Antidiabetic Dapagliflozin

ʻO ka Diabetes mellitus kahi laulā āpau o nā maʻi maʻi o nā ʻano kumu mua. ʻO kahi hiʻohiʻona maʻamau no nā ʻano āpau o ka maʻi diabetes is hyperglycemia - kiʻekiʻe koko koko. Hana ʻia ka Hyperglycemia ma ke kumu o ka hana ʻole o ka hana a i ʻole ka hana o ka insulin (ʻaʻole hiki i ka insulin ke hoʻopiha i nā pono āpau o ke kino, a i ʻole a pau ʻole).
ʻO ka insulin he hormone, ke "kī" e hiki ke wehe i nā pūpū no ka hoʻomaʻamaʻa kūpono o ke kō. Ka mea, he kūpono no ka pono a me ka hana pono o nā kaʻina āpau i ke kino. Hoʻokumu ʻia ka insulin e nā hana kūikawā - nā pihi beta pancreatic. ʻElua mau ʻano o ka insulin i hana ʻia - huna ʻia basal (pono, kumu, hāʻawi i ke kiʻekiʻe o ke kōpaʻa koko me ka ʻole ka lawe ʻana i ka ʻai) a me ka postprandial (pancreatic insulin hana e hoʻoulu ʻia e ka meaʻai, ke lilo koke i mea e pono ai ka hoʻōla nui aʻe o ka ʻoi).

Inā hōʻike mua ka poʻe maʻi i ka mellitus maʻi miki, pono loa e hoʻoholo he aha nā ʻano maʻi e ala nei no ka mālama kūpono ʻana. ʻO ka mea maʻamau ka mea maʻamau a me ka maʻi diabetes type 2. Ma ka hoʻomaʻamaʻa, aia kekahi, akā ʻaʻole pālahalaha lākou.

Pehea e mālama ai i ka maʻi maʻi type 1?

Kāhea ʻia ʻo ke ʻano maʻi type 1 ka ʻano mea i hilinaʻi ʻia i insulin. Ma muli o ka hanaʻino ʻana o nā pū beta pancreatic, pau ka hana i ka insulin. I nā maʻi e hōʻemi nei i kēia maʻi, pono ka lawelawe ʻana i ka insulin i ka pae maʻamau. ʻO ka poʻe me ka maʻi type type 1 e huli pinepine i ka mālama koʻikoʻi. ʻO ke ʻano kēia, ʻo ka insulin hana lōʻihi, ka hoʻokaʻawale i ka mea huna o ka insulin basal, e mālama ʻia i ke ahiahi (a i ke kakahiaka a i ke ahiahi), a ma ke ao, me ke ʻano he kānāwai, ma mua o ka ʻai, ua hoʻohui ʻia ka insulin pōkole e hōʻemi i ka glycemia postprandial.

Ua hoʻohana maikaʻi kekahi mau mea maʻi i kahi pami insulin. He polokalamu kēia e hāʻawi ai i ka insulin i nā manawa maʻamau e like me nā pono o ka mea maʻi i ka dermis, kahi e komo ai ia.

Pehea e mālama ai i ka maʻi maʻi type 2?

ʻO ka maʻi diabetes 2, ʻaʻole like me ka mea mua, ke kūʻokoʻa nei ka insulin. ʻO kēia ke kumu e hua ai ka pancreas i ka insulin, akā ʻaʻole i lawa ka pae o ka hoʻouka ʻana i nā koi o ke kino a i ʻole nā ​​ʻamona i hoʻolilo ʻia i kāna hana (ma ke ʻano o kēia ʻano i kapa ʻia ʻo ka pale ʻana o ka insulin).

He aha nā lāʻau lapaʻau e lawe ai?

ʻO ke kumu no ka mālama ʻana o ka maʻi mellitus type 2 i ka hoʻonui ʻana i ka ʻike ʻana i nā kiko i ka insulin (no ka laʻana, e hoʻohana ana i kahi lāʻau lapaʻau e loaʻa ana i ka Metformin, Pioglitazone, ua hana nui ʻia i loko o nā pā papa) a hoʻonui paha i ka hana mai nā cell beta pancreatic i ka manawa kūpono (sulfonylurea lāʻau lapaʻau i ka manawa kūpono. , Nā Glinides, nā ʻāpana pū). I kēia manawa, hoʻohana ʻia nā lāʻau lapaʻau e pili ana i ka hopena ma luna o ka pūnaehana incretin a, ma ka hope, ma ke kāpae ʻana i nā nui o ke kōpaʻa mai ke kino me ka urine (Glyflosins). Hoʻohana ka poʻe hana nui mai kēia mau pūʻulu i ke ʻano o nā papa no ka mālama ʻana. Pēlā, ua hōʻiliʻili ʻia kēia mau lāʻau i nā lāʻau lapaʻau hypoglycemic waha.

ʻO ka Metformin ka lāʻau lapaʻau mua loa no ke koho no ka maʻi lā 2. Hoʻonui ia i ka hoʻōla hilo i ka mākala uaua. Inā lawa ka hopena o ka lāʻau, a laila e hoʻohui pū ʻia nā mea hoʻohui antidiabetic. Loaʻa nā hopena ʻaoʻao o kēia lāʻau lapaʻau. Hiki i nā mea maʻi maʻalahi hele aku i ke kani ʻana, flatulence, nausea, kahi kinikini i ka waha. ʻAʻole hiki ke hōʻemi ʻia nā hopena maikaʻi ʻole i ka ʻōpū gastrointestinal ma o ka lawe ʻana i ka lāʻau lapaʻau ma hope o ka ʻai ʻana, ma ke ʻano he kānāwai, ma hope o nā hebedoma 2-3 o ka mālama ʻana, nāwaliwali. Hiki ke lawelaweʻia ka metformin a hiki i 3 mau lā i ka lā. Pono e hoʻokaʻawaleʻia ka waiʻona i ka wā e lawe nei i kēia lāʻau lapaʻau. Loaʻa ka lāʻau lapaʻau i ke ʻano o nā papa.

ʻO ka hui glitazone ka mea i ka pioglitazone mea, kahi lāʻau lapaʻau ʻaʻole wale e hoʻonui i ka naʻau o nā kopa i ka insulin, akā he hopena maikaʻi hoʻi i ka kiko o nā palaka i loko o ke koko, ke koko a pale aku i ka hoʻōla ʻana i ka protein nui e nā keiki. I ka wā mālama, hiki ke hoʻohana wale ʻia (inā ʻaʻole hemahema ka mea maʻi o Metformin), a hiki ke hui pū ʻia me nā ʻaila antidiabetic waha. ʻO nā hopena ʻaoʻao o ka lāʻau hiki ke hoʻohui i ka hōʻiliʻili o ka wai ma loko o ke kino, ka loaʻa ʻana o ka paona, i loko o ka hui hoʻohui - hypoglycemia. Hana ʻia nā hoʻomākaukau a kēia pūʻulu i ke ʻano o nā papa.

Sulfonylureas

ʻO nā hui derivatives o Sulfonylurea he mau mea hou o ka hoʻonui ʻana i ka hana insulin e nā ʻenehana aepela o nā mokupuni o Langerhans. Hoʻohana pinepine ʻia kēia mau lāʻau i loko o ka hui hoʻohui ʻana no ka maʻi diabetes type 2. ʻO nā papa i loaʻa i nā derivatives sulfonylurea i koho ʻia i loko o ka hapalua hola ma mua o ka papaʻaina. Inā hoʻokomo ʻia kahi mea hoʻohui mai kēia pūʻulu i nā papa hoʻokuʻu i paʻa ʻia, e lawe koke ʻia ka lāʻau lapaʻau ma mua o a i ka wā o ka pāʻina.

Hiki i nā derivatives o Sulfonylurea ke hoʻopili me nā lāʻau ʻē aʻe e lawe nei ka mea maʻi, i nā lāʻau lapaʻau ʻehā ʻē aʻe. No laila, he mea pono i ka hoʻomaopopo ke kauka i nā lāʻau āpau i lawe ʻia. ʻO nā hopena koʻikoʻi nā hypoglycemia a me ke kaumaha. Me ka lōʻihi o ka mālama ʻana me nā kiʻekiʻe kiʻekiʻe o ka hoʻomākaukau ʻana o ka sulfonylurea, hiki ke hoʻopau ʻia i ka insulin i loko o ka pancreas, ma muli o ke ʻano i hoʻokomo ʻia i ka insulin i loko o ka subcutaneous tissue o ka mea maʻi. Hoʻomoe a me nā derivatives sulfonylurea - nā papa. ʻAʻole kūpono ka alkohol i ka papa o nā lāʻau lapaʻau!

I kēia manawa, aia nā hui o ka lāʻau lapaʻau maʻi kaukē i ka mākeke e loaʻa i kēia mau ʻano hana: Glimepiride, Gliclazide, Glipizide a me Gliburide.

Hana nā hui ʻoihana ma nā pūpū beta o nā mokupuni o Langerhans e like me ka sulfonylureas. ʻO ia, hāʻawi lākou i ka hoʻonui ʻana i ka huna ʻana i ka insulin. Lawe ʻia nā Glinids ma kahi o ka ʻai kai. Nā papa ʻōlelo.

ʻO nā mea e pili ana i ka ʻōnaehana incretin

ʻO nā incretins he mau mea hou o ka ʻano o nā protein a i ʻole nā ​​hormones a hua ʻia i loko o ka membousous o ka gastrointestinal tract ma hope o ka ʻai ʻana. Mai ka wahi gastrointestinal, hoʻopili ʻia lākou i loko o ke koko. ʻO ka hana nui o ka incretins ka mālama i nā pae glucose o ke koko.

ʻO ka peptide-like like Glucan-1 (ka inoa o ka lāʻau lapaʻau i loaʻa i ke ʻano o GLP-1) ʻo ia ke ʻano huaʻāina nui loa, kahi i loaʻa i ka papa piha o nā lāʻau lapaʻau. Hoʻokumu ʻia ka GLP-1 e nā ʻāpana ma hope o ka ʻai. Inā hana pono i kāna hana a me nā hana excretion, hoʻokuʻu ʻo ia i ka 70% o ka insulin e pono ai no ka hana ʻana i ke kō i loko o ka hapa i lawe ʻia. ʻO ka puka huahana ka papa.

Nā Glyphlosins

ʻO Glyphlosins ka hui hou o nā lāʻau lapaʻau no ka mālama ʻana i nā maʻi maʻi 2. Hoʻopili lākou i nā hana kūikawā i loko o nā pūpū, kahi e alakaʻi ai i ka hoʻonui ʻana i ka glucose o ka urinary. Mahalo i kēia kaʻina hana, hiki ke pale aku i nā nui o ke kō i loko o ka pāʻai a hoʻēmi i nā pae o ka glucose koko.

I kēia manawa, ua kākau inoaʻo Dapagliflozin, Canagliflosin a me Empagliflosin i ke kālepa.

ʻO Dapagliflozin lāua ʻo Empagliflozin i lawe ʻia ma hoʻokahiʻano hoʻokahi i kēlā me kēia lā, me ka manaʻo o ka ʻai ʻana, a hiki pū ke hui pū me nā lāʻau lapaʻaka antidiabetic waha. ʻO ke ʻano o ka lāʻau lapaʻau ka ʻōpala.

Hoʻohana ʻia ʻo Canagliflozin ma hoʻokahi o ka pae hoʻokahi no kēlā me kēia lā, ʻoi loa ka manawa ma ka ʻahaʻaina mua. He kūpono no ka hui pū me nā mea hana waha hypoglycemic waha. Hana ʻia ia i ke ʻano o nā papa.

ʻO ka hoʻonohonohoʻana o ka lāʻau lapaʻau a me ke ʻano o ka hoʻokuʻu

I loko o ke keʻena lāʻau lapaʻau, kūʻai aku ʻo Dapagliflozin e like me nā papa melemele. Ma muli o ka nui, ua hūʻā ʻia lākou me ka hōʻailona ʻana i ka "5" ma ke alo a me ka "1427" ma ka ʻaoʻao, a me ke daimana paha me nā hōʻailona "10" a me "1428".

