Vildagliptin analogues

Ntshav qab zib mellitus yog ib yam mob tshwm sim. Ntau cov tshuaj tau tsim los kho mob. Txhawm rau kom txo qis qab zib, cov tshuaj ua haujlwm Vildagliptin yog lus zais.

Tab sis nws tsis haum rau txhua tus neeg mob, yog li cov tuam txhab muag tshuaj sib txawv ntau tus naj npawb hloov chaw, zoo ib yam li hauv spectrum ntawm kev nqis tes ua. Nyeem cov lus qhia rau kev siv, tus nqi thiab tshuaj xyuas cov khoom pheej yig ntawm Vildagliptin.

Cov lus qhia rau kev siv

Vildagliptin yog ib yam tshuaj hypoglycemic. Cov tshuaj yog rau cov pab pawg ntawm stimulators ntawm islet pancreatic apparatus.

Cov tshuaj tuaj yeem siv tau tsis hais lub plab lossis puv plab. Qhov muaj cov zaub mov tsis cuam tshuam rau cov txheej txheem kev nqus.

Cov tshuaj tau pom zoo los ntawm tus kws kho mob rau kev kho mob raws li cov kev ntsuas tau ua thiab cov txiaj ntsig tau los ntawm qhov mob hnyav ntawm tus kab mob txuas ntxiv. Cov koob tshuaj tau muab rau ib leeg zuj zus rau txhua tus neeg mob, yog li ntawd, cov kev cai dav dav raug muab rau kev siv dav dav.

Thaum coj los kho kev siv ib hom tshuaj zoo lossis thaum sib koom ua ke siv 2 tshuaj, ntau npaum yuav tsum tsis pub tshaj 50 thiab 100 mg ib hnub ib zaug.

Kev tiv thaiv ob yam muaj xws li tshuaj:

Kev siv tshuaj zoo ib yam, nrog rau kev kho ua ke, nyob rau hauv tus nqi ntawm 100 mg, yuav tsum tau ua rau kev tswj hwm txhua hnub rau peb-txoj kev kho - Metformin + Vildagliptin + sulfonylurea derivatives.

Kev nkag mus ntawm koob tshuaj 50 mg rau hauv lub cev - ua ib hnub ib zaug (sawv ntxov lossis yav tsaus ntuj)Cov. Nrog rau cov kev cai xav tau ntawm 100 mg - siv cov dragees tshwm sim 2 zaug hauv ib hnub, tom qab sawv thiab ua ntej yuav mus pw.

Cov tshuaj yaj yeeb Nws tsuas yog kho rau kev kho mob rau tus neeg mob tus mob ntshav qab zib hom 2 xwbCov. Cov tshuaj yog siv los ua kev kho tus kheej lossis ua ib feem ntawm kev sib txuam tshuaj.

Txhawm rau kho tau tus kab mob insidious, ob yam khoom xyaw nquag yuav tsum muaj. Hauv qhov no, cov tshuaj txuas ntxiv hauv qab no tau cais tshwj xeeb:

• Cov tshuaj insulin
• Ib qho tshuaj twg uas ua kom ntshav qab zib plasma tsawg dua.

Vildagliptin yog cov tshuaj nquag muaj nyob hauv cov tshuaj nyob rau hauv lub npe lag luam Galvus. Lub tom kawg muaj nyob rau hauv daim ntawv ntawm ib puag ncig dragee, dawb nyob rau hauv cov xim, muaj ntau yam engravings ntawm ib tug neeg sab.

Cov tshuaj ua kom nquag plias hauv lub viav vias yog - 50 mg. Tsis tas li ntawd, anhydrous lactose thiab magnesium stearate siv. Kev siab me ntsis los ntawm sodium carboxymethyl hmoov txhuv nplej siab.

Cov tshuaj nquag ua yog cov tseem ceeb ntawm Galvus thiab muaj lub zog zoo. Cov chaw muag tshuaj hauv thaj tsam sib txawv muag cov tshuaj hauv tus nqi li ntawm 1150 txog 1300 rubles.

Vildagliptin muaj cov lej ntau yam ua tawm los ntawm ob lub tuam txhab lag luam Lavxias thiab cov neeg txawv teb chaws. Cov tshuaj zoo los ntawm hom kev tsim tawm tsis hloov, yog li ntawd feem ntau yuav, cov tshuaj uas pheej yig dua.

Txhua cov lus txhais rau vildagliptin yog tshuaj hypoglycemic. Lawv yog cov cuam ​​tshuam rau tib neeg lub cev, txo qis ntshav ntshav qab zib ntau ntau. Yog li ntawd, lawv cov contraindications thiab cov kev mob tshwm sim yuav luag sib luag.

Nws yog txwv tsis pub siv rau cov neeg hauv cov xwm txheej:

• Kev nkag siab tshwj xeeb rau cov nquag muaj,
• Qabzib tsis kam,
• Cov me nyuam qis dua 18 xyoo
• Ketoacidosis
• Yam I ntshav qab zib
• Lub sijhawm uas yug menyuam,
• Lub sijhawm pub mis rau menyuam,
• Tshuaj insulin ntxiv
• Tsis hlauv.

Sab phiv tshwm sim nrog nkag tsis yog nyob rau hauv daim ntawv ntawm:

• Mob taub hau, kiv taub hau,
• Kev ua xua,
• Xeev siab, tsis qab plab,
• Kev nkees nkees
• Kev ntshav siab.

Muaj qee kis thaum qee cov tshuaj raug tswj hwm, cov nyhuv hauv qab no ntxiv rau kev npau taws:

• Galvus Met - co thiab tsaj,
• Trazhenta, Onglisa - nasopharyngitis, pancreatitis,
• Glucovans, Gluconorm - lactic acidosis, mob hauv plab, ploj poob,
• Janumet - qaug zog, lub qhov ncauj qhuav, peripheral edema, pancreatitis,
• Amaril M - lub siab tsis meej, kev xiam oob khab, tsis meej pem nco qab, kev nyuaj siab,
• Gliformin - tom qab kev qhia hauv lub qhov ncauj kab noj hniav, ib qho kev sib tsoo ntawm cov hlau, zoo li lub plab zom mov.

Lwm yam tshuaj tsis tshua pom kev phiv, lossis tag nrho cov xwm txheej muaj qhia tau.

Lavxias

Vildagliptin analogues uas ua los ntawm cov tuam txhab pharmacological ua lag luam suav nrog cov npe me - Diabefarm, Formmetin, Gliformin, Gliclazide, Glidiab, Glimecomb. Cov tshuaj ntxiv yog tsim tawm txawv teb chaws.

Vildagliptin tsis yog siv nws tus kheej hauv ib qho ntawm cov kev hloov pauv. Nws yog hloov los ntawm cov tshuaj uas zoo sib xws uas muaj lub luag haujlwm rau qhov pom ntawm qhov kev ua thiab qhov zoo ntawm kev sib kis hauv tib neeg lub cev.

Cov tshuaj yeeb dej caw tseem ceeb raug rho tawm hauv cov lus sib piv ntawm Vildagliptin:

• Metformin - Gliformin, Formmetin,
• Glyclazide - Diabefarm, Glidiab, Glyclazide,
• Glyclazide + Metformin - Glimecomb.

Tsuas yog ob yam tshuaj lom tau tshawb pom tias tiv thaiv cov piam thaj hauv siab ntau hauv lub cev. Yog tias txhua tus tsis sib haum nrog cais, cov tshuaj sib xyaw ua ke hauv kev kho mob sib xyaw (Glimecomb).

Ntawm tus nqi, cov tuam ntxhab Lavxias yog poob qis dua txawv teb chaws. Cov neeg ua haujlwm txawv teb chaws loj hlob hauv tus nqi, muaj ntau dua 1000 rubles.

Formetin (119 rubles), Diabefarm (130 rubles), Glidiab (140 rubles) thiab Gliclazide (147 rubles) yog cov tshuaj pheej yig hauv tebchaws Lavxias. Gliformin tseem kim dua - 202 rubles. rau qhov nruab nrab ntawm 28 ntsiav tshuaj. Qhov tseem kim tshaj plaws yog Glimecomb - 440 rubles.

Nrau zoov

Cov tshuaj kho mob kom tshem tawm cov kev ua kom ntshav qab zib mellitus, tsim tawm hauv lwm lub teb chaws, tshwm sim hauv cov khoom loj dua li kev hloov pauv hauv tsev.

