Yanumet (50

Mapiritsi okhala ndi mafilimu, 50 mg / 500 mg, 50 mg / 850 mg, 50 mg / 1000 mg.

Piritsi limodzi lili

ntchito: citagliptin phosphate monohydrate 64.25 mg (wofanana ndi 50 mg sitagliptin maziko oyambira) ndi metformin hydrochloride 500 mg / 850 mg / 1000 mg.

zokopa: microcrystalline cellulose, polyvinylpyrrolidone (povidone), sodium stearyl fumarate, sodium lauryl sulfate, madzi oyeretsedwa.

The Shell zikuchokera Mlingo wa 50 mg / 500 mg: Opadry®II Pink 85 F94203 (mowa wa polyvinyl, titanium dioxide (E 171), macrogol / polyethylene glycol 3350, talc, red iron oxide (E 172), iron ironideide (E 172),

Ma Shell amapanga mlingo wa 50 mg / 850 mg: Opadry®II Pink 85 F94182 (mowa wa polyvinyl, titanium dioxide (E 171), macrogol / polyethylene glycol 3350, talc, red iron oxide (E 172), iron ironideide (E 172),

Ma Shell amapanga mlingo wa 50 mg / 1000 mg: Opadry®II Red 85 F15464 (mowa wa polyvinyl, titanium dioxide (E 171), macrogol / polyethylene glycol 3350, talc, red iron oxide (E 172), iron ironideide (E 172).

50/500 mg mapiritsi:

Mapiritsi okhala ndi mawonekedwe a Capsule, biconvex, wokutidwa ndi chikuto cha filimu ya mtundu wa pinki wopepuka, cholembedwa "575" mbali imodzi ndi yosalala mbali inayo.

50/50 mg mapiritsi:

Mapiritsi okhala ndi mawonekedwe a Capsule, biconvex, wokutidwa ndi chithunzi cha pinki, ndipo mawu olembedwa "515" adawoneka mbali imodzi ndi osalala mbali inayo.

50/1000 mg mapiritsi:

Mapiritsi okhala ndi mawonekedwe a Capsule, biconvex, wokutidwa ndi chimbale chofiyira chofiyira, cholembedwa "577" chokhala mbali imodzi ndi yosalala mbali inayo.

Mankhwala

Pharmacokinetics

Kafukufuku wokhudzana ndi bioequivalence mwa odzipereka athanzi apeza kuti kutenga Janumet (sitagliptin / metformin hydrochloride) ndi bioequivalent pakutenga sitagliptin phosphate ndi metformin hydrochloride padera. Zotsatirazi zikuwonetsa kuchuluka kwa zinthu za pharmacokinetic pazomwe zimagwira.

Mafuta Ndi kamlomo kamlomo ka 100 mg, sitagliptin amatengeka mwachangu ndikufika pazokwanira za plasma wozungulira (Median Tmax) pambuyo pa maola 1 mpaka 4, dera lalitali lomwe limayang'aniridwa ndi AUC ya sitagliptin mu plasma ndi 8.52 μmol • ola, Cmax 950 nmol . AUC ya sitagliptin mu plasma imawonjezeka molingana ndi mlingo. Mtheradi bioavailability wa sitagliptin pafupifupi 87%. Popeza kudya kwa munthawi yomweyo kwa sitagliptin ndi chakudya chamafuta ambiri sizimakhudza ma pharmacokinetics a mankhwalawa, sitagliptin angagwiritsidwe ntchito mosasamala kanthu za kudya. AUC ya sitagliptin mu plasma imachulukana molingana ndi mlingo.

Kugawa. Pafupifupi kuchuluka kwa magawidwe ofanana pakatha kumwa kwa sitagliptin pa 100 mg ndi pafupifupi malita 198. Gawo la sitagliptin limasinthiratu ndi mapuloteni amadzi a m'madzi ochepa - 38%.

Kupenda. Pafupifupi 79% ya sitagliptin amachotsedwa mu mkodzo. Kusintha kwa kagayidwe kachakudya ka mankhwala ndi kochepa - pafupifupi 16% amachikonza mu ma metabolites.

