium calcium phosphate.

Rau sildagliptin, tus nqi nyob ntawm lub pob, tshwj xeeb rau 28 ntsiav tshuaj koj yuav tsum them 1,596-1724 rubles. Daim ntawv muab tshuaj muab rau, cov khoom txee lub neej yog 1 xyoos. Cov tshuaj tsis tas yuav tshwj xeeb rau kev khaws cia. Qhib ntim tau khaws cia rau ntawm lub qhov rooj tub yees rau ib hlis.

Pharmacokinetics ntawm sitagliptin

Qhov nqus ntawm cov tshuaj tshwm sim sai sai, nrog kev ntsuas kev noj qab haus huv ntawm 87%. Qhov nqus ntshav tsis nyob ntawm lub sijhawm ntawm kev nkag thiab cov khoom noj ntawm cov zaub mov, tshwj xeeb, cov khoom noj muaj roj tsis hloov pauv pharmacokinetic ntawm qhov ua kom ntau ntxiv.

Hauv kev sib npaug, kev siv ntxiv ntawm 100 ntsiav tshuaj ntsiav tshuaj tsub kom thaj tsam hauv qab AUC nkhaus, uas yog qhov cim ntawm kev tos cov khoom xa tuaj raws sijhawm, los ntawm 14%. Ib koob tshuaj ntawm 100 mg ntsiav tshuaj tuaj yeem lav qhov muab faib tawm ntawm 198 l.

Ib feem me me ntawm incretin mimetic yog metabolized. Rau lub cev khoom noj tau nrhiav pom tias tsis muaj peev xwm inhibit DPP-4. Kev hlais tawm (QC) - 350 ml / min. Lub ntsiab tseem ceeb ntawm cov tshuaj yog tshem tawm los ntawm lub raum (79% nyob rau hauv daim ntawv tsis txawv txav thiab 13% hauv daim ntawv tshuaj tiv thaiv), qhov seem yog tawm los ntawm txoj hnyuv.

Txhawm rau saib xyuas lub nra hnyav rau lub raum hauv cov neeg mob ntshav qab zib nrog daim ntawv ntev (CC - 50-80 ml / min.), Qhov ntsuas yog zoo ib yam, nrog CC 30-50 ml / min. ob npaug ntawm AUC qhov tseem ceeb tau pom, nrog CC hauv qab 30 ml / min. - plaub zaug. Cov xwm txheej zoo li no qhia kom muaj feem kaum koob tshuaj.

Nrog cov kab mob hepatic pathologies ntawm kev mob hnyav ib nrab, Cmax thiab AUC nce li 13% thiab 21%. Hauv cov ntawv loj, cov pharmacokinetics ntawm sitagliptin tsis hloov pauv ntau, vim tias cov tshuaj feem ntau yog tawm los ntawm lub raum.

Leej twg muaj qhia incretinomimetic

Cov tshuaj yog tawm rau cov ntshav qab zib hom 2 ntxiv rau kev noj zaub mov kom tsawg thiab muaj cov leeg ua haujlwm txaus.

Nws yog siv los ua ib qho yeeb tshuaj thiab sib koom tes kho nrog metformin, sulfonylurea kev npaj lossis thiazolidinediones. Nws kuj tseem siv tau qhov kev txhaj tshuaj insulin yog tias qhov kev xaiv no pab daws qhov teeb meem ntawm kev tiv thaiv insulin.

Txog kev kho mob pob qij txha, peb cov neeg nyeem tau siv DiabeNot siv tau zoo. Pom qhov nrov ntawm cov khoom no, peb tau txiav txim siab muab nws rau koj kom txaus siab.

Phiv Txheej Xwm

Kev txiav txim los ntawm kev txheeb xyuas, feem ntau ntawm txhua tus neeg mob ntshav qab zib tau txhawj xeeb txog qhov ua tsis taus pa, mob qhov quav. Hauv kev kuaj sim, hyperuricemia, txo qis kev ua haujlwm ntawm lub qog ua haujlwm lub qog ua haujlwm, thiab mob leukocytosis tau sau tseg.

