Cov lus qhia rau kev siv tshuaj Vildagliptin > Kev khomob thiab kev tiv thaiv

Hom 2 mob ntshav qab zib mellitus yog kab mob metabolic uas tsim los ntawm kev ua txhaum ntawm kev cuam tshuam ntawm kev cuam tshuam ntawm cov tshuaj insulin nrog cov cell.

Cov tib neeg muaj qhov ua tsis tau zoo no yuav tsis tuaj yeem tswj cov suab thaj kom zoo los ntawm kev noj zaub mov noj thiab cov txheej txheem tshwj xeeb. Cov kws kho mob sau ntawv rau Vildagliptin, uas ua kom qis thiab ua kom cov piam thaj tsis pub dhau.

Cov ntaub ntawv dav dav, muaj pes tsawg leeg thiab daim ntawv tso tawm

Vildagliptin yog tus sawv cev ntawm chav kawm tshiab ntawm cov tshuaj uas nquag siv hauv kev kho mob ntshav qab zib hom 2. Nws stimulates pancreatic islets thiab inhibits kev ua si ntawm dipeptidyl peptidase-4. Nws muaj cov nyhuv hypoglycemic.

Cov tshuaj muaj peev xwm ua tau raws li kev kho mob tseem ceeb, thiab ua ke nrog lwm cov tshuaj. Nws ua ke nrog sulfonylurea derivatives, nrog thiazolidinedione, nrog metformin thiab insulin.

Vildagliptin yog lub npe thoob ntiaj teb rau cov khoom xyaw nquag. Ntawm kev lag luam pharmacological muaj ob qho tshuaj nrog rau qhov khoom siv no, lawv cov npe lag luam yog Vildagliptin thiab Galvus. Thawj zaug tsuas yog Vildagliptin, qhov thib ob - kev sib xyaw ntawm Vildagliptin thiab Metformin.

Daim ntawv tso tawm: cov ntsiav tshuaj nrog qhov ntau npaum ntawm 50 mg, ntim - 28 daim.

Pharmacodynamics thiab pharmacokinetics

Vildagliptin yog ib yam tshuaj uas cuam tshuam nrog dipeptidyl peptidase nrog kev pom tseeb hauv GLP thiab HIP. Cov tshuaj hormones yog txaws mus rau hauv cov hnyuv li ntawm 24 teev thiab nce ntxiv hauv kev teb rau kev noj zaub mov. Cov tshuaj ntxiv txhim kho kev nkag siab ntawm cov hlwb betta rau qabzib. Qhov no ua rau muaj lub luag haujlwm ntawm kev ua haujlwm ntawm cov piam thaj hauv cov piam thaj ntawm insulin.

Nrog rau kev nce hauv GLP, muaj qhov nce ntxiv hauv kev pom ntawm alpha hlwb rau qab zib, uas ua kom muaj kev ua haujlwm ntawm cov piam thaj hauv kev ua haujlwm ntawm insulin. Muaj ib qho txo qis hauv cov lipids hauv cov ntshav thaum kho. Nrog rau qhov txo hauv glucagon, qhov txo qis hauv insulin kuj tshwm sim.

Cov tshuaj ua kom muaj zog sai sai, nce qib ntawm cov tshuaj hormones hauv cov ntshav tom qab 2 teev .Txoj kab mob protein tsawg tau sau tseg - tsis pub dhau 10%. Vildagliptin yog sib npaug faib ntawm cov qe ntshav liab thiab ntshav ntshav. Qhov siab tshaj plaws tshwm sim tshwm sim tom qab 6 teev. Cov tshuaj zoo dua nqus rau ntawm lub plab khoob, nrog rau cov zaub mov, qhov kev tawm tsam poob qis rau qee yam me me - los ntawm 19%.

Nws tsis ua kom muaj zog thiab tsis ncua isoenzymes, nws tsis yog qhov substrate. Nws muaj nyob hauv ntshav ntshav tom qab 2 teev. Ib nrab-lub neej los ntawm lub cev yog 3 teev, tsis hais noj ntau npaum li cas. Biotransformation yog qhov tseem ceeb ntawm kev nthuav dav. 15% ntawm cov tshuaj tawm hauv cov quav, 85% - los ntawm ob lub raum (hloov pauv 22,9%). Qhov kev xav ntau tshaj plaws ntawm cov tshuaj tau tiav tsuas yog tom qab 120 feeb.

Kev taw qhia thiab contraindications

Qhov tseem ceeb qhia rau kev teem caij yog hom ntshav qab zib 2. Vildagliptin yog qhov kev kho mob tseem ceeb, kev kho ob yam sib xyaw ua ke (nrog kev koom nrog tshuaj ntxiv), thiab peb-txoj kev kho (nrog rau kev koom nrog ntawm ob lub tshuaj).

Hauv thawj kis, kev kho mob yog nqa tawm ua ke nrog kev tawm dag zog lub cev thiab tshwj xeeb xaiv kev noj haus. Yog hais tias monotherapy yog qhov ua tsis muaj txiaj ntsig, ib txoj nyuaj siv nrog kev sib txuam ntawm cov tshuaj hauv qab no: Sulfonylurea derivatives, Thiazolidinedione, Metformin, insulin.

