Tsim Tshuaj Ntshav Qab Zib Tshiab

Saxagliptin yog ib qho tshuaj hypoglycemic uas tau siv hauv kev kho mob rau kev kho mob rau cov ntshav qab zib tsis-insulin. Hauv tsab xov xwm peb yuav soj ntsuam saxagliptin - cov lus qhia rau kev siv.

Saib xyuas! Hauv kev faib tawm tswv yim-tshuaj kho-tshuaj (ATX), saxagliptin yog qhia los ntawm code A10BH03. International Lub Npe Tsis Muaj Nyiaj (Latin): Saxagliptin.

Daim ntawv tso tawm

Saxagliptin (С18Н25N3O2, Mg = 315.41 g / mol) muaj nyob hauv cov tshuaj hauv daim ntawv dawb crystalline hmoov, uas tsuas yog soluble me ntsis hauv dej. Cov tshuaj muaj nyob rau hauv daim ntawv ntawm cov ntsiav tshuaj nrog zaj duab xis txheej ntawm 2.5 mg thiab 5 mg. Lub npe tshuaj lag luam: "Ongliza".

Pharmacodynamics thiab pharmacokinetics: lus piav qhia

Saxagliptin yog qhov thib peb gliptin pom zoo hauv Lavxias. Gliptins yog cov tshuaj tiv thaiv kev tiv thaiv ntawm cov nyias nyias cov nyias nyias. DPP-4 yog lub luag haujlwm rau qhov kev xem ntawm incretins. Cov incretins yog tsim nyob rau hauv cov hlwb endocrine ntawm txoj hnyuv, qhov tseem ceeb tshaj plaws yog glucagon-zoo li peptide-1 (GLP-1) thiab cov kua nplaum-nyob insulinotropic polypeptide (HIP). Polypeptides yog zais cia tom qab noj mov, uas ua rau cov tshuaj tiv thaiv cov kab mob insulin muaj zais cia thiab kev cuam tshuam ntawm glucagon ntau lawm. Saxagliptin muaj cov nyhuv los tiv thaiv kab mob siab. Nws yuav tsum raug sau tseg tias DPP-4 catalyzes tsis yog tsuas yog kev rhuav tshem ntawm incretins, tab sis kuj cytokines thiab lwm yam peptides.

Tom qab kev tswj hwm ntawm qhov ncauj, saxagliptin nrawm nrawm: nce siab ntshav nce mus txog tom qab 2 teev. Qhov ncauj ntawm qhov ncauj txog kev noj qab haus huv yog li 70%. Cov tshuaj yog metabolized los ntawm CYP3A4 thiab CYP3A5 mus rau qhov nquag sib txuas - 5-hydroxysaxagliptin (M2) - zoo li lwm yam, tsis tshua muaj cov metabolites. M2 muaj kwv yees li ib nrab ntawm kev ua si pharmacological ntawm cov tshuaj. Lub plasma ib nrab-lub neej yog li 2½ teev, thiab M2 yog li 3 teev. Cov tshuaj feem ntau tawm ntawm lub cev tsis hloov pauv (70%) thiab muaj cov zis (30%). Raws li, kev ua haujlwm ntawm lub cev tsis hloov nrog qhov kev txo qis hauv lub siab ua haujlwm.

Kev taw qhia thiab contraindications

Qhov ua tau zoo thiab kev pom zoo ntawm cov tshuaj tau kawm hauv 6 qhov kev tshawb fawb luam tawm nyob rau hauv uas cov tshuaj tshiab tau sim raws li kev kho mob monotherapy lossis adjuvant therapy. Cov kev tshawb fawb no tsis kawm txog qhov cuam tshuam ntawm kev tsis muaj hlwb thiab lub neej. Cov tshuaj tsis tau piv nrog rau lwm cov glyptins.

Hauv kev tshawb pom ob zaug, cov neeg mob ntshav qab zib tau txais ntau yam tshuaj saxagliptin lossis placebo. Cov neeg mob tsis noj lwm yam tshuaj tiv thaiv kab mob. Hauv pab pawg neeg uas tau txais qhov "tsawg" txhua hnub kev noj haus, 282 tus neeg raug kho rau 12 lub lis piam. Kev kho cov tshuaj Placebo ua rau muaj HbA1c me ntsis. Ib qho tseem ceeb ntau dua txo tau ua tiav nyob rau txhua pawg uas tau siv tshuaj nrog saxagliptin. Qhov txiaj ntsig zoo tshaj plaws tau muab rau hauv ib koob tshuaj txhua hnub ntawm 5 mg ntawm saxagliptin.

Txoj kev tshawb nrhiav zaum ob, uas tau koom nrog 265 tus neeg, tau siv sijhawm 24 lub lim tiam. Peb kev noj cov tshuaj thiab cov placebo pawg tau sib piv. Thaum nruab nrab HbA1c tus nqi nce siab me ntsis nrog cov placebo, tus nqi no poob qis nrog kev noj tshuaj. Txij li 35% mus rau 41% ntawm cov neeg siv nquag muaj HbA1c tsawg dua 7%. Ntxiv rau, cov qib ntawm cov piam thaj hauv cov ntshav (ua ntej thiab tom qab 2 teev tom qab noj mov) tau qis dua thaum siv cov tshuaj ntau dua li siv cov placebo.

Kev tshawb nrhiav 24 lub lim tiam siv glibenclamide ntawm koob tshuaj 7,5-15 mg / hnub rau kev sib piv. Thaum tsis muaj txiaj ntsig txaus, metformin tau muab rau cov neeg mob. Txoj kev tshawb no koom nrog 768 cov neeg uas pib HbA1c qhov tseem ceeb yog li 7.5 txog 10%. Ua ke nrog sulfonylurea, ib koob tshuaj 2.5 mg ntawm saxagliptin tsuas yog me ntsis txo glycated hemoglobin.

Hauv lwm txoj kev tshawb nrhiav, 565 cov neeg mob ntshav qab zib tau txais ib qho tshuaj lossis cov placebo ntxiv rau txoj kev kho mob ruaj khov nrog glitazone. Txoj kev tshawb no feem ntau mob siab rau kev kawm txog cov txiaj ntsig ntawm pioglitazone. Hauv txoj kev tshawb no, muaj kev txhim kho tseem ceeb hauv kev paub txog kev zom zaub mov tau tiav hauv 24 lub lis piam uas siv cov tshuaj sib xyaw ua ke.

Hauv cov menyuam yaus thiab cov tub ntxhais hluas hnub nyoog qis dua 18 xyoo, tsis tau kawm txog cov tshuaj no. Saxagliptin kuj tseem zoo dua tsis yog yuav tsum tau sau ntawv rau cov poj niam cev xeeb tub thaum lactation.

Sab sij huam

5% ntawm cov neeg mob tau hnov ​​mob taub hau, ua pa nyuaj thiab mob txeeb zig. Cov kev mob tshwm sim zoo li no hauv cov kev tshawb fawb placebo. Qhov mob Sinusitis, mob plab, mob ncauj plab, lossis ntuav tshaj tawm ntau dua 2% ntawm cov neeg ua nrog tshuaj. Tus lej pes tsawg ntawm lymphocytes thaum siv tshuaj. Ib tus neeg mob tau mob lymphocytopenia, tab sis tom qab ntawd cov kws tshawb fawb pom tias nws tau kho hluav taws xob ntau.

Kev ua xua tsis haum (urticaria, ntsej muag o) tau pom hauv 1.5% ntawm cov neeg mob tau txais saxagliptin. Kev mob ntshav qab zib yuav luag tshwm sim thaum lub sijhawm sib koom ua ke nrog sulfonylurea. Feem ntau, saxagliptin tsis ua kom nce phaus. Txawm li cas los xij, kev siv tshuaj rau lub cev feem ntau tau pom thaum siv cov tshuaj ntawm 5 koob tshuaj rau ib hnub. Raws li qee qhov kev tshawb fawb, cov tshuaj yuav ua rau mob pancreatitis.

Tsuas tshuaj thiab tshaj

Cov tshuaj no tau txais kev pom zoo rau kev kho mob rau cov neeg laus uas tsis muaj tshuaj insulin-mob ntshav qab zib nyob rau hauv ib koob tshuaj txhua hnub ntawm 2.5 lossis 5 mg raws li kev kho mob monotherapy lossis ntxiv rau cov tshuaj metformin, sulfonylureas lossis glitazones. Kev sib xyaw nrog insulin tsis pom zoo. Thaum tsis ua haujlwm ntawm lub raum tsis ua haujlwm, qhov ntau tshaj yog 2.5 mg / hnub. Ua ntej thawj zaug kev teem caij, nws yog ib qhov tsim nyog los kuaj xyuas theem ntawm ntshav creatinine.

Kev sib txuam

Cov CYP3A4 / 5 muaj zog inhibitors - ketoconazole - tuaj yeem ua rau muaj qhov nce ntxiv ntawm ntshav ntau ntawm saxagliptin. Yog tias kev sib koom tes nrog ketoconazole yog yuav tsum tau, qhov koob tshuaj txhua hnub yuav tsum tsis pub tshaj 2.5 mg. Tsis muaj zog CYP3A4 / 5 inhibitors, xws li diltiazem, tsis tas yuav txo koob tshuaj. Raws li kev paub dhau los, cov tshuaj tsis cuam tshuam cov kinetics ntawm lwm cov tshuaj.

Saksagliptin - analogues thiab hloov chaw:

Kev xav ntawm tus kws kho mob ntshav qab zib thiab ntshav qab zib txog cov tshuaj.

Glyptins tsuas yog siv rau kev kho mob hom 2 ntshav qab zib. Cov tshuaj ntawm cov pab pawg no tuaj yeem ua rau ntshav qab zib hauv siab kom ntau, yog li yuav tsum tau ceev faj. Hauv cov tshuaj feem ntau muaj kev nyab xeeb ntawm qhov kev phiv tshuaj thiab qhov ua tau zoo.

Stanislav Alexandrovich, mob ntshav qab zib

Lawv tso ntshav qab zib ib xyoo dhau los. Kuv sim hloov cov khoom noj thaum xub thawj, xyaum ntau yam, tab sis tsis muaj ib yam dab tsi tau txais txiaj ntsig. Tus kws kho mob tau sau ob peb yam tshuaj uas tsis pab. Kuv tau haus saxagliptin tau 3 lub hlis lawm. Kuv tsis hnov ​​mob dab tsi tshwm sim, tab sis glycemia xa rov qab mus rau qhov qub.