Ntawm lwm qhov cuam tshuam los ntawm qhov tsis paub (qhov sib txuas nrog incretin mimetic tsis tau muaj pov thawj) - ua mob ua pa, mob caj pas, mob pob txha taub hau, txhaws ntswg). Qhov tshwm sim ntawm cov ntshav qog nqaij hlav zoo ib yam li cov txiaj ntsig hauv pawg tswj tau txais cov placebo.

Qhia Txog Kev Sib Koom Tes Nrog Tshuaj

Nrog rau kev siv sib npaug ntawm sitagliptin nrog metformin, rosiglitazone, qhov ncauj qhov kev tiv thaiv, glibenclamide, warfarin, simvastatin, pharmacokinetics ntawm pab pawg no tsis hloov pauv.

Concurrent coj ntawm sitagliptin nrog digoxin tsis cuam tshuam qhov hloov pauv ntawm kev noj tshuaj. Cov ntsiab lus zoo ib yam yog muab los ntawm kev qhia thiab ntawm kev cuam tshuam ntawm sitagliptin thiab cyclosporin, ketoconazole.

Sildagliptin - analogues

Sitagliptin yog lub npe tshuaj thoob ntiaj teb rau nws cov yeeb tshuaj; nws lub npe lag luam yog Januvius. Ib qho tshuaj yeeb yaj kiab tuaj yeem suav tau tias yog qhov sib xyaw ua ke siv tshuaj Yanumet, uas suav nrog sitagliptin thiab metformin. Galvus belongs rau cov pab pawg ntawm DPP-4 inhibitors (Novartis Pharma AG, Switzerland) nrog cov nquag vildagliptin, tus nqi 800 rubles.

Kev siv tshuaj hypoglycemic kuj tsim nyog rau ATX code ntawm qib 4:

• Nesina (Takeda Pharmaceuticals, Asmeskas, raws li alogliptin),
• Onglisa (Bristol-Myers Squibb Tuam Txhab, raws li saxagliptin, tus nqi - 1800 rubles),
• Trazhenta (Bristol-Myers Squibb Tuam Txhab, Ltalis, Tebchaws Askiv, nrog rau cov khoom muaj txiaj ntsig linagliptin), tus nqi - 1700 rubles.

Cov tshuaj txhaum loj no tsis suav nrog hauv cov tshuaj tshwj xeeb, puas tsim nyog sim ntawm koj tus kheej qhov kev pheej hmoo thiab pheej hmoo nrog koj pob nyiaj thiab kev noj qab haus huv?

Kev Soj Ntsuam Sitagliptin

Kev txiav txim los ntawm cov lus ceeb toom ntawm cov ntsiab lus sib tham, Januvius feem ntau yog kho rau cov neeg mob ntshav qab zib nyob rau theem pib ntawm tus kab mob. Txog sitagliptin, kev tshuaj xyuas ntawm cov kws kho mob thiab cov neeg mob qhia tias kev siv ntawm incretinomimetic muaj ntau nuances.

Januvia yog kev tsim yeeb tshuaj tshiab thiab tsis yog txhua tus kws kho mob tau txais kev paub txaus siv nws. Txog thaum nyuam qhuav, metformin yog thawj cov tshuaj kab; tam sim no, Januvia kuj tseem raug kho raws li kev kho mob monotherapy. Yog tias nws lub peev xwm tau txaus, ntxiv nws nrog metformin thiab lwm yam tshuaj tsis pom zoo.

Tus mob ntshav qab zib yws tias cov tshuaj tsis tas ua raws li cov lus teev tseg, dhau sij hawm nws cov hauj lwm txo qis. Qhov teeb meem ntawm no tsis tau siv tshuaj kho mob, tab sis nyob rau hauv cov yam ntxwv ntawm tus kabmob: hom 2 mob ntshav qab zib - mob ntev, mob hnyav pathology.

