Cov tshuaj ua piv txwv ntawm cov tshuaj vildagliptin * metformin * (vildagliptin * metformin *)

Tshuaj qhov ncauj hypoglycemic. Vildagliptin - tus sawv cev ntawm chav kawm ntawm kev txhawb nqa ntawm cov twj tsis sib xws ntawm cov leeg nqaij ntawm cov txiav, xaiv yam tshuaj tiv thaiv qhov 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 rau ntau zog ntawm GLP-1 thiab HIP, vildagliptin ua rau muaj kev nkag siab ntau ntxiv ntawm cov pancreatic cells-hlwb rau cov piam thaj, uas ua rau muaj kev txhim kho hauv cov kua dej-npauj insulin secretion.

Thaum siv vildagliptin ntawm koob tshuaj 50-100 mg ib hnub rau cov neeg mob uas muaj hom 2 mob ntshav qab zib mellitus, qhov kev txhim kho ntawm kev ua haujlwm ntawm pancreatic cells-hlwb yog sau tseg. Qeb kev txhim kho ntawm kev ua haujlwm ntawm β-hlwb yog nyob ntawm qhov kev puas tsuaj 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 ntshav qabzib.

Los ntawm kev nce siab ntawm cov endogenous GLP-1, vildagliptin tsub kom lub hlwb α-hlwb rau cov kua nplaum ntev, uas ua rau muaj kev txhim kho hauv cov kua nplaum-raws li 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 qhov sib piv ntawm insulin / glucagon tiv thaiv keeb kwm ntawm hyperglycemia, vim qhov nce ntawm cov ntsiab lus ntawm GLP-1 thiab HIP, ua rau muaj cov suab thaj hauv cov ntshav ntau zuj zus los ntawm lub siab ob qho tib si hauv lub sijhawm prandial thiab tom qab noj mov, uas ua rau txo qis hauv cov concentration ntawm cov piam thaj hauv ntshav ntshav.

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 cells-hlwb.

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.

Thaum kev sib xyaw ntawm vildagliptin thiab metformin tau siv los ua thawj zaug kev kho mob rau cov neeg mob ntshav qab zib hom 2 ntshav qab zib, qhov kev noj tshuaj txo qis hauv HbA1c thiab lub cev hnyav tau pom dhau 24 lub lis piam piv nrog kev kho mob monotherapy nrog cov tshuaj no. Cov neeg mob ntshav qab zib tsawg tsawg nyob rau ob pawg kho mob.

Hauv qhov kev tshawb fawb soj ntsuam siv vildagliptin ntawm koob tshuaj 50 mg ib zaug ib hnub rau 6 lub hlis ntawm cov neeg mob uas muaj ntshav qab zib hom 2 ua ke nrog kev mob raum tsis txaus (GFR> 30 txog 1500 mg) nrog glimepiride (> 4 mg /) Hauv kev sim tshuaj, HbA1c qib kev ntsuas pom tau nce tsawg dua 0.76% (qhov pib - qhov nruab nrab ntawm 8.8%).

Cov Tshuaj Pharmacokinetics

Vildagliptin tau nrawm nrawm los ntawm kev noj nrog lub peev xwm txog ntawm 85%. Hauv kev kho mob ntau npaum li cas, qhov nce ntawm Cmax ntawm vildagliptin hauv ntshav thiab AUC yog yuav luag ncaj qha rau cov feem ntau ntawm cov tshuaj ntau dua.

Tom qab noj rau hauv lub plab khoob, lub sijhawm nce mus txog Cmax ntawm vildagliptin hauv ntshav ntshav yog 1 h 45 min. Nrog kev noj mov nrog kev noj mov ib txhij, kev nqus ntawm cov tshuaj txo qis me ntsis: muaj qhov Cmax raug txo qis li 19% thiab nce ntxiv thaum lub sijhawm nce mus txog 2 teev 30 feeb. Txawm li cas los xij, kev noj mov tsis cuam tshuam rau qib 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. Kev faib tawm ntawm vildagliptin tshwm sim pom tias yog tus mob ntxiv, Vd hauv kev sib luag tom qab kev tswj hwm yog 71 L.

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 cov cyano tivthaiv. Txog 4% ntawm cov koob tshuaj ntawm cov tshuaj undergo 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. Vildagliptin tsis yog qhov tseem ceeb ntawm CYP450 isoenzymes, tsis inhibit thiab tsis ntxias cytochrome P450 isoenzymes.