Cov tshuaj hauv qab no yog qhov txawv, uas muaj peev xwm tshem tawm qhov nce ntxiv ntawm cov piam thaj hauv cov ntshav ntawm tib neeg.

• Tebchaws Asmeskas - Trazhenta, Januvia, Combogliz Prolong, Nesina, Yanumet,
• Netherlands - Onglisa,
• Lub teb chaws Yelemees - Galvus Met, Glibomet,
• Fabkis - Amaril M, Glucovans,
• Ireland - Vipidia,
• Spain - Avandamet,
• Is Nrias teb - Gluconorm.

Cov tshuaj txawv teb chaws suav nrog Galvus, muaj Vildagliptin. Nws tso tawm yog teem rau hauv Switzerland. Cov lus txhais tsis tiav tsis tau.

Hauv kev sib pauv yog muaj cov tshuaj zoo ib yam, tab sis nrog sib txawv hauv lub ntsiab. Cov tshuaj yeeb dej caw ntawm ib qho khoom siv thiab kev tivthaiv ob qho:

• Linagliptin - Trazhenta,
• Sitagliptin - Onglisa,
• Saxagliptin - Januvius,
• Alogliptin benzoate - Vipidia, Nesina,
• Rosiglitazone + Metformin - Avandamet,
• Saksagliptin + Metformin - Comboglyz Prolong,
• Glibenclamide + Metformin - Gluconorm, Glucovans, Glibomet,
• Sitagliptin + Metformin - Yanumet,
• Glimepiride + Metformin - Amaril M.

Cov tshuaj txawv teb chaws muaj tus nqi siab dua. Yog li Gluconorm - 176 rubles, Avandamet - 210 rubles thiab Glukovans - 267 rubles yog pheej yig tshaj. Siab me ntsis hauv cov nqi - Glibomet thiab Glimecomb - 309 thiab 440 rubles. raws li.

Cov nqe hauv nruab nrab yog Amaril M (773 rubles). Tus nqi them los ntawm 1000 rubles. ua los ntawm cov tshuaj:

• Vipidia - 1239 rub.,
• Galvus Met - 1499 rub.,
• Onglisa - 1592 rubles.,
• Trazhenta - 1719 rubles.,
• Januvia - 1965 rub.

Qhov uas kim tshaj plaws yog Combogliz Prolong (2941 rubles) thiab Yanumet (2825 rubles).

Yog li, Galvus, uas muaj cov tshuaj nquag Vildagliptin, tsis yog cov tshuaj uas kim tshaj plaws. Nws tau teev nyob rau hauv nruab nrab nqe qeb, coj mus rau hauv tus account tag nrho cov tshuaj txawv teb chaws.

Galvus ntsiav tshuaj

Galvus yog ib qho tshuaj hypoglycemic tsim los tswj ntshav qab zib hauv cov neeg mob ntshav qab zib hom 2. Cov tshuaj phiv tshuaj yog vildagliptin. Ua tsaug rau cov tshuaj, kev tswj zoo ntawm glucagon thiab insulin metabolism yog nqa tawm. Raws li European Antidiabetic Association, kev siv cov tshuaj no hauv kev kho mob monotherapy tsuas yog tias muaj contraindications rau metformin. Ua tib zoo nyeem cov lus qhia rau kev siv Galvus ntsiav tshuaj thiab cov npe txwv.

INN, tuam ntxhab, nqi

Galvus yog hom tshuaj muaj npe kev lag luam. INN (npe thoob ntiaj teb nonproprietary) - vildagliptin. Nws tau ua nyob hauv Spain (Novartis Pharmaceutica) thiab hauv Switzerland (Novartis Pharma).

Koj tuaj yeem yuav cov tshuaj hauv txhua lub tsev muag tshuaj tau raws li kws kho mob sau tseg. Tus nqi rau ib pob ntawm 28 ntsiav tshuaj yog los ntawm 724 txog 956 rubles.

Pharmacological kev txiav txim

Vildagliptin yog chav kawm tshwj xeeb ntawm cov tshuaj tsim los txhawb kev islet apparatus ntawm lub txiav, uas yog lub luag hauj lwm rau xaiv inhibition ntawm DPP-4. Qhov no nce qhov kev tsim kho ntawm kev sib txuas ntawm cov glucagon-zoo li peptide ntawm thawj hom, nrog rau cov insulinotropic qabzib-polypeptide insulinotropic. Thaum cov as-ham nkag rau hauv cov hnyuv, cov tshuaj hormones incretin yog tsim thiab lawv ntxias cov kua dej hauv lub cev tsim tawm. Qhov tshwm sim no tau tshawb pom hauv 1960 tom qab lawv pom ib txoj hauv kev los ntsuas qhov kub siab ntawm cov kua dej hauv cov ntshav.

GLP-1 (glucagon-zoo li peptide-1) tau suav hais tias yog qhov zoo tshaj plaws-paub, txij li tiv thaiv keeb kwm ntawm hom II mob ntshav qab zib mellitus nws yog nws qhov kev cia siab uas poob qis hauv thawj qhov chaw. Raws li rau DPP-4 inhibitors, lawv nce qib ntawm cov tshuaj hormones, thiab tiv thaiv lawv qhov kev xeb ntxiv.

Tseem Ceeb! Thaum siv cov vildagliptin rau 12-52 lub lis piam, cov concentration ntawm cov piam thaj thiab glycated hemoglobin hauv cov ntshav ntawm lub plab khoob yog qhov txo qis.

Cov Tshuaj Pharmacokinetics

Vildagliptin hauv lub cev yog nqus tau sai sai, qhov tiag ntawm bioavailability nce mus txog 85%. Thaum noj cov tshuaj ntawm ib plab khoob, qhov siab tshaj plaws hauv cov ntshav tau sau cia tsawg dua ob teev. Los nrog cov zaub mov, cov tshuaj yuav nqus 19% qeeb dua, li ob thiab ib nrab teev.

Kev faib tawm cov tshuaj tshwm sim hauv txoj kev sib npaug ntawm cov ntshav liab thiab ntshav ntshav. Qhov tseem ceeb ntawm kev tshem tawm vildagliptin raug suav hais tias yog biotransformation. 85% ntawm cov tshuaj yog ua rau lub raum, tshuav 15% - dhau los ntawm txoj hnyuv.

Nws raug nquahu kom siv "Galvus" hauv kev kho mob ntshav qab zib ua ke nrog kev saib xyuas ntawm kev noj haus kom zoo thiab kev tawm dag zog. Kev qhia rau kev siv tshuaj yog:

• kev pib siv tshuaj kho mob rau cov neeg mob uas tsis muaj cov nyhuv ntawm kev noj haus thiab ua kom ib ce muaj zog ua ke nrog metformin,
• raws li kev kho mob monotherapy - rau cov neeg mob ntshav qab zib uas yuav tsum tsis txhob noj tshuaj metformin, lossis tsis muaj kev hloov pauv zoo los ntawm kev noj haus thiab qoj ib ce,
• ob txoj kev kho nrog thiazolidinedione thiab metformin, insulin, yog tias tsis muaj tshwm sim los ntawm kev kho mob,
• ua ke nrog kev kho peb zaug nrog sulfonylurea thiab metformin derivatives,
• cov kev kho mob triple kho mob nrog cov tshuaj insulin thiab metformin, yog tias tsis muaj kev tswj hwm kiag rau theem ntawm glycemia nrog txhua yam ntawm cov txheej txheem saum toj no.

Tsuas tshuaj, chav kawm, lub sijhawm ntawm cov txheej txheem kho raug xaiv tus kheej los ntawm tus kws kho mob tau kawm.

Cov Yuav Tsum Muaj

Zoo li txhua yam tshuaj, Galvus muaj ntau qhov kev txwv tseem ceeb ntawm kev siv, uas txhua tus neeg mob yuav tsum paub txog.
Nkag nkag:

Nrog kev ceev faj tshwj xeeb, cov tshuaj yog tshuaj tawm tsam ntawm keeb kwm ntawm mob hnyav, mob siab, theem davhlau ya nyob twg ntawm lub raum pathology thiab qib peb lub plawv tsis ua haujlwm.

