Yanumet (50

Cov ntsiav tshuaj zaj duab xis, 50 mg / 500 mg, 50 mg / 850 mg, 50 mg / 1000 mg.

Ib ntsiav tshuaj muaj

yam tshuaj: citagliptin phosphate monohydrate 64.25 mg (sib npaug rau 50 mg sitagliptin free puag) thiab metformin hydrochloride 500 mg / 850 mg / 1000 mg.

tus zam: microcrystalline cellulose, polyvinylpyrrolidone (povidone), sodium stearyl fumarate, sodium lauryl sulfate, dej lim.

Plhaub muaj pes tsawg leeg rau kev siv tshuaj ntau npaum li 50 mg / 500 mg: Opadry®II Paj Yeeb 85 F94203 (polyvinyl cawv, titanium dioxide (E 171), macrogol / polyethylene glycol 3350, talc, liab hlau oxide (E 172), dub hlau oxide (E 172),

Plhaub muaj pes tsawg leeg rau qhov ntau npaum ntawm 50 mg / 850 mg: Opadry®II Paj Yeeb 85 F94182 (polyvinyl cawv, titanium dioxide (E 171), macrogol / polyethylene glycol 3350, talc, liab hlau oxide (E 172), dub hlau oxide (E 172),

Plhaub muaj pes tsawg leeg rau kev siv tshuaj ntau npaum li 50 mg / 1000 mg: Opadry®II Liab 85 F15464 (polyvinyl cawv, titanium dioxide (E 171), macrogol / polyethylene glycol 3350, talc, liab hlau oxide (E 172), dub hlau oxide (E 172).

50/500 mg ntsiav tshuaj:

Cov tshuaj ntsiav zoo li lub pob, biconvex, npog nrog zaj duab xis npog ntawm lub teeb xim xim, nrog daim ntawv sau npe "575" ntawm ib sab thiab du rau lwm sab.

50/850 mg ntsiav tshuaj:

Cov ntsiav tshuaj zoo li lub pob, biconvex, them nrog cov paj yeeb yaj paj yeeb yaj kiab, nrog cov ntawv sau "515" extruded ntawm ib sab thiab du rau sab nraud.

50/1000 mg ntsiav tshuaj:

Tshuaj ntsiav zoo li lub pob, biconvex, them nrog cov xim xaum zaj duab xis, nrog cov ntawv sau "577" extruded rau ntawm ib sab thiab du rau lwm sab.

Cov chaw muag tshuaj

Cov Tshuaj Pharmacokinetics

Cov kev tshawb fawb txog kev sib npaug ntawm kev noj qab haus huv hauv cov neeg tuaj pab dawb tau pom tias noj Janumet (sitagliptin / metformin hydrochloride) yog qhov sib npaug rau noj sitagliptin phosphate thiab metformin hydrochloride cais. Cov ntaub ntawv hauv qab no qhia txog cov chaw muag tshuaj ntawm cov tshuaj yeeb dej caw.

Kev Tsis Txaus Siab Nrog qhov ncauj ntawm 100 mg, sitagliptin nrawm nrawm thiab nce mus txog qhov siab tshaj plaws plasma ntau ntau (nruab nrab Tmax) tom qab 1-4 teev, thaj chaw nruab nrab hauv qab qhov nkhaus-sijhawm nkhaus ntawm AUC ntawm sitagliptin hauv ntshav yog 8.52 μmol • teev, Cmax 950 nmol Cov. AUC ntawm sitagliptin hauv plasma nce ntxiv hauv kev faib ua feem. Qhov tsis ncaj ncees ntawm bioavailability ntawm sitagliptin yog kwv yees li 87%. Txij li thaum sib txig ua ke ntawm sitagliptin thiab cov zaub mov uas muaj cov ntsiab lus siab rog tsis cuam tshuam rau lub pharmacokinetics ntawm cov tshuaj, sitagliptin tuaj yeem siv tau tsis hais txog kev noj zaub mov. AUC ntawm sitagliptin hauv plasma nce ntxiv hauv kev faib ua feem.

Kev xa Khoom. Qhov ntim nruab nrab ntawm kev faib tawm hauv qhov sib npaug tom qab noj cov tshuaj sitagliptin ntawm koob tshuaj 100 mg yog kwv yees li 198 litres. Tus zauv ntawm sitagliptin thim rov qab khi rau cov ntshav cov ntshav muaj protein tsawg - 38%.

Kev zom zaub mov. Kwv yees li 79% ntawm cov sitagliptin yog cov tsis hloov pauv hauv cov zis. Kev hloov pauv hauv cov tshuaj muaj tsawg heev - txog 16% yog tawm hauv cov qauv metabolites.