Ma kahi pā i nā mea i hoʻonoho ʻia nā 10 pcs. ʻO nā pōpō. I kēlā me kēia pahu kīpē he 3 a 9 paha o ia mau papa .. ʻAi nā bli a he 14 mau ʻāpana pākahi. I loko o kahi pahu o nā papa like i hiki ke loaʻa i ʻelua a ʻehā paha.

ʻO 3 mau makahiki kahi e noho ai ke ola o ka noho lāʻau. No dapagliflozin, ʻo ke kumukūʻai ma ke kikowaena pūnaewele mai ka 2497 rubles.

ʻO ka mea hana nui o ka lāʻau dapagliflozin. Ma kahi o ia mea, ua hoʻohana ʻia nā mea hoʻopihapiha: cellulose, lactose maloʻo, silicon dioxide, crospovidone, magnesium stearate.

Lapaʻau

ʻO ka papa hana, dapagliflozin, he potent inhibitor (SGLT2) o ka sodium-depend type type 2 glucose transporter. Hōʻike ʻia i loko o nā aʻalolo, ʻaʻole ia i ʻike ʻia i nā meaʻokoʻa āpau a me nā ʻōpala (70 mau ʻano like me ka hoʻokolohua). ʻO SGLT2 ka mea nui e lawe ai i ka glucose reabsorption.

ʻAʻole kū kēia kaʻina me ka maʻi type 2, ke ʻano o ka hyperglycemia. Ma ka hoʻokaʻawale ʻana i ka halihali glucose, hoʻemi ʻia ka mea pale i kona reabsorption i loko o nā pūlū a ua hoʻokuʻu ʻia. Ma muli o kēia hopena, hōʻemi ka meli - ma ka ʻōpū ʻole a ma hope o ka hoʻomaʻamaʻa ʻana, hoʻomaikaʻi ana nā waiwai o ka hemoglobin glycosylated.

ʻO ka nui o nā glucose i lawe ʻia e hilinaʻi ana i ka nui o nā waihona momona loa a me nā rate filtration glomerular. ʻAʻole ka hopena o ka mea pale i ka hana kūlohelohe o kona ake ponoʻī. Kūʻokoʻa kona mau hana i ka hana o ka insulin a me ka pae o ka ʻike ʻana iā ia.

ʻO nā hoʻokolohua me ka lāʻau lapaʻau ua hōʻoia i ka holomua o ka moku'āina o nā b-cell i kuleana no ka synthesis o ka hoʻomau i ka insulin.

Hoʻopau ke kulu ma kēia ala hoʻonāukiuki i ka hoʻohana ʻana i kaloli a me ka nalowale ʻana o ka mea kaumaha nui, he ʻokoʻa ka hopena diuretic.

ʻAʻole hopena ka lāʻau lapaʻau i nā mea hoʻohele glucose hou e hoʻohele nei iā ia ma ke kino holoʻokoʻa. Ke SGLT2, hōʻike ʻo dapagliflozin i kahi koho o 1,400 mau manawa i ʻoi aku i kona SGLT1, nona ke kuleana o ka hoʻopio o ka glucose i loko o ka ʻōpū.

Lapaʻau lāʻau

Me ka hoʻohana ʻana o Forsigi e ka maʻi maʻi maʻi a me nā poʻe ola olakino ma ka hoʻokolohua, ua ʻike ʻia kahi hoʻonui o ka hopena glucosuric. Ma nā kikoʻī kikoʻī, nānā ia i kēia: no 12 mau hebedoma, lawe aku nā maʻi maʻi i ka lāʻau i ka lā 10 gm / lā No kēia manawa o kēia manawa, neʻe ke kaukaʻe i 70 g o ka glucose, lawa ia 280 kcal / lā.

Hoʻopili pū ʻia ka lāʻau Dapagliflozin e ka diuresis osmotic. Me ka hoʻoponopono o ka lāʻau i wehewehe ʻia, ua loli ʻole ka hopena diuric no nā hebedoma 12 a ua hoʻonui ʻia ka 375 ml / lā. Ua ukali ʻia ke kaʻina hana me ka leʻo o ka liʻiliʻi o ka sodium, akā ʻaʻole ia e pili i kēia ʻike i kona ʻike i loko o ke koko.

Lapaʻau lāʻau

1. Kapehu. I ka wa e lawe kolohe ai, e hoʻopili ʻia ka lāʻau i loko o ka huehue huna a kokoke ʻo 100%. ʻAʻole pili ke komo i ka meaʻai i ka hopena o ka hoʻopili ʻana. ʻIke ʻia ka kiʻekiʻe o ka hōʻemi ʻana i ka lāʻau ma ke koko ma hope o 2 mau hola i ka wā i hoʻohana ʻia ma ka ʻōpū ʻole. ʻOi aku ka kiʻekiʻe o ka lāʻau o ka lāʻau lapaʻau, ʻoi aku ka kiʻekiʻe o ke kaila o ka plasma i kekahi mau manawa. Ma kahi kanu o 10 mg / lā. ʻo ka bioavailability kūpono piha ma kahi o 78%. I nā poʻe ola olakino ma ka hoʻokolohua, ʻaʻohe ʻai nui i ka ʻai i ka pharmacokinetics o ka lāʻau.
2. Kahele. Hoʻopaʻa ka lāʻau lapaʻau i nā ʻōnaehana koko ma ka awelika o 91%. Me nā maʻi hoʻopukapuka, no ka laʻana, ʻoi aku ka maikaʻi ʻole, e noho nei kēia hōʻailona.
3. Hāpai. ʻO TЅ i ka poʻe olakino he mau hola 12.0 ma hope o hoʻokahi pakahi no kahi papa pāpaona he 10 mg. Hoʻololi ʻia ka Dapagliflozin i loko o ka metabolite inert o dapagliflozin-3-O-glucuronide, ʻaʻohe ona hopena lapaʻau.
4. Leʻaleʻa. ʻO ka lāʻau lapaʻau me nā metabolites ka waiho ʻana me ke kōkua o nā keiki i kona ʻano kumu. Ma kahi o 75% e hoʻopio ʻia i loko o ka pāʻai, ke koena ma o ka ʻōpū. Ma kahi o 15% o dapagliflozin e puka mai ana i loko o kona ʻano akomi

ʻO ka nui o ka glucose i hoʻonā ʻia e nā keiki i nā pilikia o kā lākou hana ma muli o ka nui o ka pathology. Me nā mea ola kino, ʻo kēia hōʻailona he 85 g, me kahi ʻano māmā - 52 g, me kahi awelika - 18 g, i nā pilikia koʻikoʻi - 11 g o glucose. Hoʻopili ka mea pale i nā protein i ka hopena like ma ka maʻi maʻi a me ka hui pū. ʻAʻole i aʻo ʻia nā hopena o ka hemodialysis i nā hopena hopena.

I nā hemahema a me ka maʻalahi o ka pīpī pēpē ʻana, ʻokoʻa nā pharmacokinetics o Cmax a me AUC i ka 12% a me 36%. ʻAʻole kēlā hewa hewa i kahi hana haukapila, no laila, ʻaʻohe mea e pono ai ke hōʻemi i ka nui o kēia ʻāpana o ka maʻi maʻi. Ma ke ʻano ikaika, hoʻohālikelike kēia mau kuhikuhi i ka 40% a me 67%.

I ka wā pākeke, ʻaʻole i mālama ʻia ka hoʻololi nui loa i ka hoʻolaha ʻana i ka lāʻau (inā ʻaʻohe kumu ʻē aʻe e hoʻomāinoino ana i ke kiʻi lāʻau lapaʻau). ʻO ka nāwaliwali nā kauā, ʻoi aku ka kiʻekiʻe o ka loaʻa ʻana o dapagliflozin.

I kahi kūlana paʻa, ma nā mea maʻi me ka diabetes type 2, ʻoi aku ka nui o ka Cmax a me AUC ma mua o nā kāne maʻi i ka 22%.

ʻO nā ʻokoʻa i nā hopena i hilinaʻi ʻia no ka lāhui o ʻEulopa, Negroid a i ʻole Mongoloid lāhui i loaʻa.

Me ka nui o ke kaupaona ʻana, ʻoi aku ka liʻiliʻi o nā hōʻailona o ka hopena o ka lāʻau lapaʻau, akā, ʻaʻole i ʻike nui ʻia nā hala, e koi ana i ka hoʻoponopono ʻia.

Nā Hoʻohui

• Hoʻopili nuiʻia i nā mea o ke ʻano,
• ʻAno maʻi type 1
• Ketoacidosis
• ʻO nā maʻi ʻeha
• Ka hoʻomauʻana o ka genetic i ka glucose a me ka lactase,
• ʻLelo ʻia a me ka lactation,
• ʻO nā keiki a me nā ʻōpio (ʻaʻohe data hilinaʻi).
• Ma hope o ke ʻano o ka maʻi maʻi, i hele pū ʻia me ke kahe koko;
• ʻO Senile makahiki (mai 75 makahiki) - e like me ka lāʻau mua.

Nā papahana hana maʻamau

ʻO ke algorithm no ka mālamaʻana o dapagliflozin i ke kauka, akā ke kuhikuhi ʻia nei nā ʻōnaehana maʻamau i nā ʻōlelo kuhikuhi no ka hoʻohana.

1. Monotherapy. ʻAʻole paʻa ke kaʻaila i ka meaʻai, ʻo ka maʻamau o kēlā me kēia lā he 10 mg i ka manawa.
2. ʻO ka hoʻolālā holoʻokoʻa. I ka hui me metformin - 10 mg / lā.
3. ʻO ka hoʻolālā kumu. Ma kahi hoʻohālike o Metformin 500 mg / lā. Lawe ka Forsigu i 1 pā. (10g) i kēlā me kēia lā. Inā ʻaʻole i loaʻa ka hopena i makemake ʻia, e hoʻonui i ka hapa o Metformin.
4. Me nā maʻi hepatic. ʻO ka maʻi maʻi me ka maʻi maʻalahi i ka hoʻololi ʻana i ke akeʻaole ʻole ka pono e hoʻoponopono pono ʻia. Ma ke ʻano ikaika, hoʻomaka lākou me 5 g / lā. Me ke ʻano maʻamau o ke kino, hiki ke hoʻonui ʻia ke ʻano i ka 10 mg / lā.
5. Me nā mea hoʻohālikelike renal. Me ka ʻano maʻamau a paʻakikī, ʻaʻole i kuhikuhi ʻia ʻo Forsig (i ka wā hana ʻo creince clearance (CC)) nā hopena ʻaoʻao

Ma nā noi palekana palekana o ka lāʻau lapaʻau, 1,193 mau mea hana i hāʻawi ʻia iā Fortigu ma 10 mg / lā a me 1393 nā poʻe komo i lawe i kahi placebo. ʻO ka pinepine o nā hopena kūpono ʻole like me ka like.

I waena o nā hopena kūlike ʻole e koi ai i ka hoʻokuʻu ʻana o nā ʻoihana, ua ʻike ʻia nā mea penei:

• Hoʻonui i QC - 0.4%,
• Nā maʻi āwili o ka ʻōnaehana genitourinary - 0.3%,
• Nā lapalapa o ka ʻili - 0.2%,
• ʻO nā maʻi hoʻopoina, 0.2%
• Nā kipi o ka hoʻonohonoho paʻa - 0.2%.

Hōʻike ʻia nā kiko o nā noi ma ka papa ʻaina.

