Vipidia ntsiav tshuaj - cov lus qhia rau kev siv thiab tshuaj yeeb yaj kiab

Daim ntawv teev cov tshuaj Vipidia tshaj tawm yog zaj duab xis-ntsiav tshuaj: biconvex, oval, 12.5 mg txhua - daj, ntawm ib sab sau rau hauv tus cwj mem nrog cov ntawv sau "ALG-12.5" thiab "TAK", 25 mg txhua - lub teeb liab, ntawm “ALG-25” thiab “TAK” sau tus mem kua rau ntawm ib sab (7 hauv cov hlwv, 4 lub hlwv hauv ib lub thawv ntawv).

Composition 1 ntsiav tshuaj:

• cov tshuaj nquag: alogliptin - 12.5 lossis 25 mg (alogliptin benzoate - 17 lossis 34 mg),
• Cov khoom siv pabcuam (12.5 / 25 mg): mannitol - 96.7 / 79.7 mg, magnesium stearate - 1.8 / 1.8 mg, croscarmellose sodium - 7.5 / 7.5 mg, microcrystalline cellulose - 22 5 / 22.5 mg, hyprolose - 4.5 / 4.5 mg,
• zaj duab xis txheej: hypromellose 2910 - 5.34 mg, zas hlau oxide daj - 0.06 mg, titanium dioxide - 0.6 mg, macrogol 8000 - nyob rau hauv cov cim nyiaj, kua txho F1 (shellac - 26%, zas hlau oxide dub - 10%, ethanol - 26%, butanol - 38%) - nyob rau hauv cov kab nyiaj.

Cov Tshuaj Hauv Tshuaj

Alogliptin yog qhov muaj kev xaiv tshwj xeeb rau DPP (dipeptidyl peptidase) -4 ntau qhov kev txiav txim. Nws cov kev xaiv rau DPP-4 yog kwv yees li 10,000 zaus ntau dua nws cov txiaj ntsig rau lwm cov enzymes ntsig txog, tshwj xeeb DPP-8 thiab DPP-9. DPP-4 yog lub enzyme tseem ceeb koom nrog kev rhuav tshem cov tshuaj hormones sai uas yog tsev neeg muaj ntau ntxiv: glucose-cuam tshuam insulinotropic polypeptide (HIP) thiab glucagon-zoo li peptide-1 (HIP-1). Cov tshuaj hormones ntawm tsev neeg incretin yog tsim tawm hauv txoj hnyuv, thiab nce ntxiv hauv lawv qib yog cuam tshuam ncaj qha rau kev noj zaub mov. HIP thiab GLP-1 qhib cov tshuaj insulin thiab nws cov khoom tsim tawm los ntawm cov beta hlwb hauv ib cheeb tsam hauv cov txiav ua ke. GLP-1 kuj tseem txo cov khoom lag luam glucagon thiab txwv tsis pub muaj cov kua nplaum suab thaj.

Vim li no, alogliptin tsis yog tsuas yog nce lub ntsiab lus ntawm incretins, tab sis kuj txhim kho cov kua nplaum-cuam tshuam ntawm insulin, thiab inhibits qhov zais cia ntawm glucagon nrog kev nce ntxiv hauv cov piam thaj hauv cov ntshav. Hauv cov neeg mob uas muaj ntshav qab zib hom 2 nrog hyperglycemia, cov kev hloov hauv synthesis ntawm glucagon thiab insulin ua rau txo qis ntawm cov ntshav glycated hemoglobin HbA_1c thiab qhov txo qis hauv cov qib ntawm cov piam thaj hauv cov ntshav plasma thaum noj ntawm lub plab tas, thiab kev xav txog cov piam thaj tom qab kawg.

Cov Tshuaj Pharmacokinetics

Cov tshuaj pharmacokinetics ntawm alogliptin zoo tib yam hauv cov tib neeg muaj kev noj qab haus huv thiab hauv cov neeg mob uas muaj ntshav qab zib hom 2 ntshav qab zib. Qhov tiag ntawm bioavailability ntawm cov khoom nquag yog kwv yees li 100%. Kev tswj hwm tib lub sij hawm ntawm alogliptin nrog cov zaub mov muaj cov rog hauv cov siab ntau tsis cuam tshuam thaj chaw hauv qab qhov nkhaus-sijhawm nkhaus (AUC), yog li Vipidia tuaj yeem noj thaum twg los xij, tsis hais noj zaub mov.

Kev tswj hwm qhov ncauj ib leeg ntawm alogliptin hauv ib koob li 800 mg los ntawm cov neeg noj qab haus huv ua rau muaj qhov nqus sai ntawm cov tshuaj, uas qhov nruab nrab qhov siab tshaj plaws tau tiav tom qab 1-2 teev txij li lub sijhawm tswj hwm. Tom qab rov ua dua, saib xyuas qhov tseem ceeb ntawm kev tso tshuaj alogliptin tsis pom nyob hauv cov neeg mob uas muaj ntshav qab zib hom 2 lossis cov neeg ua haujlwm noj qab haus huv.

AUC ntawm alogliptin qhia tau hais tias qhov ncaj ncaj ib feem ntawm kev siv tshuaj, nce ntxiv nrog ib koob tshuaj Vipidia hauv kev kho mob ntau npaum li ntawm 6.25-100 mg. Qhov hloov pauv qhov sib txawv ntawm qhov ntsuas qhov muag ntawm cov neeg mob yog qhov me me thiab sib npaug li 17%.

Nrog rau ib koob tshuaj AUC (0-inf), alogliptin zoo ib yam li AUC (0-24) tom qab noj cov tshuaj zoo sib xws 1 zaug hauv ib hnub rau 6 hnub. Qhov no tau lees tias tsis muaj kev vam khom ncua sij hawm nyob rau hauv pharmacokinetics ntawm cov tshuaj tom qab rov ua dua.

