Vildagliptin - nā ʻōlelo aʻoaʻo no ka hoʻohana ʻana, nā kikowaena kūloko a me nā kumukūʻai

ʻAʻole hiki ke hoʻomau i ka hilahila me ke kōkua o nā meaʻai liʻiliʻi haʻahaʻa a me ke ʻano kino o nā mea make. Hoʻonui ka hopena o ka papa hana i kēlā me kēia makahiki. I ia mau hihia, hiki i nā papa o vildagliptin, kahi huaʻomaʻi hypoglycemic hanauna hou me ka hana ʻokoʻa ʻole e hōʻeuʻeu a i ʻole e pale ai, akā e hoʻihoʻi i ka pilina i loko o ka mokuʻāina ma waena o nā selela α a me β o nā pancreas, hiki ke kōkua.

Pehea ka lele a palekana paha no ka hoʻohana lōʻihi, a he aha ka wahi e noho ai ka vildagliptin i waena o nā analogs kūloko a me nā mea hoʻonaninani antidiabetic hou aku?

ʻO ka mōʻaukala o ka ulu puke

I ka makahiki 1902, ma Lādana, ʻelua mau kahikaha o ka naʻau kula Ernest Starling a me William Bylize i ʻike i kahi mea i loko o nā ʻōpū o ka puaʻa e hoʻoulu ʻia ai ka pancreas. 3 mau makahiki i hala mai ka ʻike abstract a hiki i kona hoʻokō maoli ʻana. I ka makahiki 1905, ua kuhikuhi ʻo Kauka Benjamin More mai Liverpool i kahi maʻi o ka maʻi maʻi maʻi 2 me kahi hapa o ka membrane mucous i ka duodenum puaʻa 14 g ʻekolu mau manawa i ka lā. I ka malama mua o ia ʻano mālama, hoʻōla ka paʻakai o ka urine mai 200 g a 28 g, a ma hope o 4 mau mahina ʻaʻole i hoʻoholo ʻia i ka ʻimi ʻana, a hoʻi ka mea maʻi i ka hana.

ʻAʻole i loaʻa ka manaʻo i ka hoʻolālā hou ʻana, no ka mea ia manawa ua nui nā manaʻo like ʻole e pili ana i ka mālama ʻana i ka maʻi maʻi ma waena, akā ua uhi ʻia nā mea āpau e ka loaʻa ʻana o ka insulin i ka 1921, no ka manawa lōʻihi i nalo aʻe nā mea āpau. Ke hoʻomau nei ʻia ka noiʻi ʻana i ka pume (ʻo ka mea i kapa ʻia ʻo ka waiwai i ka mucus ma ka ʻaoʻao kiʻekiʻe o ka ʻōpū porcine) wale nō ma hope o 30 mau makahiki.

I nā makahiki 60 o nā kenekulia hope, ua hōʻike ka poʻe aʻoaʻo ʻo M. Perley a me H. Elric i hopena hopena i hoʻonui ʻia: hoʻonui i ka hana o ka insulin i ka pae ʻana o ka hana glucose waha i hoʻohālikelike ʻia me ka infra intravenous.

I nā makahiki 70s, ua ʻike ʻia kahi glucose insulin -ropyp polypeptide (HIP) i ʻike ʻia, ka synthesize o nā pā o ka pūpū. ʻO kāna mau hana e hoʻonui i ka biosynthesis a me ka hoʻonaʻauao glucose i hilinaʻi ʻia o ka insulin, me ka lipogenesis hepatic, nā mākala a me ka kiko o ka adipose, hoʻonui i nā pūpū P, nā māhuahua i ko lākou naʻau i ka apoptosis.

