ʻO ka lāʻau Baeta: nā loiloi o nā loea a me nā mea hana, kūʻai

Ua hōʻike ʻia ka lāʻau lapaʻau no ka mellitus type type 2 no ka therapy hou i:

• halihalani,
• metformin
• kalikei
• nā hui pūpū o ka ʻekahi wana, metformin a me kahi mea hoʻopuka,
• hui me thiazolidinedione a me metformin,
• a i ka loaʻa ʻole o ka mana glycemic kūpono.

Ka hoʻoponopono ʻia ʻana

Pēlā ʻo Bayeta ka subcutaneously i lawelawe ʻia i ka ʻūhā, ka pāpale a me ka ʻōpū paha. ʻO ka ʻōmua mua he 5 mcg. E komo i 2 mau manawa i kahi lā e pili ana i ka hola 1 ma mua o ka ʻaina kakahiaka a me ka ʻaina ʻaina. Ma hope o ka ʻai ʻana, ʻaʻole pono e lawelawe ʻia ka lāʻau lapaʻau.

Inā hoʻihoʻi ka mea maʻi no kekahi kumu no ke kaʻi ʻana o ka lāʻau lapaʻau, loli hou nā inikini. Ma hope o hoʻokahi mahina o ka mālama ʻana, pono e hoʻonui ʻia ka hopena mua o ka lāʻau i ka 10 mcg.

Me ka hoʻokolohua noho ʻana o Bayet me thiazolidinedione, metformin, a i ʻole hui pū ʻana me kēia mau lāʻau lapaʻau, ʻaʻole hiki ke loli i ka hopena mua o ka thiazolidinedione a i ke metformin.

Inā ʻoe e hoʻohana i ka hui ʻana o Baeta me ka derivatives o sulfonylurea (i ka mea e hōʻemi i ka hopena o ka hypoglycemia), pono paha ʻoe e hōʻemi i ka nui o ka derivative o ka sulfonylurea.

Nā hiʻohiʻona noi

• pono e lawe ʻole ʻia ka lāʻau ma hope o ka ʻaina,
• ʻaʻole hōʻike ʻia ka hoʻolaha ʻana o ka IM lāʻau a i ʻole ʻo IV.
• ʻAʻole pono e hoʻohana ʻia ka lāʻau lapaʻau inā maloʻo a i ʻole pohā ka hopena.
• ʻAʻole pono e hoʻokele ʻia ʻo Bayetu inā ʻike ʻia nā ʻōpala i nā hopena.
• e kū'ē i ke kua o ka lāʻau no ka exenatide, hiki i ka hoʻouluʻana o ka antibody.

Nui! I loko o nā maʻi he nui i hoʻoili ʻia ke kino e like me kēlā mau antibodies, ua ʻoki ka titer a ua noho haʻahaʻa ʻia no ka 82 mau pule ma ka hoʻomau ʻia ʻana o ka therapy. Eia naʻe, ʻaʻole e pili i ka hele ʻana o nā antibodies i nā ʻano a me ke pinepine o nā hopena pā i hōʻike ʻia.

Pono ke kauka e hele ana i ka mea maʻi me ko Bayeta e alakaʻi i ka nalo o ka makemake, a e like me ke kaumaha o ke kino. He kumukūʻai kūpono loa kēia ka hoʻohālikelike ʻana i ka hopena o ka mālama ʻana.

I nā hoʻokolohua preclinical i hana ʻia ma nā kiʻi a me nā pōkole me ka hopena carcinogenic i ka wā i paʻi ʻia me ka waiwai exenatide, ʻaʻole i ʻike ʻia.

I ka helu ʻana o nā manawa o 128 i ka hoʻāʻo ʻia o ke kanaka ma nā isika, hōʻike ʻia nā rodents i ka nui o ka nui (me ka ʻole o ka hōʻike ʻana i ka malignancy) o ka adenomas C-cell thyroid.

Uaʻike nā ʻepekema ʻepekema i kēia mea me ka hoʻonui i ka ola o nā holoholona hoʻokolohua e loaʻa i ka exenatide. Kekahi luhi, akā naʻe, i hiki hewa nā luhi i ka hana iā ia. Kau lākou

• ka hoʻomohala ʻana i ka pani ʻole ʻana i ka hanu,
• hoʻoulu serum,
• ka uluʻana o ka papa o ka pilikia a me ka paʻa ʻole o ka renal ʻole, e koi pinepine ai i ka hemodialysis.

ʻO kekahi o kēia mau hōʻike i ʻike ʻia i kēlā mau mea maʻi i lawe i hoʻokahi a keu aku paha i nā lāʻau like i ka manawa like e pili ana i ka metabolism wai, ka hana māka, a i nā loli pathological ʻē aʻe i hana ʻia.

ʻO nā lāʻau lapaʻau e pili ana me nā NSAIDs, ka ACE inhibitors, a me ka diuretics. Ke koho ʻana i ka hana maʻi a me ka hoʻokuʻu ʻana i ka lāʻau lapaʻau, ka mea i koho mua i ke kumu o nā ala pathological, ua hoʻihoʻi ʻia ka hana hoʻololi o nā pēpē.

Ma hope o ka hoʻopaʻa ʻana i nā haʻawina a me nā preclinical, ʻaʻole i hōʻike ʻo exenatide i nā hōʻike o kona nephrotoxicity pololei. E kūʻē i ke kua mua o ka hoʻohana ʻana i ka lāʻau Bayeta, ua ʻike ʻia nā hihia lohi o ka pancreatitis o ka maʻi.