Tom qab kev tso tawm ib leeg ntawm kev tswj hwm cov tshuaj muaj zog Vipidia ntawm koob tshuaj 12,5 mg rau cov neeg tuaj yeem noj qab haus huv, cov ntim khoom faib rau hauv qhov davhlau ya nyob twg yog 417 l, uas qhia txog kev faib tawm zoo ntawm alogliptin hauv cov ntaub so ntswg. Qib ntawm kev khi rau cov ntshav protein yog li 20-30%.

Alogliptin tsis koom nrog hauv cov txheej txheem ntawm cov metabolism hauv lub zog, yog li 60-70% ntawm cov tshuaj muaj nyob rau hauv cov tshuaj noj yog zam tsis hloov pauv hauv cov zis.

Nrog kev qhia txog 14 C-daim ntawv lo alogliptin sab hauv, qhov muaj nyob ntawm ob lub cev tseem ceeb tau ua pov thawj: N-demethylated alogliptin, M-I (tsawg dua 1% ntawm cov khoom pib) thiab N-acetylated alogliptin, M-II (tsawg dua 6% ntawm cov khoom siv pib). M-Kuv yog ib qho kev siv tshuaj tiv thaiv kab mob uas ua rau pom muaj cov khoom tiv thaiv tsis tau zoo tiv thaiv DPP-4, zoo ib yam hauv kev ncaj qha rau alogliptin. Rau M-II, qhov kev cuam tshuam inhibitory tiv thaiv DPP-4 lossis lwm yam DPP enzymes tsis yog yam ntxwv.

Hauv cov kev tshawb fawb hauv vitro paub meej tias CYP3A4 thiab CYP2D6 koom nrog cov metabolism hauv kev txwv tsis pub muaj alogliptin. Lawv qhov kev tshwm sim tseem qhia tau tias cov tshuaj Vipidia tseem tsis yog qhov muaj txiaj ntsig ntawm CYP2B6, CYP2C9, CYP1A2 thiab cov tshuaj tiv thaiv ntawm CYP3A4, CYP1A2, CYP2D6, CYP2B6, CYP2C19, CYP2C8 lossis CYP2C9 hauv qhov kev txiav txim siab uas tau noj 25 tom qab kev noj tshuaj. Nyob rau hauv cov kab mob hauv vitro, alogliptin yuav ua rau me ntsis CYP3A4, tab sis nyob rau hauv vivo cov xwm txheej, nws cov yam ntxwv tsis tshwm nrog kev hwm txog isoenzyme no.

Hauv tib neeg lub cev, alogliptin tsis yog qhov txwv tsis pub muaj kev thauj mus los ntawm lub hauv siab lub cev ntawm cov organic cations ntawm hom thib ob thiab lub raum thauj cov organic anions ntawm hom thawj thiab thib peb.

Alogliptin tshwm sim feem ntau hauv daim ntawv ntawm (R) -enantiomer (ntau dua 99%) thiab cov nyiaj me me hauv vivo lossis tsis koom nrog txhua yam cuam tshuam nrog cov txheej txheem ntawm chiral hloov mus rau hauv (S) -enantiomer. Qhov tom kawg tsis tau txiav txim siab thaum noj Vipidia hauv kev muab tshuaj kho.

Nrog kev tswj hwm qhov ncauj ntawm 14 C-daim ntawv lo alogliptin, nws tau ua pov thawj tias 76% ntawm cov koob tshuaj tiv thaiv yog tawm hauv cov zis, thiab 13% nrog quav. Qhov nruab nrab lub raum kev tshem tawm cov tshuaj yog 170 ml / min thiab ntau dua qhov nruab nrab ntawm cov qog ntshav glomerular tus nqi kwv yees li ntawm 120 l / min, uas tso cai rau qee qhov kev tshem tawm alogliptin los ntawm kev ua kom zoo rau lub raum. Qhov nruab nrab, lub davhlau ya nyob twg ib nrab-lub neej ntawm cov nquag muaj Vipidia yog li ntawm 21 teev.

Hauv cov neeg mob uas muaj kev mob raum tsis ua haujlwm ntawm qhov txawv txav, kev tshawb fawb tau tshawb pom txog qhov tshwm sim ntawm alogliptin thaum noj hauv ib koob tshuaj 50 mg txhua hnub. Cov neeg mob nyob hauv txoj kev tshawb fawb tau muab faib ua 4 pab pawg raws li cov qauv Cockcroft - Gault, nyob ntawm qhov mob tsis zoo ntawm lub raum thiab QC (creatinine tshem tawm), tau txais cov txiaj ntsig hauv qab no:

• Pawg I (mob raum tsis ua haujlwm, CC 50–80 ml / min): AUC ntawm alogliptin ntau zog nce txog 1.7 zaus piv nrog pawg tswj hwm. Txawm li cas los xij, qhov nce no hauv AUC tseem nyob hauv qhov kam rau pawg tswj hwm,
• Pawg II (nruab nrab lub raum tsis ua hauj lwm, CC 30–50 ml / min): yuav luag 2-ntu nce ntawm AUC ntawm alogliptin tau pom piv nrog pawg tswj,
• Pawg III thiab IV (mob raum tsis ua haujlwm, CC tsawg dua 30 ml / min, thiab cov theem kawg ntawm lub raum tsis ua haujlwm yog tias tsim nyog, cov txheej txheem hemodialysis): AUC nce kwv yees 4 zaug piv nrog pawg tswj hwm. Cov neeg mob uas mob raum tsis ua haujlwm tau koom nrog txoj kev kho mob sai sai tom qab noj Vipidia. Hauv lub sijhawm peb-teev raug lim ntshav, li ntawm 7% ntawm koob tshuaj alogliptin tau tawm ntawm lub cev.

Vim li no, hauv pawg I, tsis tas yuav tsum muaj kev hloov kho koob. Hauv cov neeg mob uas lub raum tsis ua haujlwm, txhawm rau ua kom tau qhov zoo ntawm cov tshuaj nquag hauv cov ntshav ntshav, ze rau qhov ntawd rau cov neeg mob uas lub raum tsis ua haujlwm, yuav tsum tau txhaj tshuaj Vipidia kom haum. Alogliptin tsis pom zoo rau kev ua rau lub raum khiav tsis zoo, thiab rau cov neeg mob uas mob raum tsis ua haujlwm, ua ntu zus hemodialysis.

