Analogs nke ọgwụ vildagliptin * metformin * (vildagliptin * metformin *)

Ogwu hypoglycemic ọgwụ. Vildagliptin - onye nnọchite anya klas nke ihe mkpali nke ngwa ikpuchi ume, na-egbochi oke enzyme dipeptidyl-4 (DPP-4). Mkpuchi ngwa ngwa zuru ezu nke ọrụ DPP-4 (> 90%) na-eme ka mmụba nke ihe abụọ basal na nri na-akpali nri nke ụdị 1 glucagon-dịka peptide (GLP-1) na glucose na-adabere glucose polypeptide (HIP) site na eriri afọ banye na sistem sisitek ụbọchị dum.

Bawanye ụba nke GLP-1 na HIP, vildagliptin na-eme ka mmụba nke mkpụrụ ndụ panc-pancreatic cells-glucose na glucose, nke na-eduga n’ọganihu n’ime insulin na-egbochi glucose.

Mgbe ị na-eji vildagliptin na ọgwụ nke 50-100 mg kwa ụbọchị na ndị ọrịa nwere ụdị ọrịa mellitus nke 2, a na-achọpụta ọganihu na ọrụ nke mkpụrụ ndụ reat-pancreatic β-sel. Ogo nke mmezi nke ọrụ β-mkpụrụ ndụ dabere na ogo mbibi mbụ ha, yabụ na ndị mmadụ anaghị arịa ọrịa shuga mellitus (ya na plasma nkịtị), vildagliptin anaghị akpali insulin na-anaghị ebelata glucose.

Site na ịbawanye uru nke GLP-1 nke endogenous, vildagliptin na-eme ka ọgbụgba α-sel na-abawanye uru glucose, na-eduga n'ịbawanye mma na nchịkwa glucose nke glucagon. Mbelata nke glucagon ngafe n’oge nri, n’aka nke ya, na-ebute mbelata nguzogide insulin.

Mmụba na oke nke insulin / glucagon megide ndabere nke hyperglycemia, n'ihi mmụba nke mkpokọta nke GLP-1 na HIP, na-akpata mbelata mmepụta glucose site na imeju na oge prandial na mgbe nri, nke na-eduga n'ịbelata mkpokọ glucose na plasma ọbara.

Na mgbakwunye, megide ndabere nke iji vildagliptin, a na-achọpụta mbelata ọkwa nke lipids na plasma ọbara, na-ekwupụtaghị, mmetụta a esoghị na mmetụta ya na GLP-1 ma ọ bụ HIP yana mmelite arụ ọrụ nke mkpụrụ ndụ reat-pancreatic β-sel.

A maara na mmụba na GLP-1 nwere ike ibelata ikpu gastric, mana achọpụtaghị mmetụta a na iji vildagliptin.

Mgbe ị na-eji vildagliptin na ndị ọrịa 5795 nwere ụdị ọrịa shuga 2 maka izu 12 ruo 52 dị ka monotherapy ma ọ bụ na njikọta metformin, ọgwụ sulfonylurea, thiazolidinedione, ma ọ bụ insulin, ọnụ ọgụgụ dị ukwuu na-agbadata ogologo oge nke mkpokọta gemo nke ọbara (HbA1c) na glucose ọbara ọbara.

Mgbe ejiri ọgwụ vildagliptin na metformin mee ihe dị ka ọgwụgwọ mbụ maka ndị ọrịa nwere ụdị ọrịa shuga 2, a na-ahụta mbelata HbA1c na ịdị arọ ahụ karịa izu iri abụọ na anọ ma e jiri ya tụnyere monotherapy na ọgwụ ndị a. Ọrịa hypoglycemia dị ntakịrị na otu ọgwụgwọ abụọ.

N'ime omumu ihe omumu nke iji vildagliptin na onwa ogwu nke 50 mg otu ugboro kwa onwa rue onwa isii n’ime ndi oria nwere oria 2 nke oria mellitus n’azu na aha mkpuru-obi (GFR> 30 rue 1500 mg) na agwado glimepiride (> 4 mg /) N'ime ule ụlọ ọgwụ, ọkwa HbA1c ọnụ ọgụgụ gbadara agbada ji 0.76% (ntọala - nkezi nke 8.8%).

Mlọ ọgwụ

A na-etinye Vildagliptin ngwa ngwa site na ingestion na bioav adị zuru oke nke 85%. N'ime usoro ọgwụgwọ ọgwụgwọ, mmụba nke Cmax nke vildagliptin na plasma na AUC fọrọ nke nta ka ọ bụrụ nke dabara na mmụba nke ọgwụ ahụ.