E hoʻomaopopo: pono e ʻike nā mea maʻi i nā maʻi o ka maʻi pancreatitis maʻa. Ke kuhikuhi nei i ka mālama ʻana i ka maʻi maʻi, ua nānā ʻia kahi kala ʻana o ka hana ʻoi ʻana o ka pancreas.

Ma mua o ka hoʻomau ʻana me ka ʻōlelo injera o Bayeta, pono e heluhelu ʻia ka mea maʻi i nā ʻōlelo pili i hoʻohana ʻia no ka hoʻohana ʻana i ka peni ʻiwauwa, hōʻike ʻia ke kumu ma laila.

Nā Hoʻohui

1. ʻO ka heleʻana o ka maʻi ketoacidosis maʻi.
2. ʻAno maʻi type 1.
3. Kahawai
4. ʻO ka heleʻana o nā maʻi maʻi gastrointestinal.
5. ʻO ka huehalolo hopena.
6. Haumakua.
7. He 18 makahiki.
8. Hypersensitivity i nā ʻāpana o ka lāʻau.

Hāpai a me nā pēpē

I kēia mau manawa ʻelua, ua hoʻomau ʻia ka lāʻau lapaʻau. ʻO ke kumukūʻai o ke ʻano kuhihewa i kēia loiloi paha i kiʻekiʻe loa. Ua ʻike ʻia he nui nā lāʻau lapaʻau e hoʻopilikia i ka hoʻomohala ʻana o ka pūpū.

He makuahine nele ʻole a maopopo ʻole paha ke alakaʻi i nā kuhi fetal. Kokoke i nā lāʻau lapaʻau āpau i komo i ke kino o ke pēpē me ka waiū o ka makuahine, no laila e makaʻala kēia mau mahele o nā lāʻau lapaʻau.

Monotherapy

ʻO nā hopena ʻino maikaʻi i mālama ʻia i nā maʻi iʻoi aku ma mua o nā manawa i kākau ʻia penei:

Nā kūloko kūloko:

• Hōʻike pinepine ka itching i nā pūnaewele injection.
• Aobeā, ʻulaʻula a me ka ʻōpala.

Mai ka pūnaehana hana ʻana, ʻike pinepine ʻia nā hōʻike ʻike ʻia.

Pili pinepine ka ʻōnaehana kikowaena me ka dizziness. Inā mākou e hoʻohālikelike i ka lāʻau Bayeta me ka pletebo, a laila piʻi ka nui o nā hihia i hoʻopaʻa ʻia i nā maʻi hypoglycemia i ka lāʻau i wehewehe ʻia e 4%. ʻO ka mākaukau o nā episodone o ka hypoglycemia e hōʻike ʻia me ka maʻalahi a me ka maʻalahi.

Hoʻohui hui

ʻO nā hanana pōʻino i nānā ʻia i nā poʻe maʻi ma mua o hoʻokahi me ka hui pū ʻana me nā like me ka monotherapy (e ʻike i ka papa i luna).

Pane ka ʻōnaehana o ka digestive:

1. Ka manawa pinepine: ka huhū o ka makemake, nilo, ka luaʻi ʻana, ka ʻeha ʻana o ka maʻi, gastroesophageal reflux, dyspepsia.
2. ʻO ka maʻamau: ka hū a me ka ʻeha o ka ʻōpū, constipation, belching, flatulence.
3. Kekahi: polipi pancreatitis.

ʻO ka pinepine, ʻike ʻia ka nausea o ka ikaika a i ʻole ka nāwaliwali. He kūpaʻa ia a hoʻemi ʻia ʻo ia iho i ka manawa me ka loaʻa ʻole o nā hana i kēlā me kēia lā.

Pūnaehana pinepine ke kikowaena kikowaena me nā hōʻeha a me ka maʻi ʻole, ʻilihune me ka hiamoe.

Ma ka ʻāpana o ka ʻoihana endocrine, nānā pinepine ʻia ka hypoglycemia inā e hui pū ʻia ka exenatide me nā derivatives o sulfonylurea. E pili ana i kēia, pono e nānā i nā dosis o nā derivatives o ka sulfonylurea a hōʻemi iā lākou me ka piʻi nui o ka hypoglycemia.

ʻO ka hapa nui o nā maʻi hypoglycemic ma ka uluʻana ke hoʻohālikelike ʻia me ka maʻalahi. Hiki iā ʻoe ke pani i kēia mau hōʻike wale nō me ka hoʻohana waha ʻana i nā ʻaina. Ma ka ʻāpana o ka metabolism, i ka wā e lawe ai i ka lāʻau Bayeta, ʻike pinepine ʻia ka hyperhidrosis, ʻoi aku ka nui o ka dehydration e pili ana me ka hoʻopiʻi a i ʻole nā ​​maʻi ʻaʻa.

Hoʻopilikia ka ʻōnaehana urinary i nā hihia paʻakikī, me ka maikaʻi ʻole o ka aʻalolo a me ka pilikia ʻole.

Hōʻike nā hōʻike i nā hopena kūlohelohe e loaʻa ʻole ka maʻamau. Penei ka edema a i ʻole nā ​​anaphylactic hōʻike hōʻike.

Nā kūloko o ke kūloko i ka manawa o ka exenatide injection e pili ana i ka ʻohi, ka ʻulaʻula, a me ka hōʻeha ʻana i ka wahi i ʻōlelo ʻia.

Aia nā loiloi o nā hihia o ka hoʻonui ʻia sedimentation erythrocyte (ESR). He hiki nō i kēia inā i hoʻohana pū ʻia ka escinate me ka warfarin. ʻO kēlā mau hōʻike e like me nā hihia līpona e hele pū ʻia me ke koko.