• Pinepine pinepine -> 0.1,
• Hoʻohana pinepine -> 0.01, 0.001,

ʻAno o nā ʻōnaehana a me nā ʻāpana

Nā maʻi a me nā infestationsVulvovaginitis, balanitisWehewehena kāne kāne ʻO ka huʻihuʻi me ka meaʻaiʻaiʻaiHypoglycemia (me ka hoʻohui ʻana o nā hana)Kahuna Nā maʻi GastrointestinalHōʻowili ʻIli kūlokoʻOhua ʻŌnaehana musculoskeletalʻEha i ka pōpilikia ʻŌnaehana GenitourinaryDysuriaNocturia ʻIkepili haipuleʻO ka Dyslipidemia, hematocrit kiʻekiʻeʻO ka ulu o ka QC a me ka urea koko

Nā Hōʻike Manaʻo Dapagliflozin

Wahi a kahi noiʻi o nā malihini i nā kumuwaiwai papaʻa, ʻo ka hapa nui o nā maʻi maʻi maʻi ʻaʻohe huakaʻi, ua māʻona lākou me nā hopena lapaʻau.Nui ka mea i hoʻopau ʻia e ke kumukūʻai o ka pā, akā ke manaʻo pilikino e pili ana i nā makahiki, nā maʻi concomitant, ka nui o ka lehulehu i hiki ke lilo i alakaʻi no ka hoʻoholo ʻana ma ke koho ʻana iā Forsigi.

Hiki i kahi papa pilikino ke mālama ʻia e ke kauka wale nō; e koho nō hoʻi ʻo ia i nā analogues no dapagliflozin (Jardins, Invokuan) inā ʻaʻole maikaʻi ka paʻakikī.

Ma ke wikiō - nā hiʻohiʻona o Dapagliflozin i kahi ʻano lapaʻau hou.

Hoʻohana i ka waiwai Dapagliflozin

ʻO ka type 2 diabetes mellitus i ka hoʻohui i ka ʻai a me ka hana e hoʻomaikaʻi ai i ka mana glycemic i ka maikaʻi.

- hoʻohui i ka maʻi me ka metformin, derivatives o ka sulfonylurea (me ka hui pū me ka metformin), thiazolidinediones, DPP-4 inhibitors (me ka hui pū me ka metformin), hoʻomākaukau o ka insulin (me ka hui pū me kekahi a i ʻole ʻelua mau lāʻau hypoglycemic no ka hoʻohana waha ʻana i ka make) i ka lawa ʻole o ka mana glycemic kūpono,

- e hoʻomaka ana i ka hui hoʻohui me ka metformin, inā e aʻo ʻia kēia lāʻau.

ʻŌpū a me ka lactation

ʻO ka māhele FDA o ka hana no ka pūpū ʻo C.

Ua hoʻohālikelike ʻia ʻo Dapagliflozin i ka wā hāpai (hoʻohana i ka wā hāpai a ʻaʻole i aʻo ʻia nā maʻi hāpai ʻana). Inā loaʻa ka mālama ʻana i ka wā hapai, pono ke hoʻokuʻu ʻia nā lāʻau dapagliflozin.

ʻAʻole i ʻike ʻia inā e komo ʻo dapagliflozin a me / a i kāna mau metabolite hana i ka waiū umauma. ʻAʻole hiki ke kāʻili ʻia ka ʻeha i nā pēpē / pēpē. Ua hoʻohālike ʻia ka Dapagliflozin i ka manawa o ka ʻōpū.

Nā hopena ʻaoʻao o ka waiwai Dapagliflozin

Ka Palapala Hoʻohākaʻa ʻana i ka Pūnaewele

ʻO ka loiloi mua i hoʻolālā ʻia e ka ʻike i loko o ka wai i loko nā mea i loaʻa i nā hopena o nā hōʻike no ka hoʻomalu ʻia i loko o ka placebo.

ʻO ka nui nui o nā hanana hōʻeha (ʻo ka pōkole o ka manawa pōkole) i nā mea maʻi e lawe ana i ka 10 mg dapagliflozin ua like nō ia me ka hui placebo. ʻO ka nui o nā hanana ʻino e alakaʻi ai i ka hoʻokuʻu ʻana i nā mea maʻi ma ka liʻiliʻi a ma waena o nā hui mālama. ʻO nā hanana e ʻike pinepine ʻia i alakaʻi ʻia ai ka hopena o ka lāʻau dapagliflozin ma kahi maʻa o 10 mg he hoʻonui i ka hoʻoulu ʻana o ke koko (0.4%), maʻi maʻi urinary (0.3%), nausea (0.2%), dizziness (0, 2%) a me ka wikiwiki (0.2%). ʻO ka mea maʻi e lawe ana i dapagliflozin i hōʻike i ka hoʻomohala ʻana o kahi hanana ʻino mai ka ate me ka loaʻa ʻana o ka maʻi hepatitis a me nā maʻi hepatitis autoimmune.

ʻO ka hopena maʻamau loa e hōʻike ai i ka hypoglycemia, kahi hoʻomohala i hilinaʻi i ke ʻano o lalo o lalo o ke ʻano maʻi i hoʻohana ʻia i kēlā me kēia haʻawina. ʻO ka ulu ʻana o ka hypoglycemia māmā i like me nā hui mālama, e komo pū ana me ka pletebo.

Hōʻike ʻia nā hopena maikaʻi ʻole i nā hoʻokolohua lapaʻau e mālama ʻia e ka laikini i lalo (ʻo ka pōkole o ka manawa pōkole a hiki i 24 mau wiki heʻe ke ʻano o ka lawehala hypoglycemic hou). ʻAʻohe o lākou he dosis hilinaʻi. Hāʻawi ʻia ka hōʻike ʻana o ka hopena ʻino ma ke ʻano o ka hoʻōki ʻana aʻe: pinepine pinepine (≥1 / 10), pinepine pinepine (≥1 / 100, 1,2, maʻi ʻeha o ka urinary 1, ka maʻi maʻamau - vulvovaginal itching.

Mai ka ʻaoʻao o ka metabolism a me ka pōʻino: pinepine pinepine - hypoglycemia (i ke ʻano hui pū ʻana me kahi derogative sulfonylurea a i ʻole insulin) 1, ka hemahema - ke hoʻemi ʻana o BCC 1.4, make wai.

Mai ka palaki kuʻekuʻe: pinepine - constipation.

Ma ka ʻāpana o ka ʻili a me ka kiko. pinepine - hoʻonui ʻia.

Mai ka ʻōnaehana musculoskeletal a me nā ʻili pili: eha ʻeha hoʻi.

Mai nā pūpū a me ka maʻi urinary: pinepine - dysuria, polyuria 3, pinepine - nocturia.

Nā ʻikepili a me ka ʻikepili kōkua: dyslipidemia 5, kahi mahuahua o ka hematocrit 6, ke piʻi ʻana o ka ʻike o ka creatinine i loko o ke koko, ke hoʻonui pinepine ʻana i ka urea i ke koko.

1 E ʻike i ka pauku kūpono ma lalo nei no ka ʻike hou aku.

ʻO Vulvovaginitis, balanitis a me nā maʻi like ʻole, ka laʻana, ka ʻōlelo i koho ʻia e like me nā huaʻōlelo: vulvovaginal fungal infection, vaginal infusion, balanitis, fungal infection of genital organ, vulvovaginal candidiasis, vulvovaginitis, candida balanitis, genital candidiasis, infital infection, genital nā mea i loko o ke kāne, ka maʻi penile, vulvitis, bacterin vaginitis, vulvar abscess.

3 Polyuria e pili ana i nā huaʻōlelo makemake i koho ʻia: pollakiuria, polyuria a me nā mea i hoʻonui ʻia i ka urine.

4 Hoʻololi i loko o bcc ka laʻana, no ka laʻana, ka ʻōlelo i koho ʻia i makemake mua ʻia: dehydration, hypovolemia, hypotension arterial.

5 ʻO ka hoʻololi iki o nā huaʻōlelo e hōʻike nei ma kahi hapa o nā waiwai i ka pūʻulu 10 mg dapagliflozin a me ka hui plasebo, no kēlā me kēia: huina Chs - 1.4 hoʻohālikelike ʻia -0.4%, Chs-HDL - 5.5 hoʻohālikelike ʻia i ka 3.8%. Chs-LDL - 2.7 hoʻohālikelike ʻia me -1.9%, triglycerides -5.4 hoʻohālikelike ʻia -0.7%.

6 ʻO nā hoʻololi hou i ka hematocrit mai ke kīʻaha ʻo 2.15% i ka hui 10 mg dapagliflozin i hoʻohālikelike ʻia me -0.4% ma ka hui pletebo.

ʻO ka wehewehe ʻana i nā hopena kūlike maikaʻi

Hypoglycemia. ʻO ka ulu ʻana o ka hypoglycemia i hilinaʻi i ke ʻano o lalo o ke ʻano lāʻau i hoʻohana ʻia ma kēlā me kēia haʻawina.

I nā haʻawina o dapagliflozin e like me ka monotherapy, hui pū me ka metformin a hiki i 102 wiki, ke ʻano o nā hōʻeha o nā episode hypoglycemia maʻalahi (BCC. ʻO nā hopena ʻino e pili ana i ka hoʻohaʻahaʻa i ka bcc (me nā hōʻike o ka hoʻoiho, hypovolemia, a i ʻole hypotension arterial) i ʻike ʻia ma ka 0.8 a me 0.4% o nā poʻe maʻi e lawe ana i ka dapagliflozin 10 mg a me ka placebo, no kēlā me kēia; ua hōʻike ʻia nā hopena koʻikoʻi ma ka bcc hypotension nānā ʻia ma 1,5 a me 0.4% o nā maʻi e lawe ana i ka dapagliflozin a me ka placebo, ma kēlā

Hoʻohui

Diuretics. Hiki i ka Dapagliflozin ke hoʻoikaika i ka hopena diuretic o ka thiazide a me ka diuretics loop a hoʻonui i ka nui o ka hoʻomoʻewaʻi a me ka hypotension arterial (e nānā i nā "Hoʻomaʻomaʻi".

ʻO ka insulin a me nā lāʻau lapaʻau e hoʻonui ai i ka hilo i ka insulin. E pale aku i ke kua o ka hoʻohana o ka insulin a me nā lāʻau lapaʻau e hoʻonui ana i ka mea huna o ka insulin, hiki i ka hypoglycemia. No laila, i mea e hōʻemi ai i ka hopena o ka hypoglycemia me ka hoʻohana pū ʻana o dapagliflozin me ka insulin a i nā lāʻau lapaʻau e hoʻonui ana i ka huna ʻana o ka insulin, pono paha e hōʻemi i ka hopena o ka insulin a i nā lāʻau lapaʻau e hoʻonui ai i ka huna ʻana o ka insulin (e nānā i "Side effects").

ʻO ka metabolism o dapagliflozin e lawe nui ʻia e ka conjuration glucuronide ma lalo o ka mana o UGT1A9.

I ka wā noiʻi i loko o vitro ʻaʻole i hoʻoneʻe ʻo dapagliflozin i nā isoenzyme o nā pūnaehana kaomi cytochrome P450, CYP1A2, CYP2A6, CYP2B6, CYP2C8, CYP2C9, CYP2C19, CYP2D6, CYP3A4 a i ʻole ka mea i hōʻike iā CyP2A6, CYP2A6 I kēia mea, ʻaʻole i manaʻo ʻia ka hopena o dapagliflozin ma ka huakaʻi metabola o nā lāʻau concomitant e ʻano nei e kēia mauenemena.

Ka hopena o nā lāʻau ʻē aʻe ma dapagliflozin. ʻO nā haʻawina o nā hana e pili ana i nā limahana olakino, ʻo ka lawe nui ʻana i ka wai hoʻokahi o ka dapagliflozin, i hōʻike ʻia e pili ana i ka metformin, pioglitazone, sitagliptin, glimepiride, voglibose, hydrochlorothiazide, bumetanide, valsartan, a me simvastatin ʻaʻole i hoʻopilikia i ka pharmacokinetics dapaglapinagin.