Hauv cov neeg mob uas muaj lub siab ua haujlwm tsis txaus, AUC thiab qhov siab tshaj plaws ntawm alogliptin raug txo tsawg li 10% thiab 8%, feem ntau, piv nrog cov neeg mob lub siab ua haujlwm lub siab, tab sis qhov tshwm sim no tsis yog qhov tseem ceeb hauv chaw kho mob. Yog li, kev hloov kho koob tshuaj rau Vipidia rau me ntsis mus rau me ntsis tsis txaus siab hepatic (5-9 ntsiab lus raws li Child-Pugh scale) tsis yog yuav tsum tau. Tsis muaj cov ntaub ntawv tshawb fawb txog kev siv tshuaj alogliptin hauv cov neeg mob uas tsis muaj peev xwm rau hepatic txaus (ntau dua 9 ntsiab lus).

Lub cev hnyav, hnub nyoog (nrog rau kev nce qib - 65-81 xyoo), haiv neeg thiab tub los ntxhais ntawm cov neeg mob tsis muaj kev cuam tshuam loj hauv kev kho mob ntawm qhov tseem ceeb ntawm cov tshuaj, i.e. tsis tas yuav tsum tau txhaj koob tshuaj. Cov tshuaj pharmacokinetics ntawm alogliptin hauv cov neeg mob uas muaj hnub nyoog qis dua 18 xyoo tsis tau kawm.

Cov Yuav Tsum Muaj

• ntshav qab zib hom 1
• mob rau daim siab ua haujlwm ntau (ntau dua 9 ntsiab lus ntawm qhov teev menyuam yaus-Pugh, vim tsis muaj cov ntaub ntawv tshawb fawb txog kev ua tau zoo / kev nyab xeeb ntawm kev siv),
• mob ketoacidosis,
• mob plawv tsis ua hauj lwm (FC NYHA chav kawm III - IV),
• mob raum tsis ua haujlwm
• hnub nyoog txog 18 xyoo (vim tias tsis muaj cov ntaub ntawv qhia txog qhov ua tau zoo / kev nyab xeeb ntawm cov tshuaj hauv pawg neeg mob no),
• cev xeeb tub thiab lactation (vim tias tsis muaj cov ntaub ntawv qhia txog qhov ua tau zoo / kev nyab xeeb ntawm kev siv Vipidia hauv pawg neeg mob no),
• cov tib neeg tsis haum rau cov Vipidia, cov ncauj lus anamnestic txog kev ua kom lub siab mob siab rau ib qho DPP-4 inhibitor, suav nrog kev siv tshuaj anaphylactic, angioedema thiab anaphylactic poob siab.

Tus txheeb ze (kab mob / mob uas Vipidia ntsiav tshuaj yuav tsum tau siv nrog ceeb toom):

• burdened keeb kwm ntawm cov mob leeg ncaj,
• mob raum tsis ua hauj lwm,
• ternary ua ke nrog thiazolidinedione thiab metformin,
• ua ke siv nrog cov tshuaj insulin lossis sulfonylurea derivative.

Cov lus qhia rau kev siv Vipidia: txoj kev thiab ntau npaum li cas

Vipidia ntsiav tshuaj noj ntawm qhov ncauj, tsis hais txog ntawm cov pluas noj, nqos tau tag nrho, tsis tas yuav zom thiab haus nrog dej.

Qhov pom zoo rau kev noj tshuaj txhua hnub yog 25 mg hauv 1 koob tshuaj. Cov tshuaj yog noj ib leeg, hauv kev sib xyaw nrog metformin, thiazolidinedione, sulfonylurea derivatives lossis insulin, lossis los ua peb-xyaw ua ke nrog metformin, insulin lossis thiazolidinedione.

Yog tias koj ua yuam kev ib ntsiav tshuaj, koj yuav tsum noj sai li sai tau. Siv tshuaj ib zaug rau hauv ib hnub yog tsis yooj yim sua.

Thaum Vipidia raug muab tshuaj, ntxiv rau thiazolidinedione lossis metformin, lawv kev noj tshuaj tsis hloov pauv.

Txhawm rau kom txo qis qhov yuav ua rau tus mob ntshav qab zib tsawg tsawg thaum ua ke nrog sulfonylurea derivative lossis insulin, nws raug nquahu kom lawv cov koob tshuaj txo qis.

Kev teem sijhawm ntawm peb qhov sib xyaw ua ke nrog thiazolidinedione thiab metformin yuav tsum ceeb toom (cuam tshuam nrog kev pheej hmoo ntawm hypoglycemia, koob tshuaj yuav tsum tau hloov ntawm cov tshuaj no).

Thaum lub raum tsis ua haujlwm, nws raug nquahu kom soj ntsuam lub xeev ntawm lub raum ua ntej kev kho mob, thiab tom qab ntawd ib zaug siv tshuaj kho. Cov koob tshuaj txhua hnub hauv cov neeg mob uas muaj mob me me rau lub raum (nrog creatinine tshem tawm ntawm ≥ 30 txog ml 50 ml / min) yog 12,5 mg. Hauv qhov siab / davhlau ya nyob twg ntawm lub raum tsis ua haujlwm, Vipidia tsis yog yam tshuaj.

Xyuas ntawm Vipidia

Feem ntau, muaj kev xyuas zoo txog Vipidia yog cov tshuaj uas txo cov ntshav qab zib thiab tswj cov ntshav no. Cov neeg mob tau tshaj tawm tias cov nyhuv ntawm cov tshuaj mob txuas ntxiv rau ib hnub, thaum nws tsis ua rau kom qab los noj mov, thiab raws li ib feem ntawm kev kho mob ntshav qab zib ua ke, nws pab txo qhov hnyav thiab tshem tawm cov mob ceg. Tsis tas li, cov neeg mob nyiam qhov yooj yim ntawm kev siv Vipidia: nws tuaj yeem siv tau txhua lub sijhawm ntawm hnub.