Basically, he ʻoluʻolu a maʻalahi hoʻi nā hopena o ka hopena, ka mea i ʻole e koi ai i ka hoʻohemo ʻana o ka mālama ʻana.

Lapaʻau

Ke hana lāʻau lapaʻau - hypoglycemic, incretinomimetic.

ʻO ka incretins, e like me ka pona o ka ponaide-like me glucagon-1 (GLP-1), e hoʻomaikaʻi i ka hana o nā pū beta, hoʻomaikaʻi i ka huna ʻana i ka glucose o ka glucose, a me ka hoʻokaʻawale i nā mea huna glucoseagon a hoʻohaʻahaʻa i ka hoka o ka gastric ma hope o ko lākou komo ʻana i ka kaila maʻamau mai nā ʻōpū. He exenatide kahi mimetic mimetin ikaika e hoʻonui ai i ka huna ʻana i ka glucose o ka glucose a loaʻa nā hopena hypoglycemic i loaʻa i ka incretins, e hoʻomaikaʻi ana i ka mana glycemic i nā mea maʻi me ka maʻi diabetes type 2.

ʻO ka wailua amino amino o ka exenatide mahele like pū me ka pilina o ka GLP-1. Hōʻike ʻia ʻo Exenatide e hoʻopili a hoʻopili i nā mea komo GLP-1 i loko o nā kānaka i ka vitro, e alakaʻi ana i ka synthesis e hilinaʻi i ka glucose o ka insulin, a ma vivo, kahi huna o ka insulin mai nā papa beta pancreatic me ke komo ʻana o ka cyPic AMP a me / a me nā ala e ʻike ai i ka intacellular hōʻailona ala.

Hoʻomaikaʻi ʻo Exenatide i ka mana glycemic i nā maʻi me nā maʻi type 2 ma o kekahi mau mīkini.

I nā kūlana hyperglycemic, hoʻonui ka exenatide i ka huna ʻana i ka glucose i ka huna ʻana i ka insulin mai nā cell beta pancreatic. Ua kāpae kēia mea huna huna i ka hoʻōla ʻana o ka glucose i ke koko a ke hoʻokokoke nei ia i ka maʻamau, a laila e hōʻemi ʻia ka hopena o ka hypoglycemia.

ʻO ka huni ʻana o ka insulin i nā minuke 10 mua loa, ka mea i kapa ʻia ʻo ka "mana mua o ka pane ʻana i ka insulin." Ua paʻa ia i nā mea maʻi me ka diabetes type 2. Eia nō kekahi, ua lilo ka hana mua o ka hopena insulin i ka hana mua o ka beta-cell hana i ka maʻi type 2. Ua hoʻihoʻi ʻia ʻo Exenatide. a i ʻole ma ka hoʻonui mua ʻana i ka lua a me ka lua o ka pane o ka insulin i ka poʻe maʻi me nā maʻi maʻi type 2.

I ka maʻi me ka diabetes type mellitus kū'ē i ke kua o ka hyperglycemia, ke hoʻomalu nei ka hana o ka exenatide i ka nui o ka huna ʻana o ka glucagon. Eia nō naʻe, ʻaʻole e hoʻopili ʻo exenatide i ka pane o ka glucagon maʻamau i ka hypoglycemia.

Ua hōʻike ʻia i ke alakaʻi ʻana o ka exenatide i kahi i hoʻopoina i ka momona a me ka hoʻohaʻahaʻa ʻana i ka ʻai o ka meaʻai (i nā holoholona a me nā kānaka).

I nā maʻi me ka diabetes mellitus type 2, ʻo ka exenatide therapy i hui pū me ka metformin a me / a i ʻole ka hoʻomākaukau ʻana i ka haʻalulu sulfonylurea e hōʻemi i ka wikiwiki o ka hoʻokaʻa ʻana o ke koko glucose, glucose glucose postprandial, a me ka glycosylated hemoglobin index (HbA1c), ma laila e hoʻomaikaʻi ai i ka mālama glycemic i kēia mau maʻi.

Carcinogenicity, mutagenicity, hopena i ka mahele

I loko o ka noiʻi ʻana i ka carcinogenicity o exenatide i nā kiole a me nā kaole nui, me ka hoʻomalu sc scosis o nā papa 18, 70 a me 250 μg / kg / lā, ka nui o ka helu ʻana i nā adenomas C-cell me nā hōʻailona ʻole o ka hōʻino ʻana i nā kiʻī wahine i ʻike ʻia i nā papa āpau i aʻo ʻia (5 , He 22 a me 130 ka nui o ka manawa ma mua o ka MPD i kanaka. I nā kiʻī, ʻaʻole i hōʻike ka hoʻomohala o nā ʻōhua like i ka hopena carcinogenic.

ʻAʻole i loaʻa i nā hopena mutagenic a me clastogenic o exenatide i ka wā o nā hoʻokolohua.

Ma nā haʻawina o ka hua momona i nā isika, ma nā wahine wahine i loaʻa i nā kahena o 6, 68 a 760 mcg / kg / lā, e hoʻomaka ana mai ka manawa 2 wiki ma mua o ka moe ʻana a i loko o 7 mau lā o ka hāpai ʻana, ʻaʻohe hopena maikaʻi loa o ka lōkē i nā dosis a hiki i 760 mcg / kg / lā (ua ʻike ʻia ka systemic ka 390 mau manawa ma mua o MPRD - 20 mcg / lā, i helu ʻia e AUC).