Ma hope o ka hoʻohana pū ʻana o dapagliflozin a me rifampicin, kahi mea hoʻomohala o nā ʻano mea hoʻouluola a me nā ʻenehana e hoʻokaʻawale i nā lāʻau lapaʻau, 22% ka emi ʻana o ka hoʻolaha ʻana i nā systemic (AUC) o dapagliflozin i hoʻomaopopo ʻia i ka loaʻa ʻole o ka hopena koʻikoʻi i ka maʻi maʻamau i ka lā maʻamau o ka glucose i nā lālani. ʻAʻole ia e hāʻawi i ka hoʻoponopono ʻana i ka maʻa o dapagliflozin.

ʻAʻole hiki ke manaʻo ʻia kahi hopena nui o ka klinikino i ka wā e hoʻohana ʻia me nā inducers ʻē aʻe (e.g. carbamazepine, phenytoin, phenobarbital).

Ma hope o ka hoʻohana pono ʻana o ka dapagliflozin me ka waikawa mefenamic (UGT1A9 inhibitor), kahi 55% i hoʻonui ʻia i ka hoʻopōhuahua ʻana o nā system dapagliflozin, akā naʻe me ka hopena nui o ka maʻi ma ka lālaha o kēlā me kēia lā ka glucose i nā lālani. ʻAʻole ia e hāʻawi i ka hoʻoponopono ʻana i ka maʻa o dapagliflozin.

ʻO ka hopena o dapagliflozin i nā lāʻau lapaʻau ʻē aʻe. Ma nā haʻawina o nā pili i pili i nā mea kōkua olakino, ʻo ka poʻe nui i lawe i hoʻokahi pākahi, ʻo dapagliflozin, ʻaʻole i hoʻopilikia i ka pharmacokinetics o metformin, pioglitazone, sitagliptin, glimepiride, hydrochlorothiazide, bumetanide, valsartan, digoxin (substrate P-varnarfin, varfarb, Sarfarb, ) a i ka hopena anticoagulant, loiloi ʻia e INR. ʻO ka hoʻohana ʻana i hoʻokahi pākahi o dapagliflozin 20 mg a me simvastatin (kahi'āpana o ka isoenzyme CYP3A4) hopena i ka hoʻonuiʻana i ka 19% i ka simvastatin AUC a me kahi 31% simvastatin acid AUC. ʻAʻole i manaʻo nui ʻia ka hoʻonui ʻana i ka simvastatin a me ka waikawa simvastatin i kahi nui koʻikoʻi.

ʻO nā hopena o ka ulaula, kaʻai ʻana, ka lawe ʻana i nā lāʻau lapaʻau lāʻau a me ka inu ʻana i ka waiʻona ma nā lāʻau lapaʻau ʻo dapagliflozin i aʻo ʻole ʻia.

Ke keu

Ka palekana a Dapagliflozin a hōʻoluʻolu maikaʻi ʻia e nā mea kōkua olakino me ke ʻano hoʻokahi no ka 500 mg (50 mau manawa i hoʻolako ʻia). Ua hoʻoholo ʻia ʻo Glucose i loko o ka urine ma hope o ka hoʻokele ʻana (ma ka liʻiliʻi o 5 mau lā ma hope o ka lawe ʻana i ka nui o ka 500 mg), ʻoiai ʻaʻole ʻaʻohe mau mea o ka hoʻohiolo, hypotension, ʻōpala electrolyte, hopena nui i ka maʻi ma ke kikowaena QTc. ʻO ka ulu ʻana o hypoglycemia i like me ke alapine me ka pletebo. I nā haʻawina ma nā mea hana olakino a me nā mea maʻi me ka maʻi diabetes type 2 ka mea i lawe iā dapagliflozin i hoʻokahi manawa ma 100 mg (10 mau manawa nui loa i hoʻolilo ʻia) no 2 mau pule, ʻoi aku ka nui o ka ulu ʻana o hypoglycemia ma mua o ka placebo, a ʻaʻole. hilinaʻi ma ka pākale. ʻO ka ulu ʻana o nā hanana pōʻino, ʻo ka dehydration a i ʻole hypotension arterial, ka like me ka lekiō i ka hui plasebo, me ka nui o nā loli e pili ana i ka nui o nā panina ana o ka laboratori, e komo pū ana ka serum o nā electrolytes a me nā biomarkers o ka hana o ka pūpū.

I ka hihia o kahi overdose, pono ia e hoʻokō i ka mālama mālama ʻana, i ka mālama ʻana i ke kūlana o ka mea maʻi. ʻO ke kūkole o dapagliflozin e hemodialysis i aʻo ʻia i aʻo ʻia.

Kaukuhi ʻO Dapagliflozin

ʻO ka maʻi me ka hana renal impaired

ʻO ka hana o ka dapagliflozin e hilinaʻi i ka hana waha, a ua hōʻemi ʻia kēia hana i nā mea maʻi me ka lawa ʻole o ka renal a paʻa paha i loko o nā mea maʻi me ka pilikia o ka renal. Ma waena o nā mea maʻi me ka hiki ʻole o ka renal moderate (Cl creatinine 2), kahi nui o nā mea maʻi e loaʻa ana i dapagliflozin i hōʻike i ka hoʻonui ʻana o ka likinine, ka ʻoli, ka PTH a me ka hypertension arterial ma mua o nā mea maʻi e loaʻa ana i ka placebo. Ua hoʻohālikelike ʻia ʻo Dapagliflozin i loko o nā mea maʻi me ka maʻi hakahaka a i ʻole a me ka maʻi (Cl creatinine 2). ʻAʻole i aʻo ʻia ʻo Dapagliflozin i loko o kahi hana ʻino koʻikoʻi (Cl creatinine 2) a i ʻole he hopena hope loa.

Aohaoia uei ai i ke aka o ka pēpē i:

- ma mua o ka hoʻomaka ʻana o ka maʻi me dapagliflozin a ma kahi o ka manawa 1 i kēlā me kēia makahiki ma hope aku (ʻike i ka "Side effects", "Pharmacodynamics" a me "Pharmacokinetics"),

- ma mua o ka lawe ʻana i nā lāʻau lapaʻau concomitant e hiki ke hōʻemi i ka hana kidney, a me ia manawa

- i ka hihia o ka hana hōʻeha kokoke i ka modular, a ma kahi o 2-4 mau manawa i ka makahiki. Inā hōʻemi ka hana o ka keiki ma lalo o Cl creatinine 2, e kāpae i ka dapagliflozin.

ʻO nā maʻi me ka hana pūlima hemahema

Ma nā haʻawina loiloi, ua loaʻa ka ʻike kikoʻī ma ka hoʻohana ʻana o dapagliflozin i nā mea maʻi me ka hana aho lēwa. Hoʻonui ka ʻike i dapagliflozin i loko o nā mea maʻi me ka maʻi kuku o ka maʻi kaumaha (ʻike "Hoʻopā i ka hoʻohana ʻana o" a me "Pharmacokinetics").

ʻO ka poʻe maʻi i ka hopena o ka hōʻemi o ka bcc, ka hoʻomohalaʻana i ka hypotension arterial a me / a me ka nānāʻole o ka electrolyte

Ma ke ʻano o ka hana o ka hana, ʻo ka dapagliflozin e hoʻomaikaʻi i ka diuresis, i hele pū ʻia me ka emi iki o ke koko (e nānā i ka "Pharmacodynamics"). Hiki ke hoʻopuka hou ʻia ka hopena diuretic i nā mea maʻi i ka haka kiʻekiʻe o ka glucose i loko o ke koko.

Ua hoʻohaumia ʻia ʻo Dapagliflozin i nā mea maʻi e lawe ana i ka diuretics loop (e ʻike i ka "Interaction"), a i ʻole me ka BCC i hōʻalo ʻia, no ka maʻi ʻana, e like me nā maʻi maʻi (e like me nā maʻi gastrointestinal).

Pono e mālama ʻia ka makaʻala ma nā maʻi nā mea e hōʻemi ai ke koko i hoʻokahe ʻia e dapagliflozin e pilikia paha, no ka laʻana, i nā mea maʻi me nā moʻolelo o nā maʻi cardiovascular, ka mōʻaukala o hypotension, loaʻa ke ʻano antihypertensive, a i ʻole nā ​​mea maʻi maʻi.

Ke lawe nei i dapagliflozin, kiaʻi makaʻala o ka moku'āina o ka BCC a me ka paʻa ʻana o nā electrolytes (e.g. hoʻokolokolo kino, ʻike ʻana i ke koko, ʻike ʻana i nā hoʻokolohua ʻana, a me nā hematocrit) i ʻōlelo ʻia i kahi kūʻai o nā kūlana concomitant e hiki ai ke alakaʻi i ka hōʻemi o ka bcc. Me ka hoʻohaʻahaʻa ʻana i BCC, ua hoʻokaʻawale ʻia ke kaʻa kuʻuna o dapagliflozin a hiki i ke hoʻoponopono ʻia ʻana o kēia ʻano (e ʻike i nā "ʻaoʻao effects").

I ka hoʻohana ʻana i ka kūʻai aku ʻana o ka dapagliflozin, ua hōʻike ʻia ka ketoacidosis maʻi ketoacidosis maʻi, i loko o nā mea maʻi me ka diabetes mellitus type 1 a me 2, e lawe ana i nā dapagliflozin a me nā mea ʻē aʻe SGLT2, ʻoiai ʻaʻole i hoʻokumu ʻia kahi hopena kumu. ʻAʻole hōʻike ʻia ʻo Dapagliflozin no ka mālamaʻana i nā mea maʻi me ka maʻi maʻi type 1.

ʻO ka poʻe maʻi e lawe ana i ka dapagliflozin me nā hōʻailona a me nā hōʻailona e hōʻike ana i ka ketoacidosis, me ka maʻi nausea, ka luaʻi, ka ʻeha o ka ʻōpū, malaise, a me ka pōkole o ka hanu, pono lākou e nānā no ka ketoacidosis, ʻoiai inā he kahe o ke koko i lalo o 14 mmol / L. Inā kānalua ka ketoacidosis, e pono e hāʻawi i ka noʻonoʻo e hoʻolei a i ʻole ke hoʻokaʻawale i ka wā e hoʻohana ai i dapagliflozin a nānā pono i ka mea maʻi.

E pili ana nā mea kūpono i ka hoʻomohala ʻana i ka ketoacidosis me ka hana haʻahaʻa o nā hanana beta ma muli o ka maʻi pancreatic impaired (e.g., type 1 diabetes mellitus, pancreatitis a i ʻole kahi mōʻaukala o ka pancreatic), kahi hoʻemi i ka insulin dosis, hoʻemi i ka ʻai o caloric o ka meaʻai, a i ʻole ka hoʻonui ʻia ʻana o ka ʻai, insulin ma muli o nā maʻi maʻi, nā maʻi a i ʻole ka hōʻino ʻana, a me ka hōʻino ʻana i ka waiʻona. Pono e hoʻohana ʻia ʻo Dapagliflozin me ka makaʻala ʻana i kēia mau maʻi.

ʻAʻohe maʻi ʻeha.

Ke hōʻike nei i ka ʻikepili i hui ʻia ma ka hoʻohana ʻana o dapagliflozin, a hiki i 24 mau hebedoma maʻi urinary tract ua ʻike pinepine ʻia me ka hoʻohana ʻana o dapagliflozin i kahi maʻi o 10 mg hoʻohālikelike ʻia me ka placebo (e ʻike i "Side effects"). Kēia pinepine ʻia ka hoʻomohala ʻana o ka pyelonephritis, me ka loaʻa pinepine o ka hui o ka hui. E pili paha ka hoʻōla ʻana o ka maʻi pēpē i ka nui o ka ulu ʻana o ka hoʻomohala ʻana i nā maʻi o ka urinary, no laila, i ka loaʻa ʻana o ka pyelonephritis a i ʻole urosepsis, hiki i ka manawa ke kīlohelohe iki ʻole o ka hopena dapagliflozin e pono e noʻonoʻo (e ʻike i nā "ʻaoʻao effects").