Kuswana. Pambuyo pakukonzekera kwa pakamwa kwa 14C olembedwa kuti sitagliptin ndi odzipereka athanzi, pafupifupi 100% ya mankhwalawa adachotsedwa sabata limodzi ndi ndowe ndi mkodzo wa 13% ndi 87%, motero. Hafu yotsiriza ya t½ pambuyo pakamwa pakuyamwa kwa sitagliptin pa 100 mg ndi pafupifupi maola 12.4. Sitagliptin imadziunjikira ndalama zochepa pokhapokha ngati imagwiritsidwa ntchito mobwerezabwereza. Kuchotsera penipeni pafupifupi 350 ml / min.

The excretion ya sitagliptin imachitika makamaka ndi impso ndi limagwirira yogwira canalicitic secretion.

Matenda a shuga. Ma pharmacokinetics a sitagliptin mwa odwala omwe ali ndi matenda a shuga 2 amakhala ofanana ndi pharmacokinetics a odzipereka athanzi.

Matenda aimpso. Kafukufuku wofufuza pa pharmacokinetics ya mlingo wa sitagliptin (50 mg) mwa odwala omwe ali ndi vuto la impso, wofatsa (ndi creatinine chilolezo cha KK 50 - 80 ml / min), modekha (KK 30 - 50 ml / min) komanso wamkulu (KK osakwana 30 ml / min ) kuuma, komanso kwa odwala omwe ali ndi vuto la impso omwe akudwala hemodialysis, poyerekeza ndi odwala athanzi.

Odwala omwe ali ndi vuto laimpso kuwonda kwambiri, panalibe kuwonjezeka kwakukulu kwazovuta za sitagliptin m'madzi a m'magazi poyerekeza ndi gulu la oyang'anira odzipereka athanzi. Kuwonjezeka kwapafupipafupi kwa 2-pilgliptin AUC mu plasma kunawonedwa mwa odwala omwe amachepetsa mphamvu ya aimpso, ndipo kuwonjezeka kofikira kanayi kwa ezinegliptin AUC mu plasma kumawonekera kwa odwala omwe ali ndi vuto laimpso, komanso kwa odwala omwe ali ndi vuto la impso. omwe adakumana ndi hemodialysis, poyerekeza ndi gulu loyang'anira odzipereka athanzi. Sitagliptin akufotokozedwa pang'ono pa hemodialysis (13.5% mu gawo lachiyeneretso la maola atatu, lomwe linayamba maola 4 atatha kumwa mankhwalawa.

Ukalamba. Odwala okalamba (zaka 65-80), kuchuluka kwa plasma kwa sitagliptin ndi 19% okwera kuposa odwala ang'onoang'ono.

Ana. Kafukufuku wokhudza kugwiritsa ntchito sitagliptin mwa ana sanachitike.

Jenda, mtundu, index yam'mimba (BMI). Palibe chifukwa chosinthira mlingo wa mankhwalawa kutengera jenda, mtundu kapena BMI. Makhalidwewa sanakhale ndi chiwonetsero chamadokotala kwambiri pa pharmacokinetics ya sitagliptin.

Mafuta. Pambuyo pakukonzekera kwa metformin, tmax imatheka pambuyo maola 2,5. Mtheradi wa bioavailability wa metformin, mutamwa piritsi ya 500 mg, ndi pafupifupi 50-60% mwa odzipereka athanzi. Mukaperekedwa pakamwa, kachidutswa kosagwiritsa ntchito ndi 20-30% ndipo amachotsa ndowe. The pharmacokinetics of metformin mayamwa ndi nonlinear. Mukamagwiritsa ntchito metformin mu Mlingo wolimbikitsidwa, kutsata koyenera kumafikiridwa mkati mwa maola 24-48 ndipo, monga lamulo, musapitirire 1 μg / ml. M'mayeso azachipatala olamulidwa, kuchuluka kwa ma plasma ambiri a metformin (Cmax) sikunapitirire 4 μg / ml, ngakhale mutagwiritsa ntchito Mlingo waukulu. The munthawi yomweyo kutumikiridwa kwa mankhwala muyezo wa 850 mg ndi chakudya kumachepetsa digiri ndi kuchuluka kwa mayamwidwe a metformin, komwe kumatsimikiziridwa ndi kuchepa kwa ndende yayikulu mu plasma yamagazi ndi 40%, kuchepa kwa AUC ndi 25% komanso kutalika kwa nthawi kuti ifikire kuchuluka kwazowonjezereka m'madzi a m'magazi ndi mphindi 35. Kukula kwakumenekedwe ka kuchepa kumeneku sikudziwika.