Nqe (hauv Lavxias Federation)

Tus nqi ntawm cov tshuaj, tsis hais txog ntawm koob tshuaj, yog 2200 rubles toj ib hlis. Cov tshuaj tseem kim dua vildagliptin (1200 rubles ib hlis). Txawm li cas los xij, seb cov koob tshuaj uas tau pom zoo zoo ib yam yog tsis meej. Metformin yog ib qho uas pheej yig thiab muaj kev siv tshuaj: tus nqi yog 100 rubles.

Tswv yim! Ua ntej siv, nws pom zoo kom sab laj nrog tus kws kho mob. Cov tshuaj raug faib tawm nruj me ntsis los ntawm cov tshuaj noj.

Tus txheej txheem ntawm kev ua ntawm saxagliptin ntawm lub cev nyob rau hauv cov 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 kis tus kabmob ntshav qab zib hom 2 nyob hauv lub ntiaj teb tab tom loj hlob, qhov no los ntawm kev ua neej nyob ntawm tib neeg thiab kev noj zaub mov zoo. Txawm li cas los xij, chaw muag tshuaj tsis sawv tseem, tsim cov tshuaj tshiab rau kev kho mob ntshav qab zib.

Ib qho ntawm cov chav kawm tshiab ntawm cov tshuaj muaj yees yog incretin mimetics, uas suav nrog saxagliptin.

Tus txheej txheem ntawm kev txiav txim ntawm incretins

Tus incretins yog tib neeg cov tshuaj hormones tsim tawm los ntawm kev mob plab thaum cov zaub mov nkag mus. Vim lawv qhov kev txiav txim, kev tsim tawm ntawm cov tshuaj insulin ntau ntxiv, uas pab cov piam thaj rau kev nqus, uas tso tawm thaum lub plab zom mov.

Txog rau hnub tim, ob hom kev nce ntxiv tau tshawb pom:

• GLP-1 (zoo li glucone-zoo li peptide-1),
• ISU (insulinotropic polypeptide).

Cov receptors ntawm thawj yog nyob rau hauv txawv plab hnyuv siab raum, uas tso cai rau nws mus nthuav dav cov nyhuv. Qhov thib ob yog tswj los ntawm pancreatic β-cell receptors.

Ntawm cov txheej txheem tseem ceeb ntawm lawv cov kev txiav txim yog:

• nce tso pa tawm ntawm cov tshuaj hormone insulin los ntawm pancreatic cells,
• npleem hauv plab zom mov,
• txo nyob rau hauv glucagon ntau lawm,
• tsis qab los noj mov thiab zoo nkaus li lub siab puv,
• txhim kho lub plawv thiab cov hlab ntsha, muaj qhov cuam tshuam zoo ntawm cov leeg hlwb.

Nrog rau kev nce hauv insulin ntau lawm, cov piam thaj tau zoo dua tuaj, tab sis yog tias qhov nws ib txwm ua, cov txheej txheem zais cia nres thiab tus neeg tsis muaj kev pheej hmoo ntawm lub qog ntshav qab zib. Kev txo qis hauv cov khoom ntawm glucagon, tus insulin antagonist, ua rau txo qis kev noj haus ntawm daim siab glycogen thiab kev tso tawm cov piam thaj dawb, thaum tib lub sijhawm ua rau muaj kev nce ntxiv ntawm kev noj glycogen hauv cov leeg. Yog li ntawd, cov piam thaj siv tam sim ntawd ntawm qhov chaw tsim khoom, tsis tas nkag mus rau cov ntshav.

Thaum kev tso tawm ntawm lub plab tau qeeb, zaub mov nkag mus rau txoj hnyuv hauv ntu me me, uas txo qhov nqus ntawm cov piam thaj rau hauv cov ntshav thiab, yog li ntawd, nce ntxiv hauv nws cov concentration. Ua rau cov khoom me, nws yuav yooj yim dua los ntawm lub cev. Hauv qhov no, qhov kev txo qis hauv qab los noj mov ntau dhau lawm txoj hauv kev.

Kev cuam tshuam rau hauv cov kab mob ntshav kom deb li deb tau tsuas yog sau tseg, tab sis tsis tau kawm. Nws pom tias incretins pab β-hlwb ntawm tus txiav ua kom rov qab sai.

Nws tsis yooj yim sua kom tau txais cov tshuaj hormones hauv lawv daim ntawv dawb hauv qhov ntau txaus, yog li, cov kws tshawb fawb tau tsim cov qauv tshuaj (analogues) uas ua haujlwm zoo:

• rov ua dua kev nqis tes ua ntawm glucone-zoo li peptide-1,
• txo cov kev cuam tshuam ntawm kev puas tsuaj rau cov enzymes, yog li ua kom ntev lub neej ntawm cov tshuaj hormones.

Saxagliptin belongs rau pab pawg thib ob.

Tso Tawm Cov Ntawv

Saxagliptin yog ib feem ntawm cov tshuaj Onglisa, uas ua raws li inhibitor ntawm DPP-4. Cov cuab yeej no tsis yog nyob rau hauv tsoomfwv cov npe ntawm cov tshuaj tshwj xeeb, tab sis tuaj yeem muab rau cov neeg mob ntshav qab zib mellitus los ntawm kev pab nyiaj hauv peev nyiaj hauv cheeb tsam.

Cov tshuaj muaj nyob rau hauv daim ntawv ntawm cov ntsiav tshuaj nrog lub plhaub daj, muaj 2.5 mg ntawm saxagliptin lossis 5 mg ntawm nws cov hydrochloride. Cov lus sib xyaw tseem muaj cov khoom sib xyaw uas ua kom pom cov txiaj ntsig zoo. Cov tshuaj ntsiav tau sau npe cim qhia lawv cov koob tshuaj.

Cov ntsiav tshuaj tau ntim rau hauv cov hlwv pob ntawm 10 daim thiab lub thawv ntawv.

Cov lus qhia rau kev siv

Cov ntsiav tshuaj noj ntawm qhov ncauj tsis hais txog kev tau txais khoom noj. Cov tshuaj ntsiav tau nqos tag nrho thiab ntxuav nrog lub zog me me. Cov koob tshuaj yog nyob ntawm hom kev kho mob thiab kev noj qab nyob zoo ntawm tus neeg mob.

Nrog rau kev siv cais, saxagliptin raug pom zoo kom noj 5 mg ib hnub ib zaug.

Hauv kev sib xyaw ua ke nrog lwm cov tshuaj mob ntshav qab zib, kev noj tshuaj yog 5 mg rau ib hnub, tib yam siv rau qhov sib ntxiv ntawm cov kev siv tshuaj tiv thaiv hypoglycemic nrog saxagliptin.

Thaum pib thawj theem ntawm kev siv cov tshuaj nrog metformin, ntau npaum ntawm saxagliptin yog 5 milligrams, thiab metformin yog 500 milligrams ib hnub.

Rau cov neeg mob raum pathology, kev noj tshuaj yog txo rau 2.5 mg ib hnub twg. Yog tias siv cov tshuaj hemodialysis, cov tshuaj yuav qaug tom qab ua tiav. Cov nyhuv ntawm cov tshuaj thaum lub sijhawm peritoneal lim ntshav tsis tau tshawb xyuas qhov tseeb. Nyob rau hauv txhua rooj plaub, ua ntej sau ntawv yuav cov tshuaj, cov kws txawj qhia kom yauv mus soj ntsuam cov neeg mob ob lub raum.

Rau cov neeg mob siab ua lub siab pathologies, kev hloov kho koob tshuaj yog tsis tsim nyog. Txoj kev kho yog nqa tawm raws li kev pom zoo. Qhov no kuj siv rau cov neeg laus laus, qhia tias lawv tsis muaj teeb meem lub raum.

Ib txoj kev tshawb nrhiav txog cov nyhuv ntawm cov tshuaj rau ntawm tus me nyuam hauv plab hauv cov poj niam cev xeeb tub thiab cov menyuam yaus tseem tsis tau ua. Yog li, nws nyuaj rau twv seb nws yuav raug dab tsi. Rau cov neeg mob no, lwm yam pov thawj kho feem ntau siv. Yog tias tus poj niam noj saxacgliptin thaum pub mis, nws yuav tsum tsis kam pub mis.

Nyob rau hauv cov ntaub ntawv ntawm kev coj ua ib txhij nrog kev ua haujlwm CYP3A4 / 5 inhibitors, qhov kev noj tshuaj txhua hnub yog halved.

Cov no yog cov tshuaj hauv qab no:

• Ketoconazole,
• Clarithromycin
• Atazanavir
• Indinavir
• Nefazodon,
• Itraconazole
• Ritonavir
• Telithromycin,
• Nelfinavir
• Saquinavir thiab lwm tus.

Thaum noj saxagliptin, tus neeg mob txuas ntxiv siv cov lus qhia dav dav rau lub koom haum kev noj haus, ua lub cev qoj ib ce thiab soj ntsuam cov kev xav hauv lub xeev.

Dab tsi tuaj yeem hloov saxagliptin?

Kev siv saxagliptin ua lub hauv paus tseem ceeb tsuas yog tsim hauv cov tshuaj Onglise, yog tias tus neeg mob muaj cov kev mob tshwm sim, nws yuav tsum tau siv cov tshuaj analogues, uas suav nrog lwm cov tshuaj tiv thaiv ntawm DPP-4 enzyme:

1. Januvia - Ib qho ntawm thawj cov cuab yeej ntawm hom no, tsim nyob hauv Tebchaws Asmeskas. Nws yog pom tseeb nyob rau hauv ib koob tshuaj ntawm 25, 50 thiab 100 mg. Txoj cai niaj hnub yog kwv yees li 100 mg. Cov nyhuv ntawm cov tshuaj tsuas kav ib hnub. Qee lub sij hawm nws tsim tawm nyob rau hauv cov hom YanuMet, uas ntxiv cov metformin.
2. Galvus - cov tshuaj uas tsim tawm hauv Switzerland, yog siv hauv qhov ntau npaum ntawm 50 mg rau ib hnub lossis ntau dua, feem ntau siv tshuaj pleev ib ce nrog insulin.
3. Nesina - tsim tawm hauv tebchaws Ireland, raws li apolgiptin benzoate nrog tshuaj 12,5 lossis 25 mg. 1 ntsiav tshuaj noj ib zaug ib hnub.
4. Vipidia - cov tshuaj tseem ceeb ntawm cov tshuaj alogliptin, uas muaj cov txiaj ntsig zoo ib yam, noj ib hnub ib zaug ntawm kev noj tshuaj ntawm 25 mg.
5. Trazhenta - ib qho khoom siv raws li linagliptin, tau pom zoo hauv daim ntawv ntawm 5 mg ntsiav tshuaj noj ntawm qhov ncauj.