Urosepsis a me pyelonephritis. Ma ka hoʻohana ʻana i ka kūʻai aku ʻana o ka dapagliflozin, ua hōʻeha ʻia ka maʻi urinary, me ka urosepsis a me ka pyelonephritis, e koi ana i ka hoʻokipa ʻana i nā maʻi e lawe ana i nā dapagliflozin a me nā mea paʻa SGLT2. ʻO ka maʻi me nā SGLT2 inhibitors ka hoʻonui i ka hopena o ka hoʻomohala ʻana i nā maʻi maʻi urinary. Pono ka nānā ʻana o nā mea maʻi no nā hōʻailona a me nā hōʻailona o nā maʻi o ka maʻi urinary a, inā e kuhikuhi ʻia, e mālama koke ʻia (e ʻike i nā "ʻaoʻao ʻaoʻao").

I ka poʻe maʻi maʻi, ʻoi aku ka hopena o ka renal function a / a i ʻole ka hoʻohana ʻana i nā lāʻau antihypertensive, hiki ke pili i ka hana ʻana, e like me ka ACE inhibitors a me ke ʻano II ARA, ʻoi aku paha. (see"ʻO nā hopena ʻaoʻao" a me "Pharmacodynamics").

Ma kahi hui o nā mea maʻi ʻo ≥65 mau makahiki, he nui ka nui o nā mea maʻi e loaʻa ana i dapagliflozin i hoʻomohala i nā hopena e like me ka hana ʻana a hope ʻole a i ʻole ka pale i hoʻohālikelike ʻia me ka placebo. ʻO ka hopena maʻamau loa e pili ana i ka hana renal impaired he hoʻonui i ka serum creatinine concentrations, ʻo ka hapanui o nā hihia he transient a hoʻololi ʻia (e ʻike i nā "ʻaoʻao effects").

I nā poʻe maʻi elemakule, ʻoi aku ka nui o ka hōʻemi o ka hōʻemi i loko o ka BCC, a ʻoi aku ka nui o nā diuretics. ʻO ka hapa nui o nā mea maʻi ≥65 mau makahiki he nui i loaʻa iā dapagliflozin i loaʻa nā hopena pōʻino e pili ana i ka emi ʻana o ka BCC (e nānā i "Side effects").

Loaʻa ka ʻike me dapagliflozin i nā mea maʻi 75 makahiki a ʻoi aku ka nui. Hoʻohui ʻia e hoʻomaka i ka hoʻāʻo ʻana ʻo dapagliflozin i kēia heluna kanaka (e ʻike i ka "Pharmacokinetics").

Hoʻopau ʻole nā ​​puʻuwai naʻau

ʻO ka ʻike me ka hoʻohana ʻana o dapagliflozin i nā mea maʻi me ka CHF I - II papa hana e like me ka helu ʻana NYHA kaupalena ʻia, a ma ke ʻano o nā hoʻokolohua hoʻokolohua, ʻaʻole i hoʻohana ʻia ʻo dapagliflozin i nā mea maʻi me ka papa hana III - IV CHF NYHA.

Hoʻonui ka hematocrit

Ke hoʻohana nei iā dapagliflozin, ua nānā ʻia ka nui o ka hematocrit (e ʻike i nā "ʻaoʻao ʻaoʻao"), a no laila e mālama pono ʻia ka poʻe maʻi i nā maʻi me ka nui o ka nui hematocrit.

ʻO ka loiloi o nā hopena hōʻike i ka urine

Ma muli o ka ʻoihana o ka hana a dapagliflozin, e kūleʻa ka hopena o nā hoʻokaʻina o ka urine no ka glucose i loko o nā poʻe maʻi e lawe ana iā dapagliflozin.

Hoʻohui ma ka hoʻoholo o 1,5-anhydroglucitol

Ka loiloi ʻana o ka mālama glycemic me ka hoʻohana ʻana i ka manaʻo o ka 1,5-anhydroglucitol, ʻaʻole i ʻae ʻia, ʻoiai ke ana ʻana o ka 1,5-anhydroglucitol he ʻano kumu pono ʻole no ka poʻe maʻi e lawe ana i ka SGLT2 inhibitors. Pono e hoʻohana pono nā mea hana e loiloi i ka mana glycemic.

Hoʻokomo i ka hiki ke alakaʻi i nā kaʻa a hana me nā mīkini. ʻO nā haʻawina e noiʻi ai i ka hopena o dapagliflozin ma ke hiki ke lawe i ka kaʻa a hana a me nā hana me ʻaʻole i hana.

ʻO ka wehewehe ʻana i ka lāʻau lapaʻau

ʻO Dapagliflozin kahi hanohano (pale paʻa (Ki) o 0.55 nM), kahi ʻano koho hoʻohuli ʻōpiopio 2 sodium glucose cotransporter inhibitor (SGLT2). Kahi ʻia ka SGLT2 i loko o ka pūpū a ʻaʻole i ʻike ʻia ma mua o 70 mau kino ʻokoʻa ʻē aʻe (me ka pūpuna, ka hāhiu, skeletal muscle, adipose tissue, mammary glands, bladder a me ka lolo).

ʻO SGLT2 ka mea nui e lawe ai i ka glucose reabsorption i loko o ka renal tubules. ʻO ka reabsorption o ka hanu ma loko o nā ʻōpū o nā maʻi i nā mea maʻi me ka diabetes mellitus type 2 (T2DM) i hoʻomau ʻia ma ka maʻi hyperglycemia. Ma ka hoʻokaʻawale ʻana i ka hoʻololi ʻana i ka maʻi o ka glucose, ua hōʻemi ʻo dapagliflozin i kāna reabsorption i loko o ka renal tubules, e alakaʻi ana i nā hōʻiliʻili o nā huaʻai e nā keiki.

Hōʻalo i nā glucose (hopena hopena o glucosuric) ma hope o ka lawe ʻana i ka hapa mua o ka lāʻau lapaʻau, hoʻomau mau no nā 24 mau hola a hoʻomau i ka hana o ka maʻi. ʻO ka nui o ka glucose i hoʻopuka ʻia e nā keiki ma muli o kēia hana e pili ana i ka neʻe o ka glucose i ke koko a ma ka pae o ka filtration glomerular (GFR).

ʻAʻole ʻo Dapagliflozin e hoʻopili i ka hana maʻamau o ka glucose endogenous i ka pane i ka hypoglycemia. He kūʻokoʻa ka hopena o dapagliflozin o ka huna ʻana o ka insulin a me ka ʻike ʻana i ka insulin. Ma nā noiʻi haʻawina o ka lāʻau Dapagliflozin * (Dapagliflozin *) ™, ua ʻike ʻia kahi hoʻomaikaʻi ʻana i loko o ka hana β-cell (hōʻike HOMA, hōʻike loiloi homeostasis).

ʻO ka hoʻopauʻana o ka glucose e nā huaʻai i hoʻokumu ʻia e dapagliflozin me ka nalo ʻana o ka nui o nā kalori a me kahi laʻa o ke kaupaona ʻana. Dapagliflozin inhibition o ka sodium glucose cotransport i hele pū me nā diuretic nāwaliwali a me nā hopena natriuretic transient.

ʻAʻohe hopena o Dapagliflozin i nā mea lawe ʻē aʻe o ka glucose e lawe ana i ka glucose i nā kiko peripheral a hōʻike hou ʻia aku ma mua o 1,400 mau manawa nui ka koho no SGLT2 ma mua o SGLT1, ka transporter intestinal nui kuleana no ka hoʻopio ʻana i ka glucose.

Ma hope o ka lawe ʻana i ka dapagliflozin e nā limahana olakino a me nā mea maʻi me ka maʻi diabetes type 2, ua nānā ʻia kahi hoʻonui o ka glucose i hoʻopā ʻia e nā keiki. A lawe ʻia ʻo dapagliflozin ma kahi o 10 mg / lā no 12 mau pule, i nā mea maʻi me T2DM, ma kahi o 70 g nā mea puhaka i hoʻopaku ʻia e nā keiki i kēlā me kēia lā (e like me ka 280 kcal / lā). I ka poʻe maʻi me ka maʻi diabetes type 2 nāna i lawe iā dapagliflozin ma ke ʻano o 10 mg / lā no ka manawa lōʻihi (a hiki i 2 mau makahiki), mālama ka glucose i waho ma ke ʻano o ka hopena o ka maʻi.

ʻO ka hoʻopiʻiʻana o nā glucose i nā huaʻai me dapagliflozin e alakaʻi ana i ka diuresis osmotic a me ka hoʻonui o ka waihona i ka urine. ʻO ka hoʻonui ʻana i ka nui o ka urine i nā mea maʻi me ka maʻi diabetes type 2 e lawe ana i ka dapagliflozin ma kahi maʻa o 10 mg / lā i mau no 12 mau pule a ua hōʻemi ʻia ma kahi o 375 ml / lā. ʻO ka hoʻonui pū i ka nui o ka urine i ukali pū ʻia me ka hoʻonui liʻiliʻi a me ka hoʻonui nui i ka sodium excretion e nā keiki, ʻaʻole i alakaʻi i kahi hoʻololi o ke kao o ka sodium i loko o ka serum koko.

Hoʻolālā ka hoʻolālā o nā hualoaʻa o nā haʻawina hoʻomalu 13 no ka pletebo i hōʻike ʻia i ke kaomi ʻana o ke koko systolic blood (SBP) o 3.7 mm Hg. a me ke kahe koko diastolic (DBP) ma 1,8 mm Hg i ka pule 24 o ka hopena o dapagliflozin ma kahi lāʻau o 10 mg / lā i hoʻohālikelike ʻia me kahi kaila o SBP a me DBP e ka 0.5 mm Hg. ma ka hui placebo. ʻO ka emi ʻana o ke kahe o ke koko ua ʻike ʻia i nā wiki he 104 i ka mālama ʻana.

Ke hoʻohana nei iā dapagliflozin ma kahi o 10 mg / lā i nā mea maʻi me ka maʻi type kīkē me ka mana o ka glycemic kawalan a me ke ʻano hypertension, ka loaʻa ʻana o nā blockers blocker ngiotensin II, nā mea paʻa o ACE, me ka komo i ka hui pūʻana me kekahi lāʻau lapaʻau antihypertensive, kahi hōʻemi i ka hemoglobin glycosylated e 3.1% a me kahi hoʻoluhi o SBP e 4.3 mm Hg i hoʻomaopopo ʻia. ma hope o 12 mau wiki o ka lapaʻau i hoʻohālikelike ʻia me ka placebo.

ʻO ka hoʻoponopono hoʻoponopono koʻikoʻi no ka maʻi maʻi maʻi

Me ke ʻano o nā lāʻau lapaʻau, ʻoi aku ka nui o ke ʻano o ka lāʻau lapaʻau o ka maʻi. Hoʻomaopopo nā kauka i kahi mea ʻai kūikawā, ke ʻano kino, a me nā hana ʻē aʻe e kuhikuhi ana i ka hoʻolauna ʻana i ke kaumaha o ke kino. Hāʻawi kēia i ka hoʻemi ʻana i ka kiʻekiʻe o ka pale ʻana i ka insulin, e hōʻemi i ka hopena o nā huahana o ke kino i nā β-cell. Akā ʻo ia mau ʻano hana e hāʻawi i ka hopena maikaʻi i ka hoʻomaka ʻana o ka maʻi. ʻO ka hapa nui o nā poʻe maʻi e koi i ka lāʻau lapaʻau.

Hoʻokomo nā hana i ka hana hypoglycemic pili i ka hōʻailona o ka patology a me ke kūlana o ka mea maʻi. Inā i ka pae o ka hemoglobin glycated i ka papa o 6,5 - 7.0%, ʻae ʻia ka monotherapy, a ua koho ʻia nā kālā me ka liʻiliʻi o ka hopena ʻino.