Sab sij huam

Kev txhim kho ntawm kev mob siab tuaj yeem tshwm sim thaum noj vildagliptin sib xyaw nrog angiotensin-hloov enzyme inhibitors. Qhov kev tsis txaus ntseeg no yog mob hnyav, feem ntau daws ntawm nws tus kheej. Qee zaum, lub siab tuaj yeem hloov kho cov tshuaj.Qhov kev xyaum qhia pom tias qhov tshwm sim ntawm cov tsos mob zoo li no tsis tas yuav siv tshuaj kho ntxiv, nws txaus los ncua kev txais tos.

Kho mob, tawm tswv yim muab ib koob tshuaj 50 mg ob zaug ib hnub, provokes xws li mob mob tshwm sim li:

• mob taub hau
• kiv taub hau
• cem quav
• xeev siab
• peripheral o,
• nasopharyngitis.

Nrog rau kev kho ua ke nrog metformin, cov tsos mob uas zoo sib xws kuj tuaj yeem pom.
Kev kho mob nrog rau cov tshuaj insulin tuaj yeem nrog ua daus no, mob ntshav qab zib, mob plab, mob plab, lub plab tsis ua hauj lwm. Muaj qee lub ntsws qaug zog tshwm sim qee zaum qhia tawm.
Ntxiv rau qhov saum toj no, kev tshawb fawb tom qab sau npe tseg rau hauv cov neeg mob xws li mob siab, mob raum, mob pob qij txha, mob ntshav txhaws, thiab mob rau daim tawv nqaij.

Noj ntau dhau

Cov tshuaj ntawm cov tshuaj nquag mus txog 200 mg yog zoo tiv thaiv los ntawm cov neeg mob. Tsa mus rau 400 units tuaj yeem ua rau mob leeg nqaij, tsis tshua muaj kev o, nqaij pob txha, mob lipase ntau dua thiab kub cev. Txais tos ntau dua 600 mg ntawm vildagliptin provokes kev nce qib ntawm ALT thiab CPK, myoglobin, nrog rau C-reactive protein. Tsum cov tshuaj yuav pab tshem tawm cov tsos mob. Nws tsis tuaj yeem tshem tawm "Galvus" los ntawm tus neeg mob lub cev siv kev lim ntshav, tab sis koj tuaj yeem siv tus qauv hemodialysis.

Yeeb tshuaj sib cuam tshuam

Tawm tsam keeb kwm ntawm kev sib xyaw ua ke, cov nyhuv ntawm kev sib cuam tshuam nrog cov tshuaj xws li digoxin, warfarin, ramipril thiab metformin, pioglitazone, amlodipine thiab simvastatin, valsartan thiab glibenclamide tsis tau pom.

Yog tias koj noj "Galvus" nrog glucocorticosteroids, thiazides, sympathomimetics, nrog rau cov tshuaj hormones, qhov kev ua haujlwm hypoglycemic ntawm vildagliptin yog txo qis. Xws li kev tswj hwm ua ke nrog angiotensin-hloov enzyme inhibitors, kev mob hlwb yuav tshwm sim. Qhov xwm txheej no tsis tas yuav tsum tsis txiav lub tshuaj ntxiv, cov tsos mob daws nws tus kheej.

Cov lus qhia tshwj xeeb

Galvus yog ib qho tshuaj tiv thaiv kab mob, tab sis tsis muaj tshuaj ntawm cov tshuaj insulin. Tawm tsam keeb kwm yav dhau los ntawm nws txoj kev siv, nws yog ib qho tseem ceeb kom soj ntsuam kev ua haujlwm ntawm lub siab, txij li cov tshuaj nquag nquag pab txhim kho aminotransferase. Qhov no tsis tshwm sim los ntawm cov tsos mob tshwj xeeb, tab sis muaj kev pheej hmoo ntawm kev tsim kab mob siab. Yog tias muaj mob hnyav hauv plab, nws yog ib qho tsim nyog kom tsum tsis txhob noj, vim qhov no yuav qhia tau tias kev txhim kho ntawm txoj kev mob ua paug.

Kev ntshai dhau los, kev ntxhov siab tuaj yeem txo cov nyhuv ntawm kev noj tshuaj.

Yog tias koj pom xeev siab thiab tsis muaj kev sib koom ua ke, nws tsis pom zoo rau tsav tsheb lossis koom nrog kev txaus ntshai lossis kev ua haujlwm.

Ua ntej ua kev kuaj mob, nws yog ib qho tseem ceeb kom tsis txhob siv cov tshuaj rau ob hnub: hauv txhua tus neeg sawv cev uas siv thaum kuaj mob, muaj tshuaj iodine nyob rau. Nws cuam tshuam nrog vildagliptin, uas ua rau muaj kev txhim kho kev ntxhov siab rau daim siab thiab lub raum, fraught nrog kev txhim kho ntawm lactic acidosis.

Cev xeeb tub thiab lactation

Cov kev sim tshuaj qhia pom tias kev siv tshuaj tsawg kawg nkaus tsis cuam tshuam dab tsi rau kev txhim kho ntawm lub cev. Tsis muaj cov cim ntawm kev tsis txaus siab poj niam fertility tau pom. Cov lus qhia ntxaws ntxiv tseem tsis tau ua tiav, yog li ntawd, tsis txhob rov ua ib qho kev pheej hmoo ntawm leej niam thiab tus menyuam. Nws yog ib qho tseem ceeb uas yuav tsum nco ntsoov tias yog tias muaj kev ua txhaum ntawm cov ntshav qab zib hauv lub cev, nws muaj kev pheej hmoo ntawm lub plab me nyuam hauv plab, thiab qhov kev pheej hmoo ntawm kev tuag thiab cov leeg tsis muaj zog yuav nce ntxiv.

Siv rau lub sijhawm menyuam yaus thiab hnub nyoog laus

Tsis muaj kev paub dhau los ntawm kev noj tshuaj hauv cov neeg mob uas muaj hnub nyoog kaum yim, yog li ntawd nws tsis pom zoo kom suav nrog nws hauv kev kho.

Cov neeg laus dua 65 tsis tas yuav tsum tau muaj kev kho qhov tshwj xeeb thiab kev noj tshuaj rau kev siv cov tshuaj no, tab sis ua ntej siv, koj yuav tsum sab laj nrog tus kws kho mob endocrinologist, tswj xyuas lub siab thiab ob lub raum, thiab saib xyuas cov ntshav qabzib.

Piv nrog analogues

Cov ntsiav tshuaj Galvus muaj ntau cov yeeb yaj kiab, cia peb sim nkag siab lawv qhov zoo thiab qhov tsis zoo.

Lub tshuaj tiv thaiv kab mob "Galvus" yog qhov nrov ntawm cov neeg mob, muaj ntau qhov kev soj ntsuam zoo.

Vladimir, hnub nyoog 43 xyoo: “Kuv noj 50 mg nrog Metformin 500 mg txhua tag kis thiab yav tsaus ntuj tau ob xyoos. Tom qab rau lub hlis ntawm kev siv rau hauv kev ua raws li kev noj haus, qib piam thaj poob rau 4.5. Tsis tas li ntawd, nws muaj peev xwm ua kom poob ceeb thawj. Yog tias ntxov ua rau kuv hnyav txog 123 kg, tam sim no qhov hnyav mus txog 93-95 kg nrog nce li ntawm 178 cm. "

Karina, 32 xyoo: “Txawm hais tias yuav qhuas thiab pom zoo ntau yam ntawm kuv tus kws kho mob, qhov tshuaj tsis haum rau kuv. "Kuv nquag muaj kiv taub hau, tsis muaj zog thiab mob plab thaum siv, yog li kuv yuav tsum tso tseg cov tshuaj."

Svetlana, hnub nyoog 56 xyoo: “Yav dhau los, tus kws kho mob tau qhia Maninil, tab sis nws tsis tuaj, nws tsis tso piam thaj, nws txoj kev noj qab haus huv hnyav zuj zus. Ntxiv rau, Kuv raug kev txom nyem los ntawm teeb meem nrog lub plawv thiab cov hlab ntsha. Tom qab ntawv tus kws kho mob qhia kuv kom sim Galvus. Nws yog yooj yim los noj, tsuas haus ib ntsiav tshuaj ib hnub. Ua tsaug rau nws qhov kev txiav txim, qab zib txo qis kom maj mam thiab maj mam, tsis txhob poob siab, uas yog vim li cas cov kev mob tsis zoo zuj zus. Tam sim no kuv zoo siab, Kuv tuaj yeem txaus siab rau lub neej thiab ua haujlwm dua. "

Tshaj tawm, nws tuaj yeem sau tseg tias Galvus yog ib qho muaj kev nyab xeeb thiab zoo tshaj plaws tshuaj hypoglycemic muaj nyob rau ntawm cov khw muag tshuaj hauv tsev. Cov tshuaj yog qhov tsim nyog rau kev kho mob ntawm hom 2 mob ntshav qab zib mellitus, nws tuaj yeem siv rau kev kho mob sib xyaw, ua ke nrog kev tawm dag zog thiab kev noj zaub mov tshwj xeeb.

