Yanumet (50

Mbadamba ihe eji etinye fim, 50 mg / 500 mg, 50 mg / 850 mg, 50 mg / 1000 mg.

Otu mbadamba ihe

bekee arụ ọrụ: citagliptin phosphate monohydrate 64.25 mg (nke ruru 50 mg sitagliptin free base) na metformin hydrochloride 500 mg / 850 mg / 1000 mg.

ndị na-ebu ụzọ: microcrystalline cellulose, polyvinylpyrrolidone (povidone), sodium stearyl fumarate, sodium lauryl sulfate, mmiri dị ọcha.

Ihe mejupụtara shell maka usoro nke 50 mg / 500 mg: Opadry®II Pink 85 F94203 (polyvinyl mmanya, titanium dioxide (E 171), macrogol / polyethylene glycol 3350, talc, iron ironide (E 172), black iron oxide (E 172),

Ihe mejupụtara shell maka usoro nke 50 mg / 850 mg: Opadry®II Pink 85 F94182 (polyvinyl mmanya, titanium dioxide (E 171), macrogol / polyethylene glycol 3350, talc, iron ironide (E 172), black iron oxide (E 172),

Ihe mejupụtara shell maka usoro onunu ogwu nke 50 mg / 1000 mg: Opadry®II Red 85 F15464 (polyvinyl mmanya, titanium dioxide (E 171), macrogol / polyethylene glycol 3350, talc, iron ironide (E 172), black iron oxide (E 172).

Mbadamba mbadamba 50/500:

Mbadamba ụrọ ndị nwere Capsule, biconvex, kpuchie ya na fim nke agba pink na-acha odo odo, nke nwere ihe odide akpọrọ "575" n'otu akụkụ ma dị mma n'akụkụ nke ọzọ.

Mbadamba mbadamba 50/850:

Mbadamba ụrọ a kpuchiri ekpuchi, biconvex, kpuchie ya n'ọbọ ihe nkiri pink, na ihe odide ahụ "515" gbatusiri ike n'otu akụkụ ma dị mma n'akụkụ nke ọzọ.

Mbadamba mbadamba 50/1000:

Mbadamba ụrọ a kpụrụ akpụ, biconvex, kpuchie ya n'ọbọ uhie na-acha uhie uhie, nke e dere ede "577" n'akụkụ ya ma dịkwa mma n'akụkụ nke ọzọ.

Ngwongwo ogwu

Mlọ ọgwụ

Mmụta banyere bioequivalence na ndị ọrụ afọ ofufo mara mma achọpụtala na iwere Janumet (sitagliptin / metformin hydrochloride) bụ ihe dị ndụ na ịnwe sitagliptin phosphate na metformin hydrochloride iche. Ihe omuma ndi a gosiputara ihe ogwugwu nke ogwu ndi di ike.

Orkpachara anya Site na onu ogwu nke 100 mg, sitagliptin na-abanye ngwa ngwa ma rute plasma kachasị mkpa (Tmax median) mgbe awa 1-4 gachara, nkezi mpaghara n'okpuru oge ịta ahụhụ nke AUC nke sitagliptin na plasma bụ 8.52 μmol • awa, Cmax 950 nmol . AUC nke sitagliptin na plasma na-abawanye na nha. Ezigbo bioavailability nke sitagliptin dị ihe dị ka 87%. Ebe ọ bụ na oriri sitagliptin na nri nwere nnukwu abụba anaghị emetụta ọgwụ ọgwụ nke ọgwụ, enwere ike iji sitagliptin agbanyeghị nri nri. AUC nke sitagliptin na plasma na-abawanye na oke na nha.

Nkesa. Ogologo nha nke nkesa na inye aka na-ewere ọgwụ sitagliptin na ọgwụ nke 100 mg dị ihe dị ka 198 lita. Ngwurugwu sitagliptin na-ejikọghachi na protein plasma ọbara dị ala - 38%.