Ma mua o ka hōʻike ʻana i ka hana lapaʻau o ka lāʻau, ua kauoha ʻia ʻo Forksig:

• kel Luna nui (metformin),
• Nā papa DPP-4 (depeptidide peptidase-4) - Saxagliptin, Vildagliptin,
• glinids (Repaglinide, Nateglinide),
• ʻO nā pona o nā peptide glucagon like-(aGPP) - Exenatide, Lyraglutid,
• insulin

Inā loaʻa nā contraindications e lawe i kēia mau lāʻau lapaʻau, nā mea hoʻoponopono hou e hoʻohana ana i ka hoʻohana ʻana i ka sulfonylureas, nā palapala lepo, a me nā mea ʻē aʻe.

I ka hoʻomaka mua o ka hemoglobin glycated o 7.5 - 9,0%, hui pū me nā maʻi hypoglycemic maʻamau, e pili ana i nā ʻāpana āpau o ka pathogenesis o ke ʻano maʻi diabetes mellitus, pono. Eia naʻe, nā mea i hoʻohana mua ʻia o ka metformin me nā lawena hypoglycemic pinepine i alakaʻi i ka nui o ke kaumaha o ke kino a ke mea maʻi a me nā hopena ʻē aʻe. Akā ʻo ka hui pū ʻana o ka Metformin Forksig, ma ke kihi, e hōʻemi i ka haʻalulu o ka subcutaneous a me visceral adipose tissue.

Ke ʻoi aku ka kiʻekiʻe o ka hemoglobin glycated ma mua o 9.0%, pono wale ka mea maʻi i ka hoʻomehana ʻana o ka insulin, i kekahi manawa me ka maʻi āpau o hypoglycemic.

Akā ʻike nā poʻe loea ʻaʻole kūpono nā lāʻau hoʻohana mua no ka monotherapy o ka lōʻihi. No laila, ma hope o ʻekolu mau makahiki, ua hōʻike wale ka hapa hapalua o nā mea maʻi i ka hopena maikaʻi, a ma hope o 9 mau makahiki - ma kahi hapaha.

Ka hoʻohana ʻana o Forxiga i ka mālama ʻana i ka maʻi maʻi

ʻO kekahi o nā lāʻau lapaʻau i hoʻohana ʻia e hoʻohana pono ai no ka mālama ʻana i ke ʻano type II ʻano ʻo Metformin. Ua pili ka hāmeʻa:

• kūleʻa ʻona kalepa,
• nā kaʻina hana gluconeogenesis,
• ka hoʻāʻo ʻana i ka inika.

ʻAʻole hiki i ka Metformin ke alakaʻi i ka hoʻonui ʻana i ke kaumaha o ke kino, ʻaʻole ia e hoʻoulu i ka hypoglycemia. Akā ʻo kahi hapakolu o nā maʻi e hōʻike i nā hopena maikaʻi loa mai ka digestive tract. A i kekahi mau pilikia, hoʻonāukiuki nā hoʻopiʻi i ka haʻalele ʻana i nā lāʻau lapaʻau. Eia kekahi, ʻo Metformin ka mea maʻamau ma kahi o nā lāʻau lapaʻau.

I kēia hihia, he hopena ka hopena o ka Forxiga. Hoʻemi ʻia ka hopena ma ka reabsorption a lilo i ka liʻiliʻi inā i ka nānā ʻana o ka glucose glucose ma lalo o 5 mmol / L. I ka manawa like, inā ʻo ka pae o ka glycemia he 13.9 mmol / L, hoʻonui ka reabsorption i ka 70%, a ma ka 16.7 mmol / L - a i ka 80%. No laila, hoʻohālikelike ʻia me nā lāʻau lapaʻau hou e hoʻohaʻahaʻa i ka hemahema, ʻaʻole pilikino ka hypoglycemia.

Ma mua o ka hoʻohana ʻana i ka lāʻau lapaʻau, pono ʻoe e kamaʻilio mau i ke kauka. Hiki i ka hoʻoponopono hoʻoponopono kūpono ke hana wale nō ma hope o kahi hoʻopaʻa hope ʻana i ka mea maʻi.

Hoʻomākaukau hui ʻo Glyphlosin

Hoʻokomo ʻia nā inhibitors i loko o nā pūpū a loaʻa i ka hoʻonui ʻia ʻana o ka glucose i ka urine. Ma muli o kēia, aia ka emi ʻana o ke kahe o ke koko, ua puhi ʻia ka nui o nā ʻoli, e alakaʻi ana i ka kaumaha.

ʻO SGLT-2 nā lāʻau lapaʻau, e like me Jardins, Invokana, Xigduo, Wokanamet he mea hou aku nō, a no laila, ʻaʻole maopopo loa nā hopena āpau.

Aia kēia mau lāʻau i ka papa o nā inhibitor SGLT2 (ka inoa mua, no ka laʻana, ʻo Forsig he kālepa, ʻo ka lua e pili ana i ka inoa o ka waiwai ikaikaʻo Dapagliflosin).

Manaʻo mākou iāʻoe e heluhelu: pehea e lawe ai i ka metformin

Hana ka mea mālama SGLT-2 e pale i kaʻeha ma mua o ka reabsorbing i ke kahe o ke koko. No laila, hiki i ka lolo ke hoʻohaʻahaʻa i ka pae o ka glucose i ke koko a kōkua i ka wehe ʻana i kona nui mai ke kino a me ka wai.

E heluhelu hou: Jardiance - pale pale

ʻO nā keiki kīʻaha ma ke kaʻina hana i ka hoʻoili mua i ka glucose i ke koko a hoʻokaʻawale i ke koko e komo hou i loko, e mālama ana i ka hana maʻamau. Ma lalo o nā kūlana maʻamau, e hoʻoikaika ka mīkini i ke kino e hoʻohana i nā mea momona a pau.

I ka poʻe me ka nui o ke koko koko, ʻaʻole iki ka hapa liʻiliʻi o ka glucose, akā hoʻopuʻi ʻia i loko o ka urine, pale iki ka pale ʻana i ka hyperglycemia. Eia nō naʻe, nā mea lawe o ka glucose - nā protein o ka sodium - e hana e pili ana i ka 90% o ka kānana i hoʻoneʻe ʻia i loko o ke kahe wai.

Ua hōʻike ʻia ka hopena o nā lāʻau lapaʻau hou nā makahiki hou i ka ʻaha o ka Ahahui o Nā Neprologists ma ka World Kidney Day ma ka lā Malaki 13, 2017. Eia naʻe, me nā maʻi ʻoi kino ikaika, ua kuhikuhi ʻia lākou me ka mālama nui.

Pono ʻoe e ʻike: e pili ana i nā lāʻau o nā hilo ʻana i ke kō o ka waiū hou i mau huaʻaila - GLP-1

Nā hiʻohiʻona noi

Manawa kuhikuhi

ma ka hoʻohana o ka lāʻau lapaʻau

no ka hoʻohana lāʻau

pani ʻ -lelo ʻlelo

ʻO ka hoʻohālikelike propanediol dapagliflozin 6.150 mg, helu ʻia ʻo Dapagliflozin * (Dapagliflozin *) 5 mg

microcrystalline cellulose 85.725 mg, lōpihi ʻono 25,000 mg, crospovidone 5,000 mg, silika ʻonika 1,875 mg, magnesium stearate 1,250 mg,

II ʻāpana 5,000 mg (polyvinyl ka ʻāpana hoʻoneʻe hoʻoneʻe i 2.000 mg, titanium dioxide 1,177 mg, macrogol 3350 1,010 mg, talc 0,740 mg, dye iron oxide yellow 0,073 mg).

dapagliflozin propanediol monoholate 12,30 mg, helu ʻia ʻo Dapagliflozin * (Dapagliflozin *) 10 mg

microcrystalline cellulose 171.45 mg, lactose anhydrous 50.00 mg, crospovidone 10,00 mg, silika dioxide 3.75 mg, magnesium stearate 2.50 mg,

Kahelele ʻeleʻele 10.00 mg (polyvinyl ka ʻāpana hoʻoneʻe ʻokoʻa i ka 4.00 mg, ka titanium dioxide 2.35 mg, macrogol 3350 2.02 mg, talc 1.48 mg, dye iron oxide yellow 0.15 mg).

Hoʻokomo ʻia nā papa biconvex poepoe me kahi membrane kiʻi melemele, i kahakaha ʻia me "5" ma kekahi ʻaoʻao a me "1427" ma kēlā ʻaoʻao.

Ua hoʻopaʻa ʻia nā papa bosenvex Rhomboid me kahi membrane kiʻi melemele, ke kahakaha ʻia me "10" ma kahi ʻaoʻao a me "1428" ma kēlā ʻaoʻao.

Ka hoʻohana maʻi hypoglycemic no ka hoʻohana waha - type 2 glucose transporter inhibitor

ʻO Dapagliflozin * (Dapagliflozin *) kahi hanohano (pale paʻa (Ki) o 0,55 nM), kahi mea koho balota-2 glucose cotransporter inhibitor (SGLT2). Kahi ʻia ka SGLT2 i loko o ka pūpū a ʻaʻole i ʻike ʻia ma mua o 70 mau kino ʻokoʻa ʻē aʻe (me ka ate, ka ʻūlū, ke kino ʻona, ka kiko adipose, nā mea momona, ʻiliahi, a me ka lolo).

ʻO SGLT2 ka mea nui e lawe ai i ka glucose reabsorption i loko o ka renal tubules. ʻO ka reabsorption o ka hanu ma loko o nā ʻōpū o nā maʻi i nā mea maʻi me ka diabetes mellitus type 2 (T2DM) i hoʻomau ʻia ma ka maʻi hyperglycemia. Ma ka hoʻokaʻawale ʻana i ka hoʻouluʻana o ka maʻi glucose, ʻo Dapagliflozin * (Dapagliflozin *) e hoʻēmi ana i ka reabsorption i loko o ka tubal renal, e alakaʻi ana i ka hoʻohemo ʻana o ka maʻi maʻamau e nā keiki.

Hōʻalo i nā glucose (hopena hopena o glucosuric) ma hope o ka lawe ʻana i ka hapa mua o ka lāʻau lapaʻau, hoʻomau mau no nā 24 mau hola a hoʻomau i ka hana o ka maʻi. ʻO ka nui o ka glucose i hoʻopuka ʻia e nā keiki ma muli o kēia hana e pili ana i ka neʻe o ka glucose i ke koko a ma ka pae o ka filtration glomerular (GFR).

Ua hoʻomaikaʻi ʻia ka hana cell Beta (hoʻokolohua NOMA, hoʻopaʻa ʻia ka loiloi homeostasis).

ʻO ka hoʻopauʻana o ka glucose e nā huaʻai i hoʻokumu ʻia e dapagliflozin me ka nalo ʻana o ka nui o nā kalori a me kahi laʻa o ke kaupaona ʻana. Dapagliflozin inhibition o ka sodium glucose cotransport i hele pū me nā diuretic nāwaliwali a me nā hopena natriuretic transient.

ʻAʻohe mea i loaʻa i ka Dapagliflozin * (Dapagliflozin *) i nā mea lawe ʻē aʻe o ka maʻi e lawe ana i ka glucose i nā kiko peripheral a ʻoi aku paha ma mua o 1,400 mau manawa i koho ʻia no SGLT2 ma mua o SGLT1, ka mea lawe hala o ka ʻōpū ma luna o ke kuleana no ka hoʻopio ʻana i ka glucose.

Ma hope o ka lawe ʻana i ka dapagliflozin e nā limahana olakino a me nā mea maʻi me ka maʻi diabetes type 2, ua nānā ʻia kahi hoʻonui o ka glucose i hoʻopā ʻia e nā keiki. I ka lawe ʻana o dapagliflozin ma kahi o 10 mg / lā no 12 mau pule, i nā mea maʻi me T2DM, ma kahi o 70 g o ka maʻi pākahi i kēlā lā i hoʻopiʻi ʻia e nā keiki (e like me ka 280 kcal / lā). I ka poʻe maʻi me ka maʻi diabetes type 2 nāna i lawe iā Dapagliflozin * (Dapagliflozin *) ma kahi pākana o 10 mg / lā no kahi manawa lōʻihi (a hiki i 2 mau makahiki), mālama ka glucose i waho ma ke ʻano o ka hopena.