INN
Vildagliptin
Dosage daim ntawv
ntsiav tshuaj Pharmacological kev txiav txim

Tus neeg sawv cev hypoglycemic, ib lub zog ua rau lub islet apparatus ntawm lub txiav, tus xaiv inhibitor ntawm enzyme dipeptidyl peptidase-4 (DPP-4).

Cov kev txwv sai thiab ua tiav ntawm DPP-4 kev ua haujlwm (ntau dua 90%) ua rau muaj kev nce ntxiv hauv qhov chaw basal thiab txhawb (kev noj zaub mov) tso tawm ntawm hom 1 glucagon-zoo li peptide thiab qabzib-insulinotropic polypeptide los ntawm cov hnyuv mus rau hauv cov kab ke thoob plaws hnub.

Los ntawm kev nce qib ntawm glucagon-zoo li hom 1 peptide thiab glucose-dependant insulinotropic polypeptide, vildagliptin tsub kom muaj kev cuam tshuam zoo ntawm pancreatic beta hlwb rau cov piam thaj, uas ua rau muaj kev txhim kho hauv cov kua nplaum-insulin secretion.

Thaum siv nyob rau hauv ib koob tshuaj 50-100 mg ib hnub rau cov neeg mob uas muaj hom 2 mob ntshav qab zib mellitus, kev txhim kho hauv kev ua haujlwm ntawm pancreatic beta hlwb raug sau tseg.

Qib ntawm kev txhim kho ntawm kev ua haujlwm ntawm beta hlwb nyob ntawm qib ntawm lawv thawj zaug kev puas tsuaj, yog li nyob rau hauv cov tib neeg tsis raug kev mob ntshav qab zib mellitus (nrog ib qho kev sib xyaw ntawm cov piam thaj hauv cov ntshav plasma), cov tshuaj tsis txhawb kev ua haujlwm ntawm insulin thiab tsis txo qhov kev nyeem ntawm cov piam thaj.

Los ntawm nce qhov kev txiav txim siab ntawm endogenous glucagon-zoo li peptide ntawm hom 1, vildagliptin tsub kom muaj kev cuam tshuam ntawm alpha hlwb rau cov piam thaj, uas ua rau muaj kev txhim kho hauv cov kua nplaum-raws li kev cai ntawm glucagon secretion.

Kev poob qis hauv kev mloog zoo ntawm cov zom zaub mov ntau dua thaum noj mov, nyeg, ua rau muaj kev poob qis hauv cov tshuaj insulin.

Kev nce ntxiv ntawm cov insulin / glucagon piv rau cov keeb kwm ntawm hyperglycemia, vim qhov nce ntawm cov ntsiab lus ntawm glucagon-zoo li peptide ntawm hom 1 thiab glucose-nyob rau hauv cov tshuaj insulinotropic polypeptide cov ntshav qabzib, ua rau muaj qis hauv cov ntshav qabzib los ntawm lub siab (nyob rau lub sijhawm prandial thiab tom qab noj mov), uas ua rau muaj kev txo qis hauv cov ntshav qabzib hauv ntshav plasma.

Nrog rau kev siv vildagliptin, qhov kev txo qis ntawm cov concentration ntawm lipids hauv cov ntshav ntshav tau sau tseg, txawm li cas los xij, cov nyhuv no tsis cuam tshuam nrog nws cov txiaj ntsig ntawm glucagon-zoo li peptide ntawm hom 1 lossis glucose-dependant insulinotropic polypeptide thiab kev txhim kho hauv kev ua haujlwm ntawm pancreatic beta hlwb.

Ib qho kev nce ntxiv ntawm qhov kev coj ua ntawm glucagon-zoo li peptide ntawm hom 1 tuaj yeem ua rau qeeb qeeb ntawm lub plab zom mov, tab sis cov nyhuv no tsis pom nrog kev siv vildagliptin.

Thaum siv vildagliptin li monotherapy lossis hauv kev sib xyaw nrog metformin, sulfonylurea derivatives, thiazolidinedione, lossis insulin, ib qho tseem ceeb ntev ntev txo qis ntawm kev yoo glycosylated Hb thiab kev ntshav sai yog cov lus cim.
Cov Tshuaj Pharmacokinetics

AUC yog ncaj qha sib npaug rau qhov nce hauv kev txhaj tshuaj.

Thaum noj nrog zaub mov, qhov nqus dej poob qis me ntsis, Cmax poob li 19%, TCmax nce txog 2.5 teev, qhov nqus ntawm qhov nqus thiab AUC tsis hloov.

Kev sib txuas lus nrog cov protein yog qhov tsawg - 9.3%. Nws tau faib qhov sib luag ntawm cov ntshav thiab cov ntshav liab. Kev faib khoom ntim (ntawm hauv / hauv kev qhia) - 71 l.

Kev faib khoom muaj peev xwm xav tias yuav ntau heev.

Lub ntsiab ntawm txoj kev nthuav dav yog biotransformation.

69% ntawm cov tshuaj raws tau hloov pauv. Lub ntsiab metabolite - LAY151 (57% ntawm qhov koob tshuaj) yog qhov tsis muaj tshuaj thiab yog ib yam khoom ntawm cov hydrolysis ntawm cov cyano tivthaiv. Txog li 4% ntawm cov koob tshuaj tiv thaiv amide hydrolysis.

Qhov txiaj ntsig zoo ntawm DPP-4 ntawm kev siv hydrolysis ntawm cov tshuaj tau sau tseg.

Vildagliptin tsis yog metabolized nrog kev koom tes ntawm cytochrome P450 isoenzymes thiab tsis yog qhov txheej rau lawv, nws tsis inhibit lossis ntxias lawv.

T1 / 2 - 3h. Nws yog tawm los ntawm lub raum - 85% (suav nrog 23% tsis hloov), los ntawm txoj hnyuv - 15%.

Nrog rau daim siab ua haujlwm ntawm lub cev tsis muaj mob me (5-6 ntsiab lus raws li Child-Pyug) thiab nruab nrab (6-10 cov ntsiab lus raws li Child-Pyug) tom qab siv ib cov tshuaj, txo qis hauv bioavailability 20% thiab 8%, feem.

Hauv kev mob siab rau daim siab tsis zoo (12 lub ntsiab lus raws li Tus Menyuam-Pyug) kev noj qab nyob zoo nce ntxiv 22%. Ib qho nce lossis txo qis hauv qhov ntau ntawm bioavailability, tsis pub dhau 30%, tsis yog qhov tseem ceeb hauv tsev kho mob.

Tsis muaj kev sib txuam ntawm kev tsis ua haujlwm ntawm lub siab ua haujlwm tsis zoo thiab kev siv lub cev muaj peev xwm.

Hauv cov neeg mob uas muaj mob mentsis, nruab nrab, lub cev tsis txaus ua rau lub raum kev ua haujlwm, nrog qhov kawg-qib CRF (ntawm hemodialysis), tau nce Cmax ntawm 8% -66% thiab AUC los ntawm 32% -134%, uas tsis cuam tshuam nrog kev mob hnyav ntawm qhov tsis meej, nrog rau qhov nce ntawm AUC ntawm qhov tsis muaj zog ntawm metabolite. LAY151 1.6-6.7 lub sijhawm, nyob ntawm qhov hnyav ntawm kev ua txhaum. T1 / 2 tsis hloov.