Chaw Sau Ntawv. Tom qab qhov ncauj tswj hwm ntawm 14C-daim ntawv lo sitagliptin los ntawm cov neeg ua haujlwm pab noj qab haus huv, 100% cov tshuaj tau tawm hauv 1 lub lis piam nrog quav thiab tso zis ntawm 13% thiab 87%, feem. Qhov kawg ib nrab-lub neej ntawm t½ tom qab qhov ncauj tswj hwm ntawm sitagliptin ntawm ib koob ntawm 100 mg yog kwv yees li 12.4 teev. Sitagliptin accumulates hauv cov nyiaj tsawg tsawg tsuas yog siv rov qab siv dua. Kev kho lub raum tau yog kwv yees li 350 ml / min.

Kev nthuav tawm ntawm sitagliptin yog nqa los ntawm ob lub raum feem ntau los ntawm qhov ua haujlwm ntawm kev ua haujlwm ntawm kev mob hlwb.

Mob ntshav qab zib mellitus. Cov tshuaj pharmacokinetics ntawm sitagliptin hauv cov neeg mob uas muaj hom 2 mob ntshav qab zib mellitus zoo ib yam li cov pharmacokinetics ntawm cov neeg ua haujlwm noj qab haus huv.

Lub raum khiav tsis zoo. Cov ntaub ntawv tshawb fawb ntawm lub khw muag tshuaj ntawm lub koob tshuaj ntawm sitagliptin (50 mg) hauv cov neeg mob uas lub raum tsis ua haujlwm, me me (nrog creatinine tshem tawm KK 50 - 80 ml / min), mob hnyav (KK 30 - 50 ml / min) thiab mob hnyav (KK tsawg dua 30 ml / min) ) mob hnyav heev, ib yam nkaus li ntawm cov neeg mob raum-mob raum uas ua mob hemodialysis, piv nrog cov neeg mob noj qab nyob zoo.

Hauv cov neeg mob uas lub raum lub raum tsis ua haujlwm ntawm qhov mob me, tsis muaj qhov tseem ceeb hauv kev nce ntawm sitagliptin hauv cov ntshav plasma piv nrog pawg tswj hwm ntawm cov neeg ua haujlwm noj qab haus huv. Kev kwv yees kwv yees 2-ntau dua ntawm sitagliptin AUC hauv ntshav tau pom nyob rau hauv cov neeg mob uas tsis tshua mob raum, thiab kwv yees li ntawm 4-npaug ntawm sitagliptin AUC hauv ntshav tau pom nyob hauv cov neeg mob uas mob raum tsis zoo, thiab rau cov neeg mob raum lub raum. leej twg underwent hemodialysis, piv nrog pab pawg tswj hwm ntawm cov neeg ua haujlwm noj qab haus huv. Sitagliptin yog rau qee qhov me me uas tau nthuav dav thaum lub sijhawm hemodialysis (13.5% hauv 3-4 teev hauv kev lim ntshav, uas tau pib 4 teev tom qab noj tshuaj).

Laus lub caij nyoogCov. Hauv cov neeg mob laus (65-80 xyoo), ntshav ntau ntawm sitagliptin yog 19% siab dua ntawm cov neeg mob hluas.

Cov menyuamCov. Kev tshawb fawb txog kev siv cov sitagliptin hauv cov menyuam yaus tsis tau ua.

Tub los ntxhais, haiv neeg, lub cev nyhav (BMI)Cov. Tsis tas yuav hloov qhov tshuaj ntau ntxiv nyob ntawm poj niam txiv neej, haiv neeg lossis BMI. Cov yam ntxwv no tsis muaj kev cuam tshuam loj hauv lub tsev tshuaj pharmacokinetics ntawm sitagliptin.