Mgbe abatasịrị na afọ efu, oge ị ga-eru Cmax nke vildagliptin na plasma ọbara bụ 1 h 45 min. N'iji nri n'otu oge, nri nke iwere ọgwụ na-ebelata ntakịrị: enwere mbelata na Cmax site na 19% na mmụba na oge ọ ruru elekere 2 nkeji iri atọ. Agbanyeghị, iri nri anaghị emetụta ogo mmịpụta yana AUC.

Njikọ vildagliptin na protein plasma dị ala (9.3%). A na-ekesa ọgwụ ahụ n ’otu ihe n’agbata plasma na sel ọbara. Nkesa vildagliptin na - aputa ihe dika elere anya nke oma, Vd na mmezi o bula site na mgbe ochichi aka gi bu 71 L.

Biotransformation bu uzo mbu nke vildagliptin. N'ime ahụ mmadụ, 69% nke ọgwụ ọgwụ agbanwere. Isi metabolite - LAY151 (57% nke dose) bụ ọgwụ anaghị arụ ọrụ ma ọ bụ ngwaahịa nke hydrolysis nke mpaghara cyano. Ihe dị ka 4% nke ọgwụ a na-enweta amide hydrolysis.

Na nyocha nnwale, enwere mmetụta dị mma nke DPP-4 na hydrolysis nke ọgwụ ahụ. Achọpụtaghị Vildagliptin na ntinye nke cytochrome P450 isoenzymes. Vildagliptin abụghị mkpụrụ nke CYP450 isoenzymes, anaghị egbochi ma ọ bụ ghara itinye cytochrome P450 isoenzymes.

Mgbe ịgesụ ọgwụ ahụ, ihe dị ka 85% nke ọgwụ ahụ ka akụrụ na -apụta na 15% site na eriri afọ, excaltion nke akwara vildagliptin bụ 23%. T1 / 2 mgbe nchịkwa ọnụ bụ ihe dị ka awa 3, n'agbanyeghị agbanyeghị.

Mmekọ nwoke na nwoke, ntụpọ nke aru, na agbụrụ anaghị emetụta ọgwụ ọgwụ nke vildagliptin.

Ihe ngosi maka iji ogwu GALVUS

2dị ọrịa shuga abụọ:

• dị ka ọgwụ monotherapy yana usoro ọgwụgwọ nri na mmega ahụ,
• yana metformin dị ka ọgwụ ị initialụ ọgwụ ọgwụ mbụ na enweghị ezigbo ọgwụgwọ ọgwụ na mmega ahụ,
• dị ka akụkụ nke usoro nkwonkwo ọgwụ abụọ nwere usoro ọgwụ metformin, ihe dị na sulfonylurea, thiazolidinedione ma ọ bụ insulin n'ihe banyere usoro nri nri anaghị arụ ọrụ, mmega ahụ na monotherapy na ọgwụ ndị a.
• dị ka akụkụ nke usoro ọgwụgwọ atọ eji agbakọta: na njikọta ikike sulfonylurea na metformin na ndị ọrịa mbụ ejirila usoro sulfonylurea na metformin megide nzụlite nri na mmega ahụ na-enwetabeghi njikwa glycemic zuru oke,
• dị ka akụkụ nke usoro ọgwụgwọ nkwonkwo atọ: yana njikọ insulin na metformin na ndị ọrịa bụ ndị natara insulin na metformin na mbụ na nri na mmega ahụ na-enwetaghị nchịkwa zuru oke.

Usoro usoro onunu ogwu

Ejiri ọnụ ghee Galvus n'agbanyeghị nri nri.

Ekwesịrị ịhọrọ usoro usoro ọgwụ ahụ n'otu n'otu dabere na ịdị irè na ntachi obi.

Usoro ọgwụ a tụrụ aro ya n'oge monotherapy ma ọ bụ dịka akụkụ nke ọgwụgwọ njikọta abụọ na metformin, thiazolidinedione ma ọ bụ insulin (ya na metformin ma ọ bụ na-enweghị metformin) bụ 50 mg ma ọ bụ 100 mg kwa ụbọchị. N'ime ndị ọrịa nwere ụdị shuga dị oke njọ 2 na-anata insulin, a na-atụ aro Galvus na dose 100 mg kwa ụbọchị.

Galvus a na-atụ aro ka ọ bụrụ akụkụ nke usoro ọgwụgwọ nkwonkwo okpukpu atọ (vildagliptin + sulferilureaeri + metformin) bụ 100 mg kwa ụbọchị.

Ekwesịrị ịnye ọgwụ ruru 50 mg kwa ụbọchị na ọgwụ 1 n'ụtụtụ. Ekwesịrị inye ọgwụ mgbochi nke 100 mg kwa ụbọchị ugboro 50 n'ụtụtụ na mgbede.