Tom qab noj cov tshuaj, kwv yees li 85% ntawm cov koob tshuaj yog ua rau lub raum thiab 15% dhau los ntawm txoj hnyuv, lub raum ua rau tsis muaj qhov hloov pauv vildagliptin yog 23%. T1 / 2 tom qab kev tswj hwm ntawm qhov ncauj yog li 3 teev, tsis hais kev noj tshuaj npaum li cas.

Tus poj niam txiv neej, lub cev ua haujlwm ntawm lub cev, thiab haiv neeg tsis muaj kev cuam tshuam cov pharmacokinetics ntawm vildagliptin.

Kev qhia rau kev siv tshuaj GALVUS

Yam 2 Ntshav Qab Zib Hom:

• raws li monotherapy nyob rau hauv ua ke nrog kev noj haus kev tawm dag zog thiab kev tawm dag zog,
• nrog rau cov tshuaj metformin uas yog kev pib siv tshuaj kho mob nrog kev tsis muaj txiaj ntsig ntawm kev noj zaub mov zoo thiab tawm dag zog,
• ua ib feem ntawm ob qho kev sib xyaw ua ke nrog kev kho mob nrog metformin, sulfonylurea derivatives, thiazolidinedione lossis nrog insulin thaum tsis muaj kev noj haus zoo rau kev kho mob, kev tawm dag zog thiab monotherapy nrog cov tshuaj no,
• raws li ib feem ntawm txoj kev kho ua ke peb zaug: hauv kev sib xyaw nrog sulfonylurea derivatives thiab metformin hauv cov neeg mob yav tas los kho nrog sulfonylurea derivatives thiab metformin tiv thaiv keeb kwm ntawm kev noj haus thiab kev tawm dag zog thiab uas tsis tau ua tiav glycemic tswj,
• ua ib feem ntawm txoj kev kho ua ke peb zaug: ua ke nrog insulin thiab metformin hauv cov neeg mob uas tau txais insulin thiab metformin yav dhau los ntawm kev noj haus thiab kev tawm dag zog thiab tus uas tsis ua tiav glycemic tswj tau zoo.

Kev noj tshuaj ntxiv

Galvus noj ntawm qhov ncauj tsis hais txog kev noj 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 lub sij hawm monotherapy lossis ua ib feem ntawm ob qho kev sib xyaw ua ke nrog kev kho mob nrog metformin, thiazolidinedione lossis insulin (ua ke nrog metformin lossis tsis muaj metformin) yog 50 mg lossis 100 mg ib hnub. Hauv cov neeg mob uas muaj mob ntshav qab zib hom 2 ntau dua tau txais kev kho mob nrog insulin, Galvus pom zoo ntawm koob tshuaj 100 mg rau ib hnub.

Qhov pom zoo koob tshuaj Galvus ua ib feem ntawm kev sib xyaw ua ke peb zaug (vildagliptin + sulfonylurea derivatives + metformin) yog 100 mg rau ib hnub.

Ib koob tshuaj ntawm 50 mg rau ib hnub yuav tsum tau muab sau tseg 1 lub tshuaj thaum sawv ntxov. Qhov koob tshuaj 100 mg rau ib hnub yuav tsum tau noj 50 mg 2 zaug hauv ib hnub thaum sawv ntxov thiab yav tsaus ntuj.

Thaum siv raws li ib feem ntawm ob qho kev sib xyaw ua ke nrog kev kho nrog sulfonylurea derivatives, koob tshuaj pom zoo ntawm Galvus yog 50 mg 1 zaug hauv ib hnub thaum sawv ntxov. Thaum muaj kev sib xyaw nrog sulfonylurea derivatives, qhov ua tau ntawm kev siv tshuaj ntawm ib koob ntawm 100 mg rau ib hnub yog zoo ib yam li cov koob tshuaj ntawm 50 mg rau ib hnub. Nrog cov tshuaj tsis txaus ua haujlwm tiv thaiv keeb kwm yav dhau los ntawm kev siv qhov siab tshaj plaws pom zoo txhua hnub koob ntawm 100 mg, rau kev tswj hwm zoo dua ntawm glycemia, cov tshuaj ntxiv ntawm lwm cov tshuaj tiv thaiv ntshav qab zib yog qhov ua tau: metformin, sulfonylurea derivatives, thiazolidinedione lossis insulin.