Hōʻailona ka puka o ka glucose e nā keiki me dapagliflozin e alakaʻi i ka diuresis osmotic a me ka hoʻonui o ka waihona i ka urine. ʻO ka hoʻonuiʻana i ka nui o ka urine i nā mea maʻi me ka maʻi maʻi type 2 nāna i lawe iā Dapagliflozin * (Dapagliflozin *) ma kahi pākēnē o 10 mg / lā, hoʻomau no 12 mau hebedoma a helu ʻia ma kahi o 375 ml / lā. ʻO ka hoʻonui pū ʻana i ka nui o ka urine i ukali pū ʻia me ka hoʻonui liʻiliʻi a me ka pinepine o ka hoʻonui ʻana o ka sodium e nā lāʻau, ʻaʻole i alakaʻi i kahi hoʻololi o ke kao o ka sodium i loko o ka serum koko.

Ma hope o ka hoʻopale ʻana i ka waha, ʻo Dapagliflozin * (Dapagliflozin *) koke a hoʻoiho ʻia ma loko o ka ʻōpū o ka gastrointestinal a hiki ke lawe ʻia ma ka wā ʻai a ma waho o ia. ʻO ka hiki ke kau o dapagliflozin i loko o ke koko koko (Stax) e loaʻa pinepine i loko o 2 mau hola ma hope o ka wikiwiki.ʻO nā waiwai o Cmax a me AUC (ʻo ka wahi ma lalo o ka cur-time kukū) e hoʻonui i ka pā i ka nui o nā dosis o dapagliflozin.

ʻO ka bioavailability piha o dapagliflozin i ka wā i lawelawe ʻia ai i ka waha ma kahi o 10 mg o 78%. ʻO ka ʻai ʻana he hopena maʻalahi i ka lāʻau lapaʻau ʻo dapagliflozin i nā mea hana olakino maikaʻi. ʻO nā meaʻai momona nui i hoʻemi ʻia ka Stax o dapagliflozin e 50%, ua hoʻonui aku iā Ttah (manawa e hiki ai i ka plasma kiʻekiʻe) e pili ana i ka hola 1, akā ʻaʻole i hoʻopilikia ia ʻo AUC i hoʻohālikelike ʻia i ka hoʻokē ʻai. ʻAʻoleʻike nui kēia mau loli.

ʻO Dapagliflozin * (Dapagliflozin *) ma kahi o 91% e pili ana i nā protein. I nā maʻi me nā maʻi like ʻole, no ka laʻana, me ka maʻi lēwa ʻole a he hepatic function, ʻaʻole i loli kēia hōʻailona.

ʻO Dapagliflozin * (Dapagliflozin *) he Cokosile e pili pū ana me ka pilina o ka aglycon e pili ana i ka glucose ma kahi hāme a carbon-carbon, nāna e hōʻoia i kona kūpaʻa e kūʻē i ka glucosidases. ʻO ka awelika plasma hapalua-ola (T½) i nā limahana olakino he 12.9 mau hola ma hope o hoʻokahi dosis o dapagliflozin ma ke ʻano iki ma ke ʻano o ka 10 mg. ʻO Dapagliflozin * (Dapagliflozin *) i hana i ka metabolito e hana i ka metabolite nui loa o nā dapagliflozin-3-O-glucuronide.

Ma hope o ka hoʻoponopono waha ʻana o 50 mg o 14C-dapagliflozin, 61% o ka nui i lawe ʻia i ka metabolized iā dapagliflozin-3-O-glucuronide, nona ka nui o nā radio radioactivity plasma (AUC)

) - nā helu kūkā i hoʻololi ʻole ʻia no 39% o ka radioactivity plasma pau loa. ʻAʻoleʻoi aku nā pōkole o nā metabolites i koe hoʻokahi no ka 5% o ka nui o ka radioactivity plasma. ʻAiʻi aku ʻo Dapagliflozin-3-O-glucuronide a me nā metabolites ʻē aʻe i ka hopena pharmacological. Kūkū ʻia ʻo Dapagliflozin-3-O-glucuronide e ka enzyme uridine diphosphate glucuronosyl transferase 1A9 (UGT1A9), aia i loko o ka pūpū a me nā pepeha, a me Cenue cytochrome isoenzymes i liʻiliʻi i ka metabolism.

ʻO Dapagliflozin * (Dapagliflozin *) a me nā metabolites ua hoʻopiʻi ʻia loa ia e nā keiki, a he emi iho ma lalo o 2% ua waho i hoʻololi ʻia. Ma hope o ka lawe ʻana he 50 mg

Loaʻa ka C-dapagliflozin iā 96% radioaktif - 75% ma ka urine a me 21% i nā feces. Ma kahi o 15% o ka radioactivity i loaʻa i nā feces i helu ʻia e Dapagliflozin * (Dapagliflozin *).

Ma ka hoʻohālikelike (ʻoi aku ʻo AUC), ka ʻike olakino o ka dapagliflozin i loko o nā mea maʻi me ka diabetes type 2 a me ke ʻano ʻōlohelohe, maʻalahi a paʻakikī paha (e like me ka hoʻoholo ʻana ʻo Iohexol clearance) he 32%, 60%, a he 87% kiʻekiʻe ma mua o nā mea maʻi me ka maʻi type 2 a me ka hana maʻamau. ʻeha, kēlā me kēia ʻO ka nui o ka glucose i hoʻopuka ʻia e nā ʻōpū i ka lā i ka wā e lawe ai i ka dapagliflozin ma ka equilibrium i hilinaʻi ʻia i ka mokuahi o ka hana.

I nā maʻi me ka maʻi diabetes type 2 a me ka hana maʻamau maʻamau, a me ka hōʻino ʻole ʻana a me ka ikaika ʻole ʻole, 85, 52, 18 a me 11 g o nā glucose ka mea i hoʻopili ʻia i kēlā me kēia lā. ʻAʻohe hoʻākaʻawale ʻana i ka paa ʻana o dapagliflozin i nā protein i loko o nā mea hana olakino olakino a me nā mea maʻi e hiki ʻole ai ke like me ka ʻano paʻakikī. ʻAʻole i ʻike ʻia inā pili ka hemodialysis i ka hoʻolaha ʻana o dapagliflozin.

I nā mea maʻi me ka maʻi hepatic haʻahaʻa a maʻalahi paha, nā pono awelika o Cmax a me AUC o dapagliflozin he 12% a me 36% ke kiʻekiʻe, keu, ke hoʻohālikelike ʻia me nā mea hana olakino olakino. ʻAʻole koʻikoʻi kēlā mau ʻokoʻa i ia mau mea; no laila, ʻaʻole pono nā lula ʻana i ka pau ʻana o ka dapagliflozin no ka maʻi hepatic maʻalahi a me ka loli.

ʻAʻole i loaʻa ka nui o ka maʻi i ka maʻi i loko o nā mea maʻi ma lalo o nā makahiki he 70 (inā ʻaʻole ʻaʻole i manaʻo ʻia nā mea ʻē aʻe ma mua o ka makahiki). Eia nō naʻe, hiki ke hoʻonui ʻia ka loaʻa i ka ʻike ma muli o ka emi ʻana o ka hana hana i pili i ka makahiki. ʻAʻole lawa i nā hōʻike no ka poʻe maʻi ma mua o nā makahiki he 70.

I nā wahine, ʻo ka awelika AUC ka waiwai ma ka 22% ʻoi aku ka nui ma mua o nā kāne.

ʻAʻole i ʻike ʻia nā ʻokoʻa koʻikoʻi o ka maʻi o ka ʻōnaehana ma waena o nā ʻelele o nā lāhui Caucasian, Negroid a me Mongoloid.

Ua hoʻomaopopo ʻia nā hiʻona haʻahaʻa me nā piʻi kino o ke kino. No laila, i nā mea maʻi me ka hoʻohaʻahaʻa kino kino, hiki ke hoʻomaopopo ʻia i kahi liʻiliʻi i ka hoʻolaha, a i nā mea maʻi me ka nui o ke kaumaha kino - he hōʻemi i ka hoʻolaha ʻana o dapagliflozin Eia naʻe, ʻaʻole he koʻikoʻi nā hana a kēia mau ʻokoʻa.

ʻO ke kumukūʻai o ka lāʻau lapaʻau a pehea e kūʻai ai

Hiki iā ʻoe ke kūʻai aku no Forksig i loko o nā lāʻauʻai ma Moskoa, St. Petersburg a me nā kūlanakauhale ʻē aʻe o Rusia. Akāʻo ke kūʻai ʻana aku i ka lāʻau hiki ke hiki wale ma o ka lāʻau lapaʻau. Eia kekahi, ʻoi aku ka kiʻekiʻe o ke lāʻau lapaʻau ma mua o ʻEulopa. Hiki iā ʻoe ke kūʻai i ka huahana Forxiga kūlohelohe mai kahi mea kūʻai aku me ka lawe ʻana i nā māka i kuhikuhi ʻia.

Inā loaʻa ka dosage koi, a lawe ʻia ka lāʻau ma lalo o ke kauoha pololei mai Kelemania. ʻO ke kumu kūʻai o kahi pākī he 28 papa nā 90 euro. He pōmaikaʻi e kūʻai mai i kahi pahu o nā papa he 98 no ka 160 euro.

Hōʻike nā kipa

Sergey Viktorovich Ozertsev, endocrinologist: "Ma mua, nā poʻe maʻi me ka maʻi type 2 e pono e koho i ka hoʻoponopono hoʻoponopono kūpono no ka lōʻihi. I ka manawa like, ʻike pinepine lākou i ka hypoglycemia a me nā hopena ʻē aʻe. ʻO ka hoʻokolohua mau ʻana o kekahi mau lāʻau me ka neʻe ʻana o nā paila pale, ka hōʻahewa ʻia ʻana.

ʻO Olga, 42 makahiki: "Ua hōʻike ʻia ke maʻi maʻi maʻi ma ka 35 he 35. Kauka ke kauka i kahi meaʻai ikaika (loaʻa iaʻu nā pilikia koʻikoʻi me ke kaumaha). Ua hiki iaʻu ke nalo i ke kaumaha, hoʻopaʻa mau ʻia i kaʻu mau meaʻai, akā ke hoʻonui nei ka hilo. I ka wā mua, ua kuhikuhi ke kauka i nā lāʻau maʻalahi a maʻalahi, akā ua makaʻu ʻo ia i nā hopena hopena. No laila, ua hoʻoholo wau e kūʻai iā Forksigu a ʻaʻole nalowale. Lawe au ia manawa i hoʻokahi lā. Ua maikaʻi ʻo ia, he maʻamau ke kō.

Hoʻomākaukau ʻo Dapagliflozin

ʻO ke inoa kālepa no Dapagliflozin Forsyga. ^ E Ha yM. ʻO ka hui Pelekane ʻo AstraZeneca i hana i nā papa i ka pilina me ka American Bristol-Myers. No ka maʻalahi o ka hoʻohana, hiki i ka lāʻau lapaʻau ke 2 dosages - 5 a 10 mg. ʻO ka huahana kumu maʻalahi he mea maʻalahi ia mai ka hoʻopunipuni. Loaʻa ʻia nā papa o Forsig 5 mg i kahi ʻāpana a me nā ʻalopili ʻili ʻia he "5" a me "1427", 10 mg he mau kila, ka ʻohu ʻia "10" a me "1428". ʻEleʻele nā ​​papa o nā hewa ʻelua.