Mgbe ejiri ya dị ka akụkụ nke usoro nkwonkwo abuo nwere usoro ọgwụgwọ sulfonylurea, usoro akwadoro Galvus bụ 50 mg 1 oge kwa ụbọchị n'ụtụtụ. Mgbe etinyere ya na usoro sulfonylurea, ịdị irè nke ọgwụgwọ ọgwụ na ọgwụ nke 100 mg kwa ụbọchị yiri nke ahụ na 50 mg kwa ụbọchị. Site na mmetụta ọgwụgwọ na-ezighi ezi megide ndabere nke iji ọgwụ kachasị atụ aro kwa ụbọchị nke 100 mg, maka njikwa kachasị mma nke glycemia, itinye ọgwụ ndị ọzọ hypoglycemic ọgwụ ga-ekwe omume: metformin, ọgwụ sulfonylurea, thiazolidinedione ma ọ bụ insulin.

N'ime ndị ọrịa nwere nsogbu gbasara akụrụngwa dị nro na ọrụ ịwa ahụ, a chọghị ndozi usoro onunu ogwu. N'ime ndị ọrịa nwere ọrụ mkpo ya na-agafeghị oke ma ọ bụ daa arụ (gụnyere njedebe ọnụ nke ọdịda akwara na-adịghị ala ala na akwara hemodialysis), a ga-eji ọgwụ ahụ mee ihe na 50 mg otu ugboro n'ụbọchị.

N'ime ndị ọrịa agadi (> afọ 65), ọ nweghị ezi ntụzi usoro usoro onunu ogwu Galvus ka achọrọ.

Ebe ọ bụ na enweghị ahụmịhe banyere iji ọgwụ ahụ eme ihe na ụmụaka na ndị na-eto eto na-erubeghị afọ 18, a gaghị atụ aro ka iji ọgwụ ahụ na ngalaba ndị ọrịa.

Mmetụta akụkụ

Mgbe ị na-eji Galvus eme ihe maka ọgwụ monotherapy ma ọ bụ na ọgwụ ndị ọzọ, ọtụtụ mmeghachi omume dị nro bụ nke dị nro, na-adị nwa oge, ọ chọghịkwa ịkwụsị ọgwụgwọ. Achọpụtaghị njikọ ọ bụla n'etiti ugboro ole ihe ọjọọ na afọ, okike, agbụrụ, oge eji, ma ọ bụ usoro dosing.

Ihe mere angioedema n'oge ọgwụgwọ ya na Galvus bụ> 1/10 000, 3 × VGN) bụ 0.2% ma ọ bụ 0.3%, otu (ma e jiri ya tụnyere 0.2% na ndị na-ahụ maka njikwa). Mmụba na ọrụ nke enzymes imeju n'ọtụtụ ọnọdụ bụ asymptomatic, ọ nweghị ọganihu, yana mgbanwe cholestatic ma ọ bụ nke enweghị mgbakwunye.

Mkpebi ugboro ole mmeghachi omume dị njọ: ọtụtụ mgbe (> 1/10), ọtụtụ mgbe (> 1/100, 1/1000, 1/10 000, 2,5 ugboro karịa VGN).

Ebe ọ bụ na ahụmịhe nke iji Galvus mee ihe na ndị ọrịa nwere njedebe akụrụngwa ọdịda na akwara ụkwụ, a na-atụ aro ka e jiri nlezianya dezie ọgwụ ahụ na ndị ọrịa.

Ojiji nke GALVUS nke ogwu n’oge di ime na n’azu ube

Enweghị data zuru oke maka ojiji Galvus n'ime ụmụ nwanyị dị ime, ya mere ekwesighi iji ọgwụ ahụ n'oge ime. N'ihe banyere metabolism na-eme ka ọ dị ụmụ nwanyị dị ime, enwere ihe ọghọm nke ibute ọrịa ana - amụ nwa, yana ugboro ole ọrịa obi nwa na ụmụ nwụrụ anwụ.

Na nyocha nnwale, mgbe edere ya na usoro onyonyo ugboro 200 karịa ka a tụrụ aro ya, ọgwụ ahụ emepụtaghị ọmụmụ nri na mmalite nke ẹmbrayo, ọ rụpụtaghịkwa teratogenic n'ahụ nwa ebu n'afọ.

Ebe ọ bụ na amabeghị ma vartagliptin dị n'ime mmiri ara mmadụ, ekwesighi iji Galvus n'oge a na-enye nwa ara.