Txawm li cas los xij, tseem muaj kev tshuaj xyuas tsis zoo hais txog qhov ua tsis raug ntawm cov tshuaj thiab cov neeg muaj feem tsis haum rau alogliptin.

Cov kws tshaj lij ceeb toom tiv thaiv kev siv tsis raug ntawm Vipidia rau kev poob phaus.

Cov ntaub ntawv tshuaj dav dav

Cov cuab yeej no hais txog kev tsim kho tshiab hauv thaj tsam mob ntshav qab zib. Nws yog tsim rau cov neeg muaj kuaj mob ntshav qab zib hom 2. Vipidia tuaj yeem siv ob leeg tib leeg thiab ua ke nrog lwm cov tshuaj ntawm pawg no.

Koj yuav tsum nkag siab tias kev siv tshuaj tsis tswj tsis tu ncua tuaj yeem tsim kev phom sij rau tus neeg mob, yog li koj yuav tsum ua raws li kws kho mob cov lus pom zoo. Koj tuaj yeem siv tsis tau cov tshuaj yam tsis tau sau ntawv noj, tshwj xeeb tshaj yog thaum noj lwm yam tshuaj.

Lub npe lag luam rau cov tshuaj no yog Vipidia. Hauv theem thoob ntiaj teb, lub npe hu ua Alogliptin tau siv, uas los ntawm cov khoom tseem ceeb hauv nws cov muaj pes tsawg leeg.

Cov khoom yog sawv cev los ntawm oval zaj duab xis-coated ntsiav tshuaj. Lawv tuaj yeem yog daj lossis daj liab (nws nyob ntawm qhov tsuas tshuaj npaum li cas). Cov pob muaj 28 pcs. - 2 lub hau rau 14 ntsiav tshuaj.

Pharmacological kev txiav txim

Cov cuab yeej no yog ua raws Alogliptin. Nov yog ib qho ntawm cov tshuaj tshiab uas tau siv los tswj cov qib qab zib. Nws zwm rau tus naj npawb ntawm hypoglycemic, muaj lub zog zoo.

Thaum siv nws, muaj kev nce ntxiv ntawm cov piam thaj hauv cov kua dej tso kua mis thaum txo cov glucagon ntau lawm yog tias cov piam thaj hauv ntshav nce ntxiv.

Nrog tus mob ntshav qab zib hom 2, nrog hyperglycemia, cov nta ntawm Vipidia pab txhawb kom muaj kev hloov pauv zoo li:

• ua rau cov ntshav glycated hemoglobin (НbА1С),
• txo cov ntshav qabzib ntau ntau.

Qhov no ua rau cov cuab yeej no muaj peev xwm kho tau tus mob ntshav qab zib.

Kev taw qhia thiab contraindications

Cov tshuaj uas muaj qhov tshwm sim los ntawm muaj zog yuav tsum ua tib zoo siv. Cov lus qhia rau lawv yuav tsum tau ua raws txoj cai, txwv tsis pub muaj txiaj ntsig rau tus neeg mob lub cev yuav raug mob. Yog li, koj tuaj yeem siv Vipidia tsuas yog kev pom zoo ntawm cov kws tshaj lij nrog kev soj ntsuam nruj ntawm cov lus qhia.

Cov cuab yeej pom zoo rau siv nrog ntshav qab zib hom 2. Nws muab cov kev cai ntawm cov piam thaj hauv rooj plaub thaum siv tshuaj kho zaub mov tsis siv thiab qhov kev qoj ib ce tsim nyog tsis muaj. Ua tau zoo siv cov tshuaj rau monotherapy. Nws tseem raug tso cai siv nrog kev siv ua ke nrog lwm cov tshuaj uas pab txo qis dua cov piam thaj.

Ceev faj thaum siv cov tshuaj ntshav qab zib no tshwm sim los ntawm qhov muaj qhov tsis sib xws. Yog tias lawv tsis raug suav nrog, kev kho yuav tsis muaj txiaj ntsig thiab tuaj yeem ua rau muaj kev phom sij.

Vipidia tsis raug tso cai nyob rau hauv cov xwm txheej hauv qab no:

• kev tsis qaug rau lub zog ntawm cov tshuaj,
• ntshav qab zib hom 1
• lub plawv dhia tsis zoo
• daim siab mob
• mob raum ntau
• cev xeeb tub thiab lactation,
• kev tsim kho ketoacidosis los ntawm ntshav qab zib,
• tus neeg mob lub hnub nyoog txog 18 xyoo.

Cov kev ua txhaum no yog nruj contraindications rau siv.

Nws tseem muaj lub xeev hauv cov tshuaj uas tau sau tseg kom zoo:

• pancreatitis
• raum tsis ua hauj lwm ntawm mob hnyav hnyav.

Ib qho ntxiv, kev saib xyuas yuav tsum tau noj thaum sau ntawv rau Vipidia nrog rau lwm cov tshuaj los tswj cov ntshav qabzib.

Sab sij huam

Thaum kho nrog cov tshuaj no, qee zaum muaj kev phiv tshuaj nrog kev cuam tshuam ntawm cov tshuaj tshwm sim:

• mob taub hau
• kabmob kis kev ua pa
• nasopharyngitis,
• mob plab
• khaus
• daim tawv nqaij ua pob,
• mob leeg txhaj leeg
• urticaria
• kev loj hlob ntawm daim siab ua haujlwm.

Yog tias muaj kev mob tshwm sim, sab laj nrog kws kho mob. Yog tias lawv qhov tshwm sim tsis ua teeb meem rau tus neeg mob txoj kev noj qab haus huv, thiab lawv qhov kev siv tsis tau nce ntxiv, kev kho mob nrog Vipidia tuaj yeem txuas ntxiv. Qhov mob hnyav ntawm tus neeg mob yuav tsum tau tshem tawm cov tshuaj tam sim ntawd.

Tsuas tshuaj thiab tswj hwm

Cov tshuaj no yog npaj rau lub luag haujlwm. Qhov ntau npaum li cas tau muab xam rau ntawm tus kheej, raws li qhov mob hnyav, lub hnub nyoog ntawm tus neeg mob, cov kab mob sib kis thiab lwm yam ntxwv.

