Vildagliptin - cov lus qhia, analogues thiab kev xyuas cov neeg mob

Txawm hais tias muaj kev xaiv ntau ntawm cov tshuaj muaj ntshav qab zib, cov cuab yeej zoo tshaj plaws rau kev tswj glycemia tseem tsis tau pom. Vildagliptin yog ib qho tshuaj tiv thaiv kab mob siab tshaj plaws niaj hnub no. Nws tsis tsuas yog muaj qhov tsawg kawg ntawm kev phiv: nws tsis ua rau qhov hnyav nce thiab cov ntshav tsis txaus, tsis ua rau lub luag haujlwm ntawm lub plawv, nplooj siab thiab lub raum, tab sis kuj tseem ua rau lub peev xwm ntawm beta hlwb los tsim cov insulin.

Vildagliptin yog ib qho khoom siv uas ua rau muaj kev pab ntau ntxiv ntawm lub hnub nyoog - cov tshuaj hormones ntuj ntawm lub plab zom mov. Raws li kws kho mob, cov tshuaj no tuaj yeem siv tau zoo nrog kev mob ntshav qab zib ntev ntev thiab hauv cov theem pib ntawm tus kab mob, suav nrog ua ib feem ntawm kev kho mob sib xyaw.

Yuav ua li cas nrhiav tau vildagliptin

Cov lus qhia thawj zaug ntawm incretins tshwm ntau dua 100 xyoo dhau los, rov qab rau xyoo 1902. Cov tshuaj yeeb dej caw ua kom cais tawm ntawm plab hnyuv thiab hu ua secretins. Tom qab ntawd lawv lub peev xwm los txhawb qhov kev tso tawm ntawm cov enzymes los ntawm kab mob ntshav ntswg tsim nyog rau kev zom cov zaub mov tau pom. Ob peb xyoos tom qab, muaj kev tawm tswv yim tias kev zais cia kuj tseem tuaj yeem cuam tshuam cov kev ua hauv hormonal ntawm cov qog. Nws tau muab tawm tias nyob rau hauv cov neeg mob glucosuria, thaum noj cov tshuaj ntxiv sai, cov piam thaj hauv cov zis muaj tsawg dua, cov zis puas tsawg, thiab kev noj qab haus huv zoo tuaj.

Hauv xyoo 1932, qhov tshuaj hormones tau txais nws lub npe niaj hnub - glucose-tiv thaiv insulinotropic polypeptide (HIP). Nws muab tawm tias nws yog synthesized hauv cov hlwb ntawm mucosa ntawm duodenum thiab jejunum. Thaum xyoo 1983, 2 cov txiv kab ntxwv zoo li peptides (GLPs) tau raug cais tawm. Nws muab tawm tias GLP-1 ua rau cov kua dej hauv cov kua dej hauv cov lus teb rau cov ntshav qabzib, thiab nws txoj kev zais cia tsawg dua nyob rau hauv cov ntshav qab zib.

Qhov kev txiav txim ntawm GLP-1:

Mob ntshav qab zib thiab siab surges yuav yog ib yam dhau los

• Li qub ntawm qab zib -95%
• Kev tshem tawm ntawm cov hlab ntsha thrombosis - 70%
• Ntaus tau ntawm lub plawv dhia muaj zog -90%
• Kev tshem tawm ntshav siab - 92%
• Qhov nce hauv lub zog nruab hnub, txhim kho pw tsaug zog thaum hmo ntuj -97%

• stimulates insulin tso rau hauv cov neeg mob ntshav qab zib;
• prolongs muaj cov khoom noj hauv lub plab;
• txo qhov xav tau ntawm cov zaub mov, pab txhawb rau qhov poob phaus;
• muaj lub txiaj ntsig zoo ntawm lub siab thiab cov hlab ntsha;
• txo cov khoom lag luam ntau lawm hauv glucagon hauv kev txiav - cov yam tshuaj uas ua rau lub zog ntawm insulin tsis muaj zog.

Nws faib cov nce zuj zus ntxiv nrog cov enzyme DPP-4, uas yog tam sim no ntawm qhov endothelium ntawm cov hlab ntsha mus rau hauv lub plab hnyuv hnyuv, rau qhov no nws yuav siv li 2 feeb.