Ntawm cov contraindications yog:

tshuaj intolerance,
lub raum tsis ua hauj lwm zoo,
cev xeeb tub
lactase tsis muaj peev xwm
lub siab ua tsis taus haujlwm,
Cov neeg tsis tau muaj 18 xyoo
lub plawv tsis ua hauj lwm
kev pub mis
galactose intolerance.

Cov lus qhia rau kev siv

Cov ntsiav tshuaj noj ntawm qhov ncauj tsis hais txog kev noj zaub mov. Kev noj tshuaj ntau yog txiav txim los ntawm tus kws kho mob, suav txog tus neeg mob qhov mob thiab kam rau ua rau cov tshuaj.

Cov koob tshuaj pom zoo yog 50-100 mg. Hauv cov ntshav qab zib hom 2 hnyav tshaj plaws, cov tshuaj no tau sau ntawv ntawm 100 mg ib hnub twg. Ua ke nrog lwm cov tshuaj (Thaum muaj ob yam kev kho mob), qhov tshuaj txhua hnub yog 50 mg (1 ntsiav tshuaj). Nrog tsis muaj txiaj ntsig thaum lub sijhawm kho mob, cov koob nce siab txog 100 mg.

Tsis muaj cov ntaub ntawv qhia meej txog kev siv cov tshuaj thaum cev xeeb tub thiab lactation. Yog li no, pawg no yog qhov tsis xav noj raug tshuaj uas nthuav tawm. Kev saib xyuas tshwj xeeb yuav tsum tau saib xyuas hauv cov neeg mob mob siab / mob raum.

Cov tib neeg tsis tau muaj 18 xyoo tsis pom zoo siv cov tshuaj no. Nws tsis raug zoo xav kom tsav tsheb thaum noj tshuaj.

Nrog rau kev siv vildagliptin, ib qho kev nce siab hauv lub siab ua haujlwm hauv lub siab. Lub sijhawm kho mob ntev, nws raug nquahu kom kuaj xyuas biochemical los saib xyuas qhov xwm txheej thiab kev hloov kho tau.

Nrog rau kev nce aminotransferases, nws yog ib qho tsim nyog yuav tau rov qab kuaj cov ntshav. Yog tias qhov ntsuas tau nce ntxiv ntau dua 3 zaug, kev noj tshuaj raug tso tseg.

Phiv thiab haus tshaj

Ntawm qhov ua tau cov nyom tshwm sim:

asthenia
tshee hnyo, kiv taub hau, tsis muaj zog, mob taub hau,
xeev siab ntuav, ntuav, tshwm sim los ntawm leeg mob hlab pas, ua tsis tau pa,
peripheral edema,
pancreatitis
hnyav
kab mob siab
khaus tawv, urticaria,
lwm cov kev tsis haum tshuaj.

Cov tshuaj muaj kev tiv thaiv zoo los ntawm cov neeg mob, cov tshuaj tiv thaiv ib hnub ib zaug yog txog 200 mg rau ib hnub. Thaum siv ntau dua 400 ml, cov hauv qab no yuav tshwm sim: qhov kub thiab txias, o, loog ntawm qhov kawg, xeev siab, tsaus muag. Yog tias cov tsos mob tshwm sim, nws yuav tsum tau yaug lub plab thiab mus nrhiav kev pab kho mob.

Nws tseem muaj peev xwm nce qib C-reactive protein, myoglobin, creatine phosphokinase. Angioedema feem ntau pom thaum ua ke nrog ACE inhibitors. Nrog kev tshem tawm ntawm cov tshuaj, phiv ploj.

Kev sib cuam tshuam txog Yeeb Tshuaj thiab Analogs

Kev muaj peev xwm cuam tshuam ntawm cov vildagliptin nrog lwm cov tshuaj muaj tsawg. Tsis muaj tshuaj tiv thaiv los ntawm cov tshuaj uas feem ntau siv rau kev kho mob ntshav qab zib hom 2 (Metformin, Pioglitazone thiab lwm tus) thiab cov tshuaj nqaim (Amlodipine, Simvastatin).

Ib cov tshuaj tuaj yeem muaj lub npe ua lag luam lossis tib lub npe nrog cov tshuaj nquag. Hauv cov khw muag tshuaj koj tuaj yeem nrhiav Vildagliptin, Galvus. Hauv kev sib txuas nrog contraindications, tus kws kho mob sau cov tshuaj uas zoo sib xws uas pom muaj cov nyhuv kho zoo sib xws.

Cov tshuaj yeeb yaj kiab muaj xws li:

Onglisa (nquag muaj tshuaj saxagliptin),
Januvia (tshuaj - sitagliptin),
Trazenta (tivthaiv - linagliptin).

Tus nqi ntawm Vildagliptin nyob ntawm 760 txog 880 rubles, nyob ntawm cov npoo ntawm lub tsev muag tshuaj.

Cov tshuaj yuav tsum nyob ntawm qhov kub li tsawg kawg 25 degrees hauv qhov chaw qhuav.

Kev xav ntawm cov kws tshaj lij thiab cov neeg mob

Lub tswv yim ntawm cov kws paub thiab tus neeg mob tshuaj txog cov tshuaj feem ntau zoo.

