Nā ʻano o ka lālani vildagliptin * metformin * (vildagliptin * metformin *)

ʻO ka lāʻau lapaʻau hypoglycemic oral. Vildagliptin - he mākaukau o ka papa o ka hoʻoulu ʻana o ka insular apparatus o ka pancreas, sellyly pale i ka enzyme dipeptidyl peptidase-4 (DPP-4). ʻO ka wikiwiki a me ka hoʻopau ʻana i ka hana DPP-4 (> 90%) e hoʻonui ai i ka basal a me ka hoʻōla ʻia ʻana o ka meaʻai me ka peptide type 1 e like me ka GLP-1) a me ka glucose-hilinaʻi i ka insulinotropic polypeptide (HIP) mai ka ʻōpū i loko o ka ʻōnaehana ma waena o ke ao.

ʻO ka hoʻonui ʻana i nā ʻike o GLP-1 a me HIP, ʻo vildagliptin e hoʻonui i ka naʻau o ka pancreatic β-cells i ka glucose, e alakaʻi ai i kahi hoʻomaikaʻi ʻana i ka huna ʻana i ka glucose o ka glucose.

Ke koi nei i ka vildagliptin ma kahi o 50-100 mg i kēlā me kēia lā i nā mea maʻi me ka diabetes mellitus type 2, kahi hoʻomaikaʻi ʻana i ka hana o nā pancreatic β-cells ua ʻike ʻia. ʻO ka hoʻonui ʻia o ka hoʻomaikaʻi ʻana i ka hana o nā β-cell i hilinaʻi ʻia i ka nui o ko lākou hōʻeha mua ʻana, no laila i loko o ka poʻe i hōʻino ʻole i ka mellitus maʻi diabetes (me kahi pae kūlohelohe maʻamau i ka plasma koko), ʻaʻole ʻo ka vildagliptin e hoʻoulu i ka huna huna insulin a ʻaʻole e hōʻemi i ka glucose.

I ka hoʻonui ʻana i ka kao o ka endogenous GLP-1, hoʻonui ka vildagliptin i ka hoʻololi ʻana o nā seleka o ka glucose i ka glucose, e alakaʻi ai i kahi holomua o ka hoʻoponopono o ka glucose i kālai ʻia ʻana o ka paleona. ʻO ka emi ʻana o ke kiʻekiʻe o ka glucagon i ka wā o ka pāʻina, ma ka huli ʻana, e hoʻolohi i ka hōʻemi i ka pale ʻana i ka insulin.

ʻO ka hoʻonui ʻana o ka pāʻana o ka insulin / glucagon e kū'ē ana i ke kua o ka hyperglycemia, ma muli o ka hoʻonui ʻana o ka ʻike ʻana o ka GLP-1 a me ka HIP, ke hoʻolilo nei i ka emi ʻana o ka hana o ka glucose i ka ate ma ka lua o ka wā prandial a ma hope o kaʻai ʻana, ka mea e hiolo ai i ka hoʻoliʻiliʻi o ka glucose i plasma koko.

Eia kekahi, e kū'ē i ka ʻikepili o ka hoʻohana ʻana i vildagliptin, he hōʻemi i ka nui o nā lipids i ka plasma koko, akā naʻe, ʻaʻole pili kēia hopena me kona hopena i ka GLP-1 a i ka HIP a me kahi hoʻomaikaʻi hou i ka hana o nā huaʻai pancreatic β-cells.

Ua ʻike ʻia he piʻi nui ʻana o ka GLP-1 hiki ke hoʻolōʻihi i ka ʻōpū o ka gastric, akā ʻaʻole i nānā ʻia kēia hopena me ka hoʻohana ʻana o vildagliptin.

Ke hoʻohana nei i vildagliptin i 5795 nā mea maʻi me ka diabetes mellitus type 2 no nā 12 a 52 mau wiki he monotherapy a i hui pū ʻia me metformin, sulfonylurea derivatives, thiazolidinedione, a i ʻole insulin, he nui ka manawa lōʻihi o ka hōʻemi o ka neʻe o ka hemoglobin glycated (HbA1c) a me ka wikiwiki o ka hoʻoliʻi koko.

I ka manawa o ka hui pū ʻana o ka vildagliptin a me ka metformin i hoʻohana ʻia ma ke ʻano mua no ka poʻe maʻi me ka maʻi diabetes mellitus type 2, ua mālama ʻia ke ʻano o ka maʻi i ka HbA1c a me ke kaumaha o ke kino ma mua o 24 mau wiki e hoʻohālikelike ʻia me ka monotherapy me kēia mau lāʻau. ʻO nā hihia o ka hypoglycemia ka liʻiliʻi ma ka hui mālama ʻelua.

Ma kahi noiʻi haumania e hoʻohana ana i ka vildagliptin ma ke ʻano o 50 mg hoʻokahi i hoʻokahi lā no 6 mau mahina i nā maʻi me ka maʻi diabetes mellitus type 2 i hui pū ʻia me ka hōʻemi o ka renal moderate (GFR> 30 a 1500 mg) i hui pū me ka glimepiride (> 4 mg /) Ma ka hoʻokolohua lapaʻau, hōʻemi nui ka pae o ka HbA1c i ka uha ʻo 0.76% (baseline - he awelika o 8,8%).

Lapaʻau lāʻau

Hoʻopili koke ʻia ʻo Vildagliptin e ka ingestion me ka bioavailability piha o 85%. I loko o ka nui o nā pakano therapeutic, ʻo ka piʻi o Cmax o vildagliptin i loko o ka plasma a me ka AUC ma kahi kokoke i ke kiko o ka nui o ka lāʻau.