Kev siv tshuaj ntsuab ntawm cov kev tshawb pom no tau pib xyoo 1995 los ntawm lub tuam txhab kev lag luam Novartis. Cov kws tshawb fawb muaj peev xwm cais cov tshuaj uas cuam tshuam nrog kev ua haujlwm ntawm DPP-4 enzyme, uas yog vim li cas lub sijhawm ntawm GLP-1 thiab HIP nce los ntawm ntau lub sijhawm, thiab insulin synthesis tseem nce. Thawj cov tshuaj ruaj khov nrog rau xws li cov kev ua haujlwm uas tau dhau los ntawm kev kuaj xyuas kev nyab xeeb yog vildagliptin. Lub npe no tau nqus ntau cov ntaub ntawv: ntawm no yog chav kawm tshiab ntawm cov kab mob hypoglycemic "glyptin" thiab ib feem ntawm lub npe ntawm nws tus tsim Willhower, thiab hais txog kev muaj peev xwm ntawm cov tshuaj txo glycemia "gly" thiab txawm hais tias "yog", los yog dipeptidylamino-peptidase, lub enzyme DPP -4.

Kev txiav txim ntawm vildagliptin

Thaum pib ntawm lub hnub nyoog nce zuj zus hauv kev kho mob ntshav qab zib yog suav tias yog xyoo 2000, thaum tseem muaj peev xwm thaiv tau DPP-4 tau tshwm sim thawj zaug ntawm Congress ntawm Endocrinologist. Hauv lub sijhawm luv luv, vildagliptin tau nce qhov chaw muaj zog hauv cov qauv kev kho mob ntshav qab zib hauv ntau lub tebchaws hauv ntiaj teb. Hauv tebchaws Lavxias, cov tshuaj raug rau npe xyoo 2008. Tam sim no vildagliptin muaj nyob rau txhua xyoo hauv cov npe ntawm cov tshuaj tseem ceeb.

Kev vam meej sai no yog vim muaj cov cim tshwj xeeb ntawm vildagliptin, uas tau lees paub los ntawm cov txiaj ntsig ntau dua 130 cov kev tshawb fawb thoob ntiaj teb.

Mob ntshav qab zib, cov tshuaj tso cai rau koj:

1. Txhim kho glycemic tswj. Vildagliptin hauv ib koob tshuaj 50 mg txhua hnub pab txo cov suab thaj tom qab noj mov yog kwv yees li 0.9 mmol / L. Glycated hemoglobin raug txo los ntawm qhov nruab nrab 1%.
2. Ua kom cov kua nplaum ntawm lub ntsej muag nrawm dua los ntawm kev txo cov kab mob. Ntau kawg postprandial glycemia txo los ntawm kwv yees li 0.6 mmol / L.
3. Yuav txo tau ntshav siab nyob nruab hnub thiab hmo ntuj hauv thawj rau lub hlis ntawm kev kho mob.
4. Txhim kho cov lipid metabolism feem ntau los ntawm kev txo cov tshuaj ntawm cov lipoproteins uas tsis muaj ntau. Cov kws tshawb fawb txiav txim siab qhov txiaj ntsig no ua ntxiv, tsis cuam tshuam rau kev txhim kho cov nyiaj them ntshav qab zib.
5. Txo qhov hnyav thiab duav hauv cov neeg mob rog.
6. Vildagliptin yog tus cwj pwm ntawm kev zam zoo thiab kev nyab xeeb siab. Kev mob ntshav qab zib hauv lub sijhawm nws siv tsis tshua muaj: kev pheej hmoo yog 14 npaug qis dua thaum noj tshuaj sulfonylurea derivatives.
7. Cov tshuaj mus zoo nrog metformin. Hauv cov neeg mob noj cov tshuaj metformin, ntxiv ntawm 50 mg ntawm vildagliptin rau kev kho mob tuaj yeem txo qis GH ntxiv los ntawm 0.7%, 100 mg los ntawm 1.1%.