Hauv cov neeg mob uas tsis muaj teeb meem lub raum thiab lub siab mob lub siab, kev hloov kho ntau yam tsis tas yuav tsum muaj. Hauv cov neeg mob uas muaj mob qog lossis mob hnyav lub raum ua haujlwm (suav nrog cov davhlau ya nyob twg ntawm kev mob raum tsis ua haujlwm ntawm kev mob hlwb), cov tshuaj yuav tsum tau siv ntawm koob tshuaj 50 mg ib hnub ib zaug.

Hauv cov neeg mob laus (> 65 xyoo), tsis muaj kev txhim kho ntawm Galvus dosage regimen yog yuav tsum tau ua.

Txij li thaum tsis muaj kev paub hauv kev siv tshuaj nyob hauv menyuam yaus thiab tub ntxhais hluas hnub nyoog qis dua 18 xyoo, nws tsis pom zoo kom siv cov tshuaj hauv pawg no ntawm cov neeg mob.

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 me ntsis, ib ntus, thiab tsis tas yuav tsum tsis kho tawm. Tsis muaj qhov sib txheeb ze tau pom ntawm qhov ntsuas mob tshwm sim ib zaug thiab lub hnub nyoog, poj niam txiv neej, haiv neeg, sijhawm siv, lossis kev noj tshuaj ntau dua.

Qhov tshwm sim ntawm angioedema thaum kho nrog Galvus yog> 1/10 000, 3 × VGN) yog 0.2% lossis 0.3%, feem (piv nrog 0.2% hauv pawg tswj hwm). Kev nce ntxiv hauv kev ua haujlwm ntawm daim siab enzymes hauv feem ntau muaj asymptomatic, tsis vam meej, thiab tsis nrog cov kev hloov pauv cholestatic lossis nqaij tawv daj.

Kev txiav txim siab qhov ntau zaus ntawm cov kev mob tshwm sim: ntau zaus (> 1/10), feem ntau (> 1/100, 1/1000, 1/10 000, 2,5 zaug siab dua VGN).

Txij li thaum tau paub siv Galvus rau cov neeg mob uas mob raum tsis ua haujlwm ntawm lub raum nyob rau ntawm hemodialysis muaj tsawg, nws raug nquahu tias cov tshuaj tau raug txiav txim nrog kev ceev faj hauv pawg neeg mob no.

Kev siv tshuaj yeeb GALVUS thaum cev xeeb tub thiab lactation

Tsis muaj cov ntaub ntawv txaus ntawm kev siv 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.

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.

Txij li nws tsis paub meej tias vildagliptin raug tawm hauv tib neeg cov mis, Galvus yuav tsum tsis txhob siv thaum lactation.

Cov lus qhia tshwj xeeb

Txij li thaum muaj qee zaus thaum vildagliptin tau siv, qhov kev nce ntawm aminotransferases (feem ntau tsis muaj kev kuaj mob hauv lub sijhawm) tau sau tseg, ua ntej kev teem sijhawm Galvus, zoo li tsis tu ncua thaum thawj xyoo ntawm kev kho mob nrog tshuaj (1 lub sijhawm hauv 3 hlis), nws raug nquahu kom txiav txim siab biochemical tsis ua haujlwm ntawm daim siab ua haujlwm. Yog tias tus neeg mob tau ua haujlwm ntau ntxiv ntawm aminotransferases, qhov txiaj ntsig 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 kev ua haujlwm ntawm AST lossis ALT yog 3 zaug siab dua VGN (raws li kev lees paub los ntawm kev tshawb fawb ntxiv), nws raug nquahu kom thim cov tshuaj.

Nrog rau kev txhim kho jaundice lossis lwm cov cim ntawm lub siab ua haujlwm tsis zoo thaum lub sijhawm 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.

Yog tias tsim nyog, insulin txoj kev kho Galvus tsuas yog siv ua ke nrog insulin. Cov tshuaj yuav tsum tsis txhob siv rau hauv cov neeg mob uas muaj hom 1 mob ntshav qab zib mellitus lossis rau kev kho mob ntshav qab zib ketoacidosis.

Noj ntau dhau

Galvus muaj kev tiv thaiv zoo thaum muab rau ntawm ib koob li 200 mg rau ib hnub.