Wahi a nā ʻōlelo kuhikuhi, hiki ke mālama ʻia ʻo Forsigu no 3 mau makahiki. No ka mahina o ka mālama ʻana, pono ʻia ka pākeke 1, ʻo kāna kumukūʻai e pili ana i 2500 rubles. Ma ke ʻano, i ka mellitus maʻi diabetes, pono e kuhikuhi ʻia ʻo Forsigu me ka manu ʻole, ʻoiai ʻo Dapagliflozin e komo i loko o ka papa o nā lāʻau lapaʻau nui. Wahi a nā loiloi, ʻaʻole lawa loa ka loaʻa ʻana o kahi lāʻau. Hoʻolaha ʻia nā Forsig inā aia nā contraindications e lawe i ka metformin a i ole sulfonylurea, a ma nā ʻano ʻē aʻe ʻole e hiki ke hoʻokō i ka kōʻai maoli.

ʻAʻole piha nā Forsigi, no ka mea ke kū nei ka pale o patent i ka Dapagliflozin. Ua manaʻo ʻia nā hui kikowaena o Invocana (loaʻa i ka inhibitor canagliflozin SGLT2) a me Jardins (empagliflozin). ʻO ke kumukūʻai o ka mālama ʻia me kēia mau lāʻau mai ka 2800 rubles. kēlā me kēia mahina.

Nā hana lāʻau

Hoʻokomo pū mākou i kā mākou mau keiki i ka mālama pono ʻana i nā pae koko koko. I nā poʻe olakino, hiki i ka 180 g ka kānana i kānana i kēlā me kēia lā i ka wai i ka mua, aneane ʻo ia mau mea a reabsorbed a hoʻi i ka kahe koko. Ke piʻi ka hoʻoliʻiliʻi o ka glucose i nā moku i loko o ka mellitus maʻi diabetes, hoʻonui hou ʻia kona filtration ma ka renom glomeruli. I ka hōʻea ʻana i kekahi pae (e pili ana i 10 mmol / l i ka maʻi maʻi me ka pēpē olakino), kāpae ka ʻūhā hou i nā glucose āpau a hoʻomaka e hoʻoneʻe i ka nui o ka ihi.

ʻAʻole hiki i ke Glucose ke komo i nā membrane cell, no laila ke komo nei nā kime o ka sodium-glucose i kāna hana reabsorption. Aia kekahi ʻano, SGLT2, aia wale nō ma kēlā ʻaoʻao o nā nephrons kahi i loaʻa hou ka puhaka o ka glucose. I nā lālā ʻē aʻe, ʻaʻole i loaʻa ʻo SGLT2. ʻO ka hana a Dapagliflozin kahi i kau ʻia ma ka pale ʻana i ka hana o kēia transporter. Hoʻohana wale ia ma SGLT2, ʻaʻole i hoʻopilikia i nā mea lawe ʻenehana, a no laila ʻaʻole ia e hoʻopilikia i ka metabolism maʻamau.

Hoʻopili wale ʻia ʻo Dapagliflozin i nā hana o nā keiki nephrons. Ma hope o ka lawe ʻana i ka pā, hōʻaiʻē ka glucose a hoʻomaka e hoʻoiho ʻia i loko o ka paʻi i ka nui o ka nui ma mua o ka wā ma mua. Hoʻemi ʻia ka glycemia. ʻAʻole pili ka lāʻau lapaʻau i ka pae maʻamau o ke kō, no laila e lawe ʻole ia i ka hypoglycemia.

Ua hōʻike ʻia nā haʻawina ʻo ka lāʻau ʻaʻole wale e hōʻemi i ka glucose, akā pili pū i nā mea ʻē aʻe i ka hoʻomohala ʻana o nā ʻōpiopio o ka maʻi diabetes.

1. ʻO ka normalization o ka glycemia alakaʻi i kahi emi o ka pale ʻana i ka insulin, ma hope o ka hapalua o ka lawe ʻana i ka paukū e hōʻemi ʻia e ka awelika o 18%.
2. Ma hope o ka hoʻohaʻahaʻa ʻana i ka hopena o nā mea hoʻonā i ka glucose i nā cell beta, ke hoʻomaka ka hoʻihoʻi ʻana o kā lākou mau hana, e hoʻonui iki ka synthesis o ka insulin.
3. ʻO ke kūmole o ka glucose e alakaʻi i ka nalowale o nā kalori. Ke hōʻike nei nā ʻōkuhi mai i ka wā e hoʻohana ai ʻo Forsigi 10 mg i kēlā me kēia lā, kahi mea he 70 g o ka glucose i hoʻopuka ʻia, kahi mea e kū ai nā 280 kilocalories. Ma mua o 2 mau makahiki o ka hoʻokele ʻana, hiki ke hoʻolōʻihi ʻia ke kaumaha o 4.5 kg, ʻo ia ka 2.8 - ma muli o ka momona.
4. I nā maʻi maʻi me ka piʻi koko nui, ʻike ʻia kahi emi (hoʻohaʻahaʻa i ka systolic e pili ana i ka 14 mmHg). Ua mālama ʻia ka nānā ʻana no 4 mau makahiki, ua hoʻomau ʻia ka hopena ma kēia manawa. Hoʻopili ʻia kēia hopena o Dapagliflozin me kāna hopena diuretic insignificant (ʻoi aku ka nui o ka urine i ka manawa like me ka honi) a me ka momona kaumaha i ka wā e hoʻohana ai i ka lāʻau.

Nā hōʻailona no ka koho

Kuhi ʻia ʻo Dapagliflozin no nā maʻi maʻi 2. Nā pono e koi ʻia - ka hoʻohaʻahaʻa o ka nui o nā karapu i ka meaʻai, ka hana kino kino maʻamau o ka ikaika waena.

Wahi a nā ʻōlelo kuhikuhi, hiki ke hoʻohana ʻia ka lāʻau lapaʻau.

1. E like me ka mea ulu. Wahi a nā kauka, hoʻomaʻamaʻa pinepine ʻia ke koho ʻana ʻo Forsigi.
2. Hoʻohui ʻia i ka metformin, inā ʻaʻole e hāʻawi mau i ka hoʻohaʻahaʻa i ka glucose, ʻaʻohe hōʻailona no ke koho ʻana i nā papa e hoʻonui ai i ka hoʻokumu ʻana i ka insulin.
3. Ma ke ʻāpana o ka hoʻomaʻemaʻe ʻana e hoʻomaikaʻi ai i ka uku ʻana i ka maʻi diabetes.

Hoʻopilikia pōʻino o Dapagliflozin

Hoʻopili ʻia me ka Dapagliflozin, e like me nā lāʻau ʻē aʻe a pau, e pili ana i kekahi ikehu o nā hopena o nā ʻaoʻao. Ma keʻano holoʻokoʻa, helu ʻia ka ʻike palekana palekana ma ka ʻoluʻolu. Hoʻololi nā ʻōkuhi i nā hopena āpau e hiki ai, ua hoʻoholo ko lākou alapine:

1. ʻO nā maʻi Genitourinary kahi hopena koʻikoʻi o Dapagliflosin a me nā mea hoʻohālike. Hoʻohālikelike ia i ke kumu o ka hana o ka lāʻau lapaʻau - ka hoʻokuʻu o ke kuhi i ka urine. Kuhi ʻia ka pilikia o nā maʻi ma ka 5.7%, i ka hui kāohi - 3.7%. ʻO ka pinepine, ʻo nā pilikia i loaʻa i nā wahine i ka hoʻomaka o ka mālama ʻana. ʻO ka hapa nui o nā maʻi maʻi i ka maʻalahi o ke kaumaha hōʻeha a ua hoʻopau maikaʻi ʻia e nā ʻano maʻamau. ʻAʻole hoʻonui ka lāʻau i ka pyelonephritis i ka lāʻau.
2. ʻOi aku ma mua o 10% o nā maʻi, hoʻonui ka nui o ka urine. ʻO ka ulu holomua ʻo 375 ml. ʻIliʻuku ka ʻāpana urinary.
3. ʻOi aku ma mua o 1% o nā maʻi maʻi e nānā i ka constipation, ʻeha ʻeha, e ea ana. ʻO ka pilikia like ka hoʻonui ʻana i ka creatinine a i ʻole urea i ke koko.

Nā hōʻikeʻike e pili ana i ka lāʻau lapaʻau

ʻO Endocrinologists ma nā hopena o Dapagliflozin pane maikaʻi ʻia, nui ka poʻe e ʻōlelo he hiki i ka nui o ka lāʻau ke hōʻemi i ka hemoglobin glycated e ka 1% a i ʻole. ʻO ka nele o nā lāʻau lapaʻau e manaʻo ai lākou he manawa pōkole o kāna hoʻohana ʻana, kahi helu liʻiliʻi no nā noi ʻana ma hope. ʻAʻole aneane like ka Forsigu e like me ka lāʻau lapaʻau wale nō. Lapa nui nā kauka i ka metformin, glimepiride a me gliclazide, no ka mea makehewa kēia mau lāʻau, ʻike pono a kāpae i nā maʻi o nā maʻi o ka maʻi maʻi, a ʻaʻole kāpae i ka glucose, e like me Forsyga.

ʻAʻole hiki i ke Diabetics ke hoʻomau i ka lawe ʻana i kahi lāʻau hou, no ka makaʻu i nā maʻi maʻi bacterial o ka hana genitourinary. Ua ʻoi aku ka kiʻekiʻe o kēia mau maʻi i ka maʻi diabetes. Hoʻomaopopo nā wahine i ka hoʻonui ʻana o ka maʻi diabetes, hoʻonui ka nui o ka vaginitis a me ka cystitis, a hopohopo lākou e hoʻoikaika hou i ko lākou helehelena me Dapagliflozin. ʻO ka mea nui o nā mea maʻi i nā kumukūʻai Forsigi kiʻekiʻe a me ka nele o nā analogue maʻalahi.

E kū e aʻo! Manaʻo paha ʻoe i ka hoʻokele o ke ola i nā pōpoki a me ka insulin ke ala wale nō e mālama ai i ke kō i lalo o ka mālama ʻana? ʻAʻoleʻoiaʻiʻo! Hiki iā ʻoe ke hōʻoia i kēia me ʻoe e hoʻomaka e hoʻohana. heluhelu hou aku >>

Dapagliflozin (Forsyga)

ʻAno maʻi type 2 - kahi maʻi i pili i ka piʻi nui ʻana o nā maʻi o ka urinary tract (UTI) a me nā maʻi ʻōpū, e like me ka vulvovaginitis a me ka balanitis i ka wahine a me nā maʻi ʻoho fungal i nā kāne 33, 34. ʻO nā mea nui e like me ka disfunction system immune, glycosylation o nā selu uroepithelial he mea nui hoʻi ia.

E pili ana i kēia mau ʻike, ua ʻae ʻia ʻo dapagliflozin e ka FDA ma hope o ka ʻae ʻia e ka European Medicines Agency (EMEA) 16, 39.

Hoʻohālikelike

Hoike ʻia nā hoʻokolohua hoʻokolohua a me nā hoʻokolohua kūpono i kahi kikoʻī o ka hana o nā mea paʻa SGLT2. Hāʻawi kēia papa ʻai i nā hana ʻenehana kūʻokoʻa i ka insulin no ka hoʻoponopono ʻana i ka glycemia i ka diabetes type 2 me ka hoʻomanawanui maikaʻi, ka haʻalele ʻana o nā hopena maikaʻi ʻole i ke kaumaha o ke kino, ka hopena o ka hypoglycemia a me nā hopena ʻē aʻe koʻikoʻi.

ʻO ka lāʻau Forsig (dapagliflozin) i nā haʻawina mau he 104 mau hōʻike i ka lōʻihi glycemic efficacy, paʻa koʻikoʻi momona ma muli o ka momona momona a me kahi haʻahaʻa o nā kūlana hypoglycemic. ʻO Forsiga kahi koho e pili ana i ka sulfonylureas i nā maʻi i loaʻa ʻole i ko lākou mau pahuhopu me ka metformin monotherapy.