Lwm cov analogues yog siv uas muaj cov sib txawv, tab sis cov txheej txheem zoo sib xws. Tus nqi ntawm cov tshuaj sib txawv raws li lub teb chaws ntawm kev tsim khoom thiab cov tshuaj sib tov.

Tus nqi ntawm cov tshuaj Onglisa, uas suav nrog saxagliptin, los ntawm 1700 txog 1900 rubles.

Cov tshuaj tshiab tshiab tso cai rau koj sai dua thiab yooj yim los daws cov teeb meem ntawm cov piam thaj hauv cov neeg mob ntshav qab zib.

Thaum lawv cov npe tseem tsis tau dav heev, tsuas yog ib cov tshuaj uas tsim tawm ntawm saxagliptin, uas muaj cov txiaj ntsig zoo hauv kev kho mob ntshav qab zib thiab tsis ua rau lub xeev ntawm cov ntshav qab zib tsis zoo. Nyob rau tib lub sijhawm, muaj cov analogues uas muaj cov tshuaj sib txawv, tab sis nrog cov txiaj ntsig kho zoo sib xws.

Yam tshuaj mob ntshav qab zib hom 2

• 1 Hom tshuaj
  • 1.1 Cov npe ntawm cov tshuaj uas txo cov piam thaj hauv ntshav qab zib hom 2
  • 1.2 Ntsiav tshuaj uas ua rau muaj kev cuam tshuam ntawm cov hlwb rau cov tshuaj insulin
    • 1.2.1 Thiazolidinediones
  • 1.3 Cov Kev Qhuas Tus Kheej
  • 1.4 α-glucosidase inhibitors
    • 1.4.1 Txo cov kab mob tiv thaiv insulin
  • 1.5 Cov tshuaj tshiab
  • 1.6 Lwm yam tshuaj
• 2 Dab tsi yog contraindicated?

Cov tshuaj niaj hnub rau cov ntshav qab zib hom 2 ua rau lub neej ntawm cov neeg mob tag nrho. Nws paub tias cov kab mob ntshav qab zib mellitus yog qhov pathology uas tau hais tawm hauv kev tsis txaus ntawm cov tshuaj insulin hauv tib neeg lub cev, uas ua rau muaj kev cuam tshuam hauv cov metabolism ntawm carbohydrates.Qhov mob no tsis tuaj yeem kho zoo, xws li los ntswg lossis mob tob hau. Nws yog qhov nyuaj rau tshem tawm cov tsos mob ntawm cov teeb meem, yog li lub hom phiaj tseem ceeb ntawm kev kho ntshav qab zib yog los tswj tus neeg mob tus mob.

Hom tshuaj

Txhua cov tshuaj rau cov ntshav qab zib hom 2, txawm hais tias tseem ceeb tshaj yog cov ntshav qabzib, suav nrog cov yam ntxwv ntxiv rau cov neeg mob ntshav qab zib. Hauv kev ua lag luam, tag nrho cov khoom lag luam qub thiab cov tshuaj tiv thaiv kab mob kev nkeeg tshiab yog sib npaug hauv kev xav tau. Cov tshuaj kho ntshav qab zib tshiab tau raug muab faib ua ntau pawg nyob ntawm qee cov yam ntxwv. Txawm li cas los xij, nws yuav tsum nco ntsoov tias cov tshuaj insulin ntawm ib tiam neeg uas txo cov ntshav qab zib kom tsawg yuav daws tsis tau qhov teeb meem no. Nws yog ib qho tseem ceeb los saib xyuas cov khoom noj khoom haus (kom tsis txhob rog dhau), ua si lub cev thiab, qhov tseem ceeb tshaj, yuav tsum tau kuaj mob hauv cov tsev kho mob raws lub sijhawm.

Rov qab rau cov lus txheej txheem

Sau cov tshuaj uas txo cov piam thaj hauv ntshav qab zib hom 2

Kev siv tshuaj kho tus kab mob suav nrog kev siv cov tshuaj txo cov ntshav qab zib. Tag nrho cov tshuaj rau cov ntshav qab zib hom 2 tau raug muab faib ua hom:

• tshuaj kho mob biguanide,
• dipeptidyl peptidase inhibitors - IV,
• sulfonylurea derivatives,
• cov tshuaj incretinomimetic,
• α-glucosidase inhibitors,
• glitazones.

Rov qab rau cov lus txheej txheem

Thiazolidinediones

Pioglar txhim kho qhov rhiab heev ntawm cov hlwb rau cov tshuaj insulin.

Cov tshuaj niaj hnub rau kev kho mob ntshav qab zib hom 2 hauv cov neeg laus thiab cov tub ntxhais hluas, uas txiav txim siab cov lus teb ntawm cov cell mus rau qhov tshuaj hormones, hu ua thiazolidinediones. Cov yeeb yaj kiab no tsis cuam tshuam rau kev ua haujlwm ntawm tus txiav, tab sis theej ntxiv qhov ua rau muaj kev cuam tshuam ntawm cov xovtooj ntawm tes thiab cov ntaub so ntswg rau insulin, thaum txhim kho cov lipid profile. Kev mob siab txog ntshav yog los ntawm 0.5% mus rau 2%. Ntawm qhov tsis txaus ntawm cov kev kho mob, kev ua haujlwm ntawm lub plab tsis muaj qhov txawv txav, cov tshuaj kuj tseem cuam tshuam hauv cov kab mob loj xws li lub raum lossis lub plawv tsis ua haujlwm. Tshuaj ntsuab zoo tshaj plaws nyob hauv pawg no:

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.

• Piroglar
• "Diagnitazone".

Rov qab rau cov lus txheej txheem

Qhuas Kev Qhuas

Kev kho niaj hnub rau cov ntshav qab zib suav nrog kev siv av nplaum. Pab pawg ntawm cov tshuaj no muaj lub sijhawm luv luv, thaum txo qis ntawm cov kua nplaum vim tias muaj peev xwm ua tau sai ntawm cov tshuaj insulin. Prandial ntshav qab zib cov tshuaj pib ua haujlwm tam sim ntawd tom qab noj mov, muaj kev cuam tshuam cov txiav ua qab. Hom tshuaj uas nrov:

Rov qab rau cov lus txheej txheem

Α-glucosidase inhibitors

Acarbose thaiv qee cov enzymes uas yog lub luag haujlwm rau kev rhuav tshem cov carbohydrates, uas tiv thaiv cov piam thaj kom sai sai rau hauv cov ntshav.

Kev kho mob ntshav qab zib hom 2 koom nrog kev siv cov tshuaj zoo sib xws. Cov nyhuv pharmacological ntawm cov tshuaj yog raws li qib phased kev tshaib plab ntawm kev noj zaub mov carbohydrates los ntawm kev thaiv cov haujlwm ntawm cov enzymes lub luag haujlwm rau kev nqus ntawm cov carbohydrates. Feem ntau cov feem ntau, lawv sau ntawv tshuaj tsuas cov tshuaj lag luam los ntawm pab pawg no, hu ua "Acarbose". Tag nrho cov nyiaj ntawm carbohydrates, tom qab haus cov tshuaj, tsis hloov, tab sis cov txheej txheem rau kev ua cov khoom lag luam nce siab, uas txwv qhov tseem ua rau dhia hauv qabzib.

Rov qab rau cov lus txheej txheem

Txo cov tshuaj tiv thaiv insulin

Kev kho mob ntshav qab zib hom 2 suav nrog kev siv tshuaj zoo uas txo lub cev tiv thaiv cov tshuaj insulin. Daim ntawv no suav cov ntsiav tshuaj zoo tshaj plaws los ntawm pab pawg ntawm thiazolidinediones thiab biguanides. Ob pawg ntawm cov tshuaj txo cov ntshav qab zib muaj ntau qhov zoo hauv kev kho mob ntshav qab zib hom 2. Qhov laj thawj thib ib xws li cov khoom lag luam muaj txiaj ntsig yog qhov pheej hmoo ntawm cov ntshav qog ntshav qab zib tsawg. Cov hauv qab no yog cov txiaj ntsig hauv daim ntawv ntawm cov roj ntsha ua kom qis thiab, vim li ntawd, txo qhov phom sij ntawm myocardial infarction thiab lwm yam kev mob plawv. Txawm li cas los xij, ntawm qhov tod tes, yog tias cov tshuaj no tau noj, qhov tsis xav tau tshwm sim los ntawm txoj hnyuv txhaws tau.

Txawm hais tias cov tshuaj tiv thaiv kab mob feem ntau siv tsis tau yog tias tsis muaj kws kho mob sau ntawv. Nws yog qhov txaus ntshai los kho ntshav qab zib yam tsis tau sab laj nrog kws kho mob tshwj xeeb.

Rov qab rau cov lus txheej txheem

Cov tshuaj tshiab

Galvus belongs rau ntau cov tshuaj tshiab.

Cov tshuaj niaj hnub rau cov ntshav qab zib hom 2 twb tau tsim los tsim lub koob npe zoo hauv kev ua lag luam ntawm cov khoom lag luam kho mob. Cov tshuaj no tau coj los khaws cov glucagon thiab peptide-1 los ntawm kev cuam tshuam uas tsis muaj kev cuam tshuam ntawm enzyme DPP-4. Ntxiv rau qhov tseeb tias cov tshuaj txo cov suab thaj, lawv kuj cuam tshuam rau kev loj hlob ntawm glucagon, uas, nyeg, txwv qhov tsim tawm ntawm cov tshuaj insulin. Txawm hais tias cov kua qab zib ua qis dua tsis txhawb qhov nce hauv lub cev nyhav dhau los, lawv muaj cov kev ua kom tsis zoo. Yog li, yog tias tus neeg mob muaj teeb meem ntawm lub siab, nws yog qhov zoo uas yuav tsum tsis txhob noj cov tshuaj no. Kev hno tshuaj tshiab rau cov ntshav qab zib hom 2 (Victoza, Baeta) yuav siv tau thawm hnub, yog li lawv yuav ntau dua rau cov neeg mob. Cov tshuaj tshiab zoo tshaj plaws tiv thaiv tus kab mob (npe):

Rov qab rau cov lus txheej txheem

Lwm yam tshuaj

Txawv tebchaws, cov txiaj ntsig zoo tshwm sim tom qab kho mob Diabeton.