Kapehu. Ma hope o ka hoʻomalu ʻia ʻana o ka exenatide ma loko o kahi wai o 10 μg i nā mea maʻi me ka diabetes mellitus type 2, ua loaʻa koke ka exenatide, ua loaʻa nā Cmax (211 pg / ml) ma hope o nā hola 2.1. ʻO AUCo-inf ka 1036 pg · h / ml. Hoʻonui ka ʻike o Exenatide (AUC) i ka nui o ka nui o ka nui ma waena o 5 a 10 μg, inā ʻaʻole i hoʻonui ʻia ka nui o Cmax. Hoʻomaopopo ʻia ka hopena like me ka hoʻokele subcutaneous o exenatide ma ka ʻōpū, ka ʻūhā a mua pūpū.

Māhele. Vd o ka exenatide ma hope o ke kākahi ʻo sc i kahi no ka 28.3 L.

Metabolism a me ka hoʻopā ʻana. Hoʻokuʻu ʻia ia ma ka kānina glomerular i ukali ʻia e ka proteolytic degradation. ʻO ka hoʻomaʻemaʻe Exenatide he 9.1 l / h. ʻO nā hola T1 / 2 hope loa he 2.4 mau hola.ʻO kēia mau lāʻau lapaʻau ka exenatide ka kūʻokoʻa kūʻokoʻa. Hoʻoholo ʻia nā mea hou o ka exenatide ma kahi o 10 mau hola ma hope o ka pau ʻana.

ʻO ka pharmacokinetics i nā hihia lapaʻau kūikawā

Hola paʻa kino hana. I nā mea maʻi me ka hoʻohaʻahaʻa ʻole a ʻole ka pōʻino (Cl creatinine 30-80 ml / min), ʻaʻole iʻokoʻa ka ʻike o ka exenatide i nā mea maʻi me nā hana maʻamau. Eia nō naʻe, i nā mea maʻi me ka hopena o ka renal stage me ka hopena o ka dialysis, ʻo ka hōʻike o 3.37 mau manawa ma mua o nā kumuhana olakino.

Hōʻeha ka hana ʻoluʻolu. ʻAʻole i alakaʻi ʻia ka maʻi ʻo Pharmacokinetics i nā maʻi me ka maʻi a me ka maʻi ʻiʻo kahi i mālama ʻole ʻia.

Kāhea. ʻAʻole loli nā pharmacokinetics o exenatide i nā ʻelele o nā lāhui like ʻole.

Ke Kino o ke Aliʻi Mass (BMI). Ka noiʻi pharmacokinetic i loko o nā mea maʻi me ka BMI o ≥30 kg / m2 a me Exenatide

Type 2 diabetes mellitus me ka hoʻohui i ka lāʻau me ka metformin, he derivative sulfonylurea, thiazolidinedione, kahi hui o ka metformin a me kahi deralona sulfonylurea, a i hui pū paha me nā metformin a me thiazolidinedione i ka hihia o ka mana o ka glycemic control.

Nā hopena hopena o ka mea Exenatide

E hoʻohana me ka metformin a / a i ʻole turon sulfonylurea

Hōʻike ka papa i nā hopena kū'ē (ʻoi aku ma mua o ka hypoglycemia) i loaʻa me ka pinepine o ≥5% a ʻoi aku ka nui o ka pletebo i hōʻike ʻia ma ka hopena o 30 mau pule o ka exenatide ma kahi o ka metformin a / a i kahi derivative sulfonylurea.

Nā hiʻohiʻona e pili ana me nā alapine o> 1%, akā ʻo Interaction

Pono e hoʻohana ʻia ka Exenatide me ka mālama ʻana i nā maʻi i lawe i nā lāʻau lapaʻau e pono ai ke komo koke ʻana mai ka gastrointestinal tract, hiki iā ia ke hōʻalo i ka hapa ʻana o ka ʻeha. Pono e ʻōlelo ʻia nā mea maʻi e lawe i ka lāʻau lapaʻau waha, ka hopena o ka mea e hilinaʻi ana i ka paepae ʻana o ka paepae (e. Inā pono e lawe ʻia nā mea inu like me ka meaʻai, a laila e lawe ʻia i ka wā o ia mau meaʻai i ka wā ʻaʻole i hoʻokele ʻia nā exenatide.

Digoxin. Me ka hoʻokolohua ʻōhumu o ka digoxin (ma kahi kiko o 0.25 mg 1 manawa / lā) me ka exenatide (10 μg 2 mau manawa i ka lā), Cakax of digoxin emi i ka 17%, a hoʻonui ʻia ka Tmax ma nā hola he 2. Akā naʻe, ʻo ka huina o ka hopena pharmacokinetic (AUC) i loko. ʻaʻole i loli ka ʻāina kūlike.

Lovastatin. Me ka hapa hoʻokahi o ka lovastatin (40 mg) aʻo ka lawe ʻana i ka exenatide (10 μg 2 mau manawa i ka lā), hoʻemi ʻia ʻo AUC a me Cmax o lovastatin e ka nui o 40 a me 28%, kēlā, a hoʻonui ʻia ʻo Tmax ma nā hola he 4. I loko o kahi loiloi haumania 30 mau pule, ua lawelawe ʻia ka exenatide i nā mea maʻi ka loaʻa ʻana o nā HMG-CoA reductase inhibitors ʻaʻole i hui pū ʻia e nā loli me ka lipid pū o ke koko.

Lisinopril. I nā maʻi me ka hypertension arterial maʻalahi a maʻalahi paha e ka lisinopril (5-20 mg / lā), ʻaʻole i loli ʻo exenatide i kahi AUC a me Cmax o lisinopril i ka waiwai. ʻO ka Tmax o ka lisinopril ma ka equilibrium i hoʻonui ʻia e nā hola 2. ʻAʻole i hoʻololi i nā hōʻailona o nā awelika o kēlā me kēia lā ʻo SBP a me DBP.