Ntụziaka pụrụ iche

Ebe ọ bụ na, n'ọnọdụ ndị a na-adịghị ahụkebe, ojiji nke vildagliptin gosipụtara mmụba na ọrụ nke aminotransferases (ọ na-enweghị oge ngosipụta nke ụlọ ọgwụ), tupu agbapụta Galvus, yana oge niile n'afọ mbụ nke iji ọgwụ ahụ (1 oge na ọnwa atọ), a na-atụ aro ka ikpebi usoro biochemical nke ọrụ imeju. Ọ bụrụ na onye ọrịa nwere mmụba ọrụ nke aminotransferases, ọmụmụ ihe nke abụọ a ga - enyocha nsonaazụ nke abụọ, wee chọpụta oge niile usoro biochemical na - arụ ọrụ nke imeju ruo mgbe ha ga - agbanwe. Ọ bụrụ na ọrụ nke AST ma ọ bụ ALT dị elu karịa VGN (dị ka nyocha ndị a gosipụtara ugboro ugboro), a na-atụ aro ka ịkagbu ọgwụ ahụ.

Site na mmepe nke jaundice ma ọ bụ ihe ịrịba ama ndị ọzọ nke ọrụ imeju na-arịa n'oge Galvus, ekwesịrị ịkwụsị ọgwụ ọgwụ ozugbo. Mgbe ịmechara ihe ngosipụta arụmọrụ imeju, ọgwụ agaghị enwe ike ịmaliteghachi.

Ọ bụrụ na ọ dị mkpa, a na-eji Galulus insulin agwọ ya naanị yana insulin. Ekwesighi iji ọgwụ a mee ihe na ndị ọrịa nwere ụdị ọrịa shuga 1 nke mellitus ma ọ bụ maka ọgwụgwọ nke ketoacidosis nke ọrịa mamịrị.

Dodoụbiga ya ókè

A na-anabata Galvus nke ọma mgbe a na-enye ya ọgwụ nke ruru 200 mg kwa ụbọchị.

Mgbaàmà: mgbe ị na-eji ọgwụ ahụ na ọgwụ nke 400 mg kwa ụbọchị, enwere ike ịhụ ihe mgbu akwara, adịkarịghị, ngụgụ na paresthesia, ahụ ọkụ, ọzịza na mmụba dị mkpụmkpụ na mkpokọta lipase (2 ugboro karịa VGN). Site na mmụba na dose nke Galvus ruo 600 mg kwa ụbọchị, mmepe nke edema nke nsọtụ ya na paresthesias na mmụba nke mkpokọta nke CPK, ALT, protein C-reactive na myoglobin ga-ekwe omume. Ihe mgbaàmà nke ị ofụbiga mmanya ókè na mgbanwe na usoro nyocha ụlọ nyocha na-apụ n'anya mgbe ịkwụsị ọgwụ ahụ.

Ọgwụ: iwepu ọgwụ n’ahụ site na ịba ọcha n’anya. Ma, enwere ike wepu metabolism nke mbu nke vildagliptin (LAY151) site na ahu site na hemodialysis.

Mkparịta ụka ọgwụ ọjọọ

Galvus nwere ikike dị ala maka ịmekọrịta ọgwụ.

Ebe Galvus abụghị mkpụrụ nke enzymes cytochrome P450, ọ naghị egbochi ma ọ bụ na-egbochi enzymes ndị a, mmekọrịta Galvus na ọgwụ ndị na-agbanwe agbanwe, ndị na-egbochi ya, ma ọ bụ ndị na-akpata P450 adịghị ele anya. Iji vildagliptin na-eme n'otu oge emetụtaghị metabolic ọnụego ọgwụ ndị na-anọchi enzymes: CYP1A2, CYP2C8, CYP2C9, CYP2C19, CYP2D6, CYP2E1 na CYP3A4 / 5.

Nmekorita nmekorita nke ogwu Galvus ya na ogwu nke ana ejikarị ya maka ọgwụgwọ nke ụdị shuga mellitus 2 (glibenclamide, pioglitazone, metformin) ma ọ bụ nwee usoro ọgwụgwọ dị warara (amlodipine, digoxin, ramipril, simvastatin, valsartan, warfarin).

Nkọwapụta ọgwụ ọjọọ

Vildagliptin * + Metformin * (Vildagliptin * + Metformin *) - mlọ ọgwụ

Nhazi nke ọgwụ Vildagliptin * + Metformin * (Vildagliptin * + Metformin *) gụnyere ndị nnọchianya hypoglycemic abụọ nwere usoro dị iche iche: vildagliptin, nke bụ klas nke dipeptidyl peptidase-4 inhibitors (DPP-4), na metformin (n'ụdị nnọchite hydrochlorigu), . Njikọ nke ihe ndị a na-enye gị ohere ijikwa oke ike glucose ọbara n'ime ndị ọrịa nwere ụdị shuga 2 ruo awa 24.

Vildagliptin, onye nnọchi anya klas nke ndị na-akpali akpali nke ngwa ọrụ akwara, na-egbochi enzyme DPP-4, nke na-ebibi ụdị 1 glucagon-like peptide (GLP-1) na polypeptide glucose-glucose-Hulin. Metformin na-ebelata mmepụta nke glucose site na imeju, na -ebelata nnabata nke glucose na eriri afọ ma na-ebelata insulin iguzogide site na ịkwalite mbido na ojiji nke glucose site na nsụ anụ ahụ.