Kev siv tshuaj kho mob ntshav qab zib hom 2 tso cai siv lwm yam tshuaj. Tshwj xeeb, kev suav nrog kev noj zaub mov noj xws li "Ntshav Qab Zib" rau hauv cov txheej txheem kho tau ntev ntev tau coj los siv txawv teb chaws. Qhov kev kho mob zoo hauv Asmeskas no ua rau cov haujlwm ntawm cov txiav, thaum lub sij hawm cov tshuaj insulin zoo dua, thiab qhov kev pheej hmoo ntawm hypoglycemia yuav txo qis. Cov kev qhia qhia tus neeg mob tias yog koj haus cov ntsiav tshuaj kom raug, ces cov txiaj ntsig zoo yuav tsis ua rau koj nyob tos. Txawm li cas los xij, hauv kev muaj tiag qhov no tsis yog li rosy. Cov txheej txheem kev kho mob no tsis yog qhov tseem ceeb thiab tsis rho tawm cov qauv kev kho mob. Nyob rau hauv txhua rooj plaub, ib qho yuav tsum tsis txhob nqa mus nrog cov tsis paub txhais tau tias, thaum muaj kev ua xyem xyav nws yog ib qho tseem ceeb kom sab laj nrog kws kho mob.

Rov qab rau cov lus txheej txheem

Yuav ua li cas tshuaj yog contraindicated?

Ib qho tshuaj twg rau cov ntshav qab zib mellitus 2 qib muaj, ib txoj kev los sis lwm qhov, cuam tshuam rau lub cev. Tab sis nrog rau qhov no, koj yuav tsum xyuam xim nrog kev noj lwm yam tshuaj. Nrog rau qab zib nce ntxiv, nws yog qhov txaus ntshai los noj cov tshuaj pleev xim rau lub zog, sedatives, raws li lawv qhov kev txiav txim siab tuaj yeem ua rau muaj kev nce siab hauv cov ntshav qabzib. Nws yog ib qho tseem ceeb kom ua tib zoo kawm cov lus qhia ua ntej noj tshuaj, nyeem txog cov kev tsis haum thiab kev sib kis.

Hom 2 mob ntshav qab zib mellitus: daim ntawv teev cov tshuaj noj

Ntawm cov ntshav qab zib mellitus ntawm yam thib ob, tus kws kho mob, raws li txoj cai, txwv tsis tsuas yog kev kho noj zaub mov noj, ua si lub cev, tab sis kuj tshwj xeeb hypoglycemic cov tshuaj nyob rau hauv daim ntawv ntawm cov ntsiav tshuaj, uas tso cai tswj theem ntawm cov piam thaj hauv cov ntshav. Cov tshuaj yog xaiv raws cov xwm txheej ntawm tus neeg mob lub cev, qabzib hauv ntshav thiab zis, cov yam ntxwv ntawm tus kabmob thiab muaj cov kabmob me.

Niaj hnub no hauv cov khw muag khoom tshwj xeeb koj tuaj yeem nrhiav tau cov npe loj ntawm cov tshuaj tshiab uas coj los kho hom 2 ntshav qab zib. Lub caij no, nws yog ib qho tsim nyog yuav tau xaiv cov tshuaj muaj ntshav qab zib tsuas yog tom qab sab laj nrog kws kho mob, vim nws yog qhov tsim nyog yuav tsum tsis yog coj mus rau txhua tus yam ntxwv ntawm tus kab mob, contraindications, tab sis kuj tsim nyog tshuaj. Kev tswj tsis siv nrog tsis muaj lus qhia kho mob tuaj yeem ua kev puas tsuaj rau koj lub cev.

Nws yog ib qho tseem ceeb uas yuav tsum xav txog tias cov tshuaj tsis siv rau hauv kev kho mob ntshav qab zib hom 1 hauv menyuam yaus thiab xaiv ib qho zuj zus rau cov ntshav qab zib hauv cov poj niam cev xeeb tub.

Cov piam thaj hauv cov neeg ua haujlwm ntawm lub qub thiab tshiab tau muab faib ua peb hom, lawv sib txawv hauv cov tshuaj lom neeg thiab hauv txoj kev lawv cuam tshuam rau lub cev.

Kev kho mob Sulfonamide

• Cov kab mob ntshav qab zib zoo sib xws hauv ntshav qab zib pab kom ua hauj lwm ntau dua thiab xa cov tshuaj insulin rau hauv cov ntshav.
• Tsis tas li, cov tshuaj no ua kom muaj kev nkag siab ntawm cov nqaij mos, uas tso cai rau koj kom tau txais cov koob tshuaj yuav tsum tau.
• Sulfanilamides ua rau kom cov insulin ntau ntxiv rau cov hlwb.
• Cov tshuaj uas tsis muaj piam thaj yuav pab ua kom zom thiab txo cov plhaws nyob hauv lub siab.

Tau ntev, cov mob ntshav qab zib tau siv thawj cov tshuaj thawj zaug. Txhawm rau kom tau qhov kev xav tau tshuaj txhua hnub, cov neeg mob yuav tsum coj los ntawm 0,5 mus rau 2 gram ntawm sulfonamides, uas yog qhov ntau kawg. Niaj hnub no, cov tshuaj thib ob tau tsim los uas muaj ntau yam zoo dua.

Lawv kev noj ntau npaum li cas me dua, uas ua rau kom muaj kev cuam tshuam tsawg dua.

Raws li txoj cai, cov tshuaj no muaj cov nyhuv ntawm lub cev rau 6-12 teev. Lawv tau noj 0.5 ntsiav tshuaj ua ntej lossis tom qab noj mov ob zaug ib hnub.

Muaj qee kis, tus kws kho mob tau sau ntawv noj tshuaj rau peb zaug hauv ib hnub kom ua tiav cov ntshav qabzib tsawg zuj zus.

Dhau li ntawm qhov tseeb tias lawv txo cov ntshav qab zib, cov tshuaj no muaj txiaj ntsig zoo rau cov hlab ntshav, txhim kho lawv cov ntshav kev thiab tiv thaiv kev puas tsuaj rau cov hlab ntsha me. Xws li cov ntsiav tshuaj rau kev txo cov ntshav qab zib thib ob, lawv raug tshem tawm sai sai ntawm lub cev thiab tsis ua kom lub raum tsis zoo, tiv thaiv cov kabmob hauv nruab nrog los ntawm kev txhim kho ntawm cov teeb meem vim cov ntshav qab zib hom 2.

Lub caij no, xws li cov kab mob hypoglycemic zoo li sulfanilamides muaj lawv cov teeb meem:

1. Cov tshuaj no yuav tsis haum rau txhua tus neeg mob.
2. Lawv sim kom tsis txhob muab tshuaj rau cov neeg laus, uas maj mam tshem tawm cov tshuaj tawm hauv lub cev. Txwv tsis pub, cov tshuaj muaj peev xwm nthuav tawm hauv lub cev, uas feem ntau ua rau lub xeev hypoglycemic thiab coma.
3. Sulfanilamides tuaj yeem quav tshuaj ntxiv tom qab qee lub sijhawm vim tias tsib xyoos tom qab siv cov tshuaj, qhov mob rhiab ntawm cov ntaub so ntswg mus rau lawv cov teebmeem txo. Raws li qhov tshwm sim, receptors plam lawv cov hauj lwm zoo.

Xws li cov yam ntxwv tsis zoo ntawm cov tshuaj yog qhov tseeb tias sulfonamides ua rau kom cov ntshav qabzib ntau ntau, uas tuaj yeem ua rau lub ntsej muag tsis zoo. Daim ntawv ntawm cov ntshav qab zib siab phem yog tshwm sim los ntawm cov tshuaj ntawm cov pab pawg chlorpropamide thiab glibenclamide. Vim li no, kev noj tshuaj ntau npaum li cas los ntawm kws kho mob yuav tsum tau saib xyuas kom zoo thiab tsis yog rau tus kheej.

Nws yog ib qho tseem ceeb uas yuav tsum nco ntsoov tias glycemia tuaj yeem ua rau tus neeg mob plab nquag, kev haus dej haus cawv, kev siv lub cev kom muaj zog, thiab cov tshuaj aspirin. Yog li no, ua ntej koj pib siv cov tshuaj, koj yuav tsum sab laj nrog koj tus kws kho mob txog kev nyob ntawm contraindications.

Leej twg qhia rau noj tshuaj sulfa?

Cov tshuaj muaj ntshav qab zib ntawm yam tsawg no tau sau tseg hauv cov xwm txheej hauv qab no:

• Hauv kev kho mob ntshav qab zib mellitus ntawm thawj hom, yog tias cov khoom noj kho tsis tau tso cai ua kom txo qis cov ntshav qabzib hauv cov ntshav, thiab tus neeg mob tsis mob nyhav dhau los.
• Nrog mob ntshav qab zib mellitus ntawm thawj hom, yog tias tus neeg mob muaj kev rog.
• Nrog rau tsis khov kho mob ntshav qab zib mellitus ntawm thawj hom.
• Yog tias tus neeg mob tsis xav tias muaj kev cuam tshuam cov tshuaj insulin rau hom ntshav qab zib hom 1.

Qee qhov xwm txheej, sulfonamides raug muab sau ua ke nrog cov tshuaj insulin. Qhov no yog qhov tsim nyog txhawm rau txhawm rau txhim kho cov nyhuv ntawm insulin rau hauv lub cev thiab txhais cov ntshav qab zib tsis ruaj khov rau hauv daim ntawv ruaj khov.

Cov thawj sulfanilamides thawj zaug tuaj yeem noj ua ntej, thaum thiab tom qab noj mov. Hauv qhov no, ntau npaum li cas yog tau sau tseg ib tus zuj zus. Ua ntej koj pib noj cov tshuaj, koj yuav tsum ua tib zoo kawm cov lus qhia.