Ma hope o ka nānā ʻana i kahi ʻōpū ʻole, ʻo ka manawa e hiki ai i Cmax o vildagliptin i loko o ke koko koko he 1 h 45 min. Me ka hoʻoulu ʻana i ka meaʻai, ua emi iki ka nui o ka emi ʻana o ka lāʻau lapaʻau: aia ma laila ke emi ana o Cmax ma ka 19% a me ka hoʻonui ʻana i ka manawa i hiki ai i 2 mau hola 30 mau minuke. Eia naʻe, ʻaʻole pili ka ʻai i ke kiʻekiʻe o ka absorption a me AUC.

ʻO ka palena o ka vildagliptin i nā protein plasma he haʻahaʻa (9.3%). Hoʻohālikelike ʻia ka lāʻau lapaʻau ma waena o nā mika a me nā wahi koko ʻula. ʻO ka hoʻoili ʻia ʻana o vildagliptin e hiki pinepine ʻia ka nui, Vd i ka kūleʻa ma hope o ka lawelawe ʻana iv he 71 L.

ʻO Biotransformation ke ala nui o ka excretion o vildagliptin. I ke kino o ke kanaka, ua hoʻohuli ʻia ka 70% o ka nui o ka lāʻau. ʻO ka metabolite koʻikoʻi - LAY151 (57% o ka momona) he pharmacologically aktive a he mea ia o ka hydrolysis o ka māhele cyano. Ma kahi o 4% o ka loaʻaʻana o ka lāpō e lawe i ka hydrolysis amide.

Ma nā hoʻokolohua hoʻokolohua, ʻike ʻia kahi hopena maikaʻi o DPP-4 ma ka hydrolysis o ka lāʻau. ʻAʻole emailili ʻia ʻo Vildagliptin me ka komo ʻana o nā isoenzymes cytochrome P450. ʻAʻole ke kahua o Vildagliptin i kahi isoenzymes CYP450, ʻaʻole i pale i nā mea hoʻoneʻe ʻole i ka cytochrome P450 isoenzymes.

Ma hope o ka helu ʻana i ka lāʻau, ua pili ka 85% o ka nui ma ka ʻōpū a me 15% ma o ka ʻōpū, ʻo ka renal excretion o vildagliptin i loli ʻole he 23%. ʻO T1 / 2 ma hope o ka lawelawe waha ʻana he 3 hola paha, me ka manaʻo ʻole o ke ʻano.

Hoʻopilikia, ʻo ka hoʻomaʻamaʻa ʻana o ke ʻano hui kino, a me ka moʻomeheu i ka hopena o ka pharmacokinetics o vildagliptin.

Nā hōʻike no ka hoʻohanaʻana i ka lāʻau GALVUS

Kauka 2 diabetes mellitus:

• e like me ka monotherapy i ka hui ʻana me ka lāʻauʻai a me ka hoʻomaʻamaʻa ʻana,
• i ka hui pū me metformin ma mua o kahi lāʻau lapaʻau mua me ka lawa ʻole o ka hoʻokō ʻana o ka mālama ʻana i ka meaʻai a me ka hoʻomaʻamaʻa ʻana;
• ma ke ʻano he hui ʻelua o ka hui pū ʻana me ka metformin, derivatives sulfonylurea, thiazolidinedione a i ʻole insulin i ka hopena o ka hoʻoulu ʻia ʻana o ka meaʻai kūpono, hoʻomaʻamaʻa a me ka monotherapy me kēia mau lāʻau ʻana,
• ma ke ʻāpana o kahi hui triple: i hui pū ʻia me nā derivatives sulfonylurea a me ka metformin i nā mea maʻi i mālama mua ʻia me nā derogative sulfonylurea a me ka metformin e pili ana i kahi keʻakeʻa o ka meaʻai a me ka hoʻōla ʻana a me ka loaʻa ʻole i kahi kūpono glycemic control.
• ma ke ʻano he hui triple: i hui pū me ka insulin a me ka metformin i nā maʻi i loaʻa mua i ka insulin a me ka metformin ma ke keʻena o ka meaʻai a me ka hoʻomaʻamaʻa ʻana a ʻaʻole i hoʻokō i ka pono glycemic control.

Ka hoʻoponopono ʻia ʻana

Lawe ʻia ʻo Galvus i kahi ʻōlelo maʻamau, me he mea la o ka komo ʻana i ka meaʻai.

Pono ke koho ʻia o ka hoʻoponopono ʻia o ka lāʻau lapaʻau kūʻokoʻa e pili ana i ka hopena a me ka hikiʻole.

ʻO ke ʻano o ka lāʻau i manaʻo ʻia i ka wā o ka monotherapy a i ʻole ka mahele o ke ʻano hui ʻelua ʻelua me ka metformin, thiazolidinedione a i ʻole insulin (i ka hui pū me ka metformin a i ʻole metformin) he 50 mg a 100 mg o kēlā me kēia lā. I ka poʻe maʻi me ka maʻi maʻi ʻoi aku ka maʻi maʻamau 2 e loaʻa ana ka mālama me ka insulin, ua ʻōlelo ʻia ʻo Galvus i kahi maʻi o 100 mg i kēlā me kēia lā.

ʻO ka papa ʻōlelo ʻo Galvus i ʻōlelo ʻia ma ke ʻano he triple hui hoʻohui (vildagliptin + sulfonylurea derivatives + metformin) ka 100 mg i kēlā me kēia lā.

ʻO kahi paona o 50 mg i kēlā me kēia lā e pono e kuhikuhi i 1 mau wai i kakahiaka. Pono kahi wai o 100 mg no kēlā me kēia lā e 50 mg 2 mau manawa i ka lā ma ke kakahiaka a i ke ahiahi.