Warfarin. I ka hoʻokolohua ʻana i nā lāʻau lapaʻau i ʻike ʻia i nā mea olakino olakino, ua kuhi ʻia me ka hoʻomaka ʻana o warfarin 30 mau minuke ma hope o exenatide, hoʻonui ʻia ʻo Tmax o warfarin ma kahi o ka manawa he 2 i ka hopena no ka hopena o ka maʻi ma ka Cmax a me AUC. I ka manawa o ka nānā ʻana i ke kūʻai aku ma hope o ka kūʻai ʻana, ua hōʻike ʻia kekahi mau mea o ka hoʻonui i loko o INR i kekahi manawa, i hui ʻia me ka hoʻokahe ʻana me ka hoʻohana pinepine ʻana o exenatide me warfarin (pono pono ka nānā ʻana o PV, ka mea nui i ka hoʻomaka ʻana o ka mālama ʻana a i ka wā e loli ai ke ʻano).

ʻO ka hoʻohana ʻana o ka exenatide i hui pū me ka insulin, D-phenylalanine derivatives, meglitinides a alpha-glucosidase inhibitors ʻaʻole i aʻo ʻia.

Kaukahi Exenatide

Ma muli o ka hoʻonui ʻia o ka pinepine o ka hypoglycemia me ka hoʻopili pū ʻana o ka exenatide me nā derivatives o sulfonylurea, pono pono e hoʻolako no ka hōʻemi o ka haʻahaʻa o nā derivatives o ka sulfonylurea me ka hoʻonui nui aʻe o ka hypoglycemia. ʻO ka hapa nui o nā hypoglycemia i ka uluʻana he mau haʻahaʻa a maʻalahi i hoʻopaʻa ʻia a pale ʻia e ka waha o ka calcium acidate.

ʻAʻole ia i kāpae ʻia i loko / a i ʻole i ka mana m / i ka lāʻau lapaʻau.

I ka manawa o ka nānā aku ʻana ma hope o ke kūʻai aku, ua ʻike ʻia nā hihia lohi i ka hoʻomohala ʻana o ka maʻi pancreatitis ma nā mea maʻi e lawe nei i ka exenatide. Pono e hoʻomaopopo ʻia nā mea maʻi e hoʻomanawanui i ka ʻeha o ka ʻōpū puʻuwai, i hui pū ʻia e ka luaʻi, he hōʻailona ʻo ia o ka pancreatitis. Inā he kānalua o ka hoʻomohala ʻana i ka pancreatitis, exenatide a i ʻole nā ​​mea i hopohopo ʻia ʻē aʻe e hoʻihoʻi, e pono nō ke hoʻokō ʻia nā hōʻike hōʻoia, pono e hoʻomaka ʻia nā hana kūpono. Inā hoʻopaʻa ʻia ka hopena o ka maʻi pancreatitis, ʻaʻole i hāʻawi ʻia ka hoʻomau ʻia o ka mālama ʻana me ka exenatide i ka wā e hiki mai ana.

I ka wā o ka nānā ʻana i ka mākaʻi kūʻai ma hope o ke kūʻai ʻana, ua ʻike ʻia nā hihia lihilahi o ka hana ʻole o ka renal, a me ka nui o ka serum creatinine, i ka ulu ʻana i ka pilikia o ka hana ʻana i ka maʻi, a me ka hana ʻole, a me ka manawa e koi ana i ka hemodialysis. ʻO kekahi o kēia mau hihia i hōʻike ʻia i nā mea maʻi i lawe i kekahi a i ʻole he lāʻau lapaʻau i ʻike ʻia e pili ana i ka hana ʻana a me / a i nā mea maʻi nā mea maʻi nalo, ka luaʻi a me / a me nā mea maʻi me / ʻole ka hydration, ʻoiai e hoʻohana ana i nā lāʻau lapaʻau, e komo pū ana . ^ E Ha yM. ACE inhibitors, NSAIDs, diuretics. Ua hiki hou ke hana ʻana i ka lua o ka hana papaha me ka mālama ʻana i nā lāʻau mālama a me ka wehe ʻana i ka lāʻau, hiki ke hoʻopilikia i ka hana o ka renal, me ka exenatide. Ma nā hōʻike preclinical a me ka haukapila, ʻaʻole i hōʻike ka exenatide i nā nephrotoxicity pololei.

Hiki ke nānā ʻia nā anavodies e exenatide i ka wā lapaʻau me ka exenatide.

Pono e hoʻomaopopo ʻia nā mea maʻi e hiki ke mālama ʻia me ka exenatide i ka hoʻokaʻawale o ka mea momona a me / a me ke koʻikoʻi paha o ke kino a ma muli o kēia mau hopena, ʻaʻohe mea e pono ai ke hoʻololi i ka noho aliʻi dosage.

Nā Nūhou E pili ana

• Exenatide (exenat> Nā Haumaha Hoʻohana

Hoʻohana ʻia ka lāʻau lapaʻau i ka subcutaneously ma luna o ke kolu o luna a waena paha o ka poʻohiwi, ʻūhā, a i loko hoʻi o ka ʻōpū. Pēlā e like me ke kānāwai, ua ʻōlelo ʻia e hoʻololi i kēia mau pūnaewele i mea e haʻalele ai i ka hoʻokumu ʻana o nā konglomerates subcutaneous.

Pono e hoʻokō ʻia kēia maʻi e like me nā kānāwai āpau no ka hoʻohana ʻana i kahi peni syringe. Pono ka lā o ka lāʻau e mālama ai i hoʻokahi hola ma mua o nā kīʻaha nui ma waena o nā liʻiliʻi he 6 mau hola.