Lawv noj cov tshuaj muaj ntshav qab zib ntawm hom no nrog kev ceeb toom ceev faj hauv kev noj tshuaj, vim tias noj cov tshuaj tsis yog tuaj yeem ua rau cov ntshav qabzib tsawg, ua xua, xeev siab, ntuav, cuam tshuam ntawm lub plab thiab daim siab, thiab txo qis ntawm leukocytes thiab hemoglobin.

Kev kho mob Biguanide

Cov tshuaj zoo sib xws rau cov piam thaj muaj qhov sib txawv ntawm lub cev, ua rau cov piam thaj tuaj yeem nqus tau sai dua los ntawm cov leeg nqaij. Raug rau biguanides cuam tshuam nrog kev cuam tshuam ntawm cov cell receptors, uas txhim kho cov insulin ntau lawm thiab pab ua kom cov ntshav qab zib nyob li qub.

Xws li cov tshuaj ua kom muaj suab thaj muaj ntau qhov zoo:

1. Kev ua kom ntshav qabzib tsawg.
2. Txo kev nqus ntawm cov piam thaj rau hauv txoj hnyuv thiab nws tso tawm los ntawm lub siab.
3. Cov tshuaj tsis pub ua kom qabzib tuaj rau hauv lub siab.
4. Cov tshuaj tsub kom tus naj npawb ntawm receptors uas rhiab rau insulin.
5. Tshuaj yuav pab ua kom tawg thiab hlawv lub cev tsis rog.
6. Hauv qab tshuaj ntawm tshuaj, ntshav liquefies.
7. Tus neeg mob lub qab los tsawg, uas tso cai rau koj kom poob phaus.

Biguanides tsis cuam tshuam rau kev tsim cov tshuaj insulin, pab kev siv ntawm cov kua nplaum nyob rau hauv cov ntaub so ntswg, nce cov nyhuv ntawm cov tshuaj insulin lossis cov ua haujlwm hauv lub cev. Qhov no ua rau lub fact tias cov hlwb tsis deplete lawv cov peev nyiaj.

Vim yog qhov ib txwm ua rau cov tshuaj insulin ntau ntxiv hauv tus neeg mob, kev qab los noj mov ntau dhau yog txo, uas yog pab rau cov neeg mob ntshav qab zib thiab cov neeg rog dhau los lossis rog dhau. Vim tias qhov txo qis hauv kev nqus ntawm cov piam thaj mus rau hauv txoj hnyuv, cov theem ntawm lipid feem ntshav hauv cov ntshav normalizes, uas txwv tsis pub muaj kev txhim kho atherosclerosis.

Txawm li cas los xij, biguanides muaj qhov tsis zoo. Cov tshuaj no tso cai rau cov kua qaub tsim cov khoom hauv lub cev, uas ua rau cov ntaub so ntswg hypoxia lossis oxygen tshaib plab.

Cov tshuaj yuav tsum siv zoo nrog mob ntshav qab zib rau cov neeg laus thiab cov neeg uas muaj mob ntawm cov ntsws, mob siab thiab mob plawv. Txwv tsis pub, cov neeg mob yuav ntuav, xeev siab, tso quav tsis duav, mob plab, thiab ua xua.

Biguanides txwv tsis pub siv:

• Cov neeg mob laus dua 60
• nyob rau hauv lub xub ntiag ntawm tej yam ntawm hypoxia,
• Yog tias muaj kab mob siab thiab mob raum,
• nyob rau hauv muaj ib qho kev phais neeg mob hnyav, kis kab mob thiab kis mob.

Biguanides feem ntau tsuas yog kho rau cov neeg mob uas kuaj pom tus mob ntshav qab zib hom 2 mob ntshav qab zib, nrog lub cev nyhav thiab tsis muaj khesoacidosis. Tsis tas li, cov tshuaj no yog siv rau hauv kev kho mob ntshav qab zib, uas nws lub cev tsis zam sulfonamides los yog quav rau cov tshuaj no.

Biguanides, uas muaj lub npe "rov qab" hauv lub npe, cuam tshuam rau lub cev ntev dua li siv tshuaj. Koj yuav tsum tau noj cov tshuaj tsuas yog tom qab noj mov, ib qho kev ua tau yooj yim - peb zaug hauv ib hnub, ua ntev ntev - ob zaug ib hnub, sawv ntxov thiab yav tsaus ntuj.

Hom tshuaj no suav nrog cov tshuaj xws li adebit thiab glyformin. Tsis tas li, cov tshuaj no yog siv los ntawm cov neeg noj qab haus huv los txo lub cev qhov hnyav.

Cov yam ntxwv ntawm cov tshuaj Saxagliptin

Tus neeg sawv cev hypoglycemic rau kev siv lub qhov ncauj yog DPP-4 inhibitor.

Saxagliptin monohydrate yog hmoov siv lead ua los ntawm dawb mus rau lub teeb daj lossis xim av ci hauv xim, tsis-hygroscopic. Me ntsis soluble hauv dej ntawm qhov kub ntawm (24 ± 3) ° C, me ntsis soluble hauv ethyl acetate, soluble hauv methanol, ethanol, isopropyl cawv, acetonitrile, acetone thiab polyethylene glycol 400 (PEG 400). Tus luas luas lev yog 333.43.

Kws Tshuaj

Saxagliptin yog qhov muaj zog xaiv tau kev thim rov qab kev sib tw ntawm DPP-4. Hauv cov neeg mob uas muaj hom 2 mob ntshav qab zib mellitus (DM2), kev tswj hwm ntawm saxagliptin txwv tsis pub cov kev ua haujlwm ntawm DPP-4 enzyme rau 24 teev. glucagon thiab nce glucose-depend beta cell teb, uas ua rau kev nce siab hauv kev tsim tawm ntawm cov tshuaj insulin thiab C-peptide.Kev tso tawm ntawm insulin los ntawm beta hlwb ntawm tus txiav thiab txo qis hauv kev tso tawm ntawm glucagon los ntawm alpha hlwb ua rau txo qis glycemia thiab postprandial glycemia.

Cov chaw kuaj mob tau zoo thiab Kev Nyab Xeeb

Hauv kev dig muag ob zaug, xaiv ib qho, tswj kev soj ntsuam, kev kho saxagliptin tau txais los ntawm ntau dua 17,000 tus neeg mob T2DM.

Qhov ua tau zoo thiab kev nyab xeeb ntawm saxagliptin thaum noj ntawm 2.5, 5 thiab 10 mg ib hnub ib zaug tau kawm hauv rau ob qhov muag dig, qhov chaw kawm tshuaj uas muaj kev cuam tshuam nrog 4148 cov neeg mob uas muaj ntshav qab zib hom 2. Saxagliptin tau muaj nrog kev txhim kho kev tshawb fawb hauv glycated hemoglobin (HbA_1c), yoo plasma ntshav qab zib (GPN) thiab ntshav qab zib cov ntshav qab zib (PPG) ntshav plasma piv nrog kev tswj hwm.

Saxagliptin tau raug tshaj tawm li kev kho mob los ntawm kev kho mob lossis ua ke nrog kev kho mob. Kev sib xyaw ua ke nrog saxagliptin tau ntxiv rau cov neeg mob uas tsis tau ua tiav thaum lub sij hawm monotherapy nrog metformin, glibenclamide, thiazolidinediones lossis insulin, los yog los pib sib xyaw nrog metformin rau cov neeg mob uas tsis tau ua kom tiav rau hauv kev noj haus thiab kev tawm dag zog. Thaum noj saxagliptin ntawm koob tshuaj 5 mg, txo qis HbA_1s tau sau tseg tom qab 4 lub lis piam thiab GPN - tom qab 2 lub lis piam.

Hauv pawg ntawm cov neeg mob tau txais saxagliptin txuam nrog metformin, glibenclamide lossis thiazolidinediones, txo HbA_1s kuj tau sau tseg tom qab 4 lub lis piam thiab GPN - tom qab 2 lub lis piam.

Kev kawm txog kev sib xyaw nrog kev kho mob nrog saxagliptin thiab insulin (suav nrog kev sib xyaw nrog metformin) uas muaj 455 tus neeg mob T2DM pom tias txo qis hauv HbA_1s thiab BCP piv nrog cov tshuaj placebo.

Kev tshawb ntawm saxagliptin txoj kev kho nyob rau hauv kev sib xyaw nrog metformin thiab sulfonylurea derivatives hauv 257 cov neeg mob T2DM pom tias txo qis hauv HbA_lc thiab PPG piv nrog cov placebo hauv kev sib xyaw nrog metformin thiab sulfonylurea derivatives.

Cov nyhuv ntawm saxagliptin ntawm cov lipid profile zoo ib yam li cov placebo. Thaum lub sij hawm txoj kev kho nrog saxagliptin, tsis muaj nce hauv lub cev qhov hnyav.

Hauv kev tshawb nrhiav qhov sib piv ncaj qha ntawm 858 cov neeg mob uas muaj ntshav qab zib hom 2, ntxiv ntawm saxagliptin 5 mg rau metformin piv nrog kev ntxiv ntawm glipizide rau metformin qhia tau tias qhov txo qis hauv HbA_1c, txawm li cas los xij, nws tau cuam tshuam nrog tsawg dua qhov kev mob tshwm sim ntawm kev mob ntshav qab zib - 3% ntawm cov neeg mob piv nrog 36.3% nrog ntxiv ntawm glipizide, nrog rau qhov tsis muaj qhov nce ntawm lub cev qhov hnyav hauv cov neeg mob tau txais kev kho saxagliptin (−1.1 kg los ntawm thawj theem hauv pawg saxagliptin, +1.1 kg hauv pawg glipizide).

Los ntawm 104th ntawm lub lim tiam ntawm kev kho, tsawg kawg ib ntu ntawm hypoglycemia tshwm sim hauv 3.5% ntawm cov neeg mob hauv saxagliptin thiab metformin pawg thiab hauv 38.4% hauv cov glipizide thiab metformin pawg, qhov hloov ntawm lub cev qhov hnyav los ntawm thawj theem yog −1.5 kg thiab + 1.3 kg, raws li.

Hauv kev kawm TXIV (Kev tshuaj xyuas txog cov txiaj ntsig ntawm lub plawv hauv cov neeg mob ntshav qab zib noj saxagliptin), cov txiaj ntsig ntawm lub plawv tau kawm hauv 16,492 cov neeg mob ntshav qab zib hom 2 (12,959 cov neeg mob uas tau paub tseeb txog cov kab mob plawv (CVD), 3,533 cov neeg mob uas muaj ntau yam pheej hmoo rau cov mob plawv) thiab tus nqi ntawm 6.5% ≤HbA_lc CHF, tsis txaus ntseeg lub siab, lossis rov qab kho dua ntawm cov hlab ntsha txhaws piv nrog cov placebo (RR: 1.02, 95% CI: 0.94, 1.11). Tag nrho cov neeg tuag piv rau cov pawg saxagliptin thiab placebo (RR: 1.11, 95% CI: 0.96, 1.27).