I ka manawa e lilo ai ma ke ʻāpana o ka hui pūnaehana ʻelua o nā mea me ka derony o ka sulfonylurea, e pili ana i ka pualapaʻa ʻia o Galvus he 50 mg 1 mau manawa i kēlā me kēia lā i ke kakahiaka. I ka hoʻohālikelike ʻia ʻana me ka derivatives o sulfonylurea, ʻo ka maikaʻi o ka lāʻau lapaʻau ma ka maʻa o 100 mg i kēlā me kēia lā ka like o ia ma ka hāleʻa 50 mg i kēlā me kēia lā. Me ka hopena ʻole o ka lāʻau lapaʻau e kūʻē i ka hope o ka hoʻohana ʻana o ka nui o ka lā i hāpai ʻia e mālama ʻia ai i kēlā me kēia lā o 100 mg, no ka mālama pono i ka glycemia, hiki ke loaʻa ka hopena hou aku i nā lāʻau maʻi hypoglycemic: metformin, sulfonylurea derivatives, thiazolidinedione a i ʻole insulin.

I nā maʻi me nā maʻi holi a me nā hana hepatic, ʻaʻole pono ka hoʻoponopono ʻana. I nā mea maʻi me ka hana ʻole a ʻoi paha ka hopena o ka renal (e komo pū ana me ka papa hana o ka hopena ʻole ʻana i ka maʻi hemodialysis), pono e hoʻohana ʻia ka lāʻau lapaʻau ma kahi o ka 50 mg hoʻokahi i hoʻokahi lā.

I nā mea maʻi ʻelemakule (> 65 mau makahiki), ʻaʻohe pono o ke hoʻoponopono ʻana i ka pauna dosage Galvus.

No ka mea ʻaʻohe ʻike a me ka hoʻohana ʻana i ka lāʻau lapaʻau i nā keiki a me nā ʻōpio i lalo o 18 makahiki o kona mau makahiki, ʻaʻole ia e noi ʻia e hoʻohana i ka lāʻau i loko o kēia ʻano o nā maʻi.

Loaʻa ka hopena

Ke hoʻohana nei iā Galvus ma ke ʻano he monotherapy a i hui pū ʻia me nā lāʻau lapaʻau ʻē aʻe, ʻo ka hapa nui o nā hopena ʻino e maloʻo ana, ka manawa kaʻawale, ʻaʻole i koi i ka hoʻokuʻu ʻana o ka maʻi. ʻAʻole i ʻike ʻia kahi hoʻoponopono ma waena o ka pinepine o nā ʻano hopena a me ka wā o ka makahiki, ka wahine, ka lāhui, ka lōʻihi o ka hoʻohana ʻana, a i ʻole hanana regimen.

ʻO ka pohā o ka angioedema i ka wā o ka mālama ʻana me Galvus ʻo> 1/10 000, 3 × VGN) ʻo 0.2% a i 0.3% paha, kēlā me kēia (hoʻohālikelike ʻia me 0.2% i ka pūnaehana hui). ʻO ka ulu ʻana o nā hana o nā huina o ka huina ma ka hapanui o nā hihia he asymptomatic, ʻaʻole i holomua, a ʻaʻole i mālama ʻia e nā loli cholestatic a i ʻole jaundice.

Ka ʻike o ka pinepine o nā hopena kū'ē: pinepine pinepine (> 1/10), pinepine pinepine ʻia (> 1/100, 1/1000, 1/10 000, 2.5 mau manawa nui aʻe ma mua o VGN).

No ka mea ʻo ka ʻike o ka hoʻohana ʻana iā Galvus i nā maʻi me ka pau ʻole o ka hana ʻole i ke koikoi i ka hemodialysis i kaupalena ʻia, e pono no e kuhikuhi ʻia ka lāʻau lapaʻau me ka mālama ʻana i kēia mahele o nā maʻi.

ʻO ka hoʻohanaʻana i ka lāʻau GALVUS i ka wā hāpai a me ka lactation

ʻAʻohe lawa nā ʻikepili e pili ana i ka hoʻohana ʻana o Galvus i nā wahine hāpai, a no laila ʻaʻole pono nā lāʻau o ka lāʻau i ka wā hāpai. I loko o nā pilikia o ka metabolism glucose impaired i nā wahine hāpai, loaʻa ka nui o ka hoʻouluʻana i ka anomalies congenital, a me ka pinepine o ka neonatal morbidity a me ka make.

Ma nā hoʻokolohua hoʻokolohua, i ka wā i kuhikuhi ʻia ai i nā pora he 200 mau manawa i ʻoi aku ma mua o ka mea i hōʻike ʻia, ʻaʻole ka hopena o ka lāʻau lapaʻau i ka ulu me ka ulu ʻana o ka embryo a ʻaʻole i hoʻoulu i ka hopena teratogenic ma ka pūpū.

No ka mea ʻaʻole i ʻike ʻia a hoʻopili ʻia ʻo vildagliptin i ka waiū kanaka, ʻaʻole pono e hoʻohana ʻo Galvus i ka wā lactation.

Nā ʻōlelo kikoʻī

No ka mea, i nā hihia līkole, hōʻike ʻia ka hoʻohana ʻana o ka vildagliptin i ka nui o ka hana o ka aminotransferases (maʻa mau ʻaʻole hōʻike hōʻike), ma mua o ke koho ʻana iā Galvus, me ka hoʻomaʻamaʻa pinepine ʻia i ka makahiki mua o ka mālama ʻana me ka lāʻau lapaʻau (1 mau manawa i 3 mau mahina), ke kuhi ʻia e hoʻoholo i nā ʻōhua biochemical o ka hana ate. Inā he hana nui ka mea maʻi o nā aminotransferases, pono e hōʻoia ʻia kēia hopena e kahi noiʻi lua, a laila e hoʻoholo pinepine i nā ʻōhua biochemical o ka ate hana a hiki i ko lākou hoʻomaʻamaʻa ʻana. Inā he 3 mau manawa i ʻoi aku ka hana o AST a i ʻole ALT ma mua o VGN (e like me ka hōʻoia ʻana ma nā haʻawina i hoʻohālike ʻia), ʻoi ʻia ke kāpae i ka lāʻau.