Txhua cov lus ua rau qhov xaus hais tias cov kev qhia txog kev soj ntsuam kev ua tiag ntawm sitagliptin, uas yog cov qauv tshiab ntawm cov tshuaj, muab lub sijhawm txaus rau kev tswj hwm tus mob ntshav qab zib hom 2 ntawm txhua theem, los ntawm kev mob ntshav qab zib mus rau kev kho ntxiv, nrog cov tsis zoo los ntawm daim ntawv thov ntawm cov tshuaj kho mob glycemic them rau.

Daim ntawv qhia los ntawm cov xibfwb A.S. Ametov, endocrinologist-diabetologist txog qhov kev xav thiab kev coj ua ntawm siv sitagliptin - hauv video.

Khoom qab zib rau cov ntshav qab zib

Cov lus nug hais txog kev siv cov khoom qab zib confectionery los ntawm cov neeg mob ntshav qab zib tseem nyob, yog tias tsis yog qhov feem ntau, ces cuam tshuam rau ntau caum xyoo. Tsis ntseeg, txhua tus neeg tsis tau txawm tias mob nrog cov kab mob endocrine no tsawg kawg ib zaug hauv lawv lub neej tau hnov ​​tias cov khoom qab zib ua rau muaj kev phom sij rau cov neeg mob ntshav qab zib thiab tuaj yeem ua rau tsis zoo rau lub cev.Txawm li cas los xij, tsis txhob hnov ​​qab tias peb nyob hauv lub ntiaj teb niaj hnub thiab kev vam meej uas muaj ntau yam teeb meem daws teeb meem tag los yog tsawg kawg tuaj yeem kho tau. Mob ntshav qab zib mellitus tsis yog kab lus thiab kev noj mov qab zib rau tus neeg mob ntshav qab zib tsis yog txwv tsis pub txhua, tab sis ua ntej koj yuav tsum kawm qee qhov tshwj xeeb thiab tsis qab los ntawm cov zaub mov qab.

Yog lawm! Koj tau hnov ​​txoj cai: kev noj zaub mov kom qab thiab txawm tias qab zib thaum muaj tswv yim ua raws cov lus qhia yuav tsis ua mob rau lub cev hauv ib txoj kev twg, tab sis, ntawm qhov tsis sib haum, yuav tso cai rau koj los kho cov teeb meem kev noj zaub mov kom zoo uas cuam tshuam vim muaj ntshav qab zib.

Qab zib noj

Peb raug siv los nkag siab los ntawm lo lus "noj zaub mov" thiab "zaub mov noj" - tus txheej txheem uas muaj txhua yam kev sim siab los ntawm qhov xav tau, kev xav thiab qhov kev txwv uas ua rau peb tsis zoo, tab sis qhov no tsis muaj tseeb. Hauv zej zog kev kho mob, lo lus "noj zaub mov" yog hais txog cov khoom noj tshwj xeeb, nrog rau cov lus qhia ntxiv thiab cov khoom lag luam zoo tshaj plaws rau cov kabmob muaj. Kev noj haus tsis suav nrog cov khoom qab zib thiab ntxiv cov tshuaj tshwj xeeb rau txoj kev noj haus - cov khoom qab zib thiab qab zib.

Cov neeg mob puas tuaj yeem kuaj pom tus mob ntshav qab zib siv tau txhua yam? Tau kawg nws tuaj yeem ua tau, tab sis yuav ua li cas nws yuav cuam tshuam nws tus mob yog qhov teeb meem sib txawv, thiab feem ntau, kev noj zaub mov tsis tau tswj hwm yuav ua rau muaj kev vam meej ntawm tus kab mob, tshwj xeeb tshaj yog xav tias feem coob ntawm cov neeg mob ntshav qab zib muaj hom mob thib ob, uas tau tsim los ntawm kev ua neej tsis zoo, khoom noj khoom haus tsis muaj zog, thiab, ntawm chav kawm, ib qho kev txom nyem rau nws.