ʻAʻole hiki ke hoʻohui ʻia ʻo Exenatide me nā palapala hoʻohālikelike hou aku, e pale aku ai i ka hoʻomohala ʻana i ka hopena kūpono ʻole.

ʻO ka helu ʻana o BAETA

ʻO ke kūleʻa no ka hoʻokele sc, ʻaʻohe palala.

Nā mea kūʻai: sodium acetate trihydrate, glacial acetic acid, mannitol, metacresol, wai no a.

1,2 ml - peni syringe (1) - nā pākeke o ke kāleka (1).
2.4 ml - peni syringe (1) - nā pākeke o ke kāleka (1).

Ka lāʻau Hypoglycemic. ʻO Glucagon-like Peptide Receptor Agonist

Ka lāʻau Hypoglycemic. ʻO Exenatide (Exendin-4) kahi mimetin mimetic a he 39-amino acid amidopeptide. ʻO nā incretins, e like me ka ponaide-like ponaida-1 (GLP-1), e hoʻomaikaʻi i ka huna ʻana i ka glucose i ka glucose, hoʻomaikaʻi i ka hana β-cell, kaohi ʻana i ka hoʻokaʻawale me ka hoʻokahe nui ʻana o ka gastric ma hope o ko lākou komo ʻana i ka kaila ākea mai nā ʻōpū. He exenatide kahi mimetic mimetin ikaika e hoʻonui ai i ka huna ʻana i ka glucose o ka glucose a loaʻa nā hopena hypoglycemic i loaʻa i ka incretins, e hoʻomaikaʻi ana i ka mana glycemic i loko o nā mea maʻi me ka maʻi diabetes type 2.

ʻO ka mahele o ka waikawa amino o ka exenatide mahele like me ka pakanui o ke kanaka GLP-1, ma muli o ia mea i hoʻopaʻa ʻia a hoʻoulu i nā mea hoʻokipa GLP-1 i loko o nā kānaka, e alakaʻi ana i ka synthesis-hilinaʻi nui o ka glucose a me ka huna ʻana o ka insulin mai ka pancreatic cells-cells me ka komo ʻana o ka cyPic AMP a me / a i ʻole nā ​​mea ʻē aʻe intracellular i hōʻailona. ala. Hoʻonohonoho ka Exenatide i ka hoʻokuʻu ʻana o ka insulin mai nā β-cell i mua o ka piʻi ʻana o ka glucose kiʻekiʻe.

Hoʻolaha ka Exenatide i ka hana kemika a me nā hana farmacological mai ka insulin, derivatives sulfonylurea, D-phenylalanine derivatives a me meglitinides, biguanides, thiazolidinediones a me nā alpha-glucosidase inhibitors.

Hoʻonui ka Exenatide i ka mālama glycemic i nā mea maʻi me ka maʻi type 2 no ka mea hana i kēia mau hana.

I nā kūlana hyperglycemic, hoʻonui ka exenatide i ka huna nui ʻana o ka glucose i ka insulin mai ka pancreatic β-cells. Ua kāpae kēia mea huna huna i ka hoʻōla ʻana o ka glucose i ke koko a ke hoʻokokoke nei ia i ka maʻamau, a laila e hōʻemi ʻia ka hopena o ka hypoglycemia.

ʻO ka ʻōlelo huna Insulin i ka mau minuke 10 mua (i pane i ka nui o ka glycemia), ka mea i kapa ʻia ʻo ka "pae mua o ka pane ʻana i ka insulin", ua paʻa ʻia i nā mea maʻi me ka maʻi diabetes type 2. Eia kekahi, ʻo ka nalowale o ka pae mua o ka pane ʻana o ka insulin he ʻemi o nā hana o ka hana β-cell i ka maʻi diabetes type 2. Hoʻomaka hou ka mālama ʻana o ka exenatide i ka mua a me ka lua o nā lua o ka pane ʻana i ka insulin i nā maʻi maʻi me ka maʻi type 2.

I ka maʻi me ka diabetes type mellitus kū'ē i ke kua o ka hyperglycemia, ke hoʻomalu nei ka hana o ka exenatide i ka nui o ka huna ʻana o ka glucagon. Eia nō naʻe, ʻaʻole e hoʻopili ʻo exenatide i ka pane o ka glucagon maʻamau i ka hypoglycemia.

Hōʻike ʻia ka alakaʻi ʻana o ka exenatide i kahi hoʻohaʻahaʻa i ka momona a me ka hoʻohaʻahaʻa ʻana i ka ʻai o ka meaʻai, ke kāohi i ka kaomi o ka ʻōpū, kahi e alakaʻi ai i ka lohi i kona hoʻokaʻina ʻana.

I nā maʻi me ka maʻi diabetes mellitus type 2, hui exenatide i hui pū me ka metformin, thiazolidinedione a me / a i ʻole ka hoʻomākaukau ʻana i ka sulfonylurea hoʻomākaukau i ka emi ʻana o ka ʻai o ke koko glucose, glucose o ka koko postprandial, a me ka HbA 1c, ma laila e hoʻomaikaʻi ai i ka mālama glycemic i kēia mau maʻi.