Kev Tsis Txaus SiabCov. Tom qab qhov ncauj tswj hwm ntawm metformin, tmax tau mus txog tom qab 2.5 teev. Qhov tseeb txog kev noj qab haus huv ntawm metformin, thaum noj 500 ntsiav tshuaj, yog kwv yees li 50-60% hauv cov neeg tuaj noj qab haus huv. Thaum muab cov lus ntawm qhov ncauj, qhov tsis xeb tsis haum yog 20-30% thiab nws tsuas yog tso nrog quav. Cov chaw muag tshuaj ntawm metformin nqus tau yog nonlinear. Thaum siv metformin hauv cov koob tshuaj pom zoo, cov tshuaj muaj zog sib luag tau mus txog hauv 24-48 teev thiab, raws li txoj cai, tsis pub tshaj 1 μg / ml. Hauv kev tswj cov kab mob sib kis, qhov ntshav siab tshaj plaws ntawm metformin (Cmax) tsis pub tshaj 4 μg / ml, txawm tias thaum siv ntau tshaj plaws. Kev tswj hwm ib txhij ntawm cov tshuaj nyob rau hauv ib koob 850 mg nrog zaub mov txo qhov degree thiab tus nqi ntawm kev nqus ntawm metformin, uas tau lees paub los ntawm kev poob qis hauv qhov siab tshaj plaws hauv cov ntshav ntshav los ntawm 40%, qhov txo qis hauv AUC los ntawm 25% thiab kev ncua sijhawm ntawm lub sijhawm kom ncav cuag qhov siab tshaj plaws hauv ntshav ntshav los ntawm 35 feeb. Cov kab mob tseem ceeb hauv kev poob qis no tsis tau paub.

Kev xa Khoom. Plasma protein khi yog negligible. Metformin tau faib rau cov ntshav liab. Qhov siab tshaj plaws hauv cov ntshav yog qis dua ntshav, thiab tau mus txog tom qab kwv yees li lub sijhawm. Cov ntshav liab feem ntau yuav yog qhov tseem ceeb ntawm kev faib tawm. Qhov nruab nrab Vd txawv ntawm 63 - 276 litres.

Kev zom zaub movCov. Metformin ua rau tsis hloov pauv ntawm cov zis.

Chaw Sau NtawvCov. Lub raum tshem tawm ntawm metformin yog> 400 ml / min, cov tshuaj tau tawm los ntawm glomerular pom thiab tubular tso pa tawm. Tom qab qhov ncauj tswj hwm, qhov kev tshem tawm kawg ib nrab-lub neej yog kwv yees li 6.5 teev. Yog tias lub raum tsis ua haujlwm, kev ua kom lub raum txo qis hauv qhov sib piv rau theem ntawm creatinine, qhov txiaj ntsig ntawm qhov uas ib nrab lub neej muaj sia nyob ntev, uas ua rau muaj kev nce ntxiv hauv qib ntawm metformin hauv ntshav ntshav.

Cov Tshuaj Hauv Tshuaj

Yanumet yog kev sib xyaw ntawm ob cov tshuaj hypoglycemic nrog kev sib xyaw ua ke ntawm kev ua: sitagliptin phosphate, dipeptidyl peptidase 4 (DPP-4) inhibitor, thiab metformin hydrochloride, tus sawv cev ntawm chav kawm biguanide, thiab tau tsim los txhim kho glycemic tswj hauv cov neeg mob ntshav qab zib hom 2.

Sitagliptin phosphate enws yog cov nquag, xaiv tau ntau qhov ncauj inhibitor ntawm enzyme dipeptyl peptidase 4 (DPP-4) rau kev kho mob ntshav qab zib hom 2. Cov Tshuaj Hluav Taws Xob (DPP-4) yog chav kawm ntawm cov tshuaj uas ua raws li kev txhim kho zuj zus. Los ntawm inhibiting qhov enzyme DPP-4, sitagliptin tsub kom ntau ntxiv ntawm ob lub zog ua si ntau ntxiv - glucagon-zoo li peptide 1 (GLP-1) thiab glucose-nyob rau insulinotropic polypeptide (HIP). Tus incretins yog ib feem ntawm qhov kev ua haujlwm endogenous koom nrog hauv kev cai lij choj ntawm lub cev ntawm cov ntshav qabzib homeostasis. Tsuas yog nrog qhov ib txwm los yog nce cov ntshav qabzib ntau, GLP-1 thiab HIP nce insulin synthesis thiab nws tso tawm los ntawm pancreatic beta hlwb. GLP-1 kuj tseem txo qis kev zais cia ntawm glucagon los ntawm alc cell pancreatic, ua rau muaj kev txo qis hauv cov ntshav qabzib ntau lawm. Sitagliptin yog qhov muaj zog heev thiab muaj kev xaiv ntau yam ntawm DPP-4 enzyme thiab tsis thaiv cov enzymes DPP-8 lossis DPP-9. Sitagliptin sib txawv hauv nws cov qauv tshuaj thiab cov chaw muag tshuaj los ntawm GLP-1 analogues, insulin, sulfonylureas lossis meglitinides, biguanides, gamma receptor agonists ua haujlwm los ntawm peroxisome proliferator (PPARγ), alpha-glycosidase inhibitors thiab amylin analogues.

Kev siv tib lub sijhawm ntawm sitagliptin thiab metformin muaj ib qho txiaj ntsig ntxiv rau qhov kev siv ntawm GLP-1. Sitagliptin, tab sis tsis muaj metformin, ua rau kom muaj HIP ntau dua.