Tawm tsam keeb kwm yav dhau los ntawm kev noj tshuaj hauv cov neeg mob uas muaj ntshav qab zib hom 2, cov nyhuv hauv qab no yog sau tseg:

ceev ceev txo hauv qabzib,
txhim kho qhov ntsuas pom,
yooj yim ntawm kev siv
lub cev hnyav thaum lub sijhawm tshuaj monotherapy tseem zoo li qub,
kev kho nrog nrog los ntawm ib cov nyhuv antihypertensive,
cov kev mob tshwm sim tsawg tsawg,
tsis muaj cov kev mob hypoglycemic thaum noj tshuaj,
normalization ntawm lipid metabolism hauv,
kev ruaj ntseg zoo
txhim kho cov metabolism hauv carbohydrate,
haum rau ntau tus neeg mob kev mob ntshav qab zib hom 2.

Vildagliptin nyob rau hauv chav kawm ntawm kev tshawb fawb tau ua pov thawj kev ua tau zoo thiab muaj qhov ua siab ntev zoo. Raws li kev soj ntsuam cov duab thiab tshuaj ntsuam pom, tsis muaj ib qho mob ntshav qab zib hauv lub cev tau pom thaum lub sijhawm hloov tshuaj.

Vildagliptin yog suav hais tias yog ib qho tshuaj tiv thaiv hypoglycemic zoo, uas tau muab tshuaj rau cov ntshav qab zib hom 2. Nws muaj nyob hauv Daim Ntawv Qhia Npe Tshuaj (RLS). Nws yog ntawv kho raws li kev kho mob monotherapy thiab hauv kev sib xyaw nrog lwm tus neeg sawv cev. Ua raws li cov chav kawm ntawm tus kab mob, cov txiaj ntsig ntawm kev kho mob, cov tshuaj yuav tau ntxiv nrog Metmorphine, sulfonylurea derivatives, insulin. Tus kws kho mob uas tuaj koom yuav sau ntawv noj tshuaj kom yog thiab tshuaj xyuas tus neeg mob lub sijhawm. Feem ntau cov neeg mob ntshav qab zib hom 2 muaj kab mob concomitant. Qhov no ua rau ntau qhov kev xaiv ntawm kev pom cov ntshav zoo zoo-qab zib. Hauv cov xwm txheej zoo li no, insulin yog qhov feem ntau siv los txo cov ntshav qab zib. Txoj kev noj ntau dhau lawm yuav ua rau lub cev ntshav dhia, nce phaus. Tom qab txoj kev tshawb no, nws pom tias kev siv Vildagliptin nrog rau cov tshuaj insulin tuaj yeem ua tiav cov txiaj ntsig zoo. Txoj kev pheej hmoo ntawm kev tsim cov kab mob plawv, ntshav qab zib yog ua kom tsawg, lipid thiab carbohydrate metabolism zoo dua uas tsis muaj qhov hnyav ntxiv.

Frolova N. M., endocrinologist, kws kho mob ntawm qeb siab tshaj plaws

Kuv tau noj Vildagliptin rau ntau tshaj ib xyoos, tus kws kho mob tau sau ntawv rau kuv ua ke nrog Metformin. Kuv txhawj xeeb heev tias thaum kho mob ntev kuv tseem tuaj yeem nce phaus. Tab sis nws rov zoo los ntawm tsuas yog 5 kg rau kuv 85. Ntawm cov kev mob tshwm sim, Kuv qee zaum muaj cem quav thiab xeev siab. Feem ntau, txoj kev kho muab cov nyhuv yam xav tau thiab dhau yam tsis muaj kev cuam tshuam dab tsi.

Olga, hnub nyoog 44 xyoo, Saratov

Cov khoom siv vis dis aus los ntawm Dr. Malysheva txog cov khoom lag luam uas tuaj yeem siv ua ntxiv rau tshuaj rau ntshav qab zib:

Vildagliptin yog cov tshuaj zoo uas txo qis dua cov piam thaj thiab kev ua haujlwm ntawm pancreatic. Nws yuav pab cov neeg mob uas tsis muaj peev xwm ua kom cov ntshav qab zib ib txwm ua los ntawm kev tawm dag zog tshwj xeeb thiab kev noj haus.

Dosage daim ntawv

Ib ntsiav tshuaj muaj

cov tshuaj nquag - vildagliptin 50 mg,

tus zam: microcrystalline cellulose, anhydrous lactose, sodium starch glycolate hom A, magnesium stearate.

Cov ntsiav tshuaj yog dawb mus rau lub teeb daj hauv xim, puag ncig lub cev, nrog lub tiaj tus thiab bevelled, sau nrog "NVR" ntawm ib sab thiab "FB" ntawm lwm sab.

Cov chaw muag tshuaj

Cov Tshuaj Pharmacokinetics

Tom qab noj ntawm lub plab khoob, lub sijhawm nce mus rau Cmax ntawm vildagliptin hauv ntshav plasma yog 1.75 teev. Thaum noj nrog zaub mov, qhov nqus ntawm cov tshuaj tsawg dua me ntsis: muaj Cmax nqis txog 19% thiab nce Tmax mus rau 2.5 teev. Txawm li cas los xij, kev noj mov tsis cuam tshuam dabtsi degree ntawm kev nqus thiab AUC.