Metformin na-akpali njikọ intancellular glycogen site na ime ihe na glycogen synthetase ma na-akwalite ụgbọ njem glucose site na protein protein ụfọdụ na-ebugharị glucose membrane (GLUT-1 na GLUT-4).

Ihe mgbochi ngwa ngwa zuru ezu nke ọrụ DPP-4 mgbe vildagliptin na-akpata mmụba na mkpụkọ mmanụ na nri nke GLP-1 na HIP site na eriri afọ banye na mgbasa ahụ nke ụbọchị.

Bawanye uru nke GLP-1 na HIP, vildagliptin na-eme ka mmụba nke mkpụrụ ndụ panc-pancreatic cells-glucose na glucose, nke na-eduga n’ọganihu n’ime insulin na-egbochi glucose. Ogo nke mmezi nke ọrụ β-mkpụrụ ndụ dabere na ogo mbibi mbụ ha, yabụ na ndị mmadụ n’enweghi ọrịa shuga (ya na glucose n'ọbara plasma), vildagliptin anaghị akwalite izochi insulin ma ghara iwetulata glucose.

Site na ịbawanye uru nke GLP-1 nke endogenous, vildagliptin na-eme ka ọgbụgba β-sel na-abawanye uru glucose, na-eduga n'ịbawanye mma na nchịkwa glucose nke glucagon. Mbelata mgbanye glucagon dị elu mgbe nri gasịrị, n'aka nke ya, na-ebute mbelata nguzogide insulin.

Mmụba nke insulin / glucagon ruru megide ndabere nke hyperglycemia, n'ihi mmụba nke ịta ahụhụ nke GLP-1 na HIP, na-eme ka mbelata mmepụta glucose site na imeju ma n'oge nri, na-eduga n'ịbelata mkpokọta nke glucose na plasma ọbara.

Na mgbakwunye, megide nzụlite ojiji nke vildagliptin, mbelata mkpokọta lipids na plasma ọbara mgbe nri ama gasịrị, mmetụta a esonyereghị ya na nsonaazụ GLP-1 ma ọ bụ HIP na mmụba na ọrụ nke mkpụrụ ndụ akwara pancreatic. A maara na mmụba nke ịta ahụhụ nke GLP-1 nwere ike iduga na mkpochapụ afọ, agbanyeghị na ojiji nke vildagliptin, a naghị ahụ mmetụta a.

Mgbe ị na-eji vildagliptin na 5759 ndị nwere ụdị ọrịa shuga nke 2 maka izu 52 na monotherapy ma ọ bụ na njikọta metformin, ọgwụ sulfonylurea, thiazolidinedione, ma ọ bụ insulin, ọnụ ọgụgụ dị ukwuu na-agbada n'ọbara haemoglobin (HbA1c) na ibu ọnụ ọbara ọbara.

Metformin na - eme ka nnabata glucose dị n'etiti ndị ọrịa nwere ụdị ọrịa shuga nke abụọ site na iwetulata glucose plasma ma ma tupu nri.

N'adịghị ka usoro sulfonylurea, metformin anaghị akpata hypoglycemia na ndị ọrịa nwere ụdị ọrịa shuga 2 nke ọrịa mamịrị ma ọ bụ na ndị nwere ahụike (ma e wezụga n'ọnọdụ ndị pụrụ iche). Usoro ọgwụgwọ nke iji ọgwụ ahụ emeghị ka mmepe nke hyperinsulinemia. N'iji metformin mee ihe, insulin insulin anaghị agbanwe agbanwe, ebe ịba insulin na plasma na-enweghị afọ na ụbọchị nwere ike ibelata.

Site n'iji metformin mee ihe, enwere mmetụta bara uru na metabolism nke lipoproteins: mbelata nke ịba ụba nke cholesterol, cholesterol nke ogo lipoproteins dị ala na triglycerides, ejikọghị ya na nsonaazụ nke ọgwụ na ịba ụba nke glucose na plasma ọbara.

Mgbe ị na-eji ọgwụgwọ njikọta na vildagliptin na metformin na usoro ọgwụ kwa ụbọchị nke 1,500-3,000 mg nke metformin na 50 mg nke vildagliptin ugboro 2 / ụbọchị maka afọ 1, a hụrụ ọnụ ọgụgụ dị ukwuu na-agbanwe agbanwe na mgbanye glucose ọbara (kpebiri site na mbelata na HbA1c) yana mmụba na oke nke ndị ọrịa nwere mbelata Ntinye uche nke HbA1c erughi 0.6-0.7% (ma e jiri ya tụnyere ndị ọrịa nọ na-anata naanị metformin).