Cov tsos mob: thaum siv cov tshuaj ntawm ib koob ntawm 400 mg rau ib hnub, mob nqaij yuav pom, tsis tshua muaj, mob ntsws thiab cov kab mob hloov, kub taub hau, o thiab qhov nce ntawm lipase concentration (2 zaug siab dua VGN). Nrog rau qhov nce ntawm koob Galvus txog 600 mg rau ib hnub, kev txhim kho ntawm edema ntawm qhov kawg nrog paresthesias thiab kev nce ntxiv hauv qhov kev coj ua ntawm CPK, ALT, C-reactive protein thiab myoglobin yog ua 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.

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.

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

Qhia txog ntawm cov tshuaj

Vildagliptin * + Metformin * (Vildagliptin * + Metformin *) Yog Qhov - Kws Tshuaj Kho Mob

Cov sib xyaw ua ke ntawm cov tshuaj Vildagliptin * + Metformin * (Vildagliptin * + Metformin *) suav nrog ob tus kab mob hypoglycemic nrog cov txheej txheem sib txawv ntawm cov yeeb yam: vildagliptin, uas yog nyob rau hauv chav kawm ntawm dipeptidyl peptidase-4 inhibitors (DPP-4), thiab metformin (hauv daim ntawv ntawm hydrochloride), uas yog tus sawv cev ntawm Cov. Kev sib xyaw ua ke ntawm cov khoom no tso cai rau koj kom tswj tau cov ntshav qabzib ntau hauv cov neeg mob ntshav qab zib hom 2 rau 24 teev.

Vildagliptin, tus sawv cev ntawm chav kawm ntawm stimulators ntawm insular apparatus ntawm lub txiav, xaiv yam tshuaj tiv thaiv qhov enzyme DPP-4, uas rhuav tshem hom 1 glucagon-zoo li peptide (GLP-1) thiab glucose-dependant insulinotropic polypeptide (HIP). Metformin txo cov khoom nyob hauv qabzib los ntawm daim siab, txo qhov nqus ntawm cov piam thaj hauv qhov hnyuv thiab txo cov tshuaj insulin los ntawm kev txhim kho thiab kev siv cov kua nplaum los ntawm cov ntaub so ntswg.

Metformin tsim tawm cov khoom sib xyaw ua ke glycogen nrog los ntawm kev ua yeeb yam ntawm glycogen synthetase thiab txhim kho cov qabzib thauj los ntawm qee yam cov qog ua rau transporter protein (GLUT-1 thiab GLUT-4).

Kev txwv sai thiab ua tiav ntawm DPP-4 kev ua haujlwm tom qab vildagliptin ua rau muaj kev nce ntxiv hauv ob qho tib si hauv paus thiab zaub mov zais cia ntawm GLP-1 thiab HIP los ntawm cov hnyuv mus rau hauv cov kab ke hauv txhua hnub.

Ua rau kev nce siab ntawm GLP-1 thiab HIP, vildagliptin ua rau muaj kev nkag siab zoo ntxiv ntawm pancreatic cells-hlwb rau cov piam thaj, uas ua rau muaj kev txhim kho hauv cov kua dej-npauj insulin secretion. Qeb kev txhim kho ntawm kev ua haujlwm ntawm β-hlwb yog nyob ntawm qhov kev puas tsuaj ntawm lawv thawj zaug kev puas tsuaj, yog li nyob rau cov tib neeg tsis muaj ntshav qab zib mellitus (nrog ib qho kev sib xyaw ntawm cov piam thaj hauv cov ntshav plasma), vildagliptin tsis txhawb cov tshuaj insulin secretion thiab tsis txo cov ntshav qabzib.

Los ntawm kev nce siab 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-raws li kev cai ntawm glucagon secretion. Kev txo qis hauv cov ntshav qabzib hauv siab tom qab noj mov, nyeg, ua rau muaj kev poob qis hauv cov tshuaj insulin.

Kev nce ntxiv ntawm cov insulin / glucagon piv tiv thaiv cov keeb kwm ntawm hyperglycemia, vim qhov nce ntawm cov concentration ntawm GLP-1 thiab HIP, ua rau muaj kev txo qis ntawm cov ntshav qabzib ntau los ntawm lub siab ob qho tib si thaum thiab tom qab noj mov, uas ua rau muaj kev txo qis hauv cov concentration ntawm cov piam thaj hauv ntshav ntshav.