Noj haus hauv tus lej 9 yog qis-carb thiab ua raws li qhov ua tiav ntawm Asmeskas tus kws kho mob Richard Bernstein. Cov khoom noj no suav nrog tag nrho cov zaub mov yooj yim thiab muaj calories ntau, thiab rau qab zib, nws tsis suav nrog kev siv cov txiv hmab txiv ntoo thiab zaub qab zib, uas muaj cov khoom xws li qabzib - sucrose, tab sis yooj yim zom cov zaub mov (qab zib, hmoov) hloov nrog qab zib uas tsis suav nrog hauv cov khoom noj metabolism. Cov zaub mov tshwj xeeb rau ntau cov zaub mov qab thiab qab zib uas tuaj yeem npaj nrog koj tus kheej tes yog tsim, thiab tib lub sijhawm lawv yuav ua tau raws cov qauv rau kev noj haus No. 9.

Yooj yim carbohydrates - raug mob

Cov carbohydrates tau yooj yim yog cov zaub mov carbohydrates tau yooj yim uas yuav luag tawg nyob rau hauv txoj hnyuv thiab nqus mus rau hauv cov kab ke. Nws yog los ntawm cov carbohydrates uas yooj yim uas muaj kev nce ntxiv hauv insulin secretion tshwm sim. Yog tias tus neeg mob nrog cov kab mob endocrine no noj ntau ntawm cov carbohydrates yooj yim ib zaug, qhov no yuav ua rau muaj ntshav qabzib ntau ntxiv. Uas yuav ua rau muaj kev poob qis hauv kev paub zoo. Feem ntau carbohydrate yooj yim yog qab zib.

Carbohydrates yooj yim kuj muaj xws li:

• Bakery thiab confectionery khoom,
• Khoom qab zib, chocolate, cocoa,
• Ib co txiv ntoo, xws li txiv tsawb, dib liab thiab dib liab,
• Syrups, jam, zib mu.

Tag nrho cov khoom lag luam no muaj qhov siab glycemic siab, thaum lawv tsim tau qhov nce siab hauv cov concentration ntawm cov piam thaj hauv cov ntshav, uas tsis zoo rau ib tus neeg. Tshwj xeeb yog rau ntshav qab zib. Puas muaj ntshav qab zib hauv tus neeg uas niaj hnub noj cov khoom noj uas yooj yim carbohydrates? Nws yog ua tau, txij li kev pheej hmoo ntawm nws txoj kev loj hlob nce siab. Nws yog cov carbohydrates yooj yim uas tau pom zoo kom hloov los ntawm cov ntshav qab zib nrog cov qab zib thiab cov qab zib. Nws yog ib qho tseem ceeb uas yuav tsum tau ua daim ntawv me me, cov khoom qab zib rau cov neeg mob ntshav qab zib hom 1 yuav tsum nyob ntawm tes, vim tias muaj cov tshuaj insulin ntau dhau yuav pab kom tshem tau cov kev mob tshwm sim ntawm kev mob ntshav qab zib.

Cov khoom noj ua ke carbohydrates - cov txiaj ntsig

Cov khoom noj ua ke sib xyaw ua ke yog qhov tseem ceeb ntawm tib cov carbohydrates uas yooj yim, txawm li cas los xij, tus yam ntxwv tsis ua rau cov molecules sai sai thiab ua rau cov ntshav. Lawv tsis muaj cov khoom qab zib zoo, tab sis lawv muaj qhov glycemic index tsawg thiab yog qhov zoo rau cov ntshav qab zib yog cov zaub mov tseem ceeb.Kev saj ntawm cov carbohydrates ua tau yooj yim daws tau los ntawm kev ntxiv cov khoom qab zib uas tsis koom nrog hauv cov metabolism.

Dab tsi yog cov khoom qab zib hloov pauv hauv qab?