N'ime ndị ọrịa na-anata ngwakọta nke vildagliptin na metformin, mgbanwe ego na-emetụta ọnụ ọgụgụ ahụ dị ukwuu ma e jiri ya tụnyere ọnọdụ izizi. Abalị iri abụọ na anọ gachara ọgwụgwọ, n'ọtụtụ ndị ọrịa na-anata vildagliptin yana mgbakwunye metformin, mbelata ọbara systolic na ọbara diastolic dị na ndị ọrịa nwere ọbara mgbali elu.

Mgbe ejiri jikọtara vildagliptin na metformin dịka ọgwụgwọ mbụ maka ndị ọrịa nwere ụdị ọrịa shuga 2, ana-ahụbelata mbelata nke HbA1c karịa izu 24 ka e jiri ya tụnyere monotherapy na ọgwụ ndị a. Ọrịa hypoglycemia dị ntakịrị na otu ọgwụgwọ abụọ.

Mgbe ị na-eji vildagliptin (50 mg 2 ugboro / ụbọchị) n'otu oge na / na-enweghị metformin na insulin (nkezi nkezi nke 41 PIECES) na ndị ọrịa na nnwale ụlọ ọgwụ, akara HbA1c gosipụtara site na 0.72% belata nke ọma na njiri mara mbụ (ihe ngosi mbụ, nkezi nke 8.8%). Ọnọdụ nke hypoglycemia na ndị ọrịa a na-emeso dị ka nke a banyere ọrịa hypoglycemia n'òtù placebo.

Mgbe ị na-eji vildagliptin (50 mg 2 ugboro / ụbọchị) n'otu oge na metformin (> 1500 mg) na mgbakwunye na glimepiride (> 4 mg kwa ụbọchị) na ndị ọrịa na nnwale ụlọ ọgwụ, akara HbA1c na-agbadata n'ụzọ dị ukwuu site na 0.76% (site na nkezi nke 8.8%) .

Ndepụta nke analogues

Usoro onunu ogwu:

mbadamba ihe mkpuchi

1 otu mbadamba ihe mkpuchi fim nwere:
bekee arụ ọrụ: vildagliptin 50.0 mg na metformin hydrochloride 500.0 mg, 850.0 mg ma ọ bụ 1000.0 mg,
ndị na-ebu ụzọ: hyprolose, magnesium stearate, hypromellose, titanium dioxide (E 171), macrogol 4000, talc, iron oxide odo (E 172).
Mbadamba mbadamba 50 mg + 500 mg ọzọ na-etinye uhie oxide uhie (E172)

Nkọwa:
Mbadamba ihe mkpuchi. 50 mg + 500 mg: Mbadamba osisi oval nke gbara agba gbara agba, ihe mkpuchi na-acha odo odo, nke nwere odo na-acha pinki na-acha pinki. N’otu akụkụ nke mbadamba ihe akara a bụ “NVR”, n’akụkụ nke ọzọ - “LLO”.
Mbadamba ihe eji etinye fim, 50 mg + 850 mg: Mbadamba osisi oval na egbugbere ọnụ gbara agba, odo na-acha odo odo nwere agba nwere agbaji. N’otu akụkụ nke mbadamba nkume a ka akara aka "NVR", n’akụkụ nke ọzọ - "SEH".
Mbadamba ihe mkpuchi. 50 mg + 1000 mg: Mbadamba osisi oval nke gbara agba gburugburu, ihe mkpuchi gbara agba aja aja nwere agba nwere agbaji. N’otu akụkụ nke mbadamba nkume a ka akpọrọ “NVR”, n'akụkụ nke ọzọ bụ “FLO”.

Ihe mgbochi iji ogwu GALVUS MET

• ọdịda akụrụngwa ma ọ bụ ịrụ ọrụ ezinaụlọ nwere nsogbu: ya na ọkwa serin creatinine> 1.5 mg% (> 135 μmol / L) maka ụmụ nwoke na> 1.4 mg% (> 110 μmol / L)
• Ọnọdụ nnukwu nsogbu nke ị nwere ịmalite ịrịa ọrịa akụrụ: akpịrị ịkpọ nkụ (na ọnya afọ, ọgbụgbọ), ahụ ọkụ, ọrịa na-efe efe, ọnọdụ hypoxia (ujo, sepsis, ọrịa akụrụ, ọrịa bronchopulmonary).
• nnukwu obi na nkụda mmụọ, nnukwu ọrịa myocardial infarction, nnukwu ọrịa obi (oke ụjọ),
• okuku ume iku ume
• ọrụ imeju na-arụ ọrụ,
• acidosis akwara ma ọ bụ nke na-adịghị ala ala (gụnyere ketoacidosis mamịrị na mgbakwunye na ma ọ bụ na-enweghị coma). Ekwesịrị imezi ketoacidosis ọrịa mamịrị site na ọgwụgwọ insulin,
• lactic acidosis (gụnyere akụkọ ihe mere eme),
• Edeghị ọgwụ ahụ ụbọchị 2 tupu ịwa ahụ, radioisotope, ọmụmụ x-ray na ntinye nke ndị na - ahụ maka ọdịiche na n'ime ụbọchị 2 mgbe emechara ha,
• tụụrụ ime
• lactation
• ụdị shuga 1
• egbu egbu egbu, ị alcoholụ mmanya na-egbu egbu,
• rube isi na nri hypocaloric (ihe na-erughị 1000 kcal / ụbọchị),
• ụmụaka na-erubeghị afọ 18 (ikebeghị na nchekwa nke iji)
• hypersensitivity na vildagliptin ma ọ bụ metformin ma ọ bụ ihe ọ bụla ọzọ nke ọgwụ ahụ.