Ma hope o ka hoʻomalu ʻana o ka exenatide ma kahi o 10 μg i nā mea maʻi me ka diabetes mellitus type 2, ua hele koke ka exenatide a hiki i kahi C C ma hope o ka hola 2.1, ʻo ia ka 211 pg / ml, ʻO AUC o-inf ka 1036 pg × h / ml. Ke kū nei i ka exenatide, hoʻonui nui ʻo AUC i ka nui o ka hoʻonui ʻana i ka hopena mai 5 μg a 10 μg, aʻo ke kaʻina kū ʻole o ka C max. Hoʻomaopopo ʻia ka hopena like me ka hoʻokele subcutaneous o exenatide ma ka ʻōpū, ka ʻūhā a mua pūpū.

V d o exenatide mahope iho o ka hooponopono sc ana he 28.3 L.

Metabolism a me ka hoʻopā ʻana

ʻO ka exenatide hana mua ʻia e ka filomation glomerular i ukali ʻia e ka proteolytic degradation. ʻO ka wehe ʻana o Exenatide he 9.1 l / h. ʻO ka hola hope loa o T 1/2 he mau hola 2.4 ʻO kēia mau pharmacokinetic hiʻohiʻona o ka exenatide he kūʻokoʻa kūʻokoʻa. Hoʻoholo ʻia nā mea hou o ka exenatide ma kahi o 10 mau hola ma hope o ka pau ʻana.

ʻO ka pharmacokinetics i nā hihia lapaʻau kūikawā

I nā mea maʻi me ka hoʻōla ʻole a ʻole ka pōʻino (CC 30-80 ml / min), ʻaʻole i ʻokoʻa loa ka clearance exenatide mai ka hoʻomaʻemaʻe ʻana i nā mea maʻi me nā hana o ka maʻi maʻamau, no laila, ʻaʻole i koi ʻia ka hoʻoponopono ʻana o ka lāʻau. Eia naʻe, i nā mea maʻi me ka hopena o ka renal stage me ka hopena o ka dialysis, ua hōʻemi ʻia ka clearance hōʻemi i 0.9 l / h (hoʻohālikelike ʻia me 9.1 l / h i nā kumuhana olakino).

No ka mea ua hoʻopili ʻia ka exenatide e nā keiki, ua manaʻoʻiʻo ʻaʻole i loli ka ʻalā i nā lau a me ka hoʻololi ʻana o ka exenatide i ke koko.

ʻAʻole pili ka makahiki i ka maʻi pharmacokinetic o exenatide. No laila, ʻaʻole i koi ʻia ka poʻe maʻi ʻōpiopio e hoʻokō i ka hoʻoponopono hoʻoponopono ʻia.

ʻAʻole aʻo ʻia nā pharmacokinetics o exenatide i nā keiki ma lalo o 12 makahiki o nā makahiki.

Ma kahi noiʻi pharmacokinetic i nā keiki'ōpiopio 12 a 16 mau makahiki me ka type 2 diabetes mellitus, i ka manawa i kauoha ʻia ai ka exenatide i kahi maʻi o 5 μg, ua like nā pālapa pharmacokinetic me ka poʻe pākeke.

ʻAʻohe ʻanoʻokoʻa ʻē aʻe i waena o nā kāne a me nā wahine i loko o ka pharmacokinetics o exenatide.

ʻAʻole loli nā pharmacokinetics o exenatide i nā ʻelele o nā lāhui like ʻole. ʻAʻole koi ʻia ka hoʻoponopono ʻana ma ke ʻano ʻōiwi.

ʻAʻohe mea hoʻomaopopo ma waena o ka index mass body (BMI) a me exenatide pharmacokinetics. ʻAʻole koi ʻia ka hoʻoponopono ʻana ma kahi BMI.

Hōʻikeʻike BAETA

ʻO ka ʻikepili mai kā BAETA i kōkua:

- Kahi 2 diabetes mellitus ma ke ʻano he monotherapy i ka ʻai a me ka hana e hoʻokō ai i ka mana o ka glycemic kūpono.

- type type 2 diabetes mellitus as an supplement therapy for metformin, a sulfonylurea derivative, thiazolidinedione, hui pū ʻana o ka metformin a me kahi konupuna a sulfonylurea, a i hui pū me nā metformin a me thiazoldinedione inā ʻaʻole i loaʻa ka mana glycemic pili.

Loaʻa ka hopena o BAETA

ʻO ka hopena ʻino e loaʻa pinepine ai i nā hihia kaawale i kahi i hoʻohālikelike ʻia me ka hoʻōki ʻia ʻana aʻe: pinepine pinepine (≥10%), pinepine ʻia (≥1%, akā ʻano kūlohelohe. kahua wili.

Mai ka pūnaehana ʻana: pinepine - nausea, luaʻi, ʻeha, dyspepsia, hoʻoluhi ka ʻai.

Mai ka ʻaoʻao o ka pūnaehana neʻe o ka waena: pinepine - dizziness.

Ke hoʻohana nei i ka Bayeta ® ma ke ʻano he monotherapy, ʻo ka nui o ka ulu ʻana o ka hypoglycemia he 5% hoʻohālikelike ʻia me 1% pletebo.

ʻO ka hapa nui o nā hypoglycemia ma ka uluʻana he mauʻoluʻolu a maʻalahi hoʻi.

Hoʻololi ʻia nā hopena ʻino e kū pinepine ai i nā hihia i neʻe ʻia e like me ka helu ʻana aʻe nei: pinepine pinepine (≥10%), pinepine ʻia (≥1%, akā mai ka ʻaki ʻana o ka digestive: pinepine pinepine - ka uʻi, luaʻi, ʻehaʻeha, pinepine - hoʻemi. mea ʻawaʻawa, dyspepsia, gastroesophageal reflux, pinepine - ʻeha o ka ʻōpū, ka ʻūhū, ka ʻōpū, ka constipation, ka ʻono ʻole, ka lemaki, ka pancreatitis luhi pinepine, ʻoi aku ka maʻi pākaha o ka hapalua o ke ʻano a me ka hoʻohaʻahaʻa i ka wā paʻa he hana ʻaʻano ʻole.