Qhov siab tshaj plaws ntawm kev nyab xeeb tau nce mus txog 32% thiab max dhau los 18% (hauv cov neeg mob laus dua 70 xyoo) tsis yog qhov tseem ceeb hauv chaw kho mob thiab tsis cuam tshuam rau qhov inhibition ntawm DPP-4.
Kev ntsuas rau siv

Hom 2 mob ntshav qab zib mellitus: monotherapy (ua ke nrog kev kho kev noj zaub mov zoo thiab kev tawm dag zog lub cev) thiab kev kho kom sib xyaw (ua ke nrog metformin, sulfonylurea derivatives, thiazolidinedione, insulin) thaum tsis muaj txiaj ntsig kev noj zaub mov zoo, kev tawm dag zog thiab monotherapy ntawm cov tshuaj no.
Cov Yuav Tsum Muaj

Kev kub siab lub cev tsis zoo, qhov ua rau mob hepatic tsis muaj zog (nce ALT thiab AST kev ua si 2.5 zaug siab dua qhov txwv tsis pub tshaj), mob qog lossis mob raum (suav nrog thaum kawg ntawm CRF ntawm hemodialysis), cev xeeb tub, lactation, menyuam yaus (txog 18 xyoo).

Rau Lf muaj cov lactose (yeem): galactose tsis nkag siab, lactase tsis txaus lossis malabsorption ntawm qabzib-galactose.
Kev noj tshuaj ntxiv

Sab hauv, tsis hais txog kev noj zaub mov, nrog kev kho mob monotherapy lossis nrog ob feem sib xyaw nrog kev kho mob nrog metformin, thiazolidinedione lossis insulin - 50 mg / hnub (sawv ntxov) lossis 100 mg / hnub (50 mg thaum sawv ntxov thiab yav tsaus ntuj), nrog ob-txoj kev kho nrog sulfonylurea derivatives - 50 mg / hnub (thaum sawv ntxov), nrog qhov mob hnyav dua ntawm ntshav qab zib mellitus, rau cov neeg mob tau txais kev kho mob insulin - 100 mg / hnub.

Nrog cov tshuaj tsis txaus siv thaum tseem noj 100 mg / hnub, cov tshuaj ntxiv ntawm lwm cov tshuaj hypoglycemic yog ua tau: metformin, sulfonylurea derivatives, thiazolidinedione lossis insulin.

Thaum kws kho mob muab ua ke nrog sulfonylurea derivatives, cov txiaj ntsig ntawm kev kho mob ntawm kev txhaj tshuaj ntawm 100 mg / hnub zoo ib yam li cov koob tshuaj ntawm 50 mg / hnub.
Sab sij huam

Qhov ntau zaus: ntau zaus (1/10 lossis ntau dua), feem ntau (ntau tshaj li 1/100 thiab tsawg dua 1/10), qee zaum (ntau dua 1/1000 thiab tsawg dua 1/100), tsis tshua muaj (ntau tshaj li 1/10000 thiab tsawg dua 1/1000) tsis tshua muaj neeg siv (tsawg dua 1/10000).

Nrog kev kho mob monotherapy: nyob rau ib feem ntawm cov leeg poob siab - feem ntau - kiv taub hau, qee zaum - mob taub hau.

Los ntawm lub plab zom mov: qee zaum - cem quav.

Los ntawm CCC: qee zaum - peripheral edema.

Thaum siv nyob rau hauv ib koob ntawm 50 mg (1-2 zaug hauv ib hnub) hauv kev sib xyaw nrog metformin: ntawm feem ntawm cov leeg ntshaus - feem ntau - kiv taub hau, mob taub hau, tshee tshee.

Thaum siv nyob rau hauv ib koob ntawm 50 mg / hnub hauv kev sib xyaw nrog sulfonylurea derivatives: los ntawm cov leeg poob siab - feem ntau - kiv taub hau, mob taub hau, asthenia, tshee tshee.

Thaum siv hauv ib koob ntawm 50 mg 1-2 zaug hauv ib hnub hauv kev sib xyaw nrog thiazolidinedione derivatives: los ntawm CCC - feem ntau - peripheral edema.

Lwm yam: feem ntau - kev nce hauv lub cev hnyav.

Thaum siv nyob rau hauv ib koob ntawm 50 mg 2 zaug ib hnub nyob rau hauv sib xyaw nrog insulin: los ntawm cov leeg poob siab - feem ntau - mob taub hau.

Los ntawm cov txheej txheem plab zom mov: feem ntau - xeev siab, pom pob, mob plab, plab zom mov.

Los ntawm sab ntawm cov metabolism: feem ntau - hypoglycemia.

Thaum lub sij hawm monotherapy los yog ua ke nrog lwm cov tshuaj, kev phiv tshuaj yog mob me ntsis, ib ntus, thiab tsis tas yuav tshem tawm cov tshuaj. Qhov xwm txheej ntawm tus mob angioedema (tsis tshua tau - ntau tshaj li ntawm 1/10000 thiab tsawg dua 1/1000) zoo ib yam li cov ntawd hauv pawg tswj hwm. Feem ntau, angioedema tau pom thaum ua ke nrog ACE inhibitors, tau mob sib khuav thiab ploj mus nrog kev kho txuas ntxiv.

Kab mob siab Hepatic ua haujlwm tsis zoo (suav nrog rau daim siab mob siab) ntawm chav kawm asymptomatic tsis tshua pom, uas feem ntau tau daws teeb meem ntawm nws tus kheej tom qab tsis kho qhov kev siv tshuaj.
Noj ntau dhau

Cov tsos mob: myalgia, hloov pev hloov pauv ntev, ua npaws, mob edema (suav nrog rau ntu), qhov hloov tshwm sim hauv lipase kev ua si (2 zaug siab dua qhov tsis pub tshaj sab sauv), cov haujlwm nce ntawm CPK, ALT, C-reactive protein thiab myoglobin.

Kev Kho Mob: kev txiav tsis siv tshuaj, kev lim ntshav (kev tshem tawm yeeb tshuaj tsis zoo li, txawm li cas los xij, lub ntsiab ntawm hydrolysis metabolite ntawm vildagliptin (LAY 151) tuaj yeem tshem tawm los ntawm hemodialysis).
Kev sib txuam

Nws muaj qhov qis tsawg rau kev sib txuam tshuaj. Vildagliptin tsis yog lub zog ntawm cytochrome P450 isoenzymes, tsis inhibit lossis induce cov enzymes no, nws cuam tshuam nrog cov tshuaj uas yog cov substrates, inhibitors, lossis inducers ntawm cytochrome P450 tsis zoo li.

Nrog rau kev siv vildagliptin tib lub sij hawm tsis cuam tshuam rau qhov tshuaj ntawm cov tshuaj uas hloov cov isoenzymes CYP1A2, CYP2C8, CYP2C9, CYP2C19, CYP2D6, CYP2E1 thiab CYP3A4 / 5.

Clinically muaj kev sib cuam tshuam nrog cov tshuaj feem ntau siv hauv kev kho mob hom 2 mob ntshav qab zib mellitus (glibenclamide, pioglitazone, metformin) lossis nrog kev kho mob nqaim (amlodipine, digoxin, ramipril, simvastatin, valsartan, warfarin) tsis tau tsim.
Cov lus qhia tshwj xeeb

Muaj qee zaus, thaum ua ntawv thov vildagliptin, qhov kev nce ntawm aminotransferases raug sau tseg (feem ntau tsis muaj kev kuaj mob pom). Ua ntej sau tshuaj thiab thaum thawj xyoo ntawm kev kho mob (1 zaug hauv 3 lub hlis), nws raug nquahu kom txiav txim siab cov kab mob biochemical ntawm lub siab ua haujlwm.

Nrog rau qhov kev nce ntawm aminotransferases, qhov tshwm sim yuav tsum paub tseeb los ntawm kev tshawb nrhiav dua, thiab tom qab ntawd ua ntu zus txiav txim siab biochemical tsis ua haujlwm ntawm daim siab ua haujlwm kom txog thaum lawv ua haujlwm.

Yog tias ib qho dhau ntawm AST lossis ALT kev ua haujlwm yog 3 zaug siab dua qhov kev txwv sab sauv ntawm qhov tsis txaus ntseeg tau lees paub los ntawm kev tshawb fawb zaum ob, pom zoo kom thim cov tshuaj.

Nrog rau kev txhim kho jaundice lossis lwm yam tshwm sim ntawm lub siab ua haujlwm tsis zoo, cov tshuaj yuav tsum tau tsum tam sim ntawd thiab tsis txuas ntxiv tom qab kev ua haujlwm ntawm lub siab ua haujlwm.

Yog tias xav tau cov tshuaj insulin, vildagliptin tsuas yog siv ua ke nrog cov tshuaj insulin.

Cov tshuaj yuav tsum tsis txhob siv rau hom 1 mob ntshav qab zib mellitus lossis rau kev kho mob ntshav qab zib ketoacidosis.