Raws li cov lus qhia, kev nqis tes ntawm Galvus, lub npe lag luam tawm rau vildagliptin, ncaj qha nyob ntawm kev muaj peev xwm ntawm pancreatic beta hlwb thiab qib qabzib. Hauv thawj hom mob ntshav qab zib thiab hauv ntshav qab zib hom 2 nrog qhov feem pua ​​loj ntawm cov hlwb tawg, vildagliptin tsis muaj zog. Hauv cov neeg muaj kev noj qab haus huv thiab nyob rau hauv cov neeg mob ntshav qab zib nrog cov piam thaj ib txwm, nws yuav tsis ua rau lub xeev tsis muaj ntshav qab zib.

Tam sim no, vildagliptin thiab nws cov analogues raug suav hais tias yog cov tshuaj ntawm kab thib 2 tom qab metformin. Lawv tuaj yeem ua tiav hloov cov tam sim no feem ntau sulfonylurea derivatives, uas tseem txhim kho cov tshuaj insulin, tab sis muaj kev nyab xeeb tsawg dua.

Pharmacokinetics ntawm cov tshuaj

Pharmacokinetic ntsuas ntawm vildagliptin los ntawm cov lus qhia rau kev siv:

Tshuaj nrog vildagliptin

Tag nrho cov cai rau vildagliptin yog txoj cai los ntawm Novartis, uas tau nqis peev ntau thiab nyiaj txiag hauv kev txhim kho thiab tua cov tshuaj hauv khw. Cov ntsiav tshuaj yog tsim nyob rau hauv Switzerland, Spain, Lub teb chaws Yelemees. Tsis ntev, kev tshaj tawm ntawm txoj kab hauv tebchaws Russia ntawm Novartis Neva ceg yuav tsum. Cov tshuaj yeeb tshuaj, uas yog vildagliptin nws tus kheej, tsuas muaj keeb kwm Swiss.

Vildagliptin muaj 2 Novartis khoom: Galvus thiab Galvus Met. Cov tshuaj nquag ntawm Galvus tsuas yog vildagliptin. Cov tshuaj muaj ib zaug tau tshuaj ntawm 50 mg.

Galvus Met yog kev sib xyaw ntawm metformin thiab vildagliptin hauv ib ntsiav tshuaj. Muaj cov tshuaj ntxiv rau: 50/500 (mg sildagliptin / mg metformin), 50/850, 50/100. Txoj kev xaiv no tso cai rau koj coj mus rau hauv tus account txog cov ntshav qab zib hauv ib tus neeg mob tshwj xeeb thiab xaiv txoj kev noj tshuaj uas yog.

Raws li cov neeg mob ntshav qab zib, noj Galvus thiab metformin hauv cov ntsiav tshuaj cais yog qhov pheej yig dua: tus nqi ntawm Galvus yog li 750 rubles, metformin (Glucophage) yog 120 rubles, Galvus Meta yog kwv yees li 1600 rubles. Txawm li cas los xij, kev kho mob nrog cov sib xyaw ua ke Galvus Metom tau lees paub tias ua haujlwm zoo dua thiab yooj yim.

Galvus tsis muaj analogues nyob hauv Russia muaj vildagliptin, txij li cov tshuaj yeeb tshuaj yuav raug txwv tsis pub siv. Tam sim no, nws yog txwv tsis pub tsuas yog tsim cov tshuaj nrog vildagliptin, tab sis kuj tseem txhim kho cov tshuaj yeeb nws tus kheej. Qhov kev ntsuas no tso cai rau cov khw tsim cov nqi ntawm cov kev tshawb fawb ntau qhov tsim nyog los sau npe rau ib yam tshuaj tshiab.

Kev ntsuas rau nkag

Vildagliptin tsuas yog qhia txog ntshav qab zib hom 2 xwb. Raws li cov lus qhia, ntsiav tshuaj tuaj yeem muab tshuaj:

1. Ntxiv rau metformin, yog tias nws cov koob tshuaj noj tsis zoo txaus los tswj ntshav qab zib.
2. Txhawm rau hloov sulfonylurea (PSM) kev npaj rau hauv cov neeg mob ntshav qab zib nrog rau kev pheej hmoo ntawm cov ntshav qab zib tsawg dua. Qhov laj thawj yuav yog hnub nyoog laus, noj zaub mov zoo, kis las thiab lwm yam qoj ib ce, neuropathy, kev ua haujlwm tsis zoo hauv lub siab thiab kev zom zaub mov.
3. Tus mob ntshav qab zib uas muaj qhov tsis haum rau PSM pawg.
4. Hloov ntawm sulfonylurea, yog tias tus neeg mob nrhiav kom ncua sijhawm pib kho cov tshuaj insulin ntau li ntau tau.
5. Raws li kev kho mob monotherapy (tsuas yog vildagliptin), yog tias noj Metformin yog contraindicated lossis tsis tuaj yeem vim muaj kev phiv loj heev.