Metabolism. Ihe dị ka 79% nke sitagliptin na-agbanwegharị na mmamịrị ya. Mgbanwe metabolic nke ọgwụ dị ntakịrị - ihe dị ka 16% dị n'ụdị metabolites.

Ojiji. Mgbe nchịkwa ọnụ nke 14C pụtara sitagliptin nke ndị ọrụ afọ ofufo nwere ahụike, ihe dị ka 100% nke ọgwụ ahụ ka emere ka izu otu ya nwee ọnya na mmamịrị nke 13% na 87%. Ogologo ndụ ọkara nke t½ mgbe nchịkwa ọnụ nke sitagliptin na dose nke 100 mg bụ ihe dị ka awa 12.4. Sitagliptin na-agbakọta na obere ntakịrị naanị na iji ya ugboro ugboro. Mkpochapu ntaramahụhụ dị ihe dịka 350 ml / min.

A na - emegharị sitagliptin n'ụzọ pụrụ iche site na akụrụ site na sistemụ na - emegharị canalicitic secretion.

Ọrịa shuga mellitus. Pharmlọ ọgwụ ọgwụ sitagliptin dị na ndị ọrịa nwere ụdị ọrịa shuga 2 nke ọrịa shuga yiri nke ndị ọrụ afọ ofufo nwere ahụ ike.

Alrụ ọrụ na-arụ ọrụ na ụlọ. Nnyocha nyocha na ọgwụ ọgwụ nke ọgwụ sitagliptin (50 mg) na ndị ọrịa nwere ọrụ ịgbazị nsogbu, dị nro (ya na krantiin KK 50 - 80 ml / min), na-agbanwe agbanwe (KK 30 - 50 ml / min) na nnukwu (KK erughị 30 ml / min ) ogo, yana ndị ọrịa nwere ọrịa akụrụ ikpeazụ nwere ọrịa ịba ọcha n'anya, ma e jiri ya tụnyere ndị ọrịa nwere ahụ ike.

N'ime ndị ọrịa nwere ọrụ mgbazinye nsogbu nke ịdị nro, ọ nweghị mmụba dị ukwuu n'ụlọ ọrụ na mkpokọta sitagliptin na plasma ọbara ma e jiri ya tụnyere ìgwè ndị ọrụ afọ ofufo nwere ahụ ike. A hụrụ ihe dị ka okpukpu abụọ nke abawanye na sitagliptin AUC na plasma na ndị ọrịa nwere obere akwara na-erughị ala, na ihe dị ka okpukpu anọ na-abawanye na sitagliptin AUC na plasma ka a hụrụ na ndị ọrịa nwere nkwarụ akwara siri ike, yana ndị ọrịa nwere ọrịa akụrụ gbasara njedebe. onye nwere onodu obia, ma e jiri ya tụnyere ndi otu ndi inyeaka mara mma. Sitagliptin dị obere ka eweputara ya n'oge ọwụwa akwara (13.5% na oge mkparịta ụka elekere 3-4, nke malitere awa 4 mgbe ị theụsịrị ọgwụ ahụ).

Agadi. N'ime ndị ọrịa agadi (afọ 65-80), plasma nwere ike ịnagide sitagliptin bụ 19% karịa ndị okenye.

Childrenmụaka. Emebeghị nnyocha banyere ojiji sitagliptin na ụmụaka.

Okike, oso, aru mmadu (BMI). Enweghị mkpa ịmegharị ọnụọgụ ọgwụ ahụ dabere na okike, agbụrụ ma ọ bụ BMI. Omume ndị a enweghị mmetụta dị ukwuu n’ụlọ ọgwụ na ọgwụ ọgwụ nke sitagliptin.