I nā makahiki 80, ua paʻi ʻia nā lono ma ka noiʻi ʻana o nā peptide like 1 glucagon-like (GLP-1), nā mea L a nā selela mai ka proglucagon. He hana kekahi i ka hana insulinotropic. Ua wehewehe ʻo Profesor G. Bell i kona ʻano a hōʻike i kahi vector hou no ka ʻimi ʻana no kahi ala mua i ka mālama ʻana i ka maʻi maʻi maʻi (hoʻohālikelike ʻia me nā metformin kūlohelohe a me ka hoʻomākaukau o ka olani.

Ke piʻi nei ka wā o ka incretins i ka makahiki 2000, i ka wā i hala ʻole ʻole ai ka hopena o ka honua, a ua hāʻawi ʻia ka leka mua ma US Congress ma kahi ʻo Profesor Rottenberg i hōʻike i kekahi mea DPP 728 me ka palau, me ka manaʻo ʻole i ka meaʻai, e kāohi ana i ka DPP-4 i loko o nā kānaka.

ʻO ka mea hana o ka inhibitor mua o DPP 728 (vildagliptin) ʻo Edwin Willhauer, he limahana o ka ʻepekema ʻekepili o ka hui Swiss Novartis.

He mea kūpono ka molekue ka mea e hoʻopaʻa paʻa ai ma o ka oxygen i ka waikawa amino e kuleana ana i ka hana catalytic o ka hoʻomāneʻalohi pilikino DPP-4.

Loaʻa i ka waiwai i kona inoa mai nā huaʻōlelo ʻekolu o kona inoa inoa - VIL, YES - Dipeptidyl Amine Peptidase, GLI - ka hopena i hoʻohana ai ʻo WHO i nā lāʻau antidiabetic, TIN - ʻo ka ʻeha e hōʻike nei i kahi inhibitor enima.

Hiki ke noʻonoʻo ʻia ka hoʻokō i ka hana a ke Kauka E. Bossi, ma laila ua ʻōlelo ʻia ʻo ka hoʻohana ʻana o vildagliptin me ka metformin e hōʻemi ana i ka helu o ka hemoglobin glycosylated ma mua o ka 1%. Ma kahi o ka hōʻemi ikaika o ka huka, nā lāʻau lapaʻau i nā mea'ē aʻe:

• Hoʻemi i ka hopena o ka hypoglycemia e 14 mau manawa, ke hoʻohālikelike ʻia me nā derivatives o ka sulfonylurea (PSM);
• Me kahi papa hana lōʻihi, ʻaʻole loaʻa ka mea maʻi i ka paona;
• Hoʻoulu i ka hana β-cell.

ʻAʻole e like me nā algorithms ʻAmelika e waiho i ka vildagliptin ma ka 2 o nā lālani haʻahaʻa i ke kō, e hoʻokomo nā kauka Lūkini i ka incretins ma 1-2-3 wahi i ke koho ʻana i nā lāʻau hypoglycemic, ʻoiai ka mea nui loa i kēia mau lā ka hoʻomākaukau a sulfanilurea.

Vildagriptin (kahi inoa inoa o ka lāʻau lapaʻau ʻo Galvus) i kū mai ma ka mākeke lāʻau Lūkini ma 2009.

Ua hele mai nā kānaka ʻepekema Lūkini i ka hopena he pono ke koho i nā hui pū ʻana o ka glycemia normalization me Galvus i hui pū me nā ʻano lāʻau like ʻole e pili ana i nā ʻano like ʻole o ka hoʻomohala ʻana o ka maʻi (insensitivity hormone, hana insulin, syntagon glucagon). I ka hoʻomaka, i ka wā o ka hemoglobin glycosylated ua ʻoi aku ma mua o 9%, i ka loaʻa ʻole o nā hōʻailona lapaʻau i hoʻolaha ʻia a i ʻole ka piʻi ʻana o ka hoʻoponopono regimen, hiki i ka hui pū ʻana o nā lāʻau lapaʻau he 2-4.