Tsis tas li ntawd, tawm tsam cov keeb kwm yav dhau los ntawm kev siv vildagliptin, qhov kev txo qis ntawm cov concentration ntawm lipids hauv cov ntshav ntshav tom qab noj mov tau 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 islet hlwb. Nws paub tias kev nce ntxiv ntawm qhov kev nkag siab ntawm GLP-1 tuaj yeem ua rau lub cev qeeb ntawm lub plab, txawm li cas los xij, tiv thaiv keeb kwm ntawm kev siv vildagliptin, cov nyhuv no tsis pom.

Thaum siv vildagliptin hauv 5759 cov neeg mob ntshav qab zib hom 2 mob ntshav qab zib mellitus rau 52 lub lis piam hauv kev kho mob monotherapy lossis hauv 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 ceev cov ntshav qabzib tau raug sau tseg.

Metformin pab kho cov ntshav qabzib nyob hauv cov neeg mob ntshav qab zib hom 2 los ntawm kev txo qis ntshav muaj ntshav qab zib ntau ua ntej thiab tom qab noj mov.

Tsis zoo li sulfonylurea derivatives, metformin tsis ua rau cov ntshav qog ntshav qab zib hauv cov neeg mob ntshav qab zib hom 2 ntshav qab zib lossis cov neeg muaj kev noj qab haus huv (tshwj tsis yog qee kis tshwj xeeb). Kev kho nrog cov tshuaj tsis ua rau kev loj hlob ntawm hyperinsulinemia. Nrog rau kev siv cov metformin, insulin secretion tsis hloov, thaum lub siab ntawm cov kua dej hauv cov ntshav ntawm lub plab khoob thiab thaum nruab hnub nws yuav txo qis.

Nrog rau kev siv cov metformin, muaj txiaj ntsig zoo rau cov metabolism ntawm lipoproteins raug sau tseg: qhov txo qis hauv kev ua tiav ntawm cov roj (cholesterol) tag nrho, cov roj cholesterol ntawm lipoproteins tsawg ntom thiab triglycerides, tsis cuam tshuam nrog cov nyhuv ntawm cov tshuaj ntawm qhov concentration ntawm cov piam thaj hauv ntshav ntshav.

Thaum siv cov kev sib xyaw ua ke nrog vildagliptin thiab metformin hauv koob tshuaj txhua hnub ntawm 1,500-3,000 mg ntawm metformin thiab 50 mg ntawm vildagliptin 2 zaug / hnub rau 1 xyoo, ib qho kev tshawb fawb tseem ceeb txo qis hauv cov ntshav qabzib cov ntsiab lus tau pom (txiav txim los ntawm HbA1c) txo qis thiab nce ntawm qhov feem ntawm cov neeg mob uas txo qis HbA1c concentration tsis yog tsawg dua 0.6-0.7% (piv nrog rau pab pawg neeg ntawm cov neeg mob uas txuas ntxiv tau txais tsuas yog metformin).

Hauv cov neeg mob uas tau txais kev sib xyaw ntawm vildagliptin thiab metformin, qhov kev ntsuas pom hnyav hauv lub cev nyhav piv nrog thawj zaug hauv lub xeev tsis tau pom. 24 lub lis piam tom qab pib kev kho mob, hauv cov pab pawg ntawm cov neeg mob tau txais vildagliptin sib xyaw nrog metformin, muaj kev poob qis hauv systolic thiab diastolic ntshav siab rau cov neeg mob ntshav siab.

Thaum kev sib xyaw ntawm vildagliptin thiab metformin tau siv los ua kev kho mob thaum xub thawj rau cov neeg mob ntshav qab zib hom 2 ntshav qab zib, qhov muaj peev xwm txo qis hauv HbA1c qhov tseem ceeb tau pom dhau 24 lub lis piam piv nrog kev kho tshuaj nrog cov tshuaj no. Cov neeg mob ntshav qab zib tsawg tsawg nyob rau ob pawg kho mob.

Thaum siv vildagliptin (50 mg 2 zaug / hnub) ib txhij nrog / tsis muaj metformin ua ke nrog cov tshuaj insulin (qhov nruab nrab koob tshuaj 41 PIECES) hauv cov neeg mob hauv kev soj ntsuam, HbA1c qhov taw qhia tau tsawg kawg yog qhov tsawg ntawm 0.72% (qhov ntsuas pib, qhov nruab nrab ntawm 8,8%). Qhov xwm txheej ntawm cov ntshav qog ntshav qab zib hauv cov neeg mob kho tau piv rau kev tshwm sim ntawm kev mob ntshav qab zib hauv cov pab pawg placebo.