Orkpachara anya. Mgbe nchịkwa ọnụ nke metformin, a na-enweta tmax mgbe awa 2.5 gachara. Ezigbo bioavailability nke metformin, mgbe ị na-ewere mbadamba 500 mg, bụ ihe dị ka 50-60% na ndị ọrụ afọ ofufo ahụike. Mgbe ejiri ọnụ na-ekwu ya, irighiri ihe ndị na-adịghị agbari bụ 20-30% ma ọ bụ fesa. Usoro ogwu nke metformin absorption abụghị nke adị. Mgbe ị na-eji metformin mee ihe na usoro ndị a tụrụ aro, a na-enweta mkpokọta nhazi n'ime awa 24-48 ma, dịka iwu, anaghị gafere 1 μg / ml. N'ime ule ụlọ ọgwụ a na-achịkwa, oke plasma nke mejupụtara metformin (Cmax) erughi 4 μg / ml, ọbụlagodi mgbe ị na-eji oke onunu. Nlekọta nke ọgwụ n’otu oge na 850 mg na nri belata ogo na ọnụego nnabata nke metformin, nke a gosipụtara site na mbelata nke ịba ụba na plasma ọbara site na 40%, mbelata na AUC site na 25% na ịgbatị oge iji ruo na ntinye uche kachasị na plasma ọbara site na 35 nkeji. Amaghi ihe banyere ulo ogwu di nkpa.

Nkesa. Mgbakwunye protein Plasma bụ nke ileghara anya. A na-ekesa Metformin n’ime sel ọbara. Oke kachasị n'ọbara dị ala karịa na plasma, a na-erute ihe dị ka otu oge ahụ. Mkpụrụ ndụ ọbara uhie yikarịrị ka akụkụ nke abụọ maka nkesa. Nkezi Vd dịgasị n'etiti lita - 276.

Metabolism. Metformin na-agbanwegharị na mmamịrị.

Ojiji. Mkpochapu akwara nke metformin bụ> 400 ml / min, ọgwụ ahụ na-apụta site na nzacha na ngwakọta tubular. Mgbe nchịkwa ọnụ gasịrị, iwepụ ọkara ndụ ikpeazụ bụ ihe dịka awa 6.5. N'ihe banyere ọrụ akụrụ na-emebi emebi, mkpochapu akwara na-agbadata n'ike n'ike nke creatinine, n'ihi nke ọkara ndụ na-adị ogologo, nke na-eduga n'ịbawanye ọkwa nke metformin na plasma.

Mlọ ọgwụ

Yanumet bụ ngwakọta nke ọgwụ hypoglycemic abụọ nke nwere usoro nkwado ihe: sitagliptin phosphate, inhibitor dipeptidyl peptidase 4 (DPP-4), na metformin hydrochloride, onye nnọchite klas biguanide, ma chekwaa iji melite nchịkwa glycemic na ndị ọrịa nwere ụdị shuga 2.

Sitagliptin phosphate eọ bụ ọrụ na - egbochi ọnụ nke onye na - egbochi enzyme dipeptyl peptidase 4 (DPP-4) maka ịgwọ ụdị ọrịa shuga 2. Inhibitors (DPP-4) bụ klaasị ọgwụ nke na - eme dị ka ndị nkwalite. Site na igbochi enzyme DPP-4, sitagliptin na-abawanye ọkwa nke homonụ abụọ na-arụ ọrụ na - glucagon-like peptide 1 (GLP-1) na glucose na-adabere insulinotropic polypeptide (HIP). Na incretins bụ akụkụ nke usoro endogenous na-etinye aka na usoro physiological nke glucose homeostasis. Naanị na nchịkọta glucose ọbara dị elu ma ọ bụ dị elu, GLP-1 na HIP na-abawanye njikọ insulin na mwepụta ya na mkpụrụ ndụ beta nke pancreatic. GLP-1 na-ebelata ihe nzuzo glucagon site na mkpụrụ ndụ alịprọkụ pịprọsis, na-eduga n'ịbelata mmelata glucose na imeju. Sitagliptin bụ ihe dị ike ma na - ahọrọ oke nke enzyme DPP-4 ma ọ dịghị egbochi enzymes nwere njikọ DPP-8 ma ọ bụ DPP-9. Sitagliptin dị iche n'ụdị kemịkalụ ya na ọgwụ ọgwụ ya na GLP-1 analogues, insulin, sulfonylureas ma ọ bụ meglitinides, biguanides, gamma receptor agonists nke peroxisome proliferator (PPARγ), alfa-glycosidase inhibitors na amylin analogues.