Tau txais cov tshuaj vildagliptin yam tsis swb yuav tsum yog sib xyaw nrog pluas noj ntshav qab zib thiab kev kawm lub cev. Muaj cov tshuaj insulin ntau heev vim tias qhov kev ntxhov siab qis qis thiab kev tswj hwm tsis tau ntawm carbohydrates tuaj yeem dhau los ua qhov tsis txaus ntseeg ua kom tiav cov nyiaj them rau ntshav qab zib. Cov kev qhia tso cai rau koj los sib xyaw ua ke vildagliptin nrog metformin, PSM, glitazones, insulin.

Cov koob tshuaj pom zoo ntawm cov tshuaj yog 50 lossis 100 mg. Nws nyob ntawm ntau qhov mob ntshav qab zib. Cov tshuaj feem ntau cuam tshuam rau postprandial glycemia, yog li nws yuav tsum tau haus ib koob tshuaj 50 mg thaum sawv ntxov. 100 mg tau muab faib sib npaug rau kev txais tos thaum sawv ntxov thiab yav tsaus ntuj.

Nquag ua yam tsis xav tau

Qhov tseem ceeb tseem ceeb ntawm vildagliptin yog qhov tsawg zaus ntawm cov kev mob tshwm sim thaum nws siv. Cov teeb meem tseem ceeb hauv cov neeg mob ntshav qab zib siv PSM thiab insulin yog hypoglycemia. Txawm hais tias qhov tseeb tias ntau zaus lawv dhau los ua ib daim ntawv me, cov kua qab zib poob yog qhov txaus ntshai rau cov hlab ntsha tsis zoo, yog li lawv sim kom zam ntau li ntau tau. Cov lus qhia rau kev siv paub tias kev pheej hmoo ntawm hypoglycemia thaum noj vildagliptin yog 0.3-0.5%. Rau kev sib piv, hauv pawg tswj hwm tsis txhob noj tshuaj, qhov kev pheej hmoo ntawm no yog ntawm 0.2%.

Kev nyab xeeb siab ntawm vildagliptin tseem muaj pov thawj vim tias thaum lub sijhawm kawm, tsis muaj ntshav qab zib yuav tsum tau thim tawm ntawm cov tshuaj vim nws cov kev mob tshwm sim, raws li muaj pov thawj los ntawm tib tus tsis kam lees ntawm kev kho mob hauv cov pab pawg noj vildagliptin thiab placebo.

Tsawg dua 10% ntawm cov neeg mob yws ntawm lub teeb pom kev zoo, thiab tsawg dua 1% yws yws txog cem quav, mob taub hau, thiab o ntawm cov tshaj. Nws tau pom tias kev siv lub sijhawm ntev ntev ntawm vildagliptin tsis ua rau muaj kev nce ntxiv hauv lub zaus ntawm nws cov kev mob tshwm sim.

Raws li cov lus qhia, contraindications kom noj cov tshuaj tsuas yog hypersensitivity rau vildagliptin, me nyuam yaus, cev xeeb tub thiab lactation. Galvus muaj lactose ua ib lub koom haum pab, yog li ntawd, thaum nws thev tsis nkag siab, cov ntsiav tshuaj no yog txwv tsis pub. Galvus Met raug tso cai, vim tias tsis muaj lactose hauv nws cov muaj pes tsawg leeg.

Noj ntau dhau

Muaj peev xwm tshwm sim ntawm kev siv ntau tshaj ntawm vildagliptin raws li cov lus qhia:

Thaum muaj kev noj ntau dhau, kho lub plab zom mov thiab kev kho mob tus yam ntxwv yog qhov tsim nyog. Vildagliptin metabolites raug ntwm los ntawm hemodialysis.