Thaum siv vildagliptin (50 mg 2 zaug / hnub) ib txhij nrog metformin (> 1500 mg) ua ke nrog glimepiride (> 4 mg ib hnub) hauv cov neeg mob hauv kev soj ntsuam, HbA1c qhov taw qhia tau tsawg zuj zus los ntawm 0.76% (los ntawm qhov nruab nrab ntawm 8,8%) Cov.

Sau cov analogues

Daim ntawv noj tshuaj:

zaj duab xis-ntsiav tshuaj ntsiav tshuaj

1 lub ntim zaj duab xis-txheej muaj:
yam tshuaj: vildagliptin 50.0 mg thiab metformin hydrochloride 500.0 mg, 850.0 mg lossis 1000.0 mg,
tus zam: hyprolose, magnesium stearate, hypromellose, titanium dioxide (E 171), macrogol 4000, talc, daj hlau oxide (E 172).
50 mg + 500 mg zaj duab xis-ntsiav tshuaj ntxiv ntxiv muaj hlau oxide liab (E172)

Kev piav qhia:
Zaj duab xis-coated ntsiav tshuaj. 50 mg + 500 mg: oval ntsiav tshuaj nrog beveled sawv, zaj duab xis-coated, lub teeb daj nrog faint pinkish zas. Ntawm ib sab ntawm lub ntsiav tshuaj yog cim "NVR", nyob rau sab nraud - "LLO".
Cov ntsiav tshuaj ua yeeb yaj kiab, 50 mg + 850 mg: oval ntsiav tshuaj nrog beveled sawv, zaj duab xis-coated daj nrog ib tug tsaus muag greyish zas. Ntawm ib sab ntawm cov ntsiav tshuaj yog cim "NVR", nyob rau sab nraud - "SEH".
Zaj duab xis-coated ntsiav tshuaj. 50 mg + 1000 mg: oval ntsiav tshuaj nrog beveled sawv, zaj duab xis-coated tsaus daj nrog greyish zas. Nyob rau ib sab ntawm cov ntsiav tshuaj sau tias "NVR", nyob rau sab nraud yog "FLO".

Cov Kev Txwv rau txoj kev siv tshuaj GALVUS MET

• lub raum tsis ua hauj lwm los yog lub raum lub raum tsis ua haujlwm: nrog tus nqi tsim cov koob tseem ceeb> 1.5 mg% (> 135 μmol / L) rau txiv neej thiab> 1.4 mg% (> 110 μmol / L) rau cov poj niam,
• muaj mob hnyav nrog kev pheej hmoo ntawm kev tsim muaj lub raum ua haujlwm: lub cev qhuav dej (nrog rau mob raws plab, ntuav), kub taub hau, mob hnyav kis, mob ntawm hypoxia (poob siab, sepsis, mob raum, kab mob ntsws).
• mob plawv thiab mob plawv tsis ua haujlwm, mob myocardial infarction, mob plawv tsis txaus (poob siab),
• ua pa tsis ua hauj lwm
• lub siab ua tsis taus haujlwm,
• mob hnyav lossis mob ntsws metabolic acidosis (suav nrog ketoacidosis uas mob ntshav qab zib ua ke nrog lossis tsis nco qab lawm). Tus kab mob ntshav qab zib ketoacidosis yuav tsum kho tus mob insulin kho,
• lactic acidosis (suav nrog keeb kwm),
• cov tshuaj tsis tau siv 2 hnub ua ntej kev phais mob, radioisotope, kev tshawb nrhiav xoo hluav taws xob nrog kev qhia ntawm cov tshuaj tiv thaiv kab mob thiab tsis pub dhau 2 hnub tom qab lawv tau ua,
• cev xeeb tub
• kev pub mis
• ntshav qab zib hom 1
• haus cawv qaug cawv, qaug cawv lom,
• ua raws li kev noj haus hypocaloric (tsawg dua 1000 kcal / hnub),
• cov me nyuam qis dua 18 xyoo (qhov ua tau zoo thiab kev nyab xeeb ntawm kev siv tsis tau tsim),
• ua kom lub cev tsis haum rau vildagliptin lossis metformin lossis lwm yam tshuaj.