Nā hiʻohiʻona lāʻau o Vildagliptinum

ʻO Vildagliptin (i ka papa ʻaina, ma ka ʻōlelo Latin, ʻo Vildagliptinum) kahi ʻelele o ka papa o nā lāʻau hypoglycemic i hoʻolālā ʻia e hōʻeuʻeu aku i nā mokupuni o Langerhans a me ka koho seleptly dipeptidyl peptidase-4. ʻO kēia kaomi i ka hopena hoʻonāukiuki i ka pona o ka pona o ka glucagon like me ka 1 peptide (GLP-1) a me ka glucose-e hilinaʻi i ka insulinotropic polypeptide (HIP) (ʻoi aku ma mua o 90%). ʻO ka hōʻemi ʻana i kāna hana, hoʻonui ka wikiwiki i ka hana o GLP-1 a me HIP mai ka pūpū i ka kahe koko i ka lā. Inā kokoke nā pili o peptide i nā mea maʻamau, hiki i ka ʻβ-cell ke maʻalahi i ka glucose, a hoʻonui ka hana o ka insulin. ʻO ka pae nui o ka hana o nā β-cell ka mea kūpono i ko lākou palekana. ʻO ke ʻano o kēia, i ka nondiabetics, ʻaʻole e pili i ka hoʻohana ʻana o vildagliptin i ka hoʻopili ʻana i ka insulin a me ka glucometer. ʻO kahi helu o 50-100 mg / lā no nā maʻi maʻi. Hāʻawi mau i ka hoʻonui paʻa ʻana i ka pono o nā β-cell.

Eia kekahi, i ka wā e hoʻonāukiuki i ka lāʻau i ka hana o ka peptide GLP-1, hoʻonui ka hōʻemi i ka glucose i loko o nā pona α e hoʻokaʻawale i ka hopena o glucagon. ʻO ka Hyperglucagonemia kahi hana koʻikoʻi i ka hoʻomohala ʻana o nā hana papa. ʻO ka meaʻokoʻa o ka lāʻau ka mea ʻaʻole ia e hoʻoulu wale i nā kaʻina hana, hoʻihoʻi ia i ka hana o nā pū a α a me β. ʻAʻole ia e hōʻoia i kona pono wale nō, akā palekana pū me ka hoʻohana lōʻihi.

I ka hoʻonuiʻana i nā ʻike o GLP-1, hoʻonui ka vildagliptin i ka hoʻololiʻana o ka selosa o ka glucose i glucose. Mālama kēia i ka mālama ʻana i ka hana o glucagon, hoʻēmi me ka wā o ka ʻai e hōʻemi i ka pale ʻana o ka insulin.

Hoʻonui ka hoʻonui ʻana i ka ratio insulin / glucagon me ka hyperglycemia e pili ana i ke kumu o kahi ihi nui o ka GLP-1 a me HIP hoʻonāukiuki i ka hōʻemi o ka huna honu glycogen i kēlā me kēia manawa, me ka mālama o ka meaʻai.

Hāʻawi kēia mau mea āpau i ka mana glycemic stabil.

E hoʻoneʻe hou ʻia kekahi mea hou e ka lipid metabolism, ʻoiai ʻaʻohe mea pili pono ma waena o ka hopena ma nā peptides a me nā β-cell i kēia mea.

I kekahi mau lāʻau lapaʻau, me ka piʻi o ka ʻike o ka GLP o ke ʻano ʻano, e hōholo ana ka hoʻokuʻu ʻia o nā ʻike i ka ʻike, akā, me ka hoʻohana ʻana o vildagliptin, ʻaʻohe mau hōʻike like i kākau ʻia.

Ua mālama ʻia nā noi nui o ka lōʻihi a me ka lōʻihi o nā puke aʻoaʻo i nā ʻāina he nui. I ka wā i pau ai ʻo Galvus i nā maʻi maʻi 5795 me nā maʻi 2 ʻano i lawe i ka lāʻau lapaʻau i kona ʻano maʻa a i ʻole hui pū me nā hypoglycemic agents i hoʻopaʻa i ka emi ʻana o ke kōʻai wikiwiki a me ka hemoglobin glycosylated.