Qhov nruab nrab, nws yuav tsum noj ib ntsiav tshuaj muaj 25 mg ntawm lub nquag ua tshuaj. Thaum siv Vipidia hauv ib qhov tshuaj 12,5 mg, qhov tshuaj txhua hnub yog 2 ntsiav tshuaj.

Nws raug nquahu kom noj cov tshuaj ib hnub ib zaug. Cov tshuaj yuav tsum ua kom qaug cawv tsis tas yuav zom. Nws raug nquahu kom haus lawv nrog dej npau. Kev txais tos yog pub ob qho tib si ua ntej thiab tom qab noj mov.

Tsis txhob siv ob zaug tshuaj ntawm cov tshuaj yog tias ib zaug tsis nco qab - qhov no tuaj yeem ua rau ploj mus. Koj yuav tsum tau noj lub niaj zaus ntawm cov tshuaj nyob rau hauv lub heev ze yav tom ntej.

Cov lus qhia tshwj xeeb thiab cov tshuaj sib cuam tshuam

Siv cov tshuaj no, nws raug nquahu kom coj mus rau hauv tus lej qee qhov tshwj xeeb kom tsis txhob muaj kev phom sij:

1. Hauv lub sijhawm ntawm kev xeeb menyuam, Vipidia yog contraindicated. Kev tshawb fawb seb qhov kev kho no cuam tshuam rau tus me nyuam hauv plab tsis tau ua dab tsi. Tab sis cov kws kho mob nyiam tsis siv nws, yog li tsis ua kom npau taws lossis txhim kho kev yug menyuam hauv plab. Tib yam mus rau kev pub mis niam.
2. Cov tshuaj tsis tau siv los kho cov menyuam yaus, vim tias tsis muaj cov ntaub ntawv qhia tseeb txog nws qhov ntxim rau cov menyuam yaus lub cev.
3. Kev laus ntawm cov neeg laus tsis yog lub laj thawj ntawm kev tshem tawm cov tshuaj. Tab sis noj Vipidia hauv qhov no yuav tsum tau soj ntsuam los ntawm kws kho mob. Cov neeg mob hnub nyoog tshaj 65 xyoos muaj qhov pheej hmoo tiv thaiv mob raum, yog li yuav tsum tau ceev faj thaum xaiv koob.
4. Rau kev ua kom lub raum tsis zoo, cov neeg mob tau raug xaj rau 12,5 mg rau ib hnub.
5. Vim tias txoj kev hem thawj ntawm kev tsim kab mob pancreatitis thaum siv cov tshuaj no, cov neeg mob yuav tsum paub tus cwj pwm tseem ceeb ntawm tus kab mob no. Thaum lawv tshwm sim, nws yog ib qho tsim nyog yuav tsum tso tseg kev kho mob nrog Vipidia.
6. Kev noj cov tshuaj tsis txhaum txoj cai lub peev xwm. Yog li, thaum siv nws, koj tuaj yeem tsav lub tsheb thiab koom nrog kev ua si uas yuav tsum muaj kev kub siab. Txawm li cas los xij, hypoglycemia tuaj yeem ua rau muaj kev nyuaj rau thaj chaw no, yog li yuav tsum tau ceev faj.
7. Cov tshuaj muaj peev xwm ua tsis zoo rau kev ua haujlwm ntawm lub siab. Yog li, ua ntej nws teem caij, yuav tsum muaj kev kuaj xyuas lub cev no.
8. Yog tias Vipidia npaj yuav siv ua ke nrog lwm cov tshuaj los txo cov ntshav qabzib, lawv cov koob tshuaj yuav tsum tau kho.
9. Kev kawm txog kev cuam tshuam ntawm cov tshuaj nrog lwm cov tshuaj tsis tau muaj kev hloov pauv ntau.

Thaum cov ntsej muag no raug suav nrog, kev kho tuaj yeem ua kom zoo dua qub thiab muaj kev nyab xeeb.

Tshuaj ua

Alogliptin muaj cov lus xaiv hais txog kev cuam tshuam ntawm qee yam enzymes, suav nrog dipeptidyl peptidase-4. Qhov no yog qhov tseem ceeb enzyme uas koom nrog kev puas tsuaj sai heev ntawm cov tshuaj hormones nyob rau hauv daim ntawv ntawm cov piam thaj-insulinotropic polypeptide qabzib. Lawv nyob hauv cov hnyuv thiab thaum noj mov txhawb kom cov kua dej hauv cov hlab ua kom txiav tawm.

Ib qho glucose-zoo li peptide, nyeg, txo qis qib glucagon thiab inhibits qhov ua haujlwm ntawm cov piam thaj hauv lub siab. Nrog rau qhov tshwm sim me lossis loj ntxiv nyob rau hauv cov theem ntawm incretins, feem tseem ceeb ntawm cov tshuaj Vipidia 25, alogliptin pib nce insulin ntau lawm thiab txo qis glucagon nrog kev nce siab ntxiv ntawm cov piam thaj hauv cov ntshav. Txhua yam no ua rau txo qis hemoglobin hauv cov neeg mob kev txom nyem los ntawm ntshav qab zib hom 2.

Vipidia 25 lossis 12,5 ntsiav tshuaj rau cov ntshav qab zib tau tso cai muag hauv cov khw muag tshuaj tshwj xeeb nkaus xwb.

Kev ntsuas rau siv

Vipidia 25 yog qhia rau mob ntshav qab zib mellitus hauv kev sib xyaw nrog lwm cov tshuaj muaj cov tshuaj insulin. Cov tshuaj yog hypoglycemic. tshuaj kho qhov ncauj, yog qhia txog kev kho mob ntshav qab zib hom 2 mob ntshav qab zib txhawm rau txhawm rau tswj cov ntshav qabzib kom tsis txhob noj zaub mov thiab ua haujlwm rau lub cev.