Kev khi ntawm vildagliptin rau plasma protein yog tsawg (9.3%). Cov tshuaj no raug muab faib sib luag ntawm cov ntshav ntshav thiab ntshav liab. Vildagliptin kev faib tawm tshwm sim txawm tias yog extravascularly, Vss nyob rau hauv kev sib npaug tom qab iv txhaj yog 71 liv.

Biotransformation yog qhov tseem ceeb ntawm kev zam ntawm vildagliptin. Hauv tib neeg lub cev, 69% ntawm cov tshuaj ntawm cov tshuaj yog 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 cyanocomponent. Txog li 4% ntawm cov koob tshuaj tiv thaiv amide hydrolysis.

Hauv kev sim tshuaj, qhov ua tau zoo ntawm DPP-4 ntawm kev hloov kho cov tshuaj hydrolysis. Vildagliptin tsis yog metabolized nrog kev koom tes ntawm cytochrome P450 isoenzymes. Hauv cov kev tshawb fawb hauv vitro tau ua pov thawj tias vildagliptin tsis inhibit lossis ntxias cytochrome P450 isoenzymes.

Tom qab noj cov vildagliptin uas muaj daim ntawv lo nrog 14C, kwv yees li 85% ntawm cov koob tshuaj tau tawm hauv cov zis, 15% nrog quav. 23% ntawm cov koob tshuaj noj ntawm qhov ncauj yog tawm ntawm lub raum tsis hloov pauv. Thaum muab rau kev noj qab haus huv cov ncauj lus, tag nrho cov ntshav thiab lub raum tshem ntawm vildagliptin yog 41 l / h thiab 13 l / h, feem. Qhov nruab nrab ib nrab-lub neej ntawm cov tshuaj tom qab kev tswj hwm tshuaj yog li 2 teev. Ib nrab-lub neej tom qab kev tswj hwm ntawm qhov ncauj yog li 3 teev thiab tsis nyob ntawm qhov koob tshuaj.

Vildagliptin yog qhov nqus tau sai thiab nws txoj kev xaim ntawm lub qhov ncauj yog 85%. Hauv cov tshuaj kho qhov ntau, qhov siab tshaj plaws ntshav plasma concentration ntawm vildagliptin thiab thaj chaw hauv qab lub plasma qhov siab-sijhawm (AUC) nkhaus yog kwv yees feem ntau ntawm cov koob tshuaj.

Cov pab pawg neeg tshwj xeeb

Tsis muaj qhov sib txawv ntawm cov chaw muag tshuaj ntawm Galvus® ntawm cov txiv neej thiab poj niam cov neeg mob hnub nyoog sib txawv thiab nrog lub cev sib txawv ntawm lub cev (BMI). Lub peev xwm ntawm Galvus® los cuam tshuam kev ua si ntawm dipeptidyl peptidase-4 (DPP-4) kuj tseem tsis yog nyob ntawm tub los ntxhais.

Qhov tos ntawm cov tshuaj pharmacokinetic ntawm cov tshuaj Galvus® ntawm lub cev qhov loj ntawm cov qhab nia tsis tau pom. Lub peev xwm ntawm cov tshuaj Galvus® los txhawm rau txwv kev ua haujlwm ntawm DPP-4 kuj tseem tsis yog nyob ntawm BMI ntawm tus neeg mob.

Lub siab ua haujlwm tsis zoo

Qhov tshwm sim ntawm daim siab ua rau ntawm lub chaw muag tshuaj ntawm Galvus® tau kawm hauv cov neeg mob uas mob me, nruab nrab thiab hnyav daim siab ua haujlwm raws li Child-Pugh (los ntawm 6 cov ntsiab lus rau mob me txog 12 ntsiab lus rau qhov hnyav) piv nrog cov neeg mob lub siab ua haujlwm. Tom qab txhaj tshuaj ib zaug xwb Galvus® (100 mg) hauv cov neeg mob uas tsis tshua muaj mob me me mus rau mob siab rau hepatic, qhov kev txo qis ntawm cov yeeb yaj kiab raug tshuaj tau pom (los ntawm 20% thiab 8%, feem), thaum nyob rau hauv cov neeg mob uas muaj mob hepatic hnyav no ntsuas tau nce los ntawm 22%. Txij li qhov hloov siab tshaj plaws (nce los yog txo qis) hauv kev qhia ntsig txog qhov kev npaj ntawm Galvus® tau txog 30%, qhov txiaj ntsig no tsis tau xav txog qhov tseem ceeb hauv chaw kho mob. Tsis muaj ib qho kev sib txuam ntawm qhov hnyav ntawm lub siab tsis ua hauj lwm thiab qhov loj ntawm qhov tau hloov pauv hauv cov kab ke uas raug rau ntawm Galvus®.

Nws tsis raug nquahu kom muab cov tshuaj Galvus® rau cov neeg mob uas lub siab tsis ua haujlwm, suav nrog rau qee qhov uas ALT lossis AST qhov tseem ceeb tshaj> 3 zaug ntau dua li cov kev txwv sab sauv ntawm ib txwm ua ntej pib kho.