Me ka hoʻolālāʻana o ka jaundice a i ʻole nā ​​hōʻailona'ē aʻe o ka hana lūlū i ka manawa i ka wā e hoʻohana ʻia ai ʻo Galvus, pono koke e hoʻōki i ka lāʻau lapaʻau. Ma hope o ka hoʻohuihui ʻana i nā māka hana hana maʻi, ʻaʻole hiki ke hoʻomau ʻia ka lāʻau lapaʻau.

Inā pono, hoʻohana ʻia ka lāʻau insulin Galvus e hui pū pū me ka insulin. ʻAʻole pono e hoʻohana ʻia ka lāʻau lapaʻau i nā mea maʻi me ka diabetes mellitus type 1 a i ʻole no ka mālama ʻana i ka ketoacidosis maʻi.

Ke keu

Hoʻomaʻi maikaʻi ʻia ʻo Galvus i ka wā i hoʻokaʻawale ʻia ma kahi hapa a hiki i 200 mg i kēlā me kēia lā.

Nā hōʻailona: i ka wā e hoʻohana ai i ka lāʻau lapaʻau ma ke ʻano o 400 mg i kēlā me kēia lā, hiki ke ʻike ʻia ka ʻeha o ka naʻau, ʻā kekahi, ʻike ʻia ka pūpū a me ka parenthesia transient, maʻi, ʻūhā, a me ka hoʻonui hou ʻana i ka palu lipase (2 mau manawa kiʻekiʻe ma mua o VGN). Me ka hoʻonui o ka nui o ka maʻi o Galvus i 600 mg i kēlā me kēia lā, hiki i ka hoʻomohala ʻana o ka edema o nā huluhulu me ka paresthesias a me ka hoʻonui ʻana o ka manaʻo o CPK, ALT, C-reactive protein a me myoglobin hiki. ʻO nā ʻōuli āpau o kahi overdose a me nā loli i nā ʻāpana laboratorium e pau ma hope o ka hoʻokuʻu ʻana o ka lāʻau.

Hoʻomaʻamaʻa: ka wehe ʻana i ka lāʻau lapaʻau mai ke kino ma o ka dialysis ʻaʻole hiki ʻole. Eia naʻe, hiki ke hoʻoneʻe iki i ka hydrolytic metabolite nui o vildagliptin (LAY151) mai ke kino e ka hemodialysis.

Hoʻohui nūhou

He haʻahaʻa haʻahaʻa ʻo Galvus no ka hoʻopili ai i ka lāʻau.

No ka mea, ʻaʻole ʻo Galvus kahi papa o ka huina cytochrome P450, ʻaʻole ia e kālai ana a hoʻonāukiuki paha i kēia mau enzyme, ka pilina o Galvus me nā lāʻau lapaʻau he mau substrates, inhibitors, a i ʻole inducers o P450 i like ʻole. Me ka hoʻohana like ʻana o vildagliptin ʻaʻole i pili i ka helu metabola o nā lāʻau lapaʻau he poʻe hoʻohālikelike o nā enzyme: CYP1A2, CYP2C8, CYP2C9, CYP2C19, CYP2D6, CYP2E1 a me CYP3A4 / 5.

ʻO ke ʻano nui o ka maʻi ʻo Galvus me ka lāʻau lapaʻau e hoʻohana pinepine ʻia i ka mālama ʻia ʻana o ka maʻi mellitus type 2 (glibenclamide, pioglitazone, metformin) a i ʻole ka palena therapeutic liʻiliʻi (amlodipine, digoxin, ramipril, simvastatin, valsartan, warfarin) ʻaʻole i hoʻokumu.

ʻO ka wehewehe ʻana i ka lāʻau lapaʻau

Vildagliptin * + Metformin * (Vildagliptin * + Metformin *) - Lapaʻau

ʻO ka mana o ka lāʻau Vildagliptin * + Metformin * (Vildagliptin * + Metformin *) komo pū me nā manamana hypoglycemic like me nā ʻano hana like: vildagliptin, nona nā papa o ka peptidyl peptidase-4 inhibitors (DPP-4), a me ka metformin (i ke ʻano o ka hydrochloride) . ^ E Ha yM. ʻO ka hoʻohui ʻana o kēia mau mea e hiki ai iā ʻoe ke hoʻomalu hou aku i ka kaila o ke koko i ka poʻe maʻi me nā maʻi type 2 no 24 mau hola.

ʻO Vildagliptin, he mākaukau o ka papa hoʻonāukiuki o ka insular apparatus o ka pancreas, sellyly pale i ka enzyme DPP-4, ka mea e hoʻopau i ka type 1 glucagon-like peptide (GLP-1) a me ka glucose-dependantine insulinotropic polypeptide (HIP). Hoʻemi ka Metformin i ka hana o ka glucose i ka peka, e hōʻemi ana i ka lilo ʻana o ka glucose i loko o ka pūpoki a me ka hoʻohaʻahaʻa ʻana i ka kūleʻa o ka insulin ma o ka hoʻomaikaʻi ʻana i ka hoʻoulu ʻana a me ka hoʻohana ʻana i nā kūmole i nā kikoʻī peripheral.