Kugawa. Kumanga kwa mapuloteni a Plasma ndikosatheka. Metformin imagawidwa m'magazi ofiira. Kuchulukitsa kwambiri m'magazi kumakhala kocheperachepera mu plasma, ndipo kumafikira pakapita nthawi yofanana. Maselo ofiira ndi gawo limodzi lachigawikacho. Vd wapakati imasiyanasiyana pakati pa malita 63 - 276.

Kupenda. Metformin imachotsedwa mu mkodzo osasinthika.

Kuswana. Kuvomerezeka kwa aimpso kwa metformin ndi> 400 ml / min, mankhwalawa amachotseredwa ndi kusefera kwa khungu ndi kubisalira kwa tubular. Pambuyo pakamwa, kutsirizika kwa theka la moyo ndi pafupifupi maola 6.5. Pankhani ya kuwonongeka kwa impso, kutsekeka kwa impso kumatsika molingana ndi kuchuluka kwa creatinine, chifukwa chomwe theka la moyo limatenga nthawi yayitali, zomwe zimabweretsa kuwonjezeka kwa mulingo wa metformin m'madzi a m'magazi.

Mankhwala

Yanumet ndi kuphatikiza kwa mankhwala awiri a hypoglycemic omwe ali ndi njira yowonjezera yochitira: sitagliptin phosphate, dipeptidyl peptidase 4 (DPP-4) inhibitor, ndi metformin hydrochloride, woimira kalasi ya biguanide, ndipo adapangidwa kuti apititse patsogolo kuwongolera kwa glycemic kwa odwala omwe ali ndi matenda a shuga a 2.

Sitagliptin phosphate eNdi inhibitor yogwira mtima, yosankha kwambiri ya pulottyl peptidase 4 (DPP-4) yochizira matenda a shuga. Inhibitors (DPP-4) ndi gulu la mankhwala omwe amagwira ntchito ngati othandizira othandizira incretin. Mwa kuletsa enzyme DPP-4, sitagliptin imachulukitsa kuchuluka kwa mahomoni awiri omwe amagwira ntchito - glucagon-ngati peptide 1 (GLP-1) ndi insulinotropic polypeptide (HIP) ya glucose. Ma incretins ndi gawo limodzi la masinthidwe amkati omwe amaphatikizidwa ndi kuyendetsa thupi kwa glucose homeostasis. Pokhapokha ngati pali magazi ena abwinobwino kapena okwera pamagazi, GLP-1 ndi HIP zimawonjezera kaphatikizidwe ka insulin ndikumasulidwa kwa maselo a beta a pancreatic. GLP-1 imathandizanso kubisa kwa glucagon ndi ma cell a pancreatic alpha, zomwe zimatsogolera kuchepa kwa kupanga kwa shuga kwa chiwindi. Sitagliptin ndi inhibitor yamphamvu komanso yosankha kwambiri ya DPP-4 ndipo siyimaletsa michere yogwirizana kwambiri ya DPP-8 kapena DPP-9. Sitagliptin imasiyana mu kapangidwe kake ka mankhwala ndi zochita zamapangidwe amtundu wa GLP-1, insulin, sulfonylureas kapena meglitinides, biguanides, gamma receptor agonists omwe amathandizidwa ndi peroxisome proliferator (PPARγ), alpha-glycosidase inhibitors ndi ma amylin analogues.