Txoj kev tshawb no tau sau tseg qhov kev nce ntawm lub tsev kho mob rau lub plawv tsis ua hauj lwm hauv pab pawg saxagliptin (3.5%, 289 tus neeg mob) piv nrog cov placebo pawg (2.8%, 228 cov neeg mob) nrog cov npe nom tswv tseem ceeb (i.e., tsis muaj kev kho rau ntau cov ntsiab lus xaus) (RR: 1.27, 95% CI: 1.07, 1.51, P = 0.007). Cov neeg mob lub plawv tsis ua haujlwm lossis lub raum tsis ua haujlwm tau txais saxagliptin tsis muaj qhov tshwm sim ntau dua ntawm qhov pib qhov kawg, theem ob kawg, thiab tag nrho kev tuag piv nrog cov pab pawg.

Nyob hauv pab pawg saxagliptin, qhov muaj zog ntawm HbA qhov tseem ceeb_lc tau pom tseeb dua, thiab feem pua ​​ntawm cov neeg mob tau mus txog lub hom phiaj HbA muaj nqis_lctau siab dua hauv pawg placebo. Nyob rau tib lub sijhawm, kev tawm tsam ntawm kev kho ntshav qab zib ntau ntau lossis ntxiv ntawm cov tshuaj insulin hauv pawg saxagliptin tau ua los ntawm cov neeg mob tsawg dua li cov pab pawg placebo.

Cov neeg mob uas muaj ntshav qab zib hom 2 thiab cov neeg ua haujlwm pab dawb noj qab haus huv pom zoo sib xws ntawm pharmacokinetics ntawm saxagliptin thiab nws cov metabolite. Saxagliptin tau yoo sai sai tom qab noj rau ntawm lub plab khoob nrog kev ua tiav C_max saxagliptin thiab cov metabolite tseem ceeb hauv plasma rau 2 thiab 4 teev, feem. Nrog kev nce hauv saxagliptin koob tshuaj, ib qho kev nce ntau hauv C tau muab sau cia_max thiab AUC qhov tseem ceeb ntawm saxagliptin thiab nws cov khoom noj hluav taws xob tseem ceeb. Tom qab ib qho kev tswj hwm qhov ncauj ntawm saxagliptin ntawm koob tshuaj 5 mg los ntawm cov neeg ua haujlwm noj qab haus huv, qhov nruab nrab ntawm AUC qhov tseem ceeb ntawm saxagliptin thiab nws cov metabolite tseem ceeb yog 78 thiab 214 ng · h / ml, thiab qhov tseem ceeb ntawm C_max hauv ntshav - 24 thiab 47 ng / ml, feem.

Qhov nruab nrab ntawm lub sijhawm kawg T kawg_1/2 saxagliptin thiab nws cov metabolite tseem ceeb yog 2.5 thiab 3.1 teev, ua ntu zus, thiab tus nqi nruab nrab ntawm T_1/2 Kev txwv tsis pub ntshav DPP-4 - 27 teev. Kev ua kom tsis txhob mob ntshav DPP-4 kev ua haujlwm tsawg kawg 24 teev tom qab noj saxagliptin yog vim nws muaj kev cuam tshuam zoo rau DPP-4 thiab lub sijhawm ntev los khi rau nws. Qhov tseem ceeb tsub zuj zuj ntawm saxagliptin thiab nws cov metabolite tseem ceeb nrog rau kev siv tshuaj ntev 1 zaug nyob rau ib hnub tsis pom. Tsis muaj ib qho kev vam khom ntawm kev tshem tawm saxagliptin thiab nws lub ntsiab metabolite ntawm kev txhaj tshuaj thiab lub sijhawm ntawm kev kho mob thaum noj saxagliptin 1 zaug hauv ib hnub hauv koob tshuaj ntawm 2.5 txog 400 mg rau 14 hnub.

Tom qab lub qhov ncauj tswj hwm, tsawg kawg 75% ntawm qhov koob tshuaj saxagliptin tau nqus. Noj mov tsis muaj kev cuam tshuam loj heev rau pharmacokinetics ntawm saxagliptin hauv cov neeg tuaj noj qab haus huv zoo. Cov zaub mov tsis muaj rog ntau tsis cuam tshuam rau C_max saxagliptin, thaum AUC tau nce 27% piv nrog kev yoo mov. T_max rau saxagliptin nce ntxiv kwv yees li 0.5 teev thaum noj nrog zaub mov piv nrog kev yoo mov. Txawm li cas los xij, cov kev pauv hloov no tsis yog qhov tseem ceeb hauv tsev kho mob.

Kev khi ntawm saxagliptin thiab nws lub ntsiab metabolite rau cov ntshav cov protein tsis tseem ceeb, yog li, tuaj yeem xav tias kev faib tawm saxagliptin nrog kev hloov pauv ntawm cov protein sib xyaw ntawm cov ntshav pom nyob rau hauv hepatic lossis lub raum tsis ua haujlwm yuav tsis raug hloov pauv tseem ceeb.

Saxagliptin yog metabolized feem ntau nrog kev koom tes ntawm CYP3A4 / 5 isoenzymes ntawm cytochrome P450 nrog kev tsim cov nquag metabolite, uas cov tshuaj tiv thaiv cuam tshuam rau DPP-4 yog 2 lub sijhawm tsawg tshaj li hais hauv saxagliptin.

Saxagliptin ua tawm hauv cov zis thiab cov kua tsib. Tom qab ib koob tshuaj 50 mg ntawm daim ntawv lo 14 C-saxagliptin, 24% ntawm cov koob tshuaj tau raug tso tawm los ntawm lub raum ua qhov hloov pauv saxagliptin thiab 36% yog cov tshuaj metabolite ntawm saxagliptin. Tag nrho cov kev ua haujlwm hauv lub cev tso tawm hauv cov zis sib raug rau 75% ntawm kev lees paub ntawm saxagliptin. Qhov nruab nrab lub raum tshem tawm ntawm saxagliptin yog li 230 ml / min, qhov nqi nruab nrab CF yog li 120 ml / min. Rau cov khoom siv hluav taws xob tseem ceeb, kev kho lub raum tau piv nrog lub txiaj ntsig tseem ceeb ntawm CF.

Txog 22% ntawm tag nrho cov xov tooj cua tau pom nyob hauv cov quav.

Cov pab pawg neeg tshwj xeeb

Lub raum khiav tsis zoo. Hauv cov neeg mob uas tsis muaj lub siab lub ntsws tsis txaus, AUC qhov tseem ceeb ntawm saxagliptin thiab nws lub cev qhov tseem ceeb yog 1.2 thiab 1.7 npaug siab dua, feem ntau, ntau dua li cov neeg hauv cov neeg uas lub raum tsis ua haujlwm. Qhov nce no ntawm AUC qhov tseem ceeb tsis yog qhov tseem ceeb hauv tsev kho mob, yog li ntawd tsis tas kho qhov koob tshuaj.

Hauv cov neeg mob uas tsis tshua muaj lub raum mus rau lub raum tsis txaus, thiab rau cov neeg mob ntawm kev mob hemodialysis, AUC qhov tseem ceeb ntawm saxagliptin thiab nws cov metabolite tseem ceeb yog 2.1 thiab 4.5 npaug siab dua, feem ntau, ntau dua li cov neeg uas muaj lub raum zoo li qub. Rau cov neeg mob uas muaj mob nyhav thiab tsis ua haujlwm lub raum, nrog rau cov neeg mob ntawm kev mob hemodialysis, cov koob tshuaj saxagliptin yuav tsum yog 2.5 mg ib hnub ib zaug (saib "Kev Ceeb Toom").

Lub siab ua haujlwm tsis zoo. Hauv cov neeg mob uas tsis tshua muaj mob me me, mob nyhav thiab hnyav hnyav, tsis muaj kev hloov pauv ntau hauv cov chaw muag tshuaj ntawm saxagliptin, yog li tsis tsim nyog kho cov tshuaj rau cov neeg mob no.

Cov neeg laus cov neeg mob. Hauv cov neeg mob 65-80 xyoo, tsis muaj qhov sib txawv hauv cov chaw muag tshuaj ntawm saxagliptin piv nrog cov neeg mob uas muaj hnub nyoog yau dua (18-40 xyoo), yog li ntawd yuav tsum tau txhaj tshuaj rau cov neeg laus laus tsis tas yuav tsum tau txhaj. Txawm li cas los xij, nws yuav tsum tau yug hauv siab tias nyob hauv pawg no ntawm cov neeg mob, qhov kev txo qis ntawm lub raum ua haujlwm yog qhov ntau dua (saib "Kev Ceeb Toom").

BMI Dosage kev kho kom haum tsis pom zoo nyob ntawm BMI, uas tsis raug txheeb xyuas tias yog covariate tseem ceeb ntawm kev pom meej meej ntawm saxagliptin lossis nws cov nquag metabolite raws li cov neeg tshuaj pharmacokinetic tsom.

Paul Koob tshuaj hloov kho raws poj niam txiv neej yog tsis xav tau. Tsis muaj qhov sib txawv hauv cov chaw muag tshuaj ntawm saxagliptin ntawm tus txiv neej thiab poj niam. Cov nqi ntawm cov metabolite nquag muaj kwv yees li 25% siab dua hauv cov poj niam piv nrog cov txiv neej, tab sis qhov sib txawv no tsis zoo li yuav muaj qhov tseem ceeb hauv chaw kho mob. Raws li cov pej xeem-based pharmacokinetic tsom xam, tub los ntxhais tsis tau pom tias yog covariate tseem ceeb hauv kev tshem tawm saxagliptin thiab nws cov metabolite.

Haiv neeg thiab pawg. Pom zoo koob tshuaj raws li haiv neeg tsis pom zoo. Raws li cov pej xeem pharmacokinetic tsom xam, thaum piv cov pharmacokinetics ntawm saxagliptin thiab nws cov metabolite hauv 309 cov neeg koom nrog Caucasian haiv neeg thiab 105 tsis yog haiv neeg European (suav nrog rau rau 6 pawg neeg), tsis muaj qhov sib txawv hauv pharmacokinetics ntawm saxagliptin thiab nws cov metabolite ntawm ob haiv neeg.