Lub raum khiav tsis zoo

Hauv cov neeg mob uas tsis tshua mob, hnyav, thiab lub raum ua rau lub hlwb tsis zoo, AUC tus nqi ntawm vildagliptin tau nce ntxiv rau qhov nruab nrab 1.4, 1.7, thiab 2 zaug, ntsig txog, piv nrog cov neeg mob uas muaj lub raum ua haujlwm. AUC tus nqi ntawm metabolite LAY151 nce 1.6, 3.2 thiab 7.3 npaug, rau cov metabolite BQS867 tus nqi nce ntxiv thaj tsam li 1.5, 3 thiab 71.4, 2.7 thiab 7.3 zaug hauv cov neeg mob uas tsis mob mob raum thiab kev ua rau lub raum khiav tsis zoo, feem, thaum piv nrog cov neeg ua hauj lwm noj qab haus huv. Hauv cov neeg mob uas mob raum kawg, mob vildagliptin zoo ib yam li raug rau cov neeg mob lub raum tsis ua haujlwm. Qhov siab ntawm LAY151 hauv cov neeg mob raum-mob raum yog kwv yees li 2-3 zaug siab dua ntawm cov neeg mob lub raum tsis ua haujlwm zoo. Hauv cov neeg mob uas lub raum tsis ua hauj lwm lawm, yuav tau txhaj tshuaj (saib Ntu "Dosage thiab Administration").

Kev tshem tawm ntawm vildagliptin los ntawm hemodialysis txwv (3% hauv 3-4 teev ntawm hemodialysis tau ua tiav 4 teev tom qab noj tshuaj).

Pharmacokinetics hauv Cov Neeg Laus

Hauv cov neeg laus kawm (≥70 xyoo) uas tsis muaj lwm yam kab mob, muaj kev nce ntxiv hauv tag nrho cov Galvus® (thaum noj 100 mg ib hnub ib zaug) los ntawm 32% nrog kev nce siab hauv ntshav siab tshaj 18% piv nrog kev noj qab haus huv ntawm tus yau hnub nyoog (18-40 xyoo). Cov kev pauv hloov no tsis muaj qhov tseem ceeb rau lub chaw kuaj mob. Lub peev xwm ntawm cov tshuaj Galvus® los txhawm rau txwv kev ua haujlwm ntawm DPP-4 tsis yog nyob ntawm tus neeg mob lub hnub nyoog nyob rau hauv pawg hnub nyoog kawm.

Pharmacokinetics hauv cov menyuam yaus

Tsis muaj ntaub ntawv hais txog lub khw muag tshuaj ntawm cov tshuaj hauv cov menyuam yaus.

Tsis muaj pov thawj dab tsi cuam tshuam ntawm kev muaj haiv neeg ntawm cov tshuaj pharmacokinetics ntawm Galvus®.

Cov Tshuaj Hauv Tshuaj

Vildagliptin yog tus tswv cuab ntawm chav kawm ntawm stimulators ntawm insulin synthes los ntawm islet hlwb ntawm lub txiav thiab muaj zog xaiv inhibitor ntawm dipeptidyl peptidase-4 (DPP-4), tsim los txhim kho glycemic tswj.Raws li kev txiav txim ntawm DPP-4, qib ntawm endogenous ntau ntxiv rau cov tshuaj hormones GLP-1 (glucagon-zoo li peptide-1) thiab HIP (piam thaj-insulinotropic polypeptide) nce ntxiv ntawm lub plab tas.

Tau txais vildagliptin ua rau muaj kev cuam tshuam sai thiab ua tiav kev ua ntawm DPP-4. Hauv cov neeg mob uas muaj ntshav qab zib hom 2, vildagliptin inhibits qhov kev ua si ntawm enzyme DPP-4 rau 24 teev.

Los ntawm nce endogenous theem ntawm cov cov tshuaj hormones incretin, vildagliptin tsub kom qhov kev hnov mob ntawm cov hlwb ua rau cov piam thaj, uas ua rau cov piam thaj ntau zuj zus ntawm cov kua dej. Vildagliptin hauv ib koob tshuaj txhua txhua hnub ntawm 50-100 mg tseem ceeb txhim kho beta-cell kev ua haujlwm cim hauv cov neeg mob ntshav qab zib hom 2. Kev sib txig ntawm kev txhim kho ntawm kev ua haujlwm ntawm cov qe ntshav yog nyob ntawm thawj theem ntawm qhov tsis taus; hauv cov neeg uas tsis muaj kev mob ntshav qab zib mellitus (qib qabzib hauv qab), vildagliptin tsis txhim kho cov tshuaj insulin thiab tsis txo cov ntshav qabzib.

Los ntawm nce qib ntawm cov endogenous GLP - 1, vildagliptin tsub kom lub hlwb alpha rau cov piam thaj, txhim kho cov ntshav qabzib-tso kom tsawg ntawm glucagon. Nyeg, qhov kev tsuam tsis txaus ntawm cov zaub mov tsis zoo ntawm glucagon nyob rau hauv kev teb rau cov khoom noj ua rau muaj qhov ua kom cov tshuaj insulin tsis kam.