Pharmacokinetics o vildagliptin

ʻO ka bioavailability o ka lāʻau lapaʻau he 85%, ma hope o ka lawelawe waha a ke huhū koke ia. Ma hope o ka lawe ʻana i ka paila ma mua o ka papaʻaina, ʻike ʻia ka ʻike o ka nui loa o ka metabolite ma hope o 1 hola. 45 mau minuke Inā ʻoe e lawe i ka lāʻau lapaʻau me ka meaʻai, ua hōʻemi ʻia ka nui o ka lāʻau ma ka 19%, a ʻo ka manawa e hiki ai ke hoʻonui ʻia e 45 mau minuke. Hoʻopili palupalu ka mea paʻa i nā protein - 9% wale nō. Me ka infusion intravenous, ka nui o ka hoʻohele ʻana he 71 lita.

ʻO ke ala nui o ka excretion o ka metabolite ka biotransformation, ʻaʻole ia i hoʻololi ʻia e ka cytochrome P450, ʻaʻole ia he papa, a ʻaʻole kāohi i kēia mau maenehana. No laila, ʻo ka hiki ke pili pono i ka hoʻopili o ka maʻi ma ka palupalu.

Hoʻolaha ka puka Galvus

Hoʻopili ka hui Swiss ʻO Novartis Pharma iā Galvus i nā papa kaupaona 50 mg. I loko o ka pūnaewele olakino, ʻike ʻoe i ʻelua mau lāʻau lapaʻau e pili ana i ka vildagliptin. I hoʻokahi hihia, ua hana ka vildagliptin i mea kīnāwai, i loko o kekahi - metformin. Kuhi puka:

• "Vildagliptin" maʻemaʻe "28 tab. 50 mg kēlā me kēia;
• Vildagliptin + metformin - 30 mau lāʻau. 50/500, 50/850, 50/1000 mg kēlā me kēia.

ʻO ke koho o nā lāʻau lapaʻau a me ka regimen ka hoʻokūkū o ka endocrinologist. No ka vildagliptin, nā ʻōlelo i hoʻohana no ka hoʻohana ʻana i kahi papa inoa o nā pona maʻamau. Hoʻohana ʻia ka incretin no monotherapy a i ʻole i kahi ʻano paʻakikī (me ka insulin, metformin a me nā lāʻau lapaʻau antidiabetic). ʻO ka lā helu o kēlā me kēia lā he 50-100 mg.

Inā kauoha ʻia ʻo Galvus me ka sulfonylureas, hoʻokahi pākahi i kēlā me kēia lā he 50 mg. Me ka koho o ka papa ʻaina 1, inu ʻona i ke kakahiaka, inā ʻelua, a laila i ke kakahiaka a me ke ahiahi.

Me ka regimen vildagliptin hoʻohui + metformin + sulfonylurea derivatives, ʻo ka maʻamau maʻamau i kēlā me kēia lā e 100 mg.

ʻO ka hana nui o nā lāʻau lapaʻau ka mea i hoʻopili ʻia i loko o ke ʻano o kahi metabolite ʻole i hana ʻole ʻia; hiki ke hoʻoponopono ʻia ka hoʻoponopono ʻana me nā pathal renal.

E hoʻonoho i kahi pahu kōkua mua me ka lāʻau lapaʻau i kahi kahi hiki ʻole ke nānā ʻia o nā keiki. Nā kūlana mālama mālama - a hiki i ka 30 ° С, ola noho ʻole - a hiki i 3 mau makahiki. Hiki pōʻino e lawe i nā lāʻau i pau, no ka mea e hoʻemi ʻia ko lākou hopena, a ke ulu nei ka hopena o nā hopena maikaʻi.

Nā hōʻailona no ka hoʻohana ʻana o ka penela

ʻO ka lāʻau lapaʻau, ʻo kā lākou hana ma ke kumu o ka huaʻala i hoʻohui ʻia ia, he kūpono no ka hoʻokūkū me nā metformin a me kahi mea o sulfanylurea. Ua kūkulu ʻia ia no ka mālama ʻana i nā maʻi me ka maʻi maʻi type 2 i kēlā me kēia manawa o ka maʻi.