Hoʻonui ka Metformin i ka syntact glycogen intracellular ma ka hana ʻana i ka synthetase glycogen a hoʻonui i ka halihali glucose i kekahi mau protein transporter glucose membrane (GLUT-1 a me GLUT-4).

ʻO ka wikiwiki a me ka hoʻopau ʻana i ka hana DPP-4 ma hope o ka vildagliptin e hoʻonui i ka basal a me ka hoʻowalewale ʻana i ka ʻai o GLP-1 a me HIP mai ka ʻōpū i loko o ka ʻōnaehana ʻōnaehana i ka lā.

Ke hoʻonui nei i ka kao o GLP-1 a me HIP, ʻo vildagliptin e hoʻonui i ka naʻau o ka pancreatic β-cells i ka glucose, e alakaʻi ai i kahi hoʻomaikaʻi ʻana i ka huna ʻana i ka glucose o ka glucose. Hōʻike ka nui o ka holomua o ka hana o ka β-cell i ka pae o ko lākou hōʻeha mua ʻana, no laila i loko o nā poʻe me ka maʻi mellitus ʻole (me ka neʻe ʻana o ka glucose i ka plasma koko), ʻaʻole ʻo ka vildagliptin e hoʻoulu i ka neʻe ʻana o ka insulin a ʻaʻole e hōʻemi i ka hoʻoliʻiliʻi glucose.

I ka hoʻonui ʻana i ka kao o ka endogenous GLP-1, hoʻonui ka vildagliptin i ka ʻike ʻana o nā β-cells i ka glucose, e alakaʻi ai i kahi holomua o ka hoʻoponopono o ka glucose i kālai ʻia ʻana o ka paleona. ʻO ka emi ʻana o ka hoʻohaʻahaʻa ʻia o ka glucagon ma hope o ka papa ʻaina, ma ka huli ʻana, e hoʻoneʻe i ka pale ʻana i ka insulin.

Ke hoʻonui nei i ka pae o ka insulin / glucagon e kū'ē ana i ke kua o ka hyperglycemia, ma muli o ka hoʻonui ʻana o ka neʻe o ka GLP-1 a me HIP, e hoʻolilo i ka emi ʻana o ka hana o ka glucose i ka ate ma ka wā a ma hope o ka ʻaina, ka mea e alakaʻi ai i ka emi o ke kaʻe o ka glucose i loko o ke koko koko.

Eia kekahi, e kū'ē i ka hope o ka hoʻohana ʻana o vildagliptin, kahi i hoʻohaʻahaʻa i ka hoʻoweliweli o lipids i ka plasma koko ma hope o ka māka ʻana o ka pāʻina, akā naʻe, ʻaʻole pili kēia hopena i kona hopena i ka GLP-1 a i ka HIP a me kahi hoʻomaikaʻi ʻana i ka hana o nā kuleana pālima pancreatic. Ua ʻike ʻia ka piʻi ʻana o ka neʻe o ka GLP-1 hiki ke alakaʻi i ka ʻohi ʻana i ka ʻōpū o ka ʻōpū, akā naʻe, i ke ʻano o ka hoʻohana ʻana o vildagliptin, ʻaʻole i mālama ʻia kēia hopena.

Ke hoʻohana nei i vildagliptin i 5759 nā mea maʻi me ka diabetes mellitus type 2 no 52 mau wiki i loko o ka monotherapy a i hui pū ʻia me metformin, derivl o ka sulfonylurea, thiazolidinedione, a i ʻole insulin, he nui ka manawa nui o ka hoʻoliʻihui ʻana o ka hemoglobin glycated (HbA1c) a me ka hoʻoliʻi ʻana i ka hoʻoliʻi koko.

Hoʻoulu ka Metformin i ka hoʻohaʻahaʻa glucose i nā maʻi me ka maʻi diabetes type 2 ma ka hoʻohaʻahaʻa ʻana i nā kukuna glucose glucose ma mua a ma hope o ka ʻai.

ʻAʻole i like me derivatives sulfonylurea, ʻaʻole ka metformin i ka hypoglycemia i nā mea maʻi me ka diabetes mellitus type 2 a i nā mea olakino paha (koe i nā maʻi kūikawā). ʻAʻole ke alakaʻi i ka lāʻau lapaʻau me ka hoʻomohala ʻana o ka hyperinsulinemia. Me ka hoʻohana ʻana o ka metformin, ʻaʻole i loli ka huna ʻana o ka insulin, ʻoiai e emi ana ka ʻike ʻana o ka insulin i ka plasma ma kahi ʻōpū ʻole a i ka lā e emi ana ka lā.

Me ka hoʻohana ʻana o ka metformin, ka hopena maikaʻi i ka metabolism o nā lipoproteins i ʻike ʻia: kahi hōʻemi o ke kaomi o ka kolamu nui, kolamu o ka lipoproteins haʻahaʻa haʻahaʻa a me nā triglycerides, ʻaʻole i hoʻopili ʻia me ka hopena o ka lāʻau lapaʻau ma ka paʻa ʻana o ka glucose i ka plasma koko.

Ke hoʻohana nei i ka hopena hui me vildagliptin a me ka metformin i loko o nā lā i kēlā me kēia lā 1,500-3,000 mg o ka metformin a me 50 mg o vildagliptin 2 mau manawa / lā no 1 makahiki, he kupanaha ka nui a ka statistically i ka emi ʻana o ka hoʻoliʻoli ʻana o ke koko i mālama ʻia (i hoʻoholo ʻia e ka hoʻemi ʻana i ka HbA1c) a me ka hoʻonui ʻana ma ka hapa o ka poʻe maʻi me ka hoʻemi. ʻAʻole i emi ka hoʻoulu ʻana o HbA1c ma ka 0.6-0.7% (i hoʻohālikelike ʻia me ka pūʻulu o nā maʻi e hoʻomau wale nei i loaʻa i nā metformin).

I ka poʻe maʻi e loaʻa ana i ka hui pū ʻana me vildagliptin a me ka metformin, he loli nui i ka nui o ke koʻikoʻi o ke kino i hoʻohālikelike ʻia me nā kūlana mua. 24 mau pule ma hope o ka hoʻomaka ʻana o ka hoʻōla ʻana, ma nā pūʻulu o nā mea maʻi e loaʻa ana i ka vildagliptin i hui pū me ka metformin, i ka emi ʻana o ko systolic a me ka diastolic i ke koko i nā mea maʻi me ka maʻi hypertension arterial.

I ka manawa o ka hui pū ʻana o ka vildagliptin a me ka metformin i hoʻohana mua ʻia no ka mālama mua ʻana no nā poʻe maʻi me ka maʻi diabetes mellitus type 2, ua nānā ʻia ka nui o ka maʻi ma nā helu HbA1c ma mua o 24 mau wiki i hoʻohālikelike ʻia me ka monotherapy me kēia mau lāʻau. ʻO nā hihia o ka hypoglycemia ka liʻiliʻi ma ka hui mālama ʻelua.

Ke hoʻohana nei i vildagliptin (50 mg 2 mau manawa / lā) i ka manawa me ka / me ke metformin e hui pū me ka insulin (awelika o ka hopena o 41 PIECES) i nā mea maʻi i ka hoʻokolohua lāʻau ʻana, ʻo ka māka o ka HbA1c ua hōʻemi nui ia e ka 0.72% (i ka kuhikuhi mua, ka awelika o 8.8%). ʻO ka ulu ʻana o ka hypoglycemia i nā maʻi maʻi i mālama ʻia i ka hoʻohālikelike ʻana o ka hypoglycemia ma ka hui plasebo.

Ke hoʻohana nei i vildagliptin (50 mg 2 mau manawa / lā) i ka wā like me ka metformin (> 1500 mg) hui pū me ka glimepiride (> 4 mg i kēlā lā) i nā mea maʻi i ka hoʻokau kūpaʻa maʻi, ʻo ka mākaukau ʻo HbA1c e hōʻemi nei i ka uleʻa o 0.76% (mai kahi awelika o 8.8%) . ^ E Ha yM.

Kahi papa inoa o nā kūmole

Nā palapala ʻano:

pani ʻ -lelo ʻlelo

1 papa pāahī-kiʻi e pili ana:
mea waiwai: vildagliptin 50.0 mg a me metformin hydrochloride 500.0 mg, 850.0 mg a 1000.0 mg,
nā mea hoʻowalewale: hyprolose, magnesium stearate, hypromellose, titanium dioxide (E 171), macrogol 4000, talc, ka hao hao oxide (E 172).
50 mg + 500 mg film-coated tablet hoʻohui pū kekahi i nā ʻili hoʻohuihui ulaula (E172)

‘:Lelo:
Nā papa hana ʻulaʻī. 50 mg + 500 mg: nā papa oval me nā kihi beveled, hoʻoponi i ka ʻoni, māmā me ke aniani pinkish. Ma kekahi ʻaoʻao o ka pākaukau ke hōʻailona nei "NVR", ma kēlā ʻaoʻao - "LLO".
ʻO nā papa hana ʻoniʻoni, 50 mg + 850 mg: nā papa oval me nā kihi beveled, ʻoniʻoni i ulana ʻia me ke kala hina. Ma kekahi ʻaoʻao o ka papa pāku i hōʻailona ʻia "NVR", ma kēlā ʻaoʻao - "SEH".
Nā papa hana ʻulaʻī. 50 mg + 1000 mg: nā papa oval me nā kihi beveled, ʻoniʻoni me ke aniani hina. Ma kekahi ʻaoʻao o ka papa ua hōʻailona ʻia “NVR”, ma ka ʻaoʻao ʻo “FLO”.

Nā maʻi hoʻohālikelike i ka hoʻohana ʻana i ka lāʻau GALVUS MET

• hana ʻole ʻole a i ʻole ke hanana ʻana ʻole: a me ka pae serum creatinine> 1,5 mg% (> 135 μmol / L) no nā kāne a me> 1,4 mg% (> 110 μmol / L) no nā wahine,
• nā hana ʻoi me ka pilikia o ka hoʻomohala ʻana i ka hana renal: dehydration (me ka maʻi ʻaʻa, ka luaʻi), ke ʻano, ka maʻi maʻi o ka maʻi maʻi, nā maʻi o ka hypoxia (haʻalulu, sepsis, maʻi maʻi, nā maʻi bronchopulmonary).
• ʻoi a ka hopena puʻuwai a me ka palaualopiko o ka wīkō, kaʻai o ka myocardial infarction, ka maʻi cardiovascular failed (kūwī),
• pauna aho hanu
• lawelawe aho ʻaia,
• ka huaka a ʻo ka metabolic acidosis ʻoiʻi (me ka ketoacidosis maʻi i hui pū ʻia a i ʻole coma). Pono ke hoʻoponopono i ka ketoacidosis Diabetic e nā lāʻau insulin,
• lactic acidosis (me ka mōʻaukala),
• ʻAʻole i kuhikuhi ʻia ka lāʻau lapaʻau i 2 mau lā ma mua o ka hoʻokō ʻana, ka radioisotope, nā haʻawina x-ray me ka hoʻomaka ʻana o nā mea hoʻohālikelike a i loko o 2 mau lā ma hope o ke hoʻokō ʻana,
• hapai
• lactation
• maʻi diabetes type 1
• humuhinu maoli, huakino makehewa,
• ka mālama ʻana i kahi meaʻai hypocaloric (ʻoi aku ma mua o 1000 kcal / lā),
• nā keiki ma lalo o 18 mau makahiki o ka (a me ka palekana a me ka palekana o ka hoʻohana ʻaʻole i hoʻopaʻa ʻia),
• hypersensitivity i vildagliptin a i metformin a i ʻole kekahi mea like o ka lāʻau.

No ka mea, ua mālama ʻia nā maʻi me ka poli o ka puʻuwai i kekahi mau hihia, ua hōʻike ʻia ka acidosis lactic, ʻo ia paha kekahi o nā hopena ʻaoʻao o ka metformin, ʻaʻole pono ʻo Galvus Met i ka poʻe maʻi me nā maʻi o ka maʻi a i ʻole nā ​​mea maʻi hepatic biochemical hepatic.

Me ka mālama aka, ua aʻo ʻia e hoʻohana i nā lāʻau lāʻau e pili ana i ka metformin i nā mea maʻi ma luna o 60 mau makahiki o ka makahiki, a i ka wā e hoʻokō ai i ka hana kino koʻikoʻi ma muli o ka piʻi nui o ka lolo lactic.

ʻO nā waiwai Pharmacological

Lapaʻau lāʻau
ʻO ka pūnāwai o ka lāʻau Galvus Met ka mea komo ʻelua mau pūmole hypoglycemic me nā ʻano hana like ʻole: vildagliptin, no ka papa o ka dipeptidyl peptidase-4 inhibitors, a me metformin (ma ke ʻano o ka hydrochloride), he mākaukau o ka papa biguanide. ʻO ka hui pū ʻana o kēia mau mea e hiki ai iā ʻoe ke hoʻomaikaʻi maikaʻi i ka pae o ke kaila koko i loko o nā mea maʻi me ka diabetes type 2 i loko o 24 mau hola.

Vildagliptia
ʻO Vildagliptin, kahi lālā o ka papa o ka hoʻoulu ʻana o ka ʻāpana pancreatic apparatus, selectively kāohi ʻia i ka enzyme dipeptidyl peptidase-4 (DPP-4), ka mea e luku aku i nā type 1 like me ka peptide glucagon-like (GLP-1) a me ka glucose-dependantine insulinotropic polypeptide (HIP).
Hoʻopau ka wikiwiki a me ka hoʻopau ʻana i ka hana DPP-4 e hoʻonui i ka pā kumu a me ka hoʻowalewale ʻia ʻana o ka ʻai me GLP-1 a me HIP mai ka ʻōpū i loko o ka ʻōnaehana ʻōnaehana i ka lā a pau.
Ma ka hoʻonui ʻana i nā pae o GLP-1 a me HIP, ua hoʻonā ka vildagliptin i ka nui o ke kaohi ʻana o ka pancreatic β-cells i ka glucose, e alakaʻi ai i kahi hoʻomaikaʻi ʻana i ka huna ʻana i ka glucose o ka glucose. ʻO ka pae o ka hoʻomaikaʻi ʻana i ka hana o nā p-cell ka mea i hilinaʻi i ka pae o ko lākou hōʻeha mua ʻia, no laila i loko o ka poʻe i ʻike ʻole i ka mellitus maʻi diabetes (me ka glucose kaila maʻamau), ʻaʻole ʻo ka vildagliptin e hoʻoulu i ka huna huna ʻana a ʻaʻole e hōʻemi i ka glucose.
Ma ka hoʻonui ʻana i nā pae o ka endogenous GLP-1, hoʻonui ka vildagliptin i ka ʻike ʻana o nā cell клеток i ka glucose, e alakaʻi ai i kahi holomua o ka hoʻoponopono o ka glucose i kālai ʻia ʻana o ka paleona glucagon. ʻO ka emi ʻana o ke kiʻekiʻe o ka glucagon i ka wā o ka pāʻina, ma ka huli ʻana, e hoʻolohi i ka hōʻemi i ka pale ʻana i ka insulin.
Ke hoʻonui nei i ka pae o ka insulin / glucagon e kū'ē ana i ke kua o ka hyperglycemia, ma muli o ka hoʻonui nui ʻana o nā pae o ka GLP-1 a me HIP, e hōʻemi ana i ka hoʻoliʻina o ka glucose ma ka ate ma ka wā a ma hope o ka ʻaina, kahi e hoʻohemo ai i nā pae o ka glucose koko.
Eia kekahi, e kū'ē i ka ʻikepili o ka hoʻohana ʻana i vildagliptin, he hoʻohaʻahaʻa i ka pae o lipids i ka plasma koko ma hope o ka māka ʻana o ka pāʻina, akā naʻe, ʻaʻole pili kēia hopena i kona hopena i ka GLP-1 a i ka HIP a me kahi hoʻomaikaʻi hou i ka hana o nā kōlapa isela pancreatic.
Ua ʻike ʻia he piʻi nui ʻana o ka GLP-1 hiki ke hoʻolōʻihi i ka ʻōpū o ka gastric, akā ʻaʻole i nānā ʻia kēia hopena me ka hoʻohana ʻana o vildagliptin. Ke hoʻohana nei i vildagliptin i 5759 nā mea maʻi me ka diabetes mellitus type 2 no 52 mau wikiʻa e like me ka monotherapy a i hui pū ʻia me nā metformin, derivl o ka sulfonylurea, thiazolidinedione, a i ʻole insulin, he nui ka manawa lōʻihi o ka hōʻemi o ka neʻe o ka hemoglobin glycated (HbA_1c) a me ka hookeai koko i ke koko.

Metformin
Hoʻoulu ka Metformin i ka hoʻohaʻahaʻa glucose i nā maʻi me ka diabetes type 2 ma ka hoʻohaʻahaʻa ʻana i nā pae glucose glucose ma mua a ma hope o ka ʻai. Hoʻemi ka Metformin i ka hana o ka glucose i ka peka, e hōʻemi ana i ka lilo ʻana o ka glucose i loko o ka pūpoki a me ka hoʻohaʻahaʻa ʻana i ka kūleʻa o ka insulin ma o ka hoʻomaikaʻi ʻana i ka hoʻoulu ʻana a me ka hoʻohana ʻana i nā kūmole i nā kikoʻī peripheral. ʻAʻole i like me derivatives o sulfanylurea, ʻaʻole ka metformin i ka hypoglycemia i nā mea maʻi me ka diabetes mellitus type 2 a i nā kumuhana olakino paha (koe i nā maʻi kūikawā). ʻAʻole ke alakaʻi i ka lāʻau lapaʻau me ka hoʻomohala ʻana o ka hyperinsulinemia. Me ka hoʻohana ʻana o ka metformin, ʻaʻole i loli ka neʻe ʻana o ka insulin, ʻoiai e pae ʻia nā pae o ka insulin i ka ʻōpū ʻole a i ka lā e emi ana ka lā.
Hoʻokomo ka Metformin i ka syntact glycogen intracellular ma o ka hana ʻana ma ka synthase glycogen a hoʻonui i ka halihali glucose i kekahi mau protein transporter glucose membrane (GLUT-1 a me GLUT-4).
I ka wā e hoʻohana ai ka metformin, he hopena maikaʻi i ka metabolism o ka lipoproteins i ʻike ʻia: kahi emi o ke kiʻekiʻe o ka kolamu, ka lipoprotein haʻahaʻa haʻahaʻa a me nā triglycerides, ʻaʻole i pili pū me ka hopena o ka lāʻau lapaʻau ma ka glucose glucose glucose.

Vildagliptin + Metformin
Ke hoʻohana nei i ka hopena hui o vildagliptin / metformin i nā lā he 1500 - 3000 mg o ka metformin a me 50 mg o vildagliptin no 1 makahiki, he kupanaha ka nui o ka helu i loko o ka neʻe o ka hoʻokaʻawale ʻana o ke koko i mālama ʻia (i hoʻoholo ʻia e ka hoʻēmi ʻana ma ka pae o HbA_1c) a me ka hoʻonui ʻana o ka hapa i nā poʻe maʻi e hoʻemi ana i ka HbA_1c mau kālā ma ka liʻiliʻi he 0.6-0.7% (hoʻohālikelike ʻia me ka pūʻulu o nā maʻi i hoʻomau i loaʻa i ka metformin wale nō).
I ka poʻe maʻi e loaʻa ana i ka hui pū ʻana me vildagliptin a me ka metformin, he loli nui i ka nui o ke koʻikoʻi o ke kino i hoʻohālikelike ʻia me nā kūlana mua. 24 mau pule ma hope o ka hoʻomaka ʻana o ka hoʻōla ʻana, ma nā pūʻulu o nā maʻi e loaʻa ana i ka vildagliptin i hui pū me ka metformin, kahi i hoʻemi ʻia o ka systolic a me ka diastolic blood pressure ua hoʻohālikelike ʻia me ke kūlana mua.

Nā manaʻo hoihoi

Pehea e koho ai i ka analog kūpono
I loko o ka pharmacology, hoʻokaʻawale pinepine nā lāʻau i nā ʻ synlelo a me nā kikowaena. Hoʻokomo ʻia i ke ʻano o nā like o nā ʻano like ʻole i ke ʻano he hopena therapeutic ma ke kino. Ke hoʻohālikelike nei nā analogs i nā lāʻau lapaʻau e pili ana i nā ʻano like like ʻole, akā no ka mālama ʻana i nā maʻi like.

ʻO nā ʻokoʻa ma waena o nā maʻi a me nā maʻi bacterial
Hoʻopilikia ʻia nā maʻi maʻi e nā maʻi, nā maʻi, nā fungi a me ka protozoa. ʻO ke ʻano o nā maʻi i hoʻomake ʻia e nā maʻi a me nā maʻi like ʻole. Eia nō naʻe, e hoʻokaʻawale i ke kumu o ka maʻi ke koho ʻana i ka mālama kūpono e kōkua nui i ka hoʻokē ʻana i ka malaise a hōʻeha ʻole i ke keiki.

ʻO nā maʻi āpau ke kumu o ke anuanu pinepine
ʻIke kekahi poʻe i kahi kūlana i kahi pinepine ke keiki a a lōʻihi no ka manawa anuanu. Lawe nā mākua iā ia i nā kauka, lawe i nā hoʻokolohua, lawe i nā lāʻau lapaʻau, a ma muli o ke ʻano, ua hoʻopaʻa inoa ʻia ke keiki me ke keiki e like me ka maʻi nui. ʻAʻole i ʻike ʻia nā kumu maoli o nā maʻi ʻeha pinepine.

Urology: hana maʻi urethritis chlamydial
Loaʻa pinepine ʻia Chlamydial urethritis ma ka hana o kahi urologist. Hoʻokumu ʻia e ka intracellular parasite Chlamidia trachomatis, aia nō nā waiwai o nā huakini a me nā maʻi like, ua makemake pinepine i ka antibiotic therapy regimens no ka maʻi antibacterial. Hiki iā ia ke hana i ka mumū ʻole o ka maʻi o ka urethra i nā kāne a me nā wahine.