Kev nce qib hauv cov insulin / glucagon piv vim tias muaj cov tshuaj hormones ntau ntxiv thaum lub sijhawm hyperglycemia ua rau cov ntshav qabzib tsawg zuj zus hauv daim siab ua rau lub plab khoob thiab tom qab noj mov, yog li txo cov glycemia.

Ncua kev pawv plab zom mov, uas yog ib qho paub los ntawm kev nce GLP-1, tsis tau pom thaum lub sijhawm kho vildagliptin. Ntxiv rau, nrog kev siv vildagliptin, qhov kev txo qis ntawm lipemia tom qab noj mov tau pom, tsis cuam tshuam nrog lub zog ntawm vildagliptin ntawm kev txhim kho islet muaj nuj nqi.

Kev ntsuas rau siv

Yam 2 Ntshav Qab Zib Hom:

raws li kev kho mob monotherapy nyob rau hauv ua ke nrog kev noj haus thiab kev tawm dag zog, nrog rau cov neeg mob nrog contraindications los kho nrog metformin lossis nws tsis nkag siab,

ua ib feem ntawm kev tiv thaiv ob qho kev sib xyaw ua ke:

nrog metformin hauv cov neeg mob tsis txaus glycemic tswj, txawm hais tias qhov ntau tshaj plaws zam koob tshuaj nrog metformin monotherapy,

nrog sulfonylurea nyob rau hauv cov neeg mob uas tsis txaus glycemic tswj, txawm hais tias qhov ntau tshaj plaws zam koob tshuaj nrog metformin monotherapy thiab hauv cov neeg mob nrog contraindications rau metformin txoj kev kho lossis nws thev tsis tau,

nrog thiazolidinedione hauv cov neeg mob uas tsis muaj glycemic tswj tsis tau zoo thiab hauv cov neeg mob uas tsim nyog rau kev kho thiazolidinedione,

ua ib feem ntawm peb qhov kev sib xyaw ua ke nrog kev kho nrog sulfonylurea thiab metformin, thaum kev noj zaub mov zoo, kev tawm dag zog, thiab kev kho ob yam tsis ua rau muaj kev ua tiav ntawm kev tswj glycemic txaus,

nrog rau cov tshuaj insulin (nrog lossis tsis muaj metformin), thaum kev noj zaub mov zoo, kev tawm dag zog, thiab kev noj tshuaj insulin ruaj khov tsis ua rau muaj kev tswj glycemic txaus.

Tsuas tshuaj thiab tswj hwm

Galvus® tau noj ntawm qhov ncauj tsis hais txog kev noj zaub mov.

Qhov pom zoo koob tshuaj thaum lub sij hawm monotherapy lossis ua ib feem ntawm ob qho kev sib xyaw ua ke nrog kev kho mob nrog metformin, thiazolidinedione lossis ua ib feem ntawm peb ntu kev sib xyaw nrog kev kho nrog sulfonylurea thiab metformin lossis kev sib xyaw nrog insulin, yog 100 mg rau ib hnub, siv thaum 50 mg thaum sawv ntxov thiab 50 mg thaum yav tsaus ntuj.

Raws li ib feem ntawm ob qho kev sib xyaw ua ke nrog kev kho nrog sulfonylurea, koob tshuaj pom zoo ntawm Galvus® yog 50 mg ib hnub ib zaug thaum sawv ntxov. Hauv pawg no ntawm cov neeg mob, ib koob tshuaj 100 mg rau ib hnub tsis ua hauj lwm zoo dua li ib koob tshuaj 50 mg ib hnub twg.

Thaum siv ua ke nrog sulfonylurea, xav txog kev txo qhov koob tshuaj sulfonylurea kom txo qis kev pheej hmoo ntawm kev mob ntshav qab zib.

Tsis txhob siv cov koob tshuaj ntau tshaj 100 mg.

Yog tias tus neeg mob tsis tau noj cov tshuaj kom ncav sijhawm, Galvus® yuav tsum noj sai sai thaum tus neeg mob nco qab qhov no. Tsis txhob siv tshuaj rau ob zaug nyob rau tib hnub.

Qhov kev nyab xeeb thiab muaj txiaj ntsig ntawm vildagliptin yog ib feem ntawm kev sib koom ua ke peb qho kev kho mob nrog metformin thiab thiazolidinedione tsis tau tsim.

Cov ntaub ntawv ntxiv ntsig txog pawg neeg mob tshwj xeeb

Cov neeg laus (≥ 65 xyoo)

Thaum muab tshuaj rau cov neeg laus, cov tshuaj kho tsis tas yuav ua los tau.

Cov neeg mob uas lub raum tsis ua hauj lwm zoo

Kev txhaj tshuaj tsis tas yuav tsum tau txhaj thaum muab tshuaj rau cov neeg mob uas pib lub raum tsis ua haujlwm (nrog creatinine tshem tawm ≥ 50 ml / min). Hauv cov neeg mob uas mob raum tsis txaus lossis lub raum tsis ua haujlwm lossis mob raum thaum kawg, cov koob tshuaj pom zoo Galvus® yog 50 mg ib hnub ib zaug.