Dosage daim ntawv

12,5 mg thiab 25 mg zaj duab xis-ntsiav tshuaj txheej

Ib ntsiav tshuaj muaj

cov tshuaj nquag: alogliptin benzoate 17 mg (sib npaug rau 12.5 mg ntawm alogliptin) thiab 34 mg (sib npaug rau 25 mg ntawm alogliptin)

Cov tub ntxhais: mannitol, microcrystalline cellulose, hydroxypropyl cellulose, croscarmellose sodium, magnesium stearate

Cov sib xyaw ua ke ntawm cov zaj duab xis membrane: hypromellose 2910, titanium dioxide (E 171), hlau oxide daj (E 172), hlau oxide liab (E 172), polyethylene glycol 8000, grey number case F1

Oval biconvex ntsiav tshuaj, coated nrog zaj duab xis daj xim, sau npe "TAK" thiab "ALG-12.5" ntawm ib sab ntawm lub ntsiav tshuaj (rau qhov ntau npaum 12,5 mg),

Oval biconvex ntsiav tshuaj, zaj duab xis-xim nrog lub teeb xim liab, sau npe rau "TAK" thiab "ALG-25" ntawm ib sab ntawm lub ntsiav tshuaj (rau qhov ntau npaum li 25 mg).

Cov chaw muag tshuaj

Cov pharmacokinetics ntawm alogliptin tau kawm txog kev tshawb fawb txog kev noj qab haus huv thiab cov neeg mob ntshav qab zib hom 2. Hauv cov neeg ua haujlwm noj qab haus huv, tom qab ib qho kev tswj hwm qhov ncauj ntau txog 800 mg ntawm alogliptin, kev nqus tshuaj sai yog pom nrog qhov siab tshaj plaws ntshav ntawm ib mus txog ob teev txij li lub sijhawm kev tswj hwm (nruab nrab Tmax). Tom qab noj qhov siab tshaj plaws pom zoo siv tshuaj kho mob (25 mg), zaum kawg ib nrab-lub neej (T1 / 2) qhov nruab nrab 21 teev.

Tom qab rov ua dua txog li ntawm 400 mg rau 14 hnub hauv cov neeg mob uas mob ntshav qab zib hom 2, kev sib txuam ntawm alogliptin tsawg kawg tau pom nrog qhov nce ntawm thaj chaw hauv qab txoj kab txiav pharmacokinetic (AUC) thiab qhov siab tshaj plaws ntshav siab (Cmax) los ntawm 34% thiab 9%, feem. Nrog rau ob qho tshuaj tiv thaiv ib leeg thiab ntau koob tshuaj alogliptin, AUC thiab Cmax nce rau hauv kev faib ua feem rau qhov nce hauv koob tshuaj 25 mg txog 400 mg. Qhov coefficient ntawm kev hloov pauv ntawm AUC ntawm alogliptin ntawm cov neeg mob yog qhov me me (17%).

Qhov tseeb ntawm bioavailability ntawm alogliptin yog kwv yees li 100%. Txij li thaum noj cov tshuaj alogliptin nrog cov zaub mov uas muaj cov roj nyeem ntau, tsis muaj kev cuam tshuam rau AUC thiab Cmax tau pom, cov tshuaj no tuaj yeem noj tsis hais lub pluas noj.

Tom qab kev tso tshuaj ib leeg ntawm alogliptin ntawm koob tshuaj 12,5 mg rau cov neeg ua haujlwm noj qab haus huv, cov ntim hauv qhov davhlau ya nyob twg yog 417 L, uas qhia tau tias alogliptin zoo xa tawm hauv cov ntaub so ntswg.

Kev sib txuas lus nrog cov protein ntshav yog 20%.

Alogliptin tsis raug rau cov metabolism hauv kev nthuav dav, vim qhov ntawd los ntawm 60% mus rau 71% ntawm cov tshuaj tau muab tso tawm tsis hloov pauv hauv cov zis. Tom qab kev tswj hwm ntawm qhov ncauj ntawm 14C-daim ntawv lo alogliptin, ob lub cev me me tau txiav txim siab: N-demethylated alogliptin M-I (˂ tsawg dua 1% ntawm cov khoom pib) thiab N-acetylated alogliptin M-II (˂ tsawg dua 6% ntawm cov khoom pib). M-Kuv yog lub cev siv tshuaj tiv thaiv metabolite thiab xaiv cov tshuaj tiv thaiv ntawm DPP-4, zoo ib yam hauv kev ua rau alogliptin, M-II tsis qhia kev tiv thaiv kev ua haujlwm tiv thaiv DPP-4 lossis lwm yam DPP-nyiam enzymes. Hauv cov kev tshawb fawb hauv vitro tau qhia tias CYP2D6 thiab CYP3A4 pab txhawb cov khoom noj tsis muaj zog ntawm alogliptin. Alogliptin tshwm sim muaj ntau nyob rau hauv daim ntawv ntawm (R) enantiomer (> ntau dua 99%) thiab yauv hloov chiral mus ua ib qho (S) enantiomer me me hauv vivo. (S) -enantiomer tsis kuaj pom thaum noj cov tshuaj alogliptin hauv tshuaj kho (25 mg).

Tom qab noj 14C-daim ntawv lo alogliptin, 76% ntawm tag nrho cov tshuaj lom neeg mob yog tawm los ntawm ob lub raum thiab 13% dhau los ntawm txoj hnyuv, nce mus txog ib feem ntawm 89%

muab tshuaj rau hluav taws xob. Kev hlais tawm ntawm cov xim alogliptin (9.6 L / h) qhia tau tias muaj cov leeg zais cia. Kev ua haujlwm ntawm cov kab ke yog 14.0 l / teev.

Pharmacokinetics hauv cov pab pawg neeg mob tshwj xeeb: lub raum tsis ua haujlwm

AUC ntawm alogliptin nyob rau hauv cov neeg mob uas tsis hnov ​​mob lub raum kev ua haujlwm ntawm qhov mob me (60≤ creatinine tshem tawm (CrCl)

Sab sij huam

Txij li cov kev sim kho mob tau ua nyob rau hauv cov xwm txheej sib txawv heev, nws tsis tuaj yeem piv ncaj qha qhov nquag muaj kev phiv tshuaj pom nyob rau hauv kev soj ntsuam kev kho mob ntawm cov yeeb tshuaj nrog cov zaus uas tau pom nyob hauv kev sim kho mob ntawm lwm cov tshuaj, thiab cov ntau zaus zoo li no yuav tsis nco ntsoov qee qhov xwm txheej ntawm kev siv tshuaj hauv kev siv.