Sitagliptin txhim kho glycemic tswj ob leeg hauv monotherapy thiab hauv kev sib xyaw nrog lwm cov tshuaj.

Hauv kev sim tshuaj, sitagliptin monotherapy txhim kho glycemic tswj nrog qhov kev txo qis hauv glycated hemoglobin A1c (HbA1c), nrog rau kev yoo mov thiab tom qab noj mov qabzib. Lub lim tiam 3 (qhov kawg ntawm txoj kev yoo ntshav) muaj kev ntshav tsawg nyob rau tom qab. Qhov xwm txheej ntawm cov ntshav qog ntshav qab zib hauv cov neeg mob kho nrog sitagliptin zoo ib yam li cov tshuaj placebo. Lub cev qhov hnyav thaum kho nrog sitagliptin tsis tau nce ntxiv piv rau thawj tus nqi.

Kev ua zoo ntawm beta-cell cov cim ntsuas, suav nrog HOMA-β, proinsulin rau insulin feem ntau thiab beta-cell reactivity qhov ntsuas hauv cov ntshav khov ua rau kev kuaj mob nrog rau kev kuaj ib txwm tau kuj tau pom.

Metformin hydrochloride yog cov biguanide uas muaj cov nyhuv antihyperglycemic, uas txo cov ntshav ntshav qab zib ob leeg ntawm lub plab khoob thiab tom qab noj mov. Cov tshuaj tsis txhawb cov tshuaj insulin secretion thiab vim li ntawd nws tsis ua rau cov ntshav qog ntshav qab zib.

Qhov kev txiav txim ntawm metformin yog sib kho los ntawm peb cov txheej txheem:

txo cov piam thaj hauv cov piam thaj hauv daim siab los ntawm inhibiting gluconeogenesis thiab glycogenolysis,

Txhim kho qhov uptake thiab siv cov piam thaj nyob rau hauv cov ntaub so ntswg peripheral, hauv cov leeg nqaij los ntawm kev ua kom tsis muaj zog txaus insulin,

ua kom qeeb rau kev nqus ntawm cov piam thaj hauv cov hnyuv.

Metformin stimulates intracellular glycogen synthesis los ntawm kev ua yeeb yam ntawm glycogen synthetase, txhim kho cov piam thaj hauv kev thauj los ntawm cov roj ntsha tshwj xeeb (GLUT-1 thiab GLUT-4).

Ntxiv nrog rau cov nyhuv ntshav tsis zoo, metformin muaj cov txiaj ntsig zoo ntawm lipid metabolism. Thaum noj tshuaj, metformin txo qis cov roj (cholesterol) tag nrho, LDL thiab triglycerides.

Kev ntsuas rau siv

Janumet ua ntawv thov rau lnyob rau hauv chav kawm ntawm hom 2 mob ntshav qab zib mellitus, nyob rau hauv ua ke nrog tsis siv tshuaj txoj kev kho cov ntshav cov ntshav qabzib, nrog rau kev sib xyaw nrog lwm cov tshuaj:

Ntxiv rau kev noj haus thiab kev tawm dag zog kom txhim kho glycemic tswj nyob rau hauv cov neeg mob uas tsis muaj peev xwm ua tau ntawm metformin monotherapy ntawm qhov siab tshaj plaws zam, nrog rau cov neeg mob uas twb tau txais kev kho mob nrog kev sib xyaw ntawm sitagliptin thiab metformin.

Hauv kev sib xyaw nrog sulfonylurea derivatives (kev sib xyaw ntawm peb cov tshuaj) ua kev pabcuam ntxiv rau kev noj zaubmov thiab kev tawm dag zog hauv cov neeg mob uas tsis ua tiav glycemic tswj thaum lub sijhawm kho nrog sulfonylurea thiab metformin nyob rau hauv cov tshuaj tiv thaiv tau ntau tshaj plaws.

Ua ke nrog gamma receptor agonists ua kom los ntawm peroxisome proliferator (PPAR-γ) (piv txwv li, thiazolidinedione) (kev sib xyaw ntawm peb cov tshuaj) raws li kev noj haus ntxiv rau kev noj haus thiab kev tawm dag zog rau cov neeg mob uas tsis muaj peev xwm ntawm kev kho nrog metformin thiab PPAR-γ agonist ntawm cov tshuaj tiv thaiv ntau tshaj plaws Cov.