Ebe ọ bụ na ndị ọrịa nwere ọrụ imeju na-arụ ọrụ ụfọdụ, a chọpụtara lactic acidosis, nke nwere ike ịbụ otu n'ime mmetụta nke metformin, Galvus Met ekwesịghị iji ndị ọrịa nwere ọrịa imeju ma ọ bụ piramikal hepatic na-emebi emebi.

Na-akpachara anya, a na-atụ aro iji ọgwụ nwere metformin na ndị ọrịa karịa afọ 60, yana mgbe ị na-arụ ọrụ anụ ahụ dị ukwuu n'ihi oke ụba nke lactic acidosis.

Ngwongwo ogwu

Mlọ ọgwụ
Nhazi nke ọgwụ Galvus Met gụnyere ndị nnọchianya hypoglycemic abụọ nwere usoro dịgasị iche iche: vildagliptin, nke ndị klaasị dipeptidyl peptidase-4, na metformin (n'ụdị hydrochloride), onye nnọchite klas biguanide. Njikọ nke ihe ndị a na-enye gị ohere ijikwa ọkwa glucose ọbara ọbara n'ụzọ dị mma karịa ndị ọrịa nwere ụdị shuga 2 n'ime awa 24.

Vildagliptia
Vildagliptin, onye otu klaasị ndị na - akpali akpali nke ngwa ọrụ plọg, na - egbochi enzyme dipeptidyl peptidase-4 (DPP-4), nke na - emebi ụdị 1 glucagon-like peptide (GLP-1) na glucose-based insulinotropic polypeptide (HIP).
Ihe mgbochi na ngwa ngwa nke ọrụ DPP-4 na-ebute mmụba na ihe nzuzo nke nri nke GLP-1 na HIP site na eriri afọ banye na mgbasa ahụ nke ụbọchị.
Site na ịbawanye ọkwa nke GLP-1 na HIP, vildagliptin na-eme ka mmụba nke mkpụrụ ndụ panc-pancreatic reat-glucose na glucose, nke na-eduga n’ọganihu n’ime insulin na-egbochi glucose. Ogo nke mmezi nke ọrụ P-sel na-adabere n ’ogo mbibi mbụ ha, yabụ n’etiti ndị anaghị arịa ọrịa shuga mellitus (ya na plasma nkịtị), vildagliptin anaghị akpali insulin na-anaghị ebelata glucose.
Site na ịbawanye ọkwa nke GLP-1 nke endogenous, vildagliptin na-eme ka mkpụrụ ndụ кето to nwee glucose, na-eduga n'ịbawanye mma na nchịkwa glucose nke glucagon. Mbelata nke glucagon ngafe n’oge nri, n’aka nke ya, na-ebute mbelata nguzogide insulin.
Mmụba nke insulin / glucagon ruru megide ndabere nke hyperglycemia, n'ihi mmụba nke ọkwa nke GLP-1 na HIP, na-eme ka mbelata mmepụta glucose site na imeju ma n'oge nri, na -ebelata mbelata nke glucose ọbara.
Na mgbakwunye, megide ndabere nke iji vildagliptin, mbelata ọkwa nke lipids n'ọbara plasma mgbe e risịrị nri, ekwesịrị mmetụta a anaghị emetụta ya na nsonaazụ ya na GLP-1 ma ọ bụ HIP na mmụba na ọrụ nke mkpụrụ ndụ akwara pancreatic.
A maara na mmụba na GLP-1 nwere ike ibelata ikpu gastric, mana achọpụtaghị mmetụta a na iji vildagliptin. Mgbe ị na-eji vildagliptin na 5759 ndị nwere ụdị ọrịa shuga 2 nke mkpụrụ ọgwụ maka izu 52 dị ka monotherapy ma ọ bụ na njikọta metformin, ọgwụ sulfonylurea, thiazolidinedione, ma ọ bụ insulin, mbelata nke ukwuu ogologo oge na mkpokọta gemo nke glycated (HbA)_1c) na ibu ọnụ glukos ọbara.