Tseem li, khoom noj qab zib dab tsi uas cov neeg muaj ntshav qab zib tuaj yeem muaj? Cov kev lag luam niaj hnub kev lag luam kws tshuaj thiab zaub mov tsis tseem sawv ntsug. Ntau hom sib txuas uas ua ntsiag to ntawm lub qab zib saj ntawm saj saj, tab sis tsis yog carbohydrates, tau raug tsim. Muaj ob lub ntsiab ntawm cov tshuaj sib txuas:

Cia peb tham kom paub ntau ntxiv txog lawv, thiab tseem peb yuav nkag siab cov khoom tseem ceeb thiab cov khoom tsis zoo ntawm cov tebchaw no.

Cov khoom qab zib

Cov tshuaj no muaj cov roj carbohydrates, tab sis muaj cov ntsiab lus hauv calorie qis dua qab zib. Cov khoom qab zib muaj lub zog ntau dua thiab nrog lub ntim me dua tuaj yeem ua tiav tib yam khoom ntawm lub tais.

Hloov pauv yuav muaj xws li:

• Sorbitol yog ib hom kev qhia muaj kev noj haus muaj nyob hauv E420 cov zaub mov muaj zaub mov kho.
• Mannitol - pom hauv cov nroj tsuag thiab siv hauv kev lag luam khoom noj khoom haus ua cov khoom noj ntxiv rau hauv E421.
• Fructose - nyob hauv txhua yam txiv hmab txiv ntoo thiab zaub ntsuab. Nws ua kom txog li 80% zib ntab.
• Aspartame yog 300 - 600 lub sij hawm qab zib ntau dua qab zib, sib xws rau cov khoom noj ntxiv rau E951.

Cov khoom muaj nqis ntawm cov khoom qab zib yog cov khoom noj qab zib zoo nkauj hauv kev sib piv nrog cov suab thaj, uas tso cai rau lawv siv ntau qhov qis, thaum cov khoom noj khoom haus tsis poob nws cov qab zib. Txawm li cas los xij, cov khoom qab zib thaum nqus tau hloov mus rau hauv cov piam thaj thiab nce nws qib hauv cov ntshav, yog li nws tsis tuaj yeem siv lawv hauv qhov ntau - qhov no yuav tsum raug coj mus rau hauv cov ntshav qab zib.

Cov khoom qab zib

Zoo li cov suab thaj thiab cov kua qab zib, cov kua qab zib muaj lub suab qab zib, txawm li cas los xij, lawv cov qauv tshuaj lom neeg tsis nyob hauv txhua qhov kev ua si. Muaj ob qho tib si ntuj thiab cov khoom qab zib. Lub ntuj tso cai suav nrog: miraculin, osladin, ernandulcin. Los ua dag: saccharin, cyclamate, neotam. Cov khoom qab zib muaj pes tsawg lub cev tsis zoo thiab raug pom zoo rau siv ob hom ntshav qab zib hom 2 thiab ntshav qab zib hom 1.

Muaj ntau dua 30 hom sweeteners, feem ntau ntawm lawv peptide lossis protein xwm. Cov khoom thaj chaw kuj muaj ntau haiv neeg, los ntawm qhov ua tiav tus kheej mus rau cov piam thaj, mus txog kaum thiab ntau pua lub sijhawm ntawm kev ua qab zib. Khoom qab zib rau cov ntshav qab zib hom 2, uas yog raws li cov khoom qab zib, tuaj yeem hloov pauv tau zoo rau kev sib xyaw ua ke.

Raug mob los ntawm sweeteners thiab sweeteners

Txawm hais tias tag nrho cov txiaj ntsig ntawm kev siv sweeteners thiab sweeteners, kev siv cov tshuaj yeeb dej caw no tseem muaj qhov tsis zoo. Yog li, cov kws tshawb fawb tau ua pov thawj tias nrog kev siv tsis tu ncua thiab siv cov piam thaj hloov ntau, kev quav tshuaj rau lub hlwb. Yog tias muaj ntau cov khoom qab zib. Tom qab ntawd nyob rau ntawm neurons ntawm lub paj hlwb cov koom nrog tshiab txoj kev txhim kho uas pab txhawb kev ua txhaum ntawm lub caloric nqi ntawm cov zaub mov, tshwj xeeb, keeb kwm carbohydrate. Yog li ntawd, kev ntsuas tsis txaus ntawm cov khoom noj muaj txiaj ntsig ntawm cov zaub mov ua rau kev tsim muaj ntau dhau los, uas cuam tshuam tsis zoo rau cov txheej txheem kev zom zaub mov.