Maʻaʻaʻa ia i kēlā me kēia mau pūʻulu hui ʻelua i hui pū ʻia me metformin, sulfonylurea hoʻomākaukau, insulin a me thiazolidinedione, inā ʻo ka hana ma mua o kēia mau lāʻau lapaʻau ʻaʻole i hāʻawi i ka hopena i makemake ʻia.

Nā hiʻohiʻona a me nā hopena makemake ʻole

Hoʻopili maʻalahi ia Vildagliptin i nā maʻi maʻi maʻi ma mua o nā mea hana ʻokoʻa hypoglycemic āpau. I waena o nā contraindications:

• Intolerance intact-galage kanaka pilikino;
• ʻO ka hemahema lactose;
• ʻO nā maʻi maʻi o nā mea hana o ka hoʻohālike;
• Kuhihewa kaluhuna-galactose.

ʻAʻohe ʻikepili hilinaʻi ma ka hopena o ka nanahope o ka maʻi pediatric, nā makuahine hāpai a me ka lactating, no laila, ʻaʻole kuhikuhi ʻia kahi metabolite no kēlā mau maʻi o nā maʻi.

Ke hoʻohana nei ʻo Galvus i kekahi koho maʻi, ua hoʻopaʻa ʻia nā hopena ʻaoʻao:

• Me ka monotherapy - hypoglycemia, ka nalowale ʻana o ka hoʻonohonoho ʻana, ka ʻeha, ka pupuhi, ke hoʻololi ʻana i ke kani defecation;
• ʻO Vildagliptin me Metformin - nā haʻalulu lima a me nā hōʻailona like i nā mea ma mua;
• ʻO Vildagliptin me nā derebatives sulfonylurea - hoʻohui i ka asthenia (kahi noʻonoʻo noʻonoʻo) i ka papa inoa ma mua;
• ʻO Vildagliptin me nā derivatives thiazolidinedione - he hoʻohui i nā hōʻailona maʻamau, hiki i ka hoʻonui ʻana o ke paona kino;
• ʻO Vildagliptin a me ka insulin (i kekahi manawa me ka metformin) - nā maʻi dyspeptic, hypoglycemia, ʻeha.

I loko o kekahi mau mea maʻi, ua kākau ʻia nā hoʻopiʻi o ka urticaria, ka ʻano o ka ʻili a me ke ʻano o nā blisters, exacerbation o ka pancreatitis. ʻOiai ke papa inoa paʻa o nā hopena pono ʻole, liʻiliʻi ka liʻiliʻi o kā lākou hanana. ʻO ka hapa pinepine, ʻo kēia mau kaʻaʻiʻole o kahi ʻano pōkole a me ka hoʻopau ʻole i ka lāʻau ʻaʻole pono.

ʻO nā hiʻohiʻona o ka mālama ʻana me vildagrippin

I nā makahiki 15 i hala iho nei, ua mālama ʻia nā kūkākūkā mua o 135 no nā ʻāina ʻē aʻe. I ka pae hea e hōʻike ai i ka maʻi hypoglycemic no ke ʻano maʻi type 2?

• I ka hoʻomaka, ke hoʻopau ʻia i kahi kūlana "maʻemaʻe";
• I ka hoʻomaka me ka hui me metformin;
• I ka manawa e hoʻohui ai i ka metformin e hoʻonui ai i kona hiki;
• I nā ʻōkuhi ʻekolu: vildagliptin + metformin + PSM;
• Ke hui pū me ka insulin basal.

I kēia mau hihia a pau, hiki iā ʻoe ke hoʻohana i ka vildagliptin. ʻO kahi maʻa o 200 mg / lā ka assimilated me ka pilikia o nā pilikia ʻē aʻe, hiki i kahi overdose.