Ua ke nrog cov tshuaj insulin (kev sib xyaw ntawm peb cov tshuaj) ua ib qho kev sib ntxiv rau kev noj haus thiab kev tawm dag zog kom txhim kho glycemic tswj hauv cov neeg mob uas tsis muaj txiaj ntsig ntawm insulin thiab metformin kev kho.

Tsuas tshuaj thiab tswj hwm

Cov koob tshuaj ntawm cov tshuaj Yanumet yuav tsum tau xaiv ib tus zuj zus, suav txog qhov kev kho mob tam sim no, qhov ua tau zoo thiab kev pom zoo hauv tus neeg mob, tsis tshaj qhov siab tshaj qhov pom zoo txhua hnub koob tshuaj sitagliptin - 100 mg.

Thaum tsis muaj cov tshuaj glycemic txaus tswj nrog metformin monotherapy nyob rau hauv qhov siab tshaj plaws zam koob tshuaj. Cov koob tshuaj pom zoo thawj zaug ntawm Yanumet yuav tsum suav nrog koob tshuaj sitagliptin 50 mg 2 zaug hauv ib hnub (txhua hnub koob ntawm 100 mg) thiab koob tshuaj metformin tam sim no.

Thaum hloov los ntawm kev kho mob ua ke nrog sitagliptin thiab metformin. Qhov pib txhaj ntawm Yanumet yuav tsum yog sib npaug rau qhov kev thov siv ntawm sitagliptin thiab metformin.

Thaum tsis muaj cov tshuaj glycemic txaus tswj, metformin ua ke txoj kev kho nyob rau hauv qhov siab tshaj plaws zam koob tshuaj thiab sulfonylurea. Cov koob tshuaj ntawm cov tshuaj Yanumet yuav tsum suav nrog ib koob tshuaj sitagliptin 50 mg 2 zaug ib hnub twg (tag nrho cov koob tshuaj txhua hnub ntawm 100 mg) thiab qhov tshuaj tiv thaiv tam sim no ntawm metformin. Yog tias Janumet raug siv los ua ke nrog sulfonylurea, nws raug nquahu kom txo qis ntawm sulfonylurea kom txo qis kev pheej hmoo ntawm kev mob ntshav qab zib.

Thaum tsis muaj cov tshuaj glycemic txaus, kev sib xyaw ua ke nrog metformin ntawm qhov siab tshaj plaws zam koob tshuaj thiab PPAR-γ agonist. Cov koob tshuaj ntawm cov tshuaj Yanumet yuav tsum suav nrog ib koob tshuaj sitagliptin 50 mg 2 zaug ib hnub twg (tag nrho cov koob tshuaj txhua hnub ntawm 100 mg) thiab qhov tshuaj tiv thaiv tam sim no ntawm metformin.

Thaum tsis muaj cov tshuaj glycemic txaus nrog kev sib xyaw ua ke nrog ob qho tshuaj - insulin thiab metformin hauv qhov siab tshaj plaws zam tau. Cov koob tshuaj ntawm cov tshuaj Yanumet yuav tsum suav nrog ib koob tshuaj sitagliptin 50 mg 2 zaug ib hnub twg (tag nrho cov koob tshuaj txhua hnub ntawm 100 mg) thiab qhov tshuaj tiv thaiv tam sim no ntawm metformin. Thaum siv cov tshuaj Janumet ua ke nrog cov tshuaj insulin, nws yuav tsim nyog los txo cov koob tshuaj insulin los tiv thaiv kev pheej hmoo ntawm hypoglycemia.

Rau qhov yooj yim ntawm cov tshuaj, cov tshuaj Yanumet muaj nyob rau hauv peb qhov ntau thiab tsawg ntawm 50 mg ntawm sitagliptin ntxiv rau 500, 850 lossis 1000 mg ntawm metformin hydrochloride.

Txhua tus neeg mob yuav tsum ua raws li kev noj zaub mov nrog rau kom muaj kev faib raws li cov carbohydrate kom txaus thoob plaws ib hnub. Cov neeg rog rog rog yuav tsum ua raws li cov zaub mov tsis muaj calorie tsawg.

Yanumet yuav tsum siv 2 zaug ib hnub nrog zaub mov noj, maj mam nce cov koob tshuaj, txhawm rau txo cov kev pheej hmoo ntawm phiv los ntawm cov hnyuv txuas nrog metformin.

Cov pab pawg neeg tshwj xeeb

Cov neeg mob raum tsis ua haujlwmCov. Koob tshuaj kom haum nyob rau hauv cov neeg mob uas lub raum tsis ua haujlwm (CC ≥ 60 ml / min) tsis tas yuav. Janumet yuav tsum tsis txhob raug siv rau cov neeg mob uas mob raum lossis mob raum tsis zoo (CC