Metformin
Metformin na - eme ka nnabata glucose dị n'etiti ndị ọrịa nwere ụdị ọrịa shuga nke abụọ site na iweda ọkwa glucose plasma ma na tupu nri. Metformin na-ebelata mmepụta nke glucose site na imeju, na -ebelata nnabata nke glucose na eriri afọ ma na-ebelata insulin iguzogide site na ịkwalite mbido na ojiji nke glucose site na nsụ anụ ahụ. N'adịghị ka usoro sulfanylurea, metformin adịghị akpata hypoglycemia na ndị ọrịa nwere ụdị ọrịa shuga 2 nke ọrịa mellitus ma ọ bụ na isiokwu siri ike (ma e wezụga n'ọnọdụ ndị pụrụ iche). Usoro ọgwụgwọ nke iji ọgwụ ahụ emeghị ka mmepe nke hyperinsulinemia. N'iji metformin mee ihe, insulin insulin anaghị agbanwe agbanwe, ebe ọkwa insulin plasma na-enweghị afọ na ụbọchị nwere ike ibelata.
Metformin na - akpali intracellular glycogen synthesis site na ịme ihe na glycogen synthase ma na - akwalite ụgbọ njem glucose site na protein protein na - ebugharị glucose ụfọdụ (GLUT-1 and GLUT-4).
Mgbe ejiri metformin mee ihe, enwere mmetụta bara uru na metabolism nke lipoproteins: mbelata ọkwa nke cholesterol, obere lipoprotein cholesterol na triglycerides, adịghị ejikọ ya na nsonaazụ nke ọgwụ na ịta ahụ na plasma.

Vildagliptin + Metformin
Mgbe ị na-eji ọgwụgwọ njikọta nke vildagliptin / metformin na usoro kwa ụbọchị nke 1500 - 3000 mg nke metformin na 50 mg nke vildagliptin maka afọ 1, a hụrụ ọnụ ọgụgụ dị ukwuu na-agbanwe agbanwe nke ọnụọgụ glucose ọbara (kpebiri site na mbelata n'ọkwa HbA_1c) na mmụba na oke nke ndị ọrịa nwere mbelata na HbA_1c ruru ọkara 0.6-0.7% (ma e jiri ya tụnyere ndị ọrịa nọ na-anata naanị metformin).
N'ime ndị ọrịa na-anata ngwakọta nke vildagliptin na metformin, mgbanwe ego na-emetụta ọnụ ọgụgụ ahụ dị ukwuu ma e jiri ya tụnyere ọnọdụ izizi. Izu iri abụọ na anọ ka mmalite nke ọgwụgwọ gasịrị, n'ime ìgwè ndị ọrịa na-anata vildagliptin na mgbakwunye metformin, a chọpụtara mbelata ọbara systolic na diastolic ọbara ma e jiri ya tụnyere ọnọdụ mbụ.

Edemede na-atọ ụtọ

Etu ị ga - ahọrọ ezi aha analog
Na pharmacology, a na-ekekarị ọgwụ iji mee ka okwu na analogues. Ihe mejuputara ya bu otu uzo ma obu ozo si aru aru nke nwere aru oru aru. Site na analogs bu ọgwụ ndi nwere ihe ndi ozo di ndu, mana ndi mmadu na acho ya.

Ọdịiche dị n’etiti nje virus na nje
Ọ bụ nje virus, nje, fungi na protozoa na-ebute ọrịa ndị na-efe efe. Ọrịa na-ebute nje na nje na-abụkarị. Agbanyeghị, ịmata ihe kpatara ọrịa ahụ pụtara ịhọrọ usoro ọgwụgwọ dị mma ga-enyere gị aka ịnagide ọrịa ngwa ngwa ọ bụghị imerụ nwa ahụ.

Ihe nfụkasị bụ ihe na-akpata otutu oge
Peoplefọdụ ndị maara ọnọdụ nwatakịrị na-arịakarị ụfụ na ogologo oge. Ndị nne na nna na-akpọrọ ya gaa na nke ndị dọkịta, na-ele ule, na-a drugsụ ọgwụ ọjọọ, n'ihi ya, a na-edebanye aha nwatakịrị ahụ na dọkịta ụmụaka mgbe ọ na-arịa ọrịa. Amaghị ihe kpatara ọrịa ọrịa iku ume ugboro ugboro.

Urology: ọgwụgwọ chlamydial urethritis
Chlamydial urethritis na-ahụkarị n’omume urologist. Ọ bụ Chlamidia trachomatis nke nje intracellular, nke nwere akụrụngwa nke nje na nje, nke na-achọkarị ọgwụ mgbochi ogologo oge maka ọgwụgwọ antibacterial. O nwere ike ibute oke urera na ụmụ nwoke na ụmụ nwanyị.