Hauv kev tshuaj ntsuam xyuas ua ke ntawm 14 qhov kev soj ntsuam hauv tsev kho mob, tag nrho qhov tshwm sim ntawm qhov tshwm sim tsis zoo yog 73% hauv cov neeg mob tau txais alogliptin 25 mg, 75% hauv pawg placebo, thiab 70% hauv pawg nrog lwm cov tshuaj sib piv. Feem ntau, qhov txiav tawm tsis txaus ntseeg vim tias qhov tshwm sim tsis zoo yog 6.8% hauv pawg 25 mg alogliptin, 8.4% hauv pawg placebo, lossis 6.2% hauv pab pawg nrog lwm qhov kev sib piv.

Muaj cov ntaub ntawv tshaj tawm txog cov kev mob tshwm sim ntau tshaj li 4% hauv cov neeg mob uas tau txais alogliptin: nasopharyngitis, mob taub hau, mob ntsws.

Cov kev mob tshwm sim hauv qab no tau piav qhia hauv Ntu Lus Qhia Tshwj Xeeb:

- Cov kab mob rau daim siab

Cov kab mob ntshav qab zib hauv lub cev tau qhia tawm raws li cov ntshav piam thaj thiab / lossis kev soj ntsuam thiab cov tsos mob ntawm cov ntshav qog ntshav qab zib. Hauv kev kawm txog kev kho mob monotherapy, qhov tshwm sim ntawm hypoglycemia tau pom nyob hauv 1.5% thiab 1.6% ntawm cov neeg mob hauv alogliptin thiab placebo pawg, feem. Kev siv cov alogliptin ua qhov sib txuas rau kev kho glyburide lossis insulin tsis nce qhov tshwm sim ntawm kev mob ntshav qab zib tsawg dua piv nrog cov placebo. Hauv kev kawm kho mob monotherapy muab piv rau alogliptin nrog sulfonylureas hauv cov neeg mob laus, qhov tshwm sim ntawm kev mob ntshav qab zib tsawg yog 5.4% thiab 26% hauv alogliptin thiab glipizide pawg.

Cov kev mob tshwm sim hauv qab no tau txheeb xyuas lub sijhawm tom qab kev siv tshuaj alogliptin - kev tiv thaiv kev tsis haum (mob hlwb anaphylaxis, Quincke's edema, pob khaus, urticaria), mob tawv nqaij ntau ntxiv (nrog rau Stevens-Johnson syndrome), ua kom mob siab rau daim siab, ua kom lub siab ua haujlwm tsis zoo, ua rau lub siab tsis ua hauj lwm. thiab mob leeg, mob plab, raws plab, cem quav, xeev siab, thiab hnyuv tawm tsam.

Vim tias qhov tshwm sim tsis zoo no tau qhia tawm ntawm cov neeg tsis txaus ntseeg, nws tsis tuaj yeem ntseeg tau qhov lawv tsis tseg, yog li cov zaus raug faib raws li tsis paub.

Cov tshuaj sib cuam tshuam

Vipidium tsuas yog ua tawm los ntawm lub raum thiab tsuas yog nkag me ntsis los ntawm cytochrome (CYP) P450 enzyme system. Hauv kev kawm txog kev tshawb fawb, tsis muaj

muaj kev cuam tshuam loj nrog cov substrates lossis cytochrome inhibitors lossis nrog lwm cov tshuaj uas tau tawm los ntawm lub raum.

Hauv tshuaj ntsuam xyuas tshuaj vitro

Kev tshawb fawb hauv cov tshuaj hauv vitro qhia tias alogliptin tsis yog qhov tsis txaus siab CYP1A2, CYP2B6, CYP2C9, CYP2C19 thiab CYP3A4, thiab tseem tsis inhibit CYP1A2, CYP2C8, CYP2C9, CYP2C19, CYP3A4 thiab CYP2D6.

Hauv vivo tshuaj ntsuam kev sib cuam tshuam

Cov nyhuv ntawm alogliptin rau lwm cov tshuaj

Hauv kev sim tshuaj, cov nyhuv ntawm alogliptin rau pharmacokinetic cov tshuaj ntawm cov tshuaj uas cuam tshuam los ntawm CYP isoenzymes lossis raug tshem tawm tsis hloov pauv tsis tau tshwm sim. Raws li cov txiaj ntsig ntawm cov kev tshawb fawb pharmacokinetic tau piav qhia, kev pom zoo koob tshuaj ntawm Vipidia ™ tsis pom zoo.

Qhov tshwm sim ntawm lwm cov tshuaj rau ntawm pharmacokinetics ntawm alogliptin Tsis muaj qhov kev hloov pauv loj hauv cov chaw muag tshuaj thaum siv alogliptin concomitantly nrog metformin, cimetidine gemfibrozil (CYP2C8 / 9), pioglitazone (CYP2C8), fluconazole (CYP2C9) (CYP2C9) digoxin.

Noj ntau dhau

Qhov siab tshaj plaws ntawm alogliptin hauv kev soj ntsuam kuaj mob yog 800 mg ib zaug hauv cov neeg ua haujlwm noj qab haus huv thiab 400 mg ib zaug ib hnub rau 14 hnub hauv cov neeg mob ntshav qab zib hom 2, uas yog 32 thiab 16 lub sijhawm siab dua qhov siab tshaj plaws pom zoo siv tshuaj ntawm 25 mg. Kuj tsis pom muaj qhov tsis zoo tshwm sim dab tsi nrog cov koob tshuaj no.