Oge sitagliptin na metformin na-enwe n’otu oge na-enwe mmetụta na-agbakwunye na mkpokọta GLP-1 na-arụ ọrụ. Sitagliptin, mana ọ bụghị metformin, na-eme ka ịba ụba nke HIP nọ n'ọrụ.

Sitagliptin na-emezi njikwa glycemic ma na monotherapy yana yana ọgwụ ndị ọzọ.

N'ime ule dị iche iche, sitagliptin monotherapy kwalitere njikwa glycemic na mbelata dị ukwuu na glycated hemoglobin A1c (HbA1c), yana ibu ọnụ na glucose nri. A hụrụ mbelata glucose plasma na-ebu ọnụ site n'izu nke atọ (isi ihe). Ọnọdụ nke hypoglycemia na ndị ọrịa agwọ ọrịa sitagliptin yiri nke ahụ. Ikike anụ ahụ n'oge ọgwụgwọ na sitagliptin arịgoghị ma e jiri ya tụnyere uru mbụ.

Egosiputara odi nma nke ihe ndi mmadu n’emeputa beta-cell, tinyere HOMA-β, proinsulin ka insulin ratios na beta-cell reactivity gosiputara n’ime nnabata nnabata glucose na ndi nlere ugboro ugboro.

Metformin hydrochloride bụ biguanide nwere mmetụta antihyperglycemic, nke na-ebelata glucose plasma na afọ na-enweghị nri na mgbe ị risịrị nri. Ọgwụ ahụ anaghị akpali insulin na ya mere ọ dịghị ebute hypoglycemia.

Usoro nke metformin bụ usoro atọ ji agbazi ya:

mbelata nke mmepụta glucose na imeju site na igbochi gluconeogenesis na glycogenolysis,

Vingkwalite oriri na ojiji nke glucose na akwara anụ ahụ, na akwara anụ ahụ site na ịba ụba insulin na-abawanye ụba.

na-eji nwayọ nwayọ na-abanyekwa glucose na eriri afọ.

Metformin na - akpali intracellular glycogen synthesis site na ị mee ihe na glycogen synthetase, na - eme ka ngwakọta glucose site na protein dị iche iche (GLUT-1 na GLUT-4).

Na mgbakwunye na mmetụta hypoglycemic, metformin nwere mmetụta dị mma na metabolism lipid. Na usoro onunu ogwu, metformin lowers cholesterol zuru oke, LDL na triglycerides.

Ihe ngosi maka ojiji

Janumet etinyere lka ọ dị ụdị ọrịa mellitus nke 2, tinyere ụzọ ndị na-abụghị ọgwụ nke iji dozie ọkwa glucose ọbara, yana yana ọgwụ ndị ọzọ:

Na mgbakwunye na nri na usoro mmega iji meziwanye njikwa glycemic na ndị ọrịa na-ezighi ike nke metformin monotherapy na oke ọnagide, yana ndị ọrịa na-anata ọgwụgwọ na ngwakọta nke sitagliptin na metformin.

Na ntinye ogwu (ana - achikota ogwu ato) dika ihe mgbakwunye nri ma mekwaa mmeghachi omume n’ime ndi oria n’enwetaghi ikike glycemic zuru oke n’oge ogwugwo na sulfonylurea na metformin na oke onunu anagide.

Na mgbakwunye na gamma receptor agonists nke peroxisome proliferator (PPAR-γ) (dịka ọmụmaatụ, thiazolidinedione) (mgbakwunye nke ọgwụ atọ) dị ka mgbakwunye na nri na usoro mmega ahụ na ndị ọrịa na-ezighi ike nke ọgwụgwọ na metformin na PPAR-γ agonist na oke ịnagide ọgwụ. .