Txij li cov neeg mob uas muaj lub siab ua haujlwm tsis txaus nyob hauv qee kis, lactic acidosis raug sau tseg, uas tej zaum yog ib qho kev phiv tshuaj ntawm metformin, Galvus Met yuav tsum tsis txhob siv rau cov neeg mob siab lossis mob siab rau hepatic biochemical.

Nrog kev ceev faj, nws raug nquahu kom siv cov tshuaj muaj metformin hauv cov neeg mob hnub nyoog tshaj 60 xyoo, zoo li thaum ua haujlwm lub cev hnyav vim qhov muaj feem yuav ua mob lactic acidosis.

Cov chaw muag tshuaj

Cov Tshuaj Hauv Tshuaj
Cov sib xyaw ua ke ntawm cov tshuaj Galvus Met suav nrog ob tus kab mob hypoglycemic nrog cov txheej txheem sib txawv ntawm kev ua: vildagliptin, zwm rau hauv chav kawm ntawm dipeptidyl peptidase-4 inhibitors, thiab metformin (hauv daim ntawv ntawm hydrochloride), tus sawv cev ntawm chav kawm ntawm biguanides. Kev sib xyaw ua ke ntawm cov khoom no tso cai rau koj kom tswj tau cov ntshav qabzib ntau hauv cov neeg mob ntshav qab zib hom 2 hauv 24 teev.

Vildagliptia
Vildagliptin, tus tswvcuab ntawm cov chav kawm ntawm tus yam ntxwv ntawm lub cev tsis muaj zog, insular pancreatic apparatus, xaiv cov tshuaj tiv thaiv kom tsis txhob muaj qhov enzyme dipeptidyl peptidase-4 (DPP-4), uas rhuav tshem hom 1 glucagon-zoo li peptide (GLP-1) thiab glucose-based insulinotropic polypeptide (HIP).
Kev txwv sai thiab ua tiav ntawm DPP-4 cov haujlwm ua rau muaj kev nce ntxiv hauv ob qho tib si hauv paus thiab zaub mov zais cia ntawm GLP-1 thiab HIP los ntawm cov hnyuv mus rau hauv cov kab ke hauv nruab hnub.
Los ntawm kev nce qib ntawm GLP-1 thiab HIP, vildagliptin ua rau muaj kev nkag siab ntau ntxiv ntawm pancreatic cells-hlwb rau cov piam thaj, uas ua rau muaj kev txhim kho hauv cov kua dej-insulin secretion. Qib ntawm kev txhim kho ntawm kev ua haujlwm ntawm cov p-hlwb nyob ntawm qhov tsis raug ntawm lawv thawj zaug kev puas tsuaj, yog li nyob rau cov tib neeg tsis raug 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 muaj kev cuam tshuam ntawm клеток cov hlwb rau cov piam thaj, uas ua rau muaj kev txhim kho hauv cov kua nplaum ntawm 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 tiv thaiv cov keeb kwm ntawm hyperglycemia, vim tias qhov nce ntawm GLP-1 thiab HIP, ua rau kom cov ntshav qabzib ntau zuj zus los ntawm lub siab ob qho tib si thaum 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 txo qis hauv qib ntawm lipids nyob rau hauv cov ntshav ntshav tom qab noj mov tau 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 islet hlwb.
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 hauv 5759 cov neeg mob uas muaj hom 2 mob ntshav qab zib mellitus rau 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 (HbA_1c) thiab yoo ntshav cov kua nplaum.

Metformin
Metformin pab kho cov ntshav qabzib nyob hauv cov neeg mob uas muaj ntshav qab zib hom 2 los ntawm kev txo qis ntshav ntshav khov nyob rau ob qho ua ntej thiab tom qab noj mov. Metformin txo cov khoom nyob hauv qabzib los ntawm daim siab, txo qhov nqus ntawm cov piam thaj hauv qhov hnyuv thiab txo cov tshuaj insulin los ntawm kev txhim kho thiab kev siv cov kua nplaum los ntawm cov ntaub so ntswg. Tsis zoo li sulfanylurea derivatives, metformin tsis ua rau cov ntshav qog ntshav qab zib hauv cov neeg mob ntshav qab zib hom 2 ntshav qab zib lossis hauv cov ncauj lus noj qab haus huv (tshwj tsis yog tshwj xeeb). Kev kho nrog cov tshuaj tsis ua rau kev loj hlob ntawm hyperinsulinemia. Nrog rau kev siv cov metformin, insulin secretion tsis hloov, thaum insulin plasma theem ntawm lub plab khoob thiab thaum nruab hnub yuav tsawg zuj zus.
Metformin tsim cov tshuaj glycogen intracellular synthesis los ntawm kev ua yeeb yam ntawm glycogen synthase thiab txhim kho cov kua nplaum ntxiv los ntawm qee yam cov qog ua rau transporter protein (GLUT-1 thiab GLUT-4).
Thaum siv metformin, muaj txiaj ntsig zoo rau cov metabolism ntawm lipoproteins raug sau tseg: qhov txo qis hauv theem ntawm cov roj (cholesterol) tag nrho, cov roj cholesterol ntawm cov lipoproteins tsawg ntom thiab triglycerides, tsis cuam tshuam nrog cov nyhuv ntawm cov tshuaj ntawm ntshav qabzib concentration.