Cov neeg mob uas muaj lub siab ua haujlwm tsis zoo

Galvus® yuav tsum tsis txhob raug rau cov neeg mob uas lub siab tsis ua haujlwm, nrog rau cov neeg mob yav tas los kho, nrog kev ua si ntau ntawm alanine aminotransferase (ALT) lossis aspartate aminotransferase (AST)> 3 zaug piv nrog kev txwv siab dua ntawm ib txwm muaj (VGN).

Cov menyuam yaus thiab cov tub ntxhais hluas hnub nyoog qis dua 18 xyoo

Nws tsis pom zoo kom muab tshuaj rau cov menyuam yaus thiab cov hluas hauv qab 18 xyoo. Cov ntaub ntawv hais txog qhov ua tau zoo thiab kev nyab xeeb ntawm kev siv tshuaj Galvus® hauv cov menyuam yaus thiab cov hluas hauv qab 18 xyoo tseem tsis tau muaj.

Sab sij huam

Thaum siv Galvus® raws li kev kho mob monotherapy lossis hauv kev sib xyaw nrog lwm cov tshuaj, feem ntau cov kev phiv tshuaj yog mob sib khuav xwb, ib ntus, thiab tsis tas yuav tsum tsis kho tawm. Tsis muaj qhov sib txheeb ze tau pom ntawm qhov tshwm sim ib ntus ntawm qhov xwm txheej tsis zoo thiab hnub nyoog, poj niam txiv neej, haiv neeg, sijhawm siv, lossis noj tshuaj ntxiv.

Cov kev mob tshwm sim nram qab no yog muab faib los ntawm qhov tshwm sim ntau zaus, nrog rau qhov tshwm sim uas tau pom ua ntej tshaj plaws.

Thaum siv cov tshuajGalvus®raws li monotherapy

Thaum siv Galvus® ntawm koob tshuaj 50 mg 1 zaug / hnub lossis 2 zaug / hnub, qhov ntau zaus ntawm kev txiav tawm ntawm kev kho vim tias muaj kev txhim kho tsis haum (0.2% lossis 0.1%, feem) tsis siab tshaj qhov ntawd hauv pawg placebo (0.6%) lossis tshuaj sib piv ( 0,5%).

Tawm tsam keeb kwm yav dhau los ntawm kev kho mob monotherapy nrog Galvus® ntawm ib koob ntawm 50 mg 1 zaug / hnub lossis 2 zaug / hnub, qhov xwm txheej ntawm cov ntshav qog ntshav tsis tau nce qhov hnyav ntawm tus mob yog 0.5% (2 tus neeg ntawm 409) lossis 0.3% (4 tawm ntawm 1,082), uas piv nrog cov tshuaj kev sib piv thiab cov placebo (0.2%). Thaum siv cov tshuaj Galvus® nyob rau hauv daim ntawv ntawm monotherapy, tsis muaj kev nce hauv lub cev tus neeg mob lub cev qhov hnyav.

Kev soj ntsuam daim siab enzyme

Muaj cov ntaub ntawv tsis tshua muaj tshwm sim ntawm kev ua rau mob hepatic (suav nrog rau daim siab mob siab), uas, raws li txoj cai, yog asymptomatic thiab tsis muaj lub chaw kuaj mob. Raws li cov txiaj ntsig ntawm kev tshawb fawb tau pom, daim siab kev ua haujlwm rov ua haujlwm zoo li qub tom qab tsis ua tiav ntawm kev kho. Ua ntej pib kho nrog Galvus®, nws yog ib qho tsim nyog yuav tau kuaj xyuas lub siab kom ua haujlwm kom paub txog cov txiaj ntsig thawj zaug. Thaum kho nrog Galvus®, lub siab ua haujlwm yuav tsum tau saib xyuas txhua txhua peb lub hlis thaum thawj xyoo thiab kuaj xyuas ntu tom qab. Yog tias tus neeg mob tau ua haujlwm ntau ntxiv ntawm aminotransferases, qhov tshwm sim no yuav tsum tau lees paub los ntawm kev tshawb fawb zaum ob, thiab tom qab ntawd ua ntu zus txiav txim siab cov biochemical tsis ua haujlwm ntawm daim siab ua haujlwm kom txog thaum lawv ua haujlwm. Yog tias qhov haujlwm ntawm AST lossis ALT yog 3 zaug lossis siab dua qhov kev txwv siab dua ib txwm, nws pom zoo kom thim cov tshuaj.

Nrog rau kev muaj lub ntsej muag daj lossis lwm yam cim ntawm lub siab ua haujlwm tsis zoo nrog kev siv Galvus®, kev kho tshuaj yuav tsum nres tam sim ntawd. Tom qab ua lub siab tsis ua hauj lwm qhov ntsuas, kev kho tshuaj tsis tuaj yeem rov ua dua.