Vildagliptin analogues

Tom qab vildagliptin, ntau ntau yam tshuaj tau pom tias tuaj yeem tiv thaiv DPP-4. Tag nrho cov ntawm lawv yog cov analogues:

• Saksagliptin, cov npe lag luam Onglisa, cov tsim tawm Astra Zeneka. Kev sib xyaw ntawm saxagliptin thiab metformin yog hu ua Comboglize;
• Sitagliptin muaj nyob hauv kev npaj ntawm Januvius los ntawm lub tuam txhab Merck, Xelevia los ntawm Berlin-Chemie. Sitagliptin nrog metformin - cov tshuaj yeeb tshuaj ntawm ob lub tshuaj tiv thaiv sib xyaw Janumet, ib qho khoom sib piv ntawm Galvus Meta;
• Linagliptin muaj lub npe lag luam Trazhenta. Cov tshuaj yog lub hlwb ntawm lub tuam txhab German Beringer Ingelheim. Linagliptin ntxiv rau metformin hauv ib ntsiav tshuaj hu ua Gentadueto;
• Alogliptin yog ib qho muaj txiaj ntsig ntawm Vipidia ntsiav tshuaj, uas yog tsim hauv Tebchaws Asmeskas thiab Nyij Pooj los ntawm Takeda Pharmaceuticals. Kev sib xyaw ua ke ntawm alogliptin thiab metformin yog tsim nyob rau hauv cov cim lag luam Vipdomet;
• Gozogliptin tsuas yog qhov tshuaj nyob ib puag ncig ntawm vildagliptin. Nws yog npaj los tso nws los ntawm Satereks LLC. Ib lub voj voos ntau lawm tag nrho, suav nrog cov tshuaj pharmacological, yuav tau nqa tawm hauv cheeb tsam Moscow. Raws li cov txiaj ntsig ntawm kev sim tshuaj, kev nyab xeeb thiab ua tau zoo ntawm gozogliptin tau ze rau vildagliptin.

Hauv cov chaw muag tshuaj Lavxias, tam sim no koj tuaj yeem yuav Ongliza (tus nqi rau ib chav kawm txhua hli yog txog 1800 rubles), Combogliz (los ntawm 3200 rubles), Januvius (1500 rubles), Kselevia (1500 rubles), Yanumet (los ntawm 1800), Trazhentu ( 1700 rub.), Vipidia (los ntawm 900 rub.). Raws li tus naj npawb ntawm cov tshuaj xyuas, nws tuaj yeem sib cav tias feem ntau nrov ntawm cov analogues ntawm Galvus yog Januvius.

Cov kws kho mob tshuaj xyuas txog vildagliptin

Cov kws kho mob muab tus nqi vildagliptin ntau heev. Lawv hu rau qhov zoo ntawm cov tshuaj no lub cev muaj txiaj ntsig ntawm nws cov kev ua, kev kam rau siab, kev ua siab ntev ntawm cov nyhuv ntshav, tsis tshua muaj teeb meem ntawm lub qog ntshav qab zib, muaj txiaj ntsig ntxiv nyob rau hauv daim ntawv ntawm kev tiv thaiv kev txhim kho ntawm microangiopathy thiab txhim kho cov kev mob ntawm cov phab ntsa ntawm cov hlab ntsha loj.

Vildagliptin, tseeb, nce tus nqi kho mob, tab sis nyob rau qee kis (nquag muaj ntshav tsis txaus) tsis muaj qhov tsim nyog hloov rau nws. Cov nyhuv ntawm cov tshuaj yog suav tias yog sib npaug nrog metformin thiab PSM, sijhawm dhau mus, kev ntsuas kev noj haus cov carbohydrate txhim kho me ntsis.

Kuj nyeem qhov no:

• Glyclazide MV ntsiav tshuaj yog qhov nrov tshaj plaws tshuaj rau cov neeg mob ntshav qab zib.
• Dibicor ntsiav tshuaj - nws cov txiaj ntsig zoo li cas rau cov neeg mob ntshav qab zib (cov neeg tau txais kev pab)