Kev siv cov xaum

Hom 2 mob ntshav qab zib mellitus ntxiv rau kev noj haus thiab kev tawm dag zog kom txhim kho glycemic tswj kom zoo:

- pib kev sib txuas nrog kev kho mob nrog metformin,

- ntxiv rau kev kho mob monotherapy nrog metformin, thiazolidinediones, sulfonylurea derivatives, insulin (suav nrog kev sib xyaw nrog metformin) thaum tsis muaj glycemic tswj txaus hauv qhov kev kho no,

- ntxiv rau kev sib xyaw ua ke ntawm metformin thiab sulfonylurea derivatives thaum tsis muaj glycemic tswj tau txaus hauv qhov kev kho no.

Cov Yuav Tsum Muaj

Ua rau cov tib neeg muaj qhov tsis haum, mob ntshav qab zib tsis haum tshuaj (mob anaphylaxis lossis mob caj dab) rau DPP-4 cov tshuaj tiv thaiv kab mob ntshav qab zib, hom 1 mob ntshav qab zib mellitus (siv tsis tau kawm), mob ntshav qab zib ketoacidosis, cev xeeb tub, lactation, hnub nyoog qis dua 18 xyoo (kev nyab xeeb thiab kev kawm tsis tau zoo).

Cev xeeb tub thiab lactation

Vim tias qhov tseeb hais tias kev siv saxagliptin thaum cev xeeb tub tsis tau kawm, nws yuav tsum tsis txhob siv tshuaj thaum cev xeeb tub.

Kuj tsis paub meej tias saxagliptin kis mus rau leej niam mis li cas. Vim tias qhov tseeb ntawm kev nkag mus ntawm saxagliptin mus rau niam mis tsis tau txiav txim siab, kev pub mis niam yuav tsum tau nres rau lub sijhawm ntawm kev kho mob nrog saxagliptin lossis kev kho yuav tsum tsis ua haujlwm ntxiv, suav txog qhov kev pheej hmoo ntawm tus menyuam thiab cov txiaj ntsig rau leej niam.

FDA Fetal Action Qeb - Kwv.

Kev tshawb nrhiav qhov txaus thiab tswjhwm nruj txog kev siv saxagliptin rau cov poj niam cev xeeb tub tsis tau ua. Siv thaum cev xeeb tub yog siv tau yog tias tsim nyog.

Saxagliptin yog tso rau hauv cov mis ntawm cov lactating nyob hauv thaj tsam kwv yees li 1: 1 nrog nws cov teeb meem hauv ntshav. Kuj tsis paub meej tias saxagliptin puas zais cia rau hauv leej niam cov kua mis. Txij li ntau cov tshuaj tau muab zais rau hauv niam cov kua mis, kev ceev faj yuav tsum tau siv thaum siv saxagliptin hauv cov poj niam laus.

Cov tshuaj uas cuam tshuam nrog kev nqus ntawm cov piam thaj hauv txoj hnyuv

Niaj hnub no, cov yeeb tshuaj no tsis nrov thoob plaws hauv Lavxias, vim tias lawv muaj nqi ntau. Lub caij no, txawv teb chaws, cov tshuaj no nrov heev ntawm cov neeg mob ntshav qab zib vim lawv txoj kev ua haujlwm siab. Qhov nrov tshaj plaws yog kho cov tshuaj glucobai.

Glucobai lossis acarbose, tso cai rau koj kom maj mam ua cov txheej txheem ntawm kev nqus ntawm cov piam thaj hauv txoj hnyuv thiab nws nkag rau hauv cov hlab ntshav. Qhov no pab txo qis cov ntshav qab zib hauv txhua hom ntshav qab zib. Tsis tas li, cov tshuaj no txo ​​cov roj triglycerides ntau hauv cov ntshav, uas txhim kho cov tshuaj insulin nyob hauv cov neeg mob ntshav qab zib hom 2 ntshav qab zib, uas feem ntau ua rau atherosclerosis.

Feem ntau cov feem ntau, glucobai yog tshuaj rau hom 2 mob ntshav qab zib mellitus raws li lub ntsiab los yog kev kho mob ntxiv rau hauv kev sib xyaw nrog sulfonamides. Ntawm ntshav qab zib hom 1, cov tshuaj no yog siv ua ke nrog kev qhia ntawm insulin rau hauv lub cev. Hauv qhov no, ntau npaum li cas ntawm cov tshuaj insulin muab txo.

Txij li cov tshuaj no tsis ua rau cov tshuaj tiv thaiv hypoglycemic, glucobai feem ntau kho rau cov neeg laus. Lub sijhawm, cov tshuaj yuav muaj kev phiv, xws li tso quav xoob thiab tsam plab.

Glucobai yuav tsum tsis txhob noj los ntawm cov neeg mob hnub nyoog qis dua 18 xyoo, nrog cov kab mob ntawm lub plab zom mov, thaum cev xeeb tub lossis pub niam mis. Xws li cov tshuaj tsis pom zoo siv rau hauv gastroparesis tshwm sim los ntawm kev mob ntshav qab zib neuropathy.

Kev siv tshuaj yaj yeeb yog ua nyob rau thaum ntxov ntawm 0.05 grams peb zaug ib hnub. Yog tias tsim nyog, qhov koob tshuaj maj mam nce mus txog 0.1, 0.2 lossis 0.3 grams peb zaug ib hnub. Kev noj tshuaj ntau dua yog tsis pom zoo. Qhov tsuas tshuaj yuav tsum tau nce ntau zog zuj zus, nyob rau hauv ib ntu ntawm ib mus rau ob lis piam.

Glucobay noj tshwj xeeb ua ntej noj mov yam tsis muaj ntxo. Cov tshuaj yuav tsum tau muab ntxuav nrog qhov me me ntawm cov dej. Qhov kev txiav txim ntawm cov tshuaj pib tam sim ntawd tom qab nws nkag mus rau hauv lub plab.

Yuav noj cov tshuaj muaj piam thaj li cas

Ib hom tshuaj xws li Manilin rau ntshav qab zib yog noj ib nrab teev ua ntej noj mov. Glucobai noj tsuas yog ua ntej noj mov, nws tuaj yeem noj nrog thawj daim ntawm cov zaub mov. Yog tias tus neeg mob tsis nco qab noj tshuaj ua ntej noj mov, nws raug tso cai kom noj cov tshuaj tom qab noj mov, tab sis tsis pub dhau 15 feeb tom qab.

Txawm li cas los xij, thaum tus neeg mob tsis nco qab noj tshuaj muaj suab thaj, nws yog txwv tsis pub nce qib ntawm cov tshuaj ntxiv rau yav tom ntej. Koj yuav tsum haus tsuas yog cov tshuaj uas raug tshuaj los ntawm koj tus kws kho mob.

Noj tshuaj muaj suab thaj kom tsawg thaum cev xeeb tub

Thaum cev xeeb tub, kev siv cov tshuaj muaj suab thaj txo qis yog qhov tsis pom kev, vim tias lawv tuaj yeem nkag rau hauv tus me nyuam thiab muaj qhov tsis zoo rau kev loj hlob ntawm tus me nyuam hauv plab. Vim li no, mob ntshav qab zib hauv cov poj niam cev xeeb tub tau kho los ntawm kev tswj hwm cov tshuaj insulin thiab siv tshuaj kho mob.

Yog tias tus poj niam muaj ntshav qab zib hom 2 thiab yav tas los raug kho nrog tshuaj hypoglycemic, nws maj mam hloov mus rau hauv insulin. Tib lub sijhawm, tus kws kho mob ua tus soj ntsuam nruj nruj ntawm tus neeg mob; kuaj ntshav thiab ntshav qab zib ua ntu zus. Qhov tshuaj insulin nyob rau hauv cov tshuaj ntawd cov ntshav qab zib tau noj.

Txawm li cas los xij, kev kho mob tseem ceeb feem ntau tau tswj hwm kev noj haus thiab kho cov ntawv qhia zaub mov.

Tus poj niam cev xeeb tub uas kuaj pom tias mob ntshav qab zib yuav tsum haus tsis pub ntau tshaj 35 Kcal nyob rau ib phaus ntawm ib hnub twg. Cov zaub mov protein txhua hnub hauv ib phaus ntawm qhov hnyav tuaj yeem txog li ob gram, carbohydrates - 200-240 grams. Rog - 60-70 grams.

Nws yog ib qho tsim nyog yuav tsum tau tso pov tseg tag nrho ntawm kev zom cov zaub mov carbohydrates sai sai, uas suav nrog cov khoom siv hmoov nplej, semolina, confectionery, khoom qab zib.Hloov chaw, koj yuav tsum noj cov zaub mov uas muaj cov vitamins A, B, C, D, E, cov zaub mov thiab cov nroj tsuag.

Noj ntau dhau

Cov tsos mob ntawm intoxication tsis tau piav qhia nrog kev siv ntev ntawm saxagliptin hauv koob tshuaj kom txog 80 lub sij hawm siab dua qhov kev pom zoo.

Kev Kho Mob: Thaum noj ntau dhau, siv tshuaj kho qhov tsos mob yuav tsum siv. Saxagliptin thiab nws cov metabolite tseem ceeb yog kho los ntawm hemodialysis (kev kuaj mob ntxiv: 23% ntawm qhov hno hauv 4 teev).

Hauv kev tswj xyuas cov chaw kho mob, thaum cov neeg noj qab haus huv tau noj saxagliptin qhov ncauj 1 zaug hauv ib hnub ntawm qhov siab txog li 400 mg / hnub rau 2 lub lis piam (80 zaug siab dua MPD), tsis muaj tshuaj txhaj tsis haum tshuaj thiab tsis muaj kev cuam tshuam loj hauv QTc ntu lossis plawv dhia.

Ceev faj txog cov tshuaj saxagliptin

Kev siv saxagliptin ua ib feem ntawm kev kho mob triple nrog metformin thiab thiazolidinediones tsis tau kawm.