Kugwiritsa ntchito munthawi yomweyo sitagliptin ndi metformin kumathandizira kuti pakhale chidwi cha GLP-1. Sitagliptin, koma osati metformin, imawonjezera kuchuluka kwa HIP yogwira.

Sitagliptin imathandizira kuyendetsa glycemic ponseponse mu monotherapy komanso kuphatikiza mankhwala ena.

M'mayesero azachipatala, sitagliptin monotherapy inachititsa kuti chiwongolero cha glycemic chikule kwambiri ndikuchepetsa kwakukulu kwa glycated hemoglobin A1c (HbA1c), komanso kusala komanso kudya pambuyo pa chakudya. Kutsika kwa kudya kwa plasma glucose kumawonedwa ndi sabata lachitatu (endpoint main). Chiwopsezo cha hypoglycemia mwa odwala omwe amathandizidwa ndi sitagliptin chinali chofanana ndi placebo. Kulemera kwa thupi panthawi ya mankhwala ndi sitagliptin sikunonjezeke poyerekeza ndi mtengo woyamba.

Mphamvu zabwino za zizindikiro za beta-cell function, kuphatikiza HOMA-β, proinsulin kuwonjezereka kwa insulini komanso mawonekedwe a beta-cell reactivity mu mayeso ololera a glucose okhala ndi zitsanzo pafupipafupi.

Metformin hydrochloride ndi a greatuanide okhala ndi antihyperglycemic, omwe amachepetsa shuga m'magazi onse pamimba yopanda kanthu ndikatha kudya. Mankhwalawa samalimbitsa katemera wa insulin chifukwa chake samatsogolera ku hypoglycemia.

Machitidwe a metformin amawongolera ndi njira zitatu:

kutsika kwa kupanga kwa shuga m'chiwindi poletsa gluconeogeneis ndi glycogenolysis,

Kupititsa patsogolo mphamvu yogwiritsira ntchito glucose mu zotumphukira, mu minofu minofu mwakuwonjezera mphamvu ya insulin,

Kuchepetsa mayamwidwe a shuga m'matumbo.

Metformin imathandizira kapangidwe ka glycogen mu intracellular pochita glycogen synthetase, imakulitsa mayendedwe a glucose ndi mapuloteni ena amkati (GLUT-1 ndi GLUT-4).

Kuphatikiza pa zotsatira za hypoglycemic, metformin imathandizanso kugunda kwa lipid. Pa mankhwala othandizira, metformin amachepetsa cholesterol yonse, LDL ndi triglycerides.

Zizindikiro zogwiritsidwa ntchito

Janumet anagwiritsa ntchito lmotsatira njira ya matenda a shuga 2, kuphatikiza njira zosagwiritsa ntchito mankhwala kukonza ma shuga a m'magazi, komanso kuphatikiza mankhwala ena:

Kuphatikiza pa zakudya ndi machitidwe olimbitsa thupi kuti muchepetse kuwongolera kwa glycemic kwa odwala omwe alibe mphamvu yokwanira ya metformin monotherapy pa mlingo waukulu wololezedwa, komanso mwa odwala omwe akulandira kale chithandizo ndi kuphatikiza kwa sitagliptin ndi metformin.

Kuphatikiza ndi sulfonylurea zotumphukira (kuphatikiza mankhwala atatu) monga chowonjezera pa chakudya ndi regimen odwala omwe sanakwaniritse chiwongolero chokwanira cha glycemic panthawi ya mankhwala a sulfonylurea ndi metformin pazokulitsa kwakukulu.

Kuphatikiza pa gamma receptor agonists yoyendetsedwa ndi peroxisome proliferator (PPAR-γ) (mwachitsanzo, thiazolidinedione) (kuphatikiza kwa mankhwala atatu) monga zowonjezera pazakudya ndikuchita masewera olimbitsa thupi kwa odwala omwe ali osakwanira othandizira othandizira omwe ali ndi metformin ndi PPAR-γ agonist pamlingo waukulu wololezedwa .