Kev soj ntsuam vildagliptin nyob rau hauv cov neeg mob uas ua haujlwm hauv chav kawm qib I-III raws li kev faib tawm ntawm New York Lub Plawv Koom Tes (NYHA) tau qhia tias vildagliptin kev kho mob tsis cuam tshuam rau sab laug ventricular muaj nuj nqi lossis paug tsis zoo tam sim no lub plawv tsis piv nrog placebo. Cov kev tshawb fawb hauv NYHA chav kawm ua haujlwm III cov neeg mob noj vildagliptin muaj tsawg thiab tsis muaj cov txiaj ntsig tiav.

Tsis muaj kev paub dhau los ntawm kev siv vildagliptin hauv kev sim kho mob hauv cov neeg mob nrog cov chav kawm ua haujlwm IV raws li NYHA thiab, yog li ntawd, kev siv cov neeg mob no tsis pom zoo.

Thaum lub sij hawm preclinical toxicological kev tshawb fawb nyob rau hauv nqua ntawm liab, mob txhab rau tawv nqaij, nrog rau cov hlwv thiab kiav txhab, tau sau tseg. Txawm hais tias tsis muaj qhov mob txhab tawv nqaij ntxiv thaum sim tshuaj, nws tsis tshua muaj kev paub txog kev kho cov neeg mob tawv nqaij uas muaj ntshav qab zib. Tsis tas li ntawd, cov ntawv tshaj tawm txog qhov tshwm sim ntawm kev kub ntxhov thiab tawv nqaij ntawm cov tawv nqaij tau txais tom qab lub sijhawm tshaj tawm. Yog li, thaum muab tshuaj rau noj, nws raug nquahu kom cov neeg mob ntshav qab zib yuav soj ntsuam cov tawv nqaij tsis xws li lub hlwv lossis mob txhab.

Kev siv cov vildagliptin yog txuam nrog kev pheej hmoo ntawm kev tsim muaj tus mob ua ke kom tsis txhob mob ntxiv.

Cov neeg mob yuav tsum tau qhia txog cov yam ntxwv ntawm tus yam ntxwv ntawm tus mob pancreatitis.

Yog tias muaj kev ua xyem xyav ntawm pancreatitis, kev siv cov tshuaj yuav tsum tsis ua mus ntxiv, yog tias pom tseeb tias pancreatitis, ces Galvus® txoj kev kho yuav tsum tsis txhob rov ua dua. Kev ceev faj yuav tsum tau siv thaum siv cov tshuaj nyob rau hauv cov neeg mob uas muaj keeb kwm ntawm mob hnyav ua ntej.

Raws li koj paub, sulfonylurea ua rau cov leeg ntshav qib siab. Cov neeg mob noj cov tshuaj vildagliptin ua ke nrog sulfonylurea yog qhov pheej hmoo ntawm kev mob hypoglycemia. Qhov hno txo ntawm sulfonylurea tej zaum yuav tsum tau txhawm rau txo qis kev pheej hmoo ntawm hypoglycemia.

Cov ntsiav tshuaj muaj lactose. Cov neeg mob uas muaj keeb xeeb fructose tsis txaus ntseeg, Lapp lactase deficiency, qabzib malabsorption - galactose yuav tsum tsis txhob siv Galvus®.

Cev xeeb tub thiab lub sijhawm pub mis niam

Tsis muaj cov ntaub ntawv txaus ntawm kev siv Galvus® rau cov poj niam cev xeeb tub. Cov kev tshawb nrhiav tsiaj tau qhia txog kev muaj menyuam yaus thaum siv cov tshuaj tiv thaiv ntau. Peb paub tsis meej tias yuav muaj xwm txheej dabtsi rau tib neeg. Vim tias tsis muaj cov ntaub ntawv qhia txog tib neeg, cov tshuaj yuav tsum tsis txhob siv thaum cev xeeb tub.

Kuj tsis paub meej tias vildagliptin puas tau tawm hauv cov kua mis. Kev tshawb nrhiav tsiaj txhu tau qhia txog tso vildagliptin rau hauv cov mis. Galvus® yuav tsum tsis txhob siv thaum pub mis.

Cov kev tshawb fawb ntawm kev cuam tshuam ntawm Galvus® txog kev muaj me nyuam tsis tau ua.

Cov yam ntxwv ntawm cov nyhuv ntawm cov tshuaj ntawm lub peev xwm tsav tsheb lossis lwm yam kev phom sij uas muaj peev xwm

Cov kev tshawb fawb ntawm cov nyhuv ntawm Galvus® ntawm kev muaj peev xwm tsav tsheb lossis lwm cov txheej txheem tsis tau ua. Nrog rau kev txhim kho kiv taub hau thaum kho nrog cov tshuaj, cov neeg mob yuav tsum tsis txhob tsav tsheb lossis ua haujlwm nrog cov txheej txheem.

Noj ntau dhau

Cov tsos mob thaum siv cov tshuaj ntawm ib koob ntawm 400 mg / hnub, cov leeg mob tuaj yeem pom, tsis tshua muaj, lub ntsws thiab lub cev hloov pauv sai sai, kub taub hau, edema thiab qhov nce ntawm lipase concentration (2 zaug siab dua VGN). Nrog rau qhov nce ntxiv ntawm koob Galvus® txog 600 mg / hnub, kev txhim kho ntawm edema ntawm qhov kawg nrog paresthesias thiab qhov nce ntawm cov concentration 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 nrog hemodialysis 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.