• Inā ʻoe e lawe i hoʻokahi pākahi o 400 mg, myalgia, ʻāʻī, ke kuni, nā maʻi ʻāʻī o nā ʻōwili e kū mai ana, e piʻi ana ka pae o lipase.
• I loko o kahi waiʻeono o 600 mg, huehue nā wāwae, ka manaʻo o ka protein C-reactive, ALT, CPK, myoglobin e hoʻonui. Pono ʻia ka nānā ʻana o ka ate, inā ua ʻoi aku ka hana o ALT a i AST paha ma mua o ka maʻamau.
• Inā ʻike ʻia nā ʻōpaka hepatic (no ka laʻana, jaundice), ua kāpae ʻia ka lāʻau lapaʻau a kinai nā ʻōpala āpau.
• Ma kahi o ka insulin-dependence type 2 diabetes, hiki ke vildagliptin i hui pū me ka hormone.
• Mai hoʻohana i ka lāʻau lapaʻau no ka maʻi maʻamau o ka maʻi, me ka ʻokiʻoki ʻo ketoacidosis.

ʻAʻole i hana ʻia nā haʻawina e pili ana i ka hopena o ka piʻi ʻana o ka lewa.

Inā lawe pū ʻia ka lāʻau lapaʻau me ka lawaiʻa ʻana o ka hoʻopili ʻana, pono ʻoe e hōʻole i ka hoʻokele ʻana i ka halihali a me nā hana paʻakikī.

Nā mea hoʻohālikelike o Galvus a me kona loaʻa

I waena o nā analogue, ua loaʻa nā vildagrippin i nā lāʻau lapaʻau me kekahi mea ikaika i ka waihona a me kahi hana like.

1. ʻO Onglisa ka mea ikaika i ka saxagliptin. Kumukūʻai - mai 1900 rubles;
2. Trazhenta - ke kīʻaha kaha o nā linagliptin. ʻO ke kumu kumukūʻai he 1750 rubles;
3. ʻO Iosuavia ka mea ikaika o sitagliptin. Kumukūʻai - mai 1670 rubles.

Aia ke kahua o nā mea hana o Novartis Pharma ma Basel (Switzerland), no laila ʻo ka vildaglippin e hoʻohālikelike ʻia ke kumukūʻai me ka maikaʻi o ʻEulopa, akā e kūʻē i ke ʻano o ke kumukūʻai o ka analogue he mea kūpono loa. Hiki i kahi maʻi maʻi waena waena ke kūʻai aku i 28 mau papa o 50 mg no 750-880 rubles.

Mahalo S.A. ʻO Dogadin, ka Luna Endocrinologist o ke Teritori Krasnoyarsk, manaʻo pono ia he mea nui ka nui o nā mea maʻi i loaʻa i nā ʻenehana loea a me ka hiki ke mālama ʻia me vildagliptin no ka manuahi. Ke kali nei mākou iā ia e hōʻike mai i nā papa inoa makemake Federal. I kēia manawa, ke hoʻokomo ʻia ka lāʻau lapaʻau i loko o kahi papa inoa ma nā wahi he kanaha o ka Lūkini Lūkini a me ka papa kuhikuhi o ka hoʻolako ʻana i ka maʻi hānai ma nā hua ʻōlelo makemake e hoʻonui ʻia nei.

ʻ Professorlelo Hawaiʻi Yu.Sh. ʻO Halimov, ka Luna Kauka-Endocrinologist o St. Petersburg, i ʻōlelo ʻo ka vildagliptin he mea hilinaʻi nui i ka hana solo, maikaʻi i loko o ka duet, ʻaʻole nui loa i loko o kahi trio. ʻO ka Incretin he mea hana maʻamau i loko o ka orchestra o ka lāʻau antidiabetic, hiki iā ia ke hana i lalo o ka nalu o kahi lāʻau o ka conductor ma o kekahi kauka iʻike ʻole ʻia.