Yog tias muaj kev siv tshuaj ntau dhau ntawm Vipidia ™, nws raug nquahu kom tshem tawm cov tshuaj tsis huv tawm ntawm lub plab zom mov thiab muab kev saib xyuas kev kho mob uas tsim nyog, nrog rau kev kho tus mob. Tom qab 3 teev ntawm hemodialysis, li 7% ntawm alogliptin tuaj yeem tshem tawm. Yog li, qhov ua tau ntawm hemodialysis nyob rau hauv rooj plaub ntawm kev overdose tsis zoo li. Tsis muaj ntaub ntawv hais txog kev tshem tawm alogliptin los ntawm peritoneal lim ntshav.

Daim ntawv thov nta

Vipidia tsis raug siv los kho ntshav qab zib ntawm cov menyuam yaus thiab tub ntxhais hluas. Cov lus qhia rau kev siv tsis muaj cov ntaub ntawv hais txog kev sim kho hauv pawg neeg mob no. Hauv cov xwm txheej zoo li no, cov kws kho mob siv cov tshuaj analogues.

Rau kev kho mob ntawm qeb ntawm cov neeg laus cov neeg laus, cov tshuaj yog raug kho tiav. Rau kev kho mob ntawm cov neeg laus, siv cov tshuaj txhua hnub siv, uas tsis tas yuav kho. Txawm hais tias koj yuav tsum tsis txhob hnov ​​qab tias alogliptin, uas tau nkag mus rau hauv lub cev, muaj peev xwm cuam tshuam rau kev ua haujlwm ntawm lub siab thiab lub raum.

Kev cuam tshuam nrog lwm yam tshuaj

Nrog rau cov kev kho mob nrog Vipidia thiab lwm yam tshuaj tiv thaiv ntshav qab zib, nws yog ib qho tseem ceeb los xam thiab kho qhov ntau ntxiv los tiv thaiv qhov pib ntawm hypoglycemia.

Cov kev tshawb fawb tsis pom pom muaj kev hloov dab tsi hauv kev sib xyaw ntawm alogliptin thiab lwm yam khoom xyaw ntawm cov tshuaj kho ntshav qab zib.

Lub zog muaj zog ntawm cov tshuaj ntawm lub cev tau sau tseg, uas txwv tsis pub haus dej haus cawv. Nws yog txwv tsis pub siv cov tshuaj rau lub sijhawm ntawm kev coj tus kheej thiab pub mis rau menyuam vim qhov tsis zoo. Cov kev tshawb fawb pom tau tias cov tshuaj no tsis ua rau poob siab lossis cuam tshuam, tsis muaj peev xwm cuam tshuam rau kev ceev faj, thiab raug pom zoo rau kev siv los ntawm cov neeg tsav tsheb.

Peb muab cov luv nqi rau cov nyeem ntawm peb lub xaib!

Npaj cov haujlwm zoo sib xws

Thaum tsis muaj cov tshuaj uas yuav muaj cov muaj tib lub ntsiab lus thiab ua haujlwm. Tab sis muaj cov tshuaj uas zoo sib xws hauv nqe, tab sis tsim los ntawm lwm cov khoom xyaw nquag uas tuaj yeem ua analogues ntawm Vipidia.

Cov no suav nrog:

1. Januvia. Cov tshuaj no raug nquahu kom txo cov ntshav qab zib. Tus nquag ua hauj lwm yog sitagliptin. Nws yog tshuaj nyob hauv tib kis zoo li Vipidia.
2. GalvusCov. Cov tshuaj yog nce raws Vildagliptin. Cov khoom no yog qhov sib piv ntawm Alogliptin thiab muaj tib lub zog.
3. JanumetCov. Qhov no yog kev sib txuam ua ke nrog hypoglycemic effect. Lub ntsiab ntawm cov tseem ceeb yog Metformin thiab Sitagliptin.

Cov kws muag tshuaj kuj tseem tuaj yeem muab lwm yam tshuaj los hloov Vipidia. Yog li, nws tsis tas yuav zais los ntawm kws kho mob cov kev hloov pauv hauv lub cev cuam tshuam nrog nws qhov kev nqus.

Cov lus qhia tshwj xeeb thiab cov kev sib cuam tshuam

Cov tshuaj Vipidia tsis cuam tshuam rau kev ua haujlwm cuam tshuam nrog kev nce siab ntawm kev saib xyuas, thaum tsav tsheb lub tsheb tau tso cai thaum kho. Siv cov tshuaj tsis haum nrog lwm cov tshuaj hypoglycemic saib xyuas los ntawm cov kws kho mob saib xyuas, vim tias nws yuav tsim nyog kho qhov kev kho mob thiab txo cov tshuaj noj. Qhov no cuam tshuam nrog kev pheej hmoo ntawm kev txhim kho tus mob hypoglycemic.

Ua ntej sau cov tshuaj rau cov neeg mob uas lub raum tsis zoo, kev tshawb fawb ntxiv yog los txiav txim siab cov lus teb ntawm lub cev muaj kabmob mus rau kev noj cov tshuaj.

Yog tias muaj kev ua haujlwm tsis zoo ntawm lub raum cov tshuaj raug muab tso tseg, thiab tshuaj analogues yog tshuaj. Nrog rau qhov muaj mob hnyav ntawm cov kab mob pathology, kev noj tshuaj yog txo rau 12,5 mg. Cov khoom siv tseem ceeb, alogliptin muaj peev xwm ua rau muaj kev mob siab rau kom muaj tus mob ua paug, txhawm rau suav tias yog kis kab mob ntawm lub plab zom mov.

Cov cim qhia kev ceeb toom yuav yog cov tsos mob ntawm lub plab hauv plab nrog irradiation nyob tom qab.

Nrog cov tsos mob zoo li no, cov tshuaj tau raug muab tso tseg.Kev kho mob mus ntev nrog Vipidia tuaj yeem ua rau lub raum ua haujlwm tsis zoo, tab sis kev hloov tshuaj tsis tas yuav tsum muaj cov khoom hauv ib txwm coj los kho.

Nqe thiab analogues

Cov tshuaj Vipidia - tus nqi hauv khw muag tshuaj hauv Moscow pib ntawm 800 rubles. Tus nqi nruab nrab txawv ntawm 1000 rubles mus rau 1500 rubles.

Cov tshuaj ntawm cov tshuaj Vipidia: