Yanumet (50

ʻO nā papa hoʻoili kiʻiʻoniʻoni, 50 mg / 500 mg, 50 mg / 850 mg, 50 mg / 1000 mg.

Aia ma ka papa papa

mea waiwai: citagliptin phosphate monohydrate 64.25 mg (e like me ka 50 mg sitagliptin manuahi manuahi) a me metformin hydrochloride 500 mg / 850 mg / 1000 mg.

nā mea hoʻowalewale: microcrystalline cellulose, polyvinylpyrrolidone (povidone), sosa stearyl fumarate, sodium lauryl sulfate, wai maʻemaʻe.

Hōʻike Shell no ka waihona o 50 mg / 500 mg: Opapela®II Pink 85 F94203 (ka waiū paona polyvinyl, ka titanium dioxide (E 171), macrogol / polyethylene glycol 3350, talc, ka hao hao kaomi (E 172), ka pōpoki hao pōpole (E 172)).

Hōʻike Shell no ka waihona o 50 mg / 850 mg: Opapela®II Pink 85 F94182 (ka waiū paona polyvinyl, ka titanium dioxide (E 171), macrogol / polyethylene glycol 3350, talc, ka hao hao kaomi (E 172), ka pōpoki hao pōpole (E 172)).

Hōʻike Shell no ka waihona o 50 mg / 1000 mg: Opapela®II Red 85 F15464 (ka waiū paona polyvinyl, ka titanium dioxide (E 171), macrogol / polyethylene glycol 3350, talc, ka hao hao kaomi (E 172), ka pōpoki hao pōkole (E 172).

50/500 mg papa:

ʻO nā papa kālai Capsule, biconvex, i uhi ʻia me ka uhi kiʻi o ke kukui ʻulaʻula māmā, me kahi pūpū extruded "575" ma ka ʻaoʻao hoʻokahi a hamama ma ka ʻaoʻao.

50/850 mg papa:

ʻO nā papa kālai Capsule, biconvex, i uhi ʻia me ka sarina ʻulaʻula mālamalama, me ke kākau ʻatikala "515" i ka ʻaoʻao hoʻokahi a hamama ma ka ʻaoʻao.

50/1000 mg nā pākaukau:

ʻO nā papa kālai Capsule, biconvex, i uhi ʻia me ka wahī ʻulaʻula ʻulaʻula, me ke kākau ʻia "577" i ʻekahi i kekahi ʻaoʻao a alualu i ka ʻaoʻao.

ʻO nā waiwai Pharmacological

Lapaʻau lāʻau

Ua ʻike ʻia nā haʻawina e pili ana i ka bioequivalence i nā mea hana olakino maikaʻi ʻo ka lawe ʻana iā Janumet (sitagliptin / metformin hydrochloride) he bioequivalent e lawe i ka sitagliptin phosphate a me metformin hydrochloride ʻokoʻa. Hōʻike nā ikepili e pili ana i ka waiwai pharmacokinetic o nā mea ikaika.

Hoʻopau Me ka pāloʻi waha o 100 mg, sitagliptin koke ke kō a hiki i ka pae ʻana o ka plasma kiʻekiʻe (median Tmax) ma hope o nā hola 1-4, ʻo ka pae ʻāleʻa ma lalo o ka pihi pākeke o AUC o sitagliptin i plasma he 8.52 mol • hola, Cmax 950 nmol . ^ E Ha yM. Hoʻonui ka AUC o ka sitagliptin i ka plasma me ka hoʻohālikelike i ka nui. ʻO ka bioavailability pololei o sitagliptin ma kahi o 87%. Mai ka hoʻokomo ʻia o ka sitagliptin a me ka meaʻai me ka momona momona kahi i kū ʻole ai i ka pharmacokinetics o ka lāʻau lapaʻau, hiki ke hoʻohana ʻia ka sitagliptin e pili ana i ka ʻai o ka meaʻai. Hoʻonui ka AUC o ka sitagliptin i ka plasma i ka like me ka nui o ka nui.

Kahele. ʻO ka nui o ka laha ʻana i ka hoʻohālikelike ma hope o ka lawe ʻana i ka nui o ka sitagliptin ma kahi o 100 mg e like me 198 lita. ʻO ka hapa o sitagliptin e hoʻohuli ʻia i ka protein koko koko he haʻahaʻa - 38%.

Hāpai. Ma kahi o 79% o sitagliptin e hoʻoponopono i ka loli. ʻO ka hoʻololiʻana o ka metabolic o ka lāʻau ke liʻiliʻi - ma kahi o 16% e hoʻopiʻi ʻia i ke ʻano o nā metabolites.

Leʻaleʻa. Ma hope o ka hoʻoponopono waha ʻana o ka sitagliptin 14C-hōʻailona ʻia e nā mea kōkua olakino, ma kahi o 100% o ka lāʻau ua hoʻopau ʻia no 1 hebedoma me nā paʻi a me ka urine o 13% a me 87%. ʻO ka hapalua o ka ola hope o ka t½ ma hope o ka hoʻokolokolo waha ʻana o sitagliptin ma kahi maʻa o 100 mg ka mea ma kahi o 12,4 hola. Hoʻokipa nā Sitagliptin i nā liʻiliʻi liʻiliʻi me ka hoʻohana pinepine ʻia ʻana. ʻO ka hoʻomaʻamaʻa Renal ma kahi o 350 ml / min.

Lawe ʻia ka ʻeka o ka sitagliptin e nā ʻōpū ma o ke ʻano o ka hana huna kanalicitic.

Naʻi maʻi mellitus. ʻO nā pharmacokinetics o sitagliptin i loko o nā mea maʻi me ka diabetes mellitus type 2 like i like me nā pharmacokinetics o nā mea ola olakino.

Hola paʻa kino hana. Ka ʻimi noiʻi ʻana i ka pharmacokinetics o ka nui o ka sitagliptin (50 mg) i nā mea maʻi me ka hana ʻole ʻole o ka māla, ka ʻoluʻolu (me ka creatinine clearance KK 50 - 80 ml / min), maʻalahi (KK 30 - 50 ml / min) a me ka hōʻeha (KK ma mua o 30 ml / min ) ʻoi aku ka paʻakikī, me ka poʻe maʻi me nā maʻi hope o ka hope o ka maʻi e kau nei i ka hemodialysis, hoʻohālikelike ʻia me nā mea maʻi maʻi.

I ka poʻe maʻi me ka hana renal maʻi ʻole o ka hōʻeha ʻeha, ʻaʻohe koʻikoʻi nui o ka nui i ka ʻike ʻana o ka sitagliptin i loko o ke koko koko i hoʻohālikelike ʻia me ka hui pū o nā mea hana olakino maikaʻi. Ma kahi o ka piʻi ʻana o 2 mau pa i ka sitagliptin AUC i ka plasma i ʻike ʻia i nā mea maʻi me ka hōʻemi kino ʻana i ka papaha, a ma kahi hoʻi he 4 kuli ka nui o ka sitagliptin AUC i ka plasma ua ʻike ʻia i nā mea maʻi me ka maʻi hōʻeha o ka renal, a me nā mea maʻi ma ka maʻi hope loa. ka mea nāna i hana i hemodialysis, hoʻohālikelike me kahi pūʻali mana o nā mea hana olakino maikaʻi. ʻO Sitagliptin kahi liʻiliʻi i hoʻopili ʻia i ka wā o hemodialysis (13.5% ma kahi hālāwai dialysis 3-4 hola, i hoʻomaka i nā hola 4 ma hope o ka lawe ʻana i ka lāʻau lapaʻau).

Mamua. ^ E Ha yM. I nā poʻe maʻi maʻi (65-80 mau makahiki), ʻo ka plasma kaila o ka sitagliptin he 19% kiʻekiʻe ma mua o nā mea maʻi ʻōpio.

E na keiki. ^ E Ha yM. ʻAʻole i hana ʻia nā haʻawina e pili ana i ka hoʻohana ʻana o sitagliptin i nā keiki.

Wehe, race, index body body index (BMI). ^ E Ha yM. ʻAʻohe pono e hoʻoponopono i ka hopena o ka lāʻau lapaʻau ma muli o ka wahine, ka lāhui a me ka BMI. ʻAʻole i loaʻa kēia mau ʻano i nā hopena lapaʻau nui loa i ka pharmacokinetics o sitagliptin.

Hoʻopau. ^ E Ha yM. Ma hope o ka hoʻoponopono waha ʻana o ka metformin, hiki ke hōʻea i ka tmax ma hope o nā hola 2.5. ʻO ka bioavailability piha o ka metformin, ke lawe nei i kahi papa 500 mg, ma kahi o 50-60% i nā mea hana olakino olakino. Ke hoʻokele waha ʻia, ʻo ka hapa ʻole i hoʻopaʻa ʻia ʻia he 20-30% a hoʻopiʻi ʻia me ka feces. ʻO nā pharmacokinetics o ke kōpili o ka metformin nonlinear. I ka wā e hoʻohana ai i ka metformin i nā pona i ʻōlelo ʻia, ua hōʻemi ʻia nā ʻike kūlā i loko o nā hola 24-48 a, me ke ʻano he kānāwai, ʻaʻole iʻoi aku ma mua o 1 μg / ml. I nā hoʻokolohua hoʻokolohua paʻa, ʻo ka piʻi ʻana o ka plasma kiʻekiʻe loa o ka metformin (Cmax) ʻaʻole iʻoi aku i ka 4 μg / ml, ʻoiai ke hoʻohana nei i nā nui loa. ʻO ka hoʻokolohua i ka manawa like o ka lāʻau i loko o kahi maʻi o 850 mg me ka meaʻai e hōʻemi i ke kiʻekiʻe a me ka helu o ke kō ʻana o ka metformin, i hōʻoia ʻia e ka hoʻoluhi ʻana o ka ʻai nui ʻana o ka plasma koko me 40%, kahi hōʻemi o AUC e 25% a me ka lōʻihi o ka manawa e hiki ai i ka pae kiʻekiʻe o ke kaila o ka plasma koko e 35 mau minuke. ʻAʻole ʻike ka ʻike koʻikoʻi o kēia hakahaka.

Kahele. Hoʻololi ka pilina ʻana no ka protein. Kahi ʻia ka metformin ma loko o nā ʻāpana koko ʻula. Ka haʻahaʻa loa i ke koko ma lalo o ke kō, a ua loaʻa ma hope o ka manawa o ka manawa like. ʻO nā kelepona ʻulaʻula pinepine ka hapa ʻē aʻe o ka māhele ʻelua o ka hoʻoili. Ka awelika Vd ma waena o 63 - 276 lita.

Hāpai. ^ E Ha yM. Hoʻopili ʻia ʻo Metformin i loko o ka urine.

Leʻaleʻa. ^ E Ha yM. ʻO ka wehe ʻana i ke kumu o ka metformin ka> 400 ml / min, ua hoʻopau ʻia ke lāʻau e ka filtration glomerular a me ka hilo huna. Ma hope o ka pau ʻana o ka waha, ʻo ka pau ʻana o ka hapalua o ka ola ma kahi o 6.5 mau hola. I ka hihia o ka hana renal impaired, hoʻomaʻemaʻe ka pale ʻana i ka hapa i ka pae o ka creatinine, ma muli o kēia e ka lōʻihi loa o ka hapalua ola, e alakaʻi ana i ka hoʻonui nui o ka metformin i ka plasma koko.

Lapaʻau lāʻau

ʻO Yanumet ka hui ʻana o ʻelua mau lāʻau hypoglycemic me kahi hana hoʻohui no ka hana: sitagliptin phosphate, kahi peptidyl peptidase 4 (DPP-4), a me ka metformin hydrochloride, he mākaʻikaʻi o ka papa biguanide, a ua hoʻolālā ʻia e hoʻomaikaʻi i ka hoʻomohala glycemic i ka poʻe maʻi me ka maʻi maʻamau.

Sitagliptin phosphate ehe ia ia, ka mea maʻi lōkuhi waha paʻa loa o ka enzyme dipeptyl peptidase 4 (DPP-4) no ka mālamaʻana i ka maʻi maʻi type 2. Inhibitors (DPP-4) kahi papa o nā lāʻau lapaʻau e hana ana me ka hoʻoulu ʻia o ka penupeneke. Ma ka hoʻokaʻawale ʻana i ka enzyme DPP-4, e hoʻonui ai ka sitagliptin i nā pae o ʻelua mau huaola hou i hoʻohui ʻia - peptide e like me ka peptide 1 (GLP-1) a me ka glucose-e hilinaʻi i ka insulinotropic polypeptide (HIP). ʻO ka incretins he ʻāpana o ka pūnaehana endogenous i komo i ka hoʻoponopono o ke kino o ka glucose homeostasis. ʻO kahi wale nō maʻamau a hoʻokiʻekiʻe ʻia paha o ka hoʻoliʻi koko, ʻo GLP-1 a me HIP ka hoʻonui ʻana i ka synthesis o ka insulin a me kona hoʻokuʻu ʻana mai nā cell beta pancreatic. Hoʻololi hoʻi ka GLP-1 i ka hana huna o ka glucagon e nā ʻāpana alpha pancreatic, e alakaʻi ana i ka hōʻemi o ka hana glucose glucose. ʻO Sitagliptin kahi paʻa ikaika a maikaʻi loa o ka mea paʻa o ka enzyme DPP-4 a ʻaʻole ia e pale i nā hui kokoke e pili ana i ka DPP-8 a i ʻole DPP-9. ʻOkoʻa ka Sitagliptin i kāna hana kemika a me nā hana a ka lāʻau lapaʻau mai nā kikowaena GLP-1, insulin, sulfonylureas a me ka meglitinides, biguanides, gamma receptor agonists i hana ʻia e ka peroxisome proliferator (PPARγ), nā alpha-glycosidase inhibitors a me nā amylin analogues.

ʻO ka hoʻohana pū ʻana o sitagliptin a me metformin ka hopena hoʻohui i ka neʻe ʻana o ka GLP-1 ikaika. ʻO Sitagliptin, akā ʻaʻole i metformin, e hoʻonui i ka kao o ka HIP ikaika.

Hāpai ka sitagliptin i ka mālama glycemic ʻelua ma ka monotherapy a me ka hoʻohui pū me nā lāʻau lapaʻau ʻē aʻe.

Ma nā hoʻokolohua lapaʻau, hoʻomaikaʻi ʻia ka sitagliptin monotherapy me ka hōʻemi nui ʻana i ka glycated hemoglobin A1c (HbA1c), me ka wikiwiki a ma hope o ka ʻaʻai glucose. ʻO ka emi ʻana o ke kaila plasma kaʻai ʻana i nānā ʻia e ka wiki 3 (kahi hopena mua). ʻO ka ulu ʻana o ka hypoglycemia i nā maʻi maʻi i mālama ʻia me ka sitagliptin e like me ka pletebo. ʻAʻole i hoʻonui ʻia ke kino o ke kino i ka wā o ka mālama ʻana me ka sitagliptin i hoʻohālikelike ʻia i ka waiwai mua.

Nā hana kiko o nā beta-cell e hōʻike ana, me ka HOMA-β, proinsulin i ka hoʻohālikelike ʻana o ka insulin a me nā ʻōkuhi o ka hoʻālaʻi ʻia o ka beta-cell i ka hōʻike ʻana i ka hoʻohaʻahaʻa glucose i nā hoʻokolohua pinepine e nānā ʻia.

Metformin hydrochloride he biguanide me ka hopena antihyperglycemic, e hoʻoemi ana i ka glucose glucose ma ka ʻōpū ʻole a ma hope o ka ʻai. ʻAʻole hōʻoluʻolu ka lāʻau lapaʻau i ka mea huna o ka insulin a no laila ʻaʻole alakaʻi i ka hypoglycemia.

Hana ʻia nā hana metformin e ʻekolu mau hana:

Holo i ka hana glucose i loko o ka ate ma ka pale ʻana i ka gluconeogenesis a me ka glycogenolysis,

Hoʻonui i ka hoʻomaʻamaʻa a me ka hoʻohana ʻana i nā kūmole i loko o nā kiko peripheral, ma ka ʻoi mākala me ka hoʻonui ʻana i ka naʻau o ka insulin.

e lohi ana i ka lilo ʻana o ka glucose i loko o ka ʻōpū.

Hoʻomoe ka Metformin i ka syntact glycogen intracellular ma o ka hana ʻana i ka synthetase glycogen, e hoʻonui ana i ka halihali glucose i nā ʻōmū membrane (GLUT-1 a me GLUT-4).

Hoʻopili i nā hopena hypoglycemic, ʻo ka metformin ke hopena maikaʻi ma ka lipid metabolism. I nā dosis therapeutic, ʻo ka metformin e hōʻemi i ka nui o ka kolamu, LDL a me nā triglycerides.

Nā hōʻailona no ka hoʻohana ʻana

Ua noi ʻia ʻo Janumet i li loko o ke ʻano o ka maʻi diabetes mellitus type 2, i hui pū ʻia me nā hana ʻole-lāʻau lapaʻau e hoʻoponopono ana i ke kiʻekiʻe o ka glucose koko, a me ka hoʻohui pū me nā lāʻau ʻē aʻe:

I ka hoʻohui ʻana i ka mea ʻai a me ka hoʻoponopono ʻana e hoʻomaikaʻi ai i ka mālama glycemic i loko o nā poʻe maʻi me ka lawa ʻole o ka hoʻokō ʻana o ka metformin monotherapy i ka pākēneka, ʻānō loa, a me nā mea maʻi e loaʻa nei ke ola me ka hui ʻana o ka sitagliptin a me ka metformin.

I ka hui pū ʻana me nā derivatives sulfonylurea (kahi hui pū me ʻekolu mau lāʻau) ka hoʻohui i ka meaʻai a me ka hoʻoponopono regimen i nā maʻi e loaʻa ʻole i ka mana glycemic kūpono i ka wā mālama me ka sulfonylurea a me ka metformin i ka nui loa i kāhea ʻia.

I ka hui pū ʻana me nā agonist receptor gamma i hoʻāla ʻia e peroxisome proliferator (PPAR-γ) (no ka laʻana, thiazolidinedione) (kahi hui pū me ʻekolu mau lāʻau) ma ke ʻano he meaʻaiʻai a me ka hoʻoponopono regiment i ka poʻe maʻi me ka lawa ʻole o ka hopena o ka lapaʻau me ka metformin a me ka PPAR-γ agonist i ka nui ʻana . ^ E Ha yM.

I ka hui pū me ka insulin (kahi hui o ʻekolu mau lāʻau) e hoʻohui i ka meaʻai a me ka hoʻoponopono regimen e hoʻomaikaʻi i ka mana glycemic i ka poʻe maʻi me ka lawa o ka maikaʻi o ka insulin a me ka metformin therapy.

ʻLoe a me ke kākele

Pono ke koho o ka ʻōlelo o ka lāʻau Yanumet, me ka noʻonoʻo ʻana i ka regimen mālama ʻānō o kēia manawa, ka hana a me ka hoʻomanawanui ʻana i ka mea maʻi, ʻaʻole iʻoi aku i ka nui o ka laʻana i kēlā me kēia lā o sitagliptin - 100 mg.

I ka haʻalele ʻana o ka mālama glycemic kūpono me ka monformin monotherapy i ka nui o ka hoʻomanawanui ʻia. Pono ka ʻōlelo mua o Yanumet e kau pū me kahi o sitagliptin 50 mg 2 mau manawa i kahi lā (nui o kēlā me kēia lā he 100 mg) a me ka manawa o metformin o kēia manawa.

Ke hoʻololi nei mai ka hoʻohui hui ʻana me ka sitagliptin a me ka metformin. ʻO ka ʻōmole mua o Yanumet e hoʻohālikelike me nā pona kikoo o ka sitagliptin a me ka metformin.

I ka haʻalele ʻana i ka kontrol glycemic kūpono, metformin hui hoʻohui i ka nui loa i ʻae ʻia i ka nui a me ka sulfonylurea. ʻO ka hopena o ka lāʻau Yanumet e pono e kau i kahi mahele o sitagliptin 50 mg 2 mau manawa i kahi lā (nui o kēlā me kēia lā o 100 mg) a me ka manawa o nā metformin o kēia manawa. Inā hoʻohana ʻo Janumet i hui pū me ka sulfonylurea, e pono e hōʻemi i ka nui o ka sulfonylurea e hōʻemi i ka hopena o ka hypoglycemia.

I ka haʻalele ʻana i ka kontrol glycemic kūpono, hui pū me ka metformin i ka nui loa i ʻae ʻia i ka nui o ka dosis a me PPAR-γ agonist. ʻO ka hopena o ka lāʻau Yanumet e pono e kau i kahi mahele o sitagliptin 50 mg 2 mau manawa i kahi lā (nui o kēlā me kēia lā o 100 mg) a me ka manawa o nā metformin o kēia manawa.

I ka haʻalele ʻana i kaomi glycemic kūpono me ka hui pū ʻana me nā lāʻau ʻelua - ka insulin a me ka metformin i ka nui o ka palena i ʻae ʻia. ʻO ka hopena o ka lāʻau Yanumet e pono e kau i kahi mahele o sitagliptin 50 mg 2 mau manawa i kahi lā (nui o kēlā me kēia lā o 100 mg) a me ka manawa o nā metformin o kēia manawa. Ke hoʻohana nei i ka lāʻau lapaʻau Janumet i hui pū me ka insulin, pono paha e hōʻemi i ka nui o ka insulin e pale i ka hōʻeha o ka hypoglycemia.

No ka hōʻoluʻolu o ka dosage, ʻo ka lāʻau Yanumet ka mea i loaʻa i ʻekolu mauʻu o 50 mg o ka sitagliptin me 500, 850 a i ʻole 1000 mg o ka metformin hydrochloride.

Pono nā maʻi āpau e mālama i kahi papaʻai me ka hoʻokaʻawale kūpono o nā hāmeʻe o kālaiʻu i ke ao holoʻokoʻa. Pono nā maʻi maʻi mākeke e hahai i kahi pākeke haʻahaʻa.

Pono e hoʻohana ʻo Yanumet i ʻelua manawa i ka lā me ka meaʻai, e hoʻonui lohi ana i ka momona, i mea e hōʻemi ai i ka hopena o nā hopena o ka ʻaoʻao mai ke ʻano o ka digestivein.

Nā hui ahonui kūikawā

ʻO nā mea maʻi me ka maikaʻi ʻole o ka pūpū. ^ E Ha yM. ʻAʻole koi ʻia ka hoʻoponopono ʻana o ka maʻi ma nā maʻi me nā pilikia ʻole o ka renal (CC ≥ 60 ml / min). ʻAʻole pono ʻo Janumet e kuhikuhi i nā mea maʻi me ka pilikia ʻole a i ʻole ka paʻakikī (CC