Nyob rau lub sijhawm kho mob (nrog kev loj hlob ntawm kiv taub hau), nws yog ib qho tsim nyog yuav tsum tsis txhob tsav tsheb thiab koom nrog cov kev phom sij uas yuav tsum tau muaj kev xav ntau ntxiv thiab ceev ntawm cov kev tiv thaiv psychomotor.

Kev piav qhia ntawm cov tshuaj nquag Vildagliptin / Vildagliptin.

Cov mis C17H25N3O2, tshuaj lub npe: (S) -1-N- (3-hydroxy-1-adamantyl) glycylpyrrolidine-2-carbonitrile
Pharmacological pawg: metabolites / hypoglycemic hluavtaws thiab lwm tus neeg sawv cev.
Pharmacological kev txiav txim: tshuaj qog ntshav.

Cov chaw muag tshuaj

Vildagliptin stimulates islet apparatus ntawm lub txiav, xaiv yam inhibits dipeptidyl peptidase-4. Ua kom tiav thiab sai ntawm kev ua ntawm dipeptidyl peptidase-4 cov haujlwm ua rau muaj qhov nce ntawm qhov pib thiab qhov ua kom tsis muaj pa ntawm cov kua nplaum-insulinotropic polypeptide thiab glucagon zoo li hom 1 peptide rau hauv cov kab ke ntawm cov hnyuv thoob plaws ib hnub.Los ntawm nce cov ntsiab lus ntawm cov piam thaj-insulinotropic polypeptide thiab hom 1 glucagon-zoo li peptide, vildagliptin tsub kom cov piam thaj muaj txiaj ntsig ntawm pancreatic beta hlwb, uas ua rau muaj kev txhim kho hauv cov kua nplaum-insulin secretion. Qeb kev txhim kho hauv kev ua haujlwm ntawm cov qe ntshav yog nyob ntawm qhov kev puas tsuaj ntawm lawv thawj zaug; hauv cov neeg tsis muaj ntshav qab zib mellitus (nrog cov piam thaj hauv ntshav cov ntshav), vildagliptin tsis txhawb cov tshuaj insulin secretion thiab tsis txo cov ntshav qabzib. Los ntawm nce cov ntsiab lus ntawm endogenous glucagon-zoo li hom 1 peptide, vildagliptin tsub kom muaj kev cuam tshuam ntawm alpha hlwb rau cov piam thaj, qhov no ua rau muaj kev txhim kho hauv cov kua nplaum-raws li kev cai ntawm glucagon excretion. Kev txo qis hauv cov qib glucagon kom tsawg thaum lub caij noj mov ua rau txo qis hauv insulin. Kev nce ntawm cov insulin / glucagon piv hauv hyperglycemia, uas tshwm sim los ntawm kev nce qib ntawm cov piam thaj insulinotropic polypeptide thiab hom 1 glucagon-zoo li peptide, ua rau txo qis rau cov ntshav qabzib los ntawm lub siab ob qho tib si nyob rau lub sijhawm prandial thiab tom qab noj mov, uas ua rau muaj kev txo qis hauv cov ntshav qabzib hauv cov ntshav. Tsis tas li ntawd, thaum siv vildagliptin, cov roj ntsha lipid cov ntsiab lus raug txo qis, tab sis cov nyhuv no tsis cuam tshuam nrog cov nyhuv ntawm vildagliptin ntawm cov kua nplaum-insulinotropic polypeptide thiab glucagon-zoo li hom 1 peptide thiab kev txhim kho hauv kev ua haujlwm ntawm pancreatic beta hlwb.
Vildagliptin thaum muab cov lus hais rau lub ncauj sai sai sai, qhov tiag ntawm bioavailability yog 85%. Nce qhov siab tshaj plaws ntawm vildagliptin hauv ntshav dej thiab thaj chaw raws cov concentration-sijhawm nkhaus yuav luag ncaj qha rau cov kev nce hauv koob tshuaj vildagliptin. Qhov siab tshaj plaws thaum noj cov tshuaj hauv rau ntawm lub plab khoob yog tom qab 1 teev 45 feeb. Thaum noj tshuaj nrog cov zaub mov, tus nqi ntawm nqus ntawm vildagliptin txo qis me ntsis: muaj qhov txo qhov siab tshaj plaws los ntawm 19% thiab nce ntxiv hauv lub sijhawm nws nce mus txog 2.5 teev. Tab sis cov nyhuv ntawm qhov degree ntawm nqus thiab thaj chaw raws nkiag-lub sij hawm nkhaus tsis muaj kev noj mov. Vildagliptin nrog cov plasma protein khi qhov tsis zoo (9.3%). Vildagliptin yog sib luag faib ntawm cov qe ntshav liab thiab ntshav ntshav. Tej zaum, qhov faib tawm ntawm cov tshuaj tshwm sim extravascular, nyob rau hauv sib npaug, qhov ntim ntawm cov faib tawm tom qab kev tswj hwm tshuaj yog 71 liv. Hauv tib neeg lub cev, vildagliptin yog biotransformed 69%. Lub cev metabolite tseem ceeb yog cov tshuaj pharmacologically tsis ua haujlwm LAY151 (57% ntawm qhov koob tshuaj), uas tau tsim thaum lub sij hawm hydrolysis ntawm cov cyano tivthaiv. Txog 4% yauv kuaj amide hydrolysis. Vildagliptin nrog kev koom tes ntawm cytochrome P450 isoenzymes tsis yog metabolized. Vildagliptin tsis yog qhov tsis txaus siab lossis txwv tsis pub cytochrome CYP450 isoenzymes thiab tsis yog qhov khoob ntawm P (CYP) 450 isoenzymes. Thaum noj, kwv yees li 85% ntawm cov tshuaj tawm los ntawm lub raum, 15% raug tso tawm los ntawm txoj hnyuv, tsis hloov pauv (23%) vildagliptin raug nteg tawm los ntawm lub raum. Qhov kev tshem tawm ib nrab-lub neej yog kwv yees li 3 teev thiab tsis nyob ntawm qhov ntau npaum li cas. Tus tub los ntxhais, haiv neeg, thiab lub cev txhais tes tsis muaj kev cuam tshuam cov pharmacokinetics ntawm vildagliptin. Hauv cov neeg mob uas mob mentsis mus rau daim siab tsis ua hauj lwm nrog kev txhaj tshuaj ib zaug, qhov kev txo qis ntawm vildagliptin pom muaj teebmeem txog 20% ​​thiab 8%, feem. Hauv cov neeg mob uas muaj qhov tsis txaus siab rau daim siab hnyav, qhov muaj sia ntawm vildagliptin nce ntxiv txog 22%. Qhov txo qis lossis nce nyob rau hauv lossis ntau qhov yooj yim dua ntawm vildagliptin, uas tsis pub tshaj 30%, tsis yog qhov tseem ceeb hauv tsev kho mob. Hauv cov neeg mob uas muaj mob raum tsawg, mob hnyav thiab lub raum tsis ua haujlwm, hauv cov neeg mob uas mob raum tsis ua haujlwm, kev mob siab rau lub cev tau nce siab tshaj plaws ntawm vildagliptin los ntawm 8 - 66% thiab thaj chaw nyob rau hauv qhov nkhaus-sij hawm nkhaus los ntawm 32 - 134%, uas tsis cuam tshuam nrog qhov loj ntawm qhov kev txhaum ua haujlwm lub xeev ntawm ob lub raum, nrog rau qhov nce ntxiv hauv thaj chaw hauv qhov kev cia siab-lub sijhawm nkhaus ntawm qhov tsis muaj zog metabolite LAY151 hauv 1.6 - 6.7 npaug, uas yog nyob ntawm qhov hnyav ntawm qhov txhaum cai. Hauv qhov no, ib nrab-lub neej ntawm vildagliptin tsis hloov pauv. Hauv cov neeg mob uas muaj 70 xyoo rov hauv, kev siv tshuaj lom neeg lub cev yog qhov siab tshaj plaws ntawm 32% (qhov siab tshaj plaws ntshav ntawm 18%), uas tsis yog qhov chaw kho mob tseem ceeb thiab tsis cuam tshuam qhov inhibition ntawm dipeptidyl peptidase-4. Cov tshuaj pharmacokinetics ntawm vildagliptin hauv cov neeg mob qis dua 18 xyoo tsis tau teeb tsa.

Hom 2 mob ntshav qab zib mellitus ua ib feem ntawm kev kho mob lossis tshuaj kho mob ua ke.