Dab tsi yog qhov zais ntawm kev noj khoom qab zib rau cov ntshav qab zib

Txhua yam ingenious tau yooj yim! Ua ntej, koj yuav tsum paub meej meej txog hom mob ntshav qab zib thiab qhov kev them nyiaj rau nws cov tsos mob. Rau qhov no, kev txiav txim siab txog theem ntawm glycated hemoglobin thiab kev soj ntsuam ntawm cov kab mob microvascular ntawm cov ntshav qab zib (kev kuaj mob ntawm cov fundus ntawm ophthalmologist) tau zoo heev.

Thib ob, yog tias koj txiav txim siab noj zaub mov nrog lub siab glycemic index, koj yuav tsum xam ua ntej cov nqi ntawm cov carbohydrates uas yuav nkag mus rau lub cev thiab hloov mus rau chav ua mov ci (XE) txhawm rau kom raws sijhawm kom suav nrog qhov muaj kuab tshuaj insulin.

Thib peb, cov khoom lag luam nrog lub siab glycemic Performance index tuaj yeem hloov mus nrog cov qis-calorie ntau ntxiv nrog kev ntxiv cov khoom qab zib, uas yuav cawm koj los ntawm kev suav kev noj zaub mov carbohydrates thiab noj tshuaj insulin.

Kev tsim cov ntshav qab zib los ntawm cov khoom qab zib

Mob ntshav qab zib mellitus tuaj yeem tsim los ntawm khoom qab zib? Lo lus teb rau lo lus nug no yuav ntxhov siab koj, tab sis tej zaum. Yog tias qhov sib txig sib luag ntawm cov zaub mov noj thiab, raws li, lub zog muaj nws, thiab kev siv lub cev, tsis muaj peev xwm pom kev txhim kho ntshav qab zib muaj ntau ntxiv. Thaum siv cov hmoov nplej, dej tsis qab thiab haus cov dej hauv cov dej ntau ntau, koj khiav txoj kev pheej hmoo ntawm kev tsim kev rog, uas nyob rau qee lub sijhawm muaj kev pheej hmoo ntawm kev tsim hom ntshav qab zib 2.

Dab tsi yuav tshwm sim yog tias ib tus neeg rog dhau mus txuas ntxiv rau qhov kev ua neej no? Hauv lub cev ntawm cov neeg zoo li no, cov tshuaj uas txo qis rhiab ntawm cov ntaub so ntswg rau insulin yuav pib tsim, vim qhov no, cov hlwb hlwb ntawm tus txiav yuav pib tsim ntau cov insulin thiab vim li ntawd, cov chaw tsim khoom tshwj xeeb yuav ploj zuj zus thiab tus neeg yuav tsum tau siv cov tshuaj insulin.

Raws li cov ntaub ntawv tau txais, cov lus pom hauv qab no tuaj yeem kos tau:

• Tsis txhob ntshai cov khoom qab zib, koj tsuas yog xav paub txog qhov ntsuas.
• Yog koj tsis muaj ntshav qab zib, tsis txhob coj koj lub cev mus rau qhov chaw siab.
• Txog cov ntshav qab zib, muaj ntau txoj kev xaiv rau lub neej “qab zib” yam tsis muaj kev phom sij, peb tab tom hais txog cov khoom qab zib, qab zib thiab kev kho mob ntshav qab zib.

Tsis txhob ntshai cov kabmob, tab sis kawm kom nyob nrog nws thiab tom qab ntawd koj yuav nkag siab tias txhua qhov kev txwv tsuas yog hauv koj lub taub hau!