Siv nrog rau cov tshuaj uas tuaj yeem ua rau ntshav qab zib ntshav qab zib. Cov neeg tsim ntawm sulfonylureas thiab cov tshuaj insulin tuaj yeem ua rau cov ntshav qog ntshav qab zib, yog li, yuav txo qis kev pheej hmoo ntawm hypoglycemia thaum siv saxagliptin, qhov koob tshuaj yuav txo qis rau ntawm sulfonylureas lossis insulin tej zaum yuav tsum tau ua.

Kev ua haujlwm tsis haum siab. Cov kev tsis haum siab loj, suav nrog anaphylaxis thiab mob hlwb, tau tshaj tawm tias lub sijhawm tom qab kev siv tshuaj saxagliptin. Nrog rau kev txhim kho kev tsis haum tshuaj tiv thaiv kom tsis txhob mob siab ntxiv, koj yuav tsum tso tseg kev siv saxagliptin, soj ntsuam lwm qhov ua rau muaj kev tshwm sim, thiab hais txog kev kho mob ntshav qab zib mellitus (saib "Contraindications" thiab "Side Effects").

Kev mob caj dab Hauv kev tshaj tawm tom qab kev siv saxagliptin, cov lus ceeb toom hais txog qhov tshwm sim ntawm tus mob ntawm tus mob ua paug ncaj qha tau txais. Cov neeg mob uas siv saxagliptin yuav tsum paub txog cov tsos mob ntawm tus mob huam sai - mob ntev, mob hnyav hauv plab. Yog tias koj xav tias yog kev txhim kho ntawm pancreatitis, koj yuav tsum tsum tsis txhob noj saxagliptin (saib "Kev Txwv rau kev siv" thiab "Cov Kev Mob Phom Sij").

Qhov tshwm sim ntawm kev mob pancreatitis hauv txoj kev tshawb no TXIVpaub tseeb raws li txoj kev tshawb no yog 0.3% nyob rau hauv saxagliptin thiab cov placebo pawg hauv cov neeg ntawm txhua tus neeg mob randomized.

Kev mob caj dab Hauv kev kawm txog cov kev mob plawv hauv cov kev kawm kev koom nrog paub tseeb atherosclerotic CVDs lossis ntau yam kev pheej hmoo rau atherosclerotic CVDs (sim TXIVa) cov neeg mob hnyav rau kev mob pancreatitis tau pom zoo hauv 17 ntawm 8240 (0.2%) cov neeg mob tau txais saxagliptin, piv nrog 9 ntawm 8173 (0.1%) cov neeg mob tau txais cov placebo. Preexisting pancreatitis txaus ntshai pom muaj nyob hauv 88% (15/17) ntawm cov neeg mob tau txais saxagliptin, thiab 100% (9/9) ntawm cov neeg uas tau txais cov placebo.

Tom qab pib txoj kev tswj hwm saxagliptin, nws yog ib qho tsim nyog los soj ntsuam cov neeg mob kom paub cov cim thiab cov tsos mob ntawm tus mob pancreatitis. Yog tias pom muaj tus mob pancreatitis, saxagliptin yuav tsum tsis ua mus ntxiv tam sim thiab kev ntsuas tsim nyog. Kuj tsis paub meej tias cov neeg mob uas muaj keeb kwm mob pancreatitis yog qhov muaj kev pheej hmoo loj dua ntawm kev mob caj dab thaum siv saxagliptin.

Lub plawv tsis ua hauj lwm. Hauv kev kawm TXIV muaj qhov nce ntxiv ntawm cov zaus mus pw hauv tsev kho mob rau lub plawv tsis ua hauj lwm hauv saxagliptin pawg piv nrog pab pawg placebo, txawm hais tias kev sib raug zoo ntawm kev sib raug zoo tsis tau tsim. Ceev faj yuav tsum tau siv thaum siv saxagliptin rau cov neeg mob uas muaj feem phom sij mus pw hauv tsev kho mob rau lub plawv tsis ua hauj lwm, xws li muaj keeb kwm mob pes tsawg los yog mob raum tsis zoo. Cov neeg mob yuav tsum tau qhia rau tus yam ntxwv ntawm tus yam ntxwv ntawm lub plawv tsis ua hauj lwm thiab xav tau cov kev qhia tam sim ntawd (saib Pharmacodynamics).

Lub plawv tsis ua hauj lwm. Hauv kev kawm txog cov kev mob plawv hauv cov kev kawm kev koom nrog paub tseeb atherosclerotic CVDs lossis ntau yam kev pheej hmoo rau atherosclerotic CVDs (sim TXIV) ntau dua ntawm cov neeg mob randomized rau saxagliptin kho pab pawg (289/8280, 3.5%) tau mus pw hauv tsev kho mob rau lub plawv tsis ua haujlwm piv nrog cov neeg mob randomized rau cov placebo pawg (228/8212, 2.8%). Thaum kuaj lub sijhawm ua ntej thawj qhov xwm txheej, kev pheej hmoo ntawm tsev kho mob rau lub plawv tsis ua haujlwm siab dua hauv pab pawg saxagliptin (RR: 1.27, 95% CI: 1.07, 1.51). Cov neeg mob uas muaj lub plawv ua ntej thiab cov neeg mob raum tsis ua haujlwm muaj kev pheej hmoo siab dua mus pw hauv tsev kho mob rau lub plawv tsis ua haujlwm, tsis hais kev kho mob dabtsi.

Cov kev pheej hmoo thiab txiaj ntsig ntawm kev kho yuav tsum raug txiav txim siab hauv cov neeg mob uas muaj kev pheej hmoo ntxiv ntawm kev mob plawv tsis txaus ua ntej noj saxagliptin. Cov neeg mob yuav tsum tau saib xyuas kom paub txog cov cim thiab cov tsos mob ntawm lub plawv tsis zoo thaum kho. Cov neeg mob yuav tsum tau qhia rau cov yam ntxwv ntawm tus yam ntxwv ntawm lub plawv tsis ua hauj lwm thiab qhia cov tsos mob tam sim ntawd. Nrog rau kev txhim kho lub plawv tsis ua hauj lwm, ib qho yuav tsum tau ua raws li cov qauv tam sim no ntawm kev kho mob thiab xav txog kev txiav tawm saxagliptin.

Pob Tsuas Xyooj. Cov lus tshaj tawm tau tshaj tawm cov mob sib koom tes, suav nrog muaj zog thaum siv DPP-4 inhibitors. Hauv cov neeg mob, cov tsos mob nyem tau pom tom qab siv tshuaj los ntawm saxagliptin, thiab hauv cov neeg mob ib leeg rov mob tshwm sim thaum pom tias rov qab siv tib yam lossis lwm tus DPP-4 inhibitor. Qhov pib ntawm cov tsos mob tom qab pib siv cov tshuaj tuaj yeem nrawm lossis tshwm sim thaum kho tau ntev. Nrog rau kev txhim kho ntawm kev mob pob txha hnyav, kev tswj hwm txuas ntxiv ntawm saxagliptin hauv txhua tus neeg mob yuav tsum raug ntsuas.

Cov teebmeem macrovascular. Tsis muaj cov kev tshawb fawb soj ntsuam tau ua tiav los ua kom pom tseeb cov pov thawj ntawm kev txo qis ntawm kev pheej hmoo mob macrovascular ua rau kev kho mob saxagliptin lossis lwm yam tshuaj tiv thaiv kab mob.

Siv rau hauv pab pawg neeg mob tshwj xeeb

Cov neeg mob uas lub raum tsis ua hauj lwm zoo. Rau cov neeg mob uas tsis muaj lub raum tsis txaus (creatinine Cl> 50 ml / min), tsis tas kho qhov koob tshuaj. Rau cov neeg mob uas mob raum lossis mob raum tsis ua haujlwm (Cl creatinine ≤50 ml / min), ntxiv rau tus neeg mob hemodialysis, kev pom zoo koob tshuaj pom zoo.

Kev siv cov saxagliptin hauv cov neeg mob ntawm kev mob plab peritoneal tsis tau kawm.

Ua ntej pib kho nrog saxagliptin thiab thaum kho, nws raug nquahu kom kuaj xyuas lub raum kev ua haujlwm.

Cov neeg mob uas muaj lub siab ua haujlwm tsis zoo. Yog tias daim siab ua haujlwm tsis zoo, hloov kho me ntsis, mob nyhav thiab hnyav hnyav tsis tas yuav ua haujlwm.

Cov neeg laus cov neeg mob. Ntawm 16,492 cov neeg mob randomized rau txoj kev tshawb no. TXIV, 8561 cov neeg mob (51.9%) yog 65 xyoo lossis laus dua, thiab 2330 cov neeg mob (14.1%) yog 75 xyoo lossis laus dua. Ntawm cov no, 4290 cov neeg mob hnub nyoog 65 xyoos thiab laus dua thiab 1169 cov neeg mob hnub nyoog 75 xyoo thiab laus dua tau txais saxagliptin. Raws li kev tshawb fawb hauv kev kho mob, kev ntsuas tau zoo thiab kev nyab xeeb hauv cov neeg mob hnub nyoog 65 xyoos thiab laus dua, 75 xyoo thiab laus dua tsis txawv ntawm cov ntsuas zoo li no hauv cov neeg mob uas muaj hnub nyoog yau dua. Koob tshuaj hloov kho hauv cov neeg mob laus tsis tas yuav. Txawm li cas los xij, thaum xaiv cov koob tshuaj, nws yuav tsum tau yug los rau hauv lub siab tias hauv pawg no ntawm cov neeg mob, qhov kev txo qis ntawm lub raum kev ua haujlwm yog qhov ntau dua.

Cov menyuam. Muaj kev nyab xeeb thiab ua kom tsis raug rau cov neeg mob hnub nyoog qis dua 18 xyoo tsis tau kawm.

Kev siv yooj yim nrog cov muaj zog CYP3A4 / 5 inhibitors

Thaum siv nrog muaj zog CYP3A4 / 5 inhibitors xws li ketoconazole, atazanavir, clarithromycin, indinavir, itraconazole, nefazodone, nelfinavir, ritonavir, saquinavir thiab telithromycin, koob tshuaj pom zoo yog 2.5 mg ib hnub ib zaug.

Cuam tshuam rau kev muaj peev xwm tsav tsheb thiab tswj cov tshuab. Cov kev tshawb fawb los kawm txog cov nyhuv ntawm saxagliptin ntawm kev muaj peev xwm tsav tsheb thiab kev tswj cov tshuab tseem tsis tau ua.

Nco ntsoov tias saxagliptin yuav ua rau kiv taub hau.