Vildagliptin + Metformin
Thaum siv kev sib xyaw ua ke ntawm vildagliptin / metformin hauv koob tshuaj txhua hnub ntawm 1,500 - 3,000 mg ntawm metformin thiab 50 mg ntawm vildagliptin rau 1 xyoo, ib qho kev tshawb fawb tseem ceeb txo qis hauv cov ntshav qabzib hauv lub siab tau pom (txiav txim los ntawm HbA txo qis_1c) thiab kev nce ntxiv hauv feem ntawm cov neeg mob uas txo qis HbA_1c ntau npaum li tsawg kawg 0.6-0.7% (piv nrog rau pab pawg ntawm cov neeg mob uas txuas ntxiv kom tau txais tsuas yog metformin).
Hauv cov neeg mob uas tau txais kev sib xyaw ntawm vildagliptin thiab metformin, qhov kev ntsuas pom hnyav hauv lub cev nyhav piv nrog thawj zaug hauv lub xeev tsis tau pom. 24 lub lis piam tom qab pib kev kho mob, hauv cov pab pawg ntawm cov neeg mob tau txais vildagliptin sib xyaw nrog metformin, qhov kev poob qis ntawm systolic thiab diastolic ntshav siab tau muab piv nrog piv rau thawj lub xeev.

Cov khoom txaus nyiam

Yuav ua li cas xaiv txoj cai piv rau
Hauv khw muag tshuaj, tshuaj feem ntau muab faib ua cov lus ua kom sib piv thiab cov duab analogues. Cov txheej txheem ntawm cov lus txhais suav nrog ib los yog ntau qhov kev dhia tshuaj qub uas muaj kev kho lub cev. Los ntawm cov qauv piv txwv yog cov tshuaj uas muaj cov tshuaj sib txawv, tab sis npaj rau kev kho mob ntawm tib cov kab mob.

Qhov sib txawv ntawm cov kis thiab kab mob
Cov kab mob kis tau yog tshwm sim los ntawm cov kab mob, kab mob, hu ua fungi thiab protozoa. Cov chav kawm ntawm kab mob tshwm sim los ntawm cov kab mob thiab cov kab mob feem ntau zoo sib xws. Txawm li cas los xij, kom paub qhov txawv ntawm qhov ua rau tus mob txhais tau tias xaiv qhov kev kho mob zoo uas yuav pab tau sai sai nrog qhov malaise thiab tsis ua mob rau tus menyuam.

Kev ua xua yog qhov ua rau mob khaub thuas
Qee tus neeg tau paub txog qhov xwm txheej uas tus menyuam yaus nyob ntev thiab ntau lub sijhawm muaj tus mob khaub thuas. Cov niam txiv coj nws mus rau cov kws kho mob, ua cov kev xeem, siv tshuaj, thiab vim li ntawd, tus me nyuam twb sau npe nrog kws kho mob raws li feem ntau mob. Qhov tseeb uas ua rau mob ntsws ua pa heev tsis paub meej.

Txoj hlab zis: kho mob chlamydial urethritis
Chlamydial urethritis feem ntau pom muaj nyob ntawm txoj kev siv ntawm urologist. Nws tshwm sim los ntawm tus kab mob intracellular parasite Chlamidia trachomatis, uas muaj cov khoom ntawm ob hom kab mob thiab kab mob, uas feem ntau xav tau cov tshuaj tua kab mob ntev mus rau kev siv tshuaj tua kab mob. Nws muaj peev xwm ua rau tsis muaj qhov mob tshwj xeeb ntawm txoj hlab zis rau txiv neej thiab poj niam.