Txoj kev ntawm daim ntawv thov vildagliptin thiab koob tshuaj

Vildagliptin yog noj ntawm qhov ncauj, tsis hais txog kev noj zaub mov. Cov tshuaj ntau npaum li cas ntawm cov tshuaj yog xaiv los ntawm tus kws kho mob ib tus zuj zus, nyob ntawm kev tiv taus thiab ua haujlwm.
Thaum siv vildagliptin, kev nce ntxiv ntawm kev ua si ntawm aminotransferases yog ua tau (feem ntau tsis muaj kev kho mob tshwm sim), nws raug pom zoo los txiav txim siab cov cim biochemical ntawm lub xeev ua haujlwm ntawm daim siab ua ntej nws teem caij, nrog rau xwm yeem thaum thawj xyoo ntawm kev kho mob. Yog tias tus neeg mob tau ua haujlwm ntau dua ntawm aminotransferases, tom qab no qhov txiaj ntsig yuav tsum muaj kev lees paub los ntawm kev tshawb fawb zaum ob, thiab tom qab ntawd ua ntu zus txiav txim siab biochemical cov haujlwm ntawm lub xeev ua haujlwm ntawm lub siab kom txog thaum lawv lub cev. Yog tias qhov kev ua ntawm aminotransferases dhau los ntawm ntau dua peb zaug dhau qhov kev txwv siab tshaj ntawm qhov kev coj ua thiab tau lees paub los ntawm kev tshawb fawb zaum ob, ces vildagliptin yuav tsum tau tso tseg. Nrog kev txhim kho jaundice lossis lwm yam cim ntawm lub siab ua haujlwm tsis zoo, vildagliptin yuav tsum nres tam sim ntawd. Nrog kev ua haujlwm tsis tu ncua ntawm lub xeev kev ua haujlwm ntawm lub siab, vildagliptin tsis tuaj yeem rov ua dua. Vildagliptin yuav tsum tsis txhob siv rau cov neeg mob uas muaj mob ntshav qab zib hom 1, thiab rau kev kho mob ketoacidosis. Nrog rau kev txhim kho kiv taub hau thaum noj cov vildagliptin, cov neeg mob yuav tsum tsis txhob ua haujlwm nrog cov tshuab lossis tsav tsheb.

Cev xeeb tub thiab lactation

Hauv kev sim, thaum noj vildagliptin nyob rau hauv cov koob tshuaj uas yog 200 zaug ntau dua li qhov tau pom zoo, cov tshuaj tsis ua rau kev loj hlob thaum ntxov ntawm menyuam yaus, kev tsis muaj peev xwm thiab tsis dhau qhov kev cuam tshuam teratogenic rau cov menyuam hauv plab. Tsis muaj cov ntaub ntawv txaus ntawm kev siv vildagliptin hauv cov poj niam cev xeeb tub, yog li nws yuav tsum tsis txhob siv thaum cev xeeb tub. Nws tseem tsis tau paub meej tias vildagliptin kis mus rau leej niam cov kua mis, yog li nws yuav tsum tsis txhob siv thaum lactation.

Galvus kev qhia

Muaj pes tsawg leeg
1 tab. muaj cov vildagliptin 50 mg,
tus neeg muaj txiaj ntsig: MCC, anhydrous lactose, sodium carboxymethyl hmoov txhuv nplej siab, magnesium stearate,

Ntim
hauv ib pob ntawm 14, 28, 56, 84, 112 thiab 168 pcs.

Pharmacological kev txiav txim
GALVUS - vildagliptin - ib tus sawv cev ntawm chav kawm ntawm stimulators ntawm insular apparatus ntawm lub txiav, xaiv yam inhibits enzyme dipeptidyl peptidase-4 (DPP-4). Kev txwv sai thiab ua tiav ntawm DPP-4 kev ua haujlwm (> 90%) ua rau muaj kev nce ntxiv ntawm ob qho tib si hauv paus thiab zaub mov zais cia ntawm hom 1 glucagon-zoo li peptide (GLP-1) thiab glucose-tiv thaiv insulinotropic polypeptide (HIP) los ntawm cov hnyuv mus rau hauv cov kab ke rau txhua hnub.
Ua kom ntau ntxiv ntawm GLP-1 thiab HIP, vildagliptin ua rau muaj kev cuam tshuam ntau ntxiv ntawm kev txiav txim siab ntawm pancreatic? Cov cell rau cov piam thaj, uas ua rau muaj kev txhim kho hauv cov kua dej-insulin secretion. Thaum ua ntawv thov vildagliptin ntawm koob tshuaj 50-100 mg / hauv cov neeg mob uas muaj hom 2 mob ntshav qab zib mellitus, kev txhim kho hauv kev ua haujlwm ntawm pancreatic? Qib kev txhim kho ntawm?-Ua haujlwm tau zoo nyob ntawm qhov tsis raug ntawm lawv thawj zaug kev puas tsuaj, yog li ntawm cov neeg tsis mob ntshav qab zib mellitus (nrog cov ntshav qabzib hauv qab), vildagliptin tsis txhawb cov tshuaj insulin secretion thiab tsis txo cov piam thaj.
Los ntawm kev nce qib ntawm cov endogenous GLP-1, vildagliptin tsub kom lub hlwb β-hlwb rau cov kua nplaum ntev, uas ua rau muaj kev txhim kho hauv cov kua nplaum-cov kev cai ntawm glucagon secretion. Kev txo qis hauv cov theem ntawm glucagon ntau dhau ntawm lub sijhawm noj mov, nyeg, ua rau muaj kev poob qis hauv insulin tsis kam.
Kev nce ntxiv ntawm cov insulin / glucagon piv rau cov keeb kwm ntawm hyperglycemia, vim tias qhov nce ntawm GLP-1 thiab HIP, ua rau cov ntshav qabzib ntau zuj zus los ntawm lub siab ob qho tib si nyob rau lub sijhawm prandial thiab tom qab noj mov, uas ua rau txo qis ntshav qabzib ntau ntau.
Tsis tas li ntawd, tawm tsam cov keeb kwm yav dhau los ntawm kev siv vildagliptin, qhov kev txo qis ntawm cov lipids hauv cov ntshav plasma raug sau tseg, txawm li cas los xij, cov nyhuv no tsis cuam tshuam nrog nws cov nyhuv ntawm GLP-1 lossis HIP thiab kev txhim kho ntawm kev ua haujlwm ntawm pancreatic?
Nws paub txog tias kev nce hauv GLP-1 tuaj yeem qeeb plab zom mov, tab sis cov nyhuv no tsis pom nrog kev siv vildagliptin.
Thaum siv vildagliptin nyob rau hauv 5795 cov neeg mob uas muaj ntshav qab zib hom 2 mellitus li 12 txog 52 lub limtiam li monotherapy lossis kev sib xyaw nrog metformin, sulfonylurea derivatives, thiazolidinedione, lossis insulin, qhov tseem ceeb ntev ntev txo qis nyob rau hauv cov concentration ntawm glycated hemoglobin (HbA1c) thiab kev ntshav sai yog qhov tseem ceeb.

Galvus, cim rau kev siv
Yam 2 Ntshav Qab Zib Hom:
- raws li monotherapy nyob rau hauv ua ke nrog kev noj haus txoj kev kho thiab qoj ib ce,
- ua ib feem ntawm ob qho kev sib xyaw ua ke nrog kev kho mob nrog metformin, sulfonylurea derivatives, thiazolidinedione lossis insulin thaum tsis muaj kev noj haus zoo rau kev noj zaub mov zoo, kev tawm dag zog thiab monotherapy nrog cov tshuaj no.

Cov Yuav Tsum Muaj
Kev tsis haum xeeb rau vildagliptin thiab lwm yam hauv Galvus,
cov menyuam yaus hnub nyoog qis dua 18 xyoo (qhov ua tau zoo thiab kev nyab xeeb tsis pom zoo).
Nrog saib xyuas:
kev ua txhaum loj ntawm daim siab, suav nrog cov neeg mob uas muaj kev ua haujlwm ntawm daim siab enzymes ntau dua (ALT lossis AST> 2,5 zaug siab dua qhov kev txwv siab tshaj ntawm ib txwm - 2.5 × VGN),
Mob raum los sis mob raum (nrog rau qhov kawg ntawm CRF ntawm hemodialysis) - kev paub txog kev siv yog tsawg, cov tshuaj tsis pom zoo rau pawg neeg no,
tsis tshua muaj cov kab mob tsis huv - galactose intolerance, lactase deficiency lossis malabsorption ntawm qabzib-galactose.