Kuphatikiza ndi insulin (kuphatikiza mankhwala atatu) monga chowonjezera pa zakudya ndikuchita masewera olimbitsa thupi kuti muchepetse kulamulidwa kwa glycemic mwa odwala osakwanira insulin ndi mankhwala a metformin.

Mlingo ndi makonzedwe

Mlingo wa mankhwalawa Yanumet ayenera kusankhidwa payekhapayekha, potengera njira zomwe zilili pakanthawi kachipatala, kugwiritsa ntchito bwino komanso kulolera kwa wodwalayo, osapitirira muyeso womwe umalimbikitsidwa tsiku lililonse la sitagliptin - 100 mg.

Popeza kukonzekera kwa glycemic kokwanira ndi metformin monotherapy pazipita kololedwa. Mlingo woyamba wa Yanumet uyenera kuphatikiza mlingo wa sitagliptin 50 mg kawiri pa tsiku (okwanira tsiku lililonse 100 mg) ndi mlingo womwe ulipo wa metformin.

Mukamasintha kuchokera ku mankhwala ophatikiza ndi sitagliptin ndi metformin. Mlingo woyambirira wa Yanumet uzikhala wofanana ndi Mlingo wa sitagliptin ndi metformin.

Palibe kupezeka kwa glycemic control, kuphatikiza kwa mankhwala a metformin muyezo wolekerera komanso sulfonylurea. Mlingo wa mankhwala Yanumet uyenera kuphatikiza mlingo wa sitagliptin 50 mg 2 kawiri pa tsiku (okwanira tsiku lililonse la 100 mg) ndi mlingo womwe ulipo wa metformin. Ngati Janumet amagwiritsidwa ntchito limodzi ndi sulfonylurea, ndikofunikira kuti muchepetse mlingo wa sulfonylurea kuti muchepetse chiopsezo cha hypoglycemia.

Pokhapokha pakutha kwa glycemic control, kuphatikiza mankhwala ndi metformin pazomwe zimalekerera piritsi komanso PPAR-γ agonist. Mlingo wa mankhwala Yanumet uyenera kuphatikiza mlingo wa sitagliptin 50 mg 2 kawiri pa tsiku (okwanira tsiku lililonse la 100 mg) ndi mlingo womwe ulipo wa metformin.

Popeza kukonzekera mokwanira glycemic ndi kuphatikiza mankhwala awiri mankhwala - insulin ndi metformin pazipita kololera. Mlingo wa mankhwala Yanumet uyenera kuphatikiza mlingo wa sitagliptin 50 mg 2 kawiri pa tsiku (okwanira tsiku lililonse la 100 mg) ndi mlingo womwe ulipo wa metformin. Mukamagwiritsa ntchito mankhwala Janumet osakanikirana ndi insulin, pangafunikire kuchepetsa mlingo wa insulin kuti mupewe chiopsezo cha hypoglycemia.

Pofuna kuchepetsa Mlingo, Yanumet ya mankhwala imapezeka mu Mlingo wa 50 mg wa sitagliptin kuphatikiza 500, 850 kapena 1000 mg wa metformin hydrochloride.

Odwala onse ayenera kutsatira zakudya zomwe zimagwiritsidwa ntchito tsiku lonse. Odwala onenepa kwambiri ayenera kutsatira zakudya zamafuta ochepa.

Yanumet iyenera kugwiritsidwa ntchito kawiri pa tsiku ndi chakudya, pang'onopang'ono kuwonjezera mlingo, kuti muchepetse chiopsezo cha zotsatira zoyipa zamagetsi zomwe zimagwidwa ndi metformin.

Magulu apadera a odwala

Odwala omwe ali ndi vuto la impso. Kusintha kwa Mlingo kwa odwala ofooka aimpso (CC ≥ 60 ml / min) sikofunikira. Janumet sayenera kutumizidwa kwa odwala omwe ali ndi pakati kapena aimpso kwambiri (CC