Na insulin (ngwakọta nke ọgwụ atọ) dị ka mgbakwunye na nri nri na usoro mmega iji meziwanye njikwa glycemic na ndị ọrịa na-ezughị oke nke insulin na usoro ọgwụgwọ metformin.

Usoro onunu ogwu na nhazi

A ga-ahọpụta ọgwụ ọgwụ Yanumet n'otu n'otu, na-eburu n'uche usoro ọgwụgwọ dị ugbu a, ịdị mma na ntachi obi na onye ọrịa, ọ karịa gafere sitagliptin kachasị akwadoro kwa ụbọchị - 100 mg.

Na enweghị nchịkwa glycemic zuru oke na metformin monotherapy na oke ọnụọgụ ịnagide. Usoro izizi nke Yanumet kwesịrị ịgụnye ọgwụ sitagliptin 50 mg ugboro 2 kwa ụbọchị (ngụkọta kwa ụbọchị nke 100 mg) yana usoro metformin dị ugbu a.

Mgbe ị na-agbanwe na ọgwụgwọ ejikọtara na sitagliptin na metformin. Mkpụrụ mbụ nke Yanumet kwesịrị ịha nhata ka ọgwụ etinyere sitagliptin na metformin etinyere.

Na enweghị nchịkwa nchịkwa zuru oke, usoro ọgwụgwọ njikọta metformin na oke ọnagide na sulfonylurea. Ọgwụ nke ọgwụ Yanumet kwesịrị ịgụnye ọgwụ sitagliptin 50 mg ugboro abụọ kwa ụbọchị (ngụkọta kwa ụbọchị nke 100 mg) yana usoro metformin dị ugbu a. Ọ bụrụ na a na-eji Janumet eme ihe na njikọta nke sulfonylurea, ọ ga-adị mma ka ịbelata dose nke sulfonylurea iji belata ihe ize ndụ nke hypoglycemia.

Na enweghị nchịkwa nchịkwa zuru oke, njikọta ọgwụgwọ na metformin na oke ọnagide na predi-on agonist. Ọgwụ nke ọgwụ Yanumet kwesịrị ịgụnye ọgwụ sitagliptin 50 mg ugboro abụọ kwa ụbọchị (ngụkọta kwa ụbọchị nke 100 mg) yana usoro metformin dị ugbu a.

Enweghị njikwa glycemic zuru oke na usoro njikọta ọgwụ ọgwụ abụọ - insulin na metformin na oke ọnagide. Ọgwụ nke ọgwụ Yanumet kwesịrị ịgụnye ọgwụ sitagliptin 50 mg ugboro abụọ kwa ụbọchị (ngụkọta kwa ụbọchị nke 100 mg) yana usoro metformin dị ugbu a. Mgbe ị na-eji ọgwụ ọgwụ Janumet na insulin, ọ nwere ike ịdị mkpa iji belata ọgwụ insulin iji gbochie ihe ize ndụ nke hypoglycemia.

Maka ịdị mfe nke usoro onunu ogwu, ọgwụ Yanumet dị na usoro atọ nke 50 mg nke sitagliptin gbakwunyere 500, 850 ma ọ bụ 1000 mg nke metformin hydrochloride.

Ndị ọrịa niile kwesịrị ịgbaso nri na nkesa zuru oke nke oriri carbohydrate ụbọchị niile. Ndị ọrịa nwere oke ibu kwesịrị ịgbaso nri kalori.

Ekwesịrị iji nri Yanumet ugboro abụọ n'ụbọchị, jiri nwayọọ nwayọọ na-abawanye dose ahụ, iji belata ihe ize ndụ nke mmetụta ndị sitere na usoro nri nri na-emetụta metformin.

Ndị otu ọrịa pụrụ iche

Ọrịa enweghị akụrụ. Ime mgbanwe n'ime ndị ọrịa nwere nsogbu gbasara obere akwara (CC ≥ 60 ml / min) achọghị. Ekwesighi inye ndenye ọgwụ Janumet ọrịa nwere nsogbu gbasara akụrụngwa ma ọ bụ nnukwu ọdịda (CC