Tsuas tshuaj thiab tswj hwm
Galvus noj ntawm qhov ncauj, tsis hais txog ntawm kev ua zaub mov.
Cov tshuaj ntau npaum li cas ntawm cov tshuaj yuav tsum tau xaiv ib tus zuj zus nyob ntawm qhov siv tau thiab ua siab ntev.
Qhov pom zoo koob tshuaj ntawm cov tshuaj thaum monotherapy lossis ua ib feem ntawm ob qho kev sib xyaw ua ke nrog kev kho mob nrog metformin, thiazolidinedione lossis insulin yog 50 lossis 100 mg ib hnub ib zaug. Hauv cov neeg mob uas muaj mob ntshav qab zib hom 2 ntau dua uas tau txais kev kho mob insulin, Galvus pom zoo ntawm koob tshuaj 100 mg / hnub.
Ib koob tshuaj 50 mg / hnub yuav tsum yog 1 koob noj thaum sawv ntxov, ib koob tshuaj 100 mg / hnub - 50 mg 2 zaug hauv ib hnub thaum sawv ntxov thiab yav tsaus ntuj.

Cev xeeb tub thiab lactation
Hauv kev sim tshuaj, thaum kho nyob rau hauv cov koob tshuaj 200 zaug ntau dua li kev pom zoo, cov tshuaj tsis ua rau muaj qhov tsis taus thiab kev txhim kho thaum ntxov ntawm lub cev thiab tsis ua qhov cuam tshuam teratogenic rau tus me nyuam hauv plab. Tsis muaj cov ntaub ntawv txaus ntawm kev siv tshuaj Galvus hauv cov poj niam cev xeeb tub, thiab yog li ntawd cov tshuaj yuav tsum tsis txhob siv thaum cev xeeb tub. Thaum muaj teeb meem cov piam thaj hauv kev xeeb tub hauv cov poj niam cev xeeb tub, muaj qhov muaj feem yuav ua mob txhawm rau txhawm rau txhawm rau txhawm rau txhawm rau txhawm rau txhawm rau txhawm rau txhawm rau txhawm rau txhawm rau txhawm rau txhawm rau tuag, thiab ua kom tuag.
Txij li nws tsis paub meej tias vildagliptin nrog niam lub mis tso tawm rau hauv tib neeg, Galvus yuav tsum tsis txhob siv thaum lactation.

Sab sij huam
Thaum siv Galvus raws li kev xav tshuaj lossis ua kom sib xyaw nrog lwm cov tshuaj, feem ntau cov kev phiv tshuaj yog mob me ntsis, ib ntus, thiab tsis tas yuav tsum tsis kho tawm. Tsis muaj qhov sib txheeb ze tau pom ntawm qhov tshwm sim tsis zoo (AE) thiab hnub nyoog, poj niam txiv neej, haiv neeg, sijhawm siv, lossis noj tshuaj ntxiv. Qhov tshwm sim ntawm angioneurotic edema thaum kho nrog Galvus yog ≥1 / 10,000. Tawm tsam keeb kwm ntawm kev kho mob nrog Galvus, kev mob siab rau hepatic (suav nrog mob siab) thiab asymptomatic flow tsis tshua pom. Feem ntau, cov kev ua txhaum thiab kev hloov pauv ntawm daim siab ua haujlwm los ntawm cov cai los daws teeb meem ntawm nws tus kheej yam tsis muaj teeb meem tom qab tsis txiav kev kho mob. Thaum siv cov tshuaj Galvus hauv koob tshuaj 50 mg 1 lossis 2 zaug hauv ib hnub, qhov ntau zaus ntawm kev nce siab hauv kev ua haujlwm ntawm daim siab daim siab (ALT lossis AST ≥3 × VGN) yog 0.2 lossis 0.3%, ntsig txog (piv nrog 0.2% hauv pawg tswj) Cov. Kev nce ntxiv ntawm kev ua haujlwm ntawm daim siab enzymes hauv feem ntau yog asymptomatic, tsis tau nce zuj zus, thiab tsis yog nrog cov kev hloov pauv ntawm cholestatic lossis nqaij tawv.

Cov lus qhia tshwj xeeb
Muaj qee zaus, thaum ua ntawv thov vildagliptin, qhov kev nce ntawm aminotransferases raug sau tseg (feem ntau tsis muaj kev kuaj mob pom). Ua ntej sau tshuaj thiab thaum thawj xyoo ntawm kev kho mob (1 zaug hauv 3 lub hlis), nws raug nquahu kom txiav txim siab cov kab mob biochemical ntawm lub siab ua haujlwm. Nrog rau qhov kev nce ntawm aminotransferases, qhov tshwm sim yuav tsum paub tseeb los ntawm kev tshawb nrhiav dua, thiab tom qab ntawd ua ntu zus txiav txim siab biochemical tsis ua haujlwm ntawm daim siab ua haujlwm kom txog thaum lawv ua haujlwm. Yog tias ib qho dhau ntawm AST lossis ALT kev ua haujlwm yog 3 zaug siab dua qhov kev txwv sab sauv ntawm qhov tsis txaus ntseeg tau lees paub los ntawm kev tshawb fawb zaum ob, pom zoo kom thim cov tshuaj. Nrog rau kev txhim kho jaundice lossis lwm yam tshwm sim ntawm lub siab ua haujlwm tsis zoo, cov tshuaj yuav tsum tau tsum tam sim ntawd thiab tsis txuas ntxiv tom qab kev ua haujlwm ntawm lub siab ua haujlwm. Yog tias xav tau cov tshuaj insulin, vildagliptin tsuas yog siv ua ke nrog cov tshuaj insulin. Cov tshuaj yuav tsum tsis txhob siv rau hom 1 mob ntshav qab zib mellitus lossis rau kev kho mob ntshav qab zib ketoacidosis. Nyob rau lub sijhawm kho mob (nrog kev loj hlob ntawm kiv taub hau), nws yog ib qho tsim nyog yuav tsum tsis txhob tsav tsheb thiab koom nrog cov haujlwm phom sij uas yuav tsum muaj kev xav ntau ntxiv thiab ceev ntawm cov kev tiv thaiv psychomotor.

Yeeb tshuaj sib cuam tshuam
Galvus muaj qhov pheej hmoo tsawg rau kev sib txuam tshuaj. Txij li Galvus tsis yog cov keeb ntawm cytochrome P450 enzymes, tsis yog nws inhibit lossis ntxias cov enzymes no, kev sib cuam tshuam ntawm Galvus nrog tshuaj uas yog cov substrates, inhibitors, lossis inducers ntawm P450 yog qhov tsis zoo. Nrog rau kev siv vildagliptin tib lub sij hawm tseem tsis cuam tshuam rau qhov tshuaj ntawm cov tshuaj uas hloov cov enzymes: CYP1A2, CYP2C8, CYP2C9, CYP2C19, CYP2D6, CYP2E1 thiab CYP3A4 / 5.

Noj ntau dhau
Cov tsos mob thaum siv cov tshuaj ntawm koob tshuaj 400 mg /, cov leeg mob tuaj yeem pom, tsis tshua muaj mob ntsws thiab cov kab mob hloov mus los ntev, ua npaws, edema thiab ib qho kev hloov pauv hauv lipase concentration (2 zaug siab dua VGN). Nrog rau qhov nce ntawm koob Galvus txog rau 600 mg /, kev txhim kho ntawm edema ntawm qhov kawg nrog paresthesias thiab kev nce ntxiv hauv qhov kev coj siab ntawm CPK, ALT, C-reactive protein thiab myoglobin yog tau. Tag nrho cov tsos mob ntawm kev haus ib ce thiab hloov cov kev hloov hauv chaw kuaj ploj tom qab tsis siv tshuaj.
Kev Kho Mob: tshem tawm cov tshuaj ntawm lub cev los ntawm kev lim ntshav yog qhov tsis zoo. Txawm li cas los xij, lub ntsiab hydrolytic metabolite ntawm vildagliptin (LAY151) tuaj yeem tshem tawm hauv lub cev los ntawm hemodialysis.

Cia rau cov neeg mob
Hauv qhov chaw tsaus li ntawm qhov kub thiab txias tsis siab tshaj 25 ° C.