Mai ka ʻaoʻao o ka pūnaehana loko ma waena: pinepine - dizziness, headache, jarang - hiamoe.

Mai ka ʻōnaehana endocrine: pinepine loa - hypoglycemia (i hui pū ʻia me kahi derogative sulfonylurea). No ka mea ke hoʻonui pinepine nei o ka hypoglycemia me ka hoʻopili pū ʻana me ka lāʻau Bayeta ® me ka huaʻala sulfonylurea, pono pono e hoʻolako no ka hōʻemi o ka haʻahaʻa o nā dermoni sulfonylurea me ka hoʻonui nui aʻe o ka hypoglycemia. ʻO ka hapa nui o nā hypoglycemia i ka uluʻana he mauʻoluʻolu a maʻalahi paha, a ua mālama ʻia e ka hoʻokomo o waha i nā ʻaina.

Mai ka ʻaoʻao o ka hana o ka metabolism: pinepine - hyperhidrosis, luhi - dehydration (pili me ka puki, ka luaʻi a me / a me nā maʻi).

Mai ka pūnaehana urinary: luhi - functioning a renal impaired, komo kaulike ʻole o ka hana renalous, exacerbation o ke papa o ka lawelawe ʻole i kahi aʻi, hoʻonui i ka serum creatinine.

Nā ʻano maʻi alolika: loaʻa ʻole - angioedema, ʻaʻole liʻiliʻi loa - ka hopena anaphylactic.

Nā kūmole kūloko: pinepine - hōʻeha i ka wahi i ʻōlelo ʻia, ʻaʻole liʻiliʻi - ʻūhā, ʻulaʻula hoʻi i ka wahi i ʻōlelo ʻia.

Nā mea hou: pinepine - haʻalulu, nāwaliwali.

Ua hōʻike ʻia i nā hihia he nui o ka manawa coagulation me ka hoʻohana ʻana i ka warfarin a me ka exenatide, a ʻike pinepine ʻole ʻia hoʻi e ke koko.

Ma ka laulā, ka hopena o ka ʻaoʻao a i ʻole me ka hoʻohaʻahaʻa i ka ikaika a ʻaʻole i alakaʻi i ka haʻalele ʻana o ka hana.

Nā leka uila (post-marketing)

Nā maʻi kūnekele: emi pinepine - ka hopena anaphylactic.

Hōʻalo i nā meaʻai a me ka metabolism: hakakā nui - ka hoʻoheheʻe, e pili pinepine ana me ka maʻi mualala, ka luaʻi a me / a i ʻole ke kaumaha ʻana, ka hoʻoluhi momona.

Mai ka pūnaehana nūhou: dysgeusia, mau hiamoe.

Mai ka pūnaehana ʻana: belching, constipation, flatulence, jarang - pancreatitis koʻikoʻi.

Mai ka ʻōnaehana urinary: kahi hoʻololi o ka hana o ka kidney, incl. kaulike ʻole o ka hana hema, exacerbation of kidney renal failed, pale ʻole i ka hana renal, hoʻonui i ka serum creatinine concentration.

ʻO nā hopena dermatological: rula maculopapular, hōʻeha o ka ʻili, urticaria, angioedema, alopecia.

ʻO nā haʻawina Laboratory: kahi hoʻonui i INR (i ka wā i hui pū me ka warfarin), i kekahi mau hanana pili i ka hoʻomohala ʻana o ke koko.

Ma ka hihia o kahi overdose (pā i 10 mau manawa a ʻo ka nui loa i ʻōlelo ʻia ai), ʻike ʻia kēia mau hōʻailona i ka maʻi nui: neʻeha a me ka luaʻi ʻana, a me ka hoʻolālā wikiwiki hoʻi o ka hypoglycemia.

Hoʻomaʻamaʻa: lawe ʻia ka hana hōʻailona hōʻailona, ​​me ka hoʻokaʻawale ʻana o nā kūpuna o ka glucose i ka hihia o ka hypoglycemia koʻikoʻi.

Pono e hoʻohana ʻia ʻo Bayeta ® me ka akahele i ka poʻe maʻi e hoʻomākaukau ana i nā mākau waha e koi ana i ka hoʻopio koke ʻana mai ka ʻeha o ka gastrointestinal, ʻoiai Hiki ke hōʻole ʻo Baeta ® i ka inu ʻana i ka ʻōpū. Pono e hoʻomaopopo ʻia nā mea maʻi e lawe i ka lāʻau lapaʻau waha, ka hopena o ka mea e hilinaʻi ana i ka paepae ʻana o ka paepae (me ka laʻana, ka antibiotics) a ma kahi o 1 mau hola ma mua o ka hoʻokele ʻana o exenatide. Inā pono e lawe ʻia nā mea inu like me ka meaʻai, a laila e lawe ʻia i ka wā o ia mau meaʻai i ka wā ʻaʻole i hoʻokele ʻia nā exenatide.

Me ka hoʻokolohua hui ʻole o ka digoxin (0.25 mg 1 manawa / lā) me ka mākaukau Baeta ®, hōʻemi ka C max o ka digoxin i ka 17%, a hoʻonui ka nui o T max i nā hola he 2 mau. Akā naʻe, ʻaʻole i loli ka AUC i ka mokuʻina o ka waiwai.

Me ka hoʻomaka ʻana o Bayeta ®, ua hōʻemi ʻia ʻo AUC a me C max o lovastatin e ka 40% a me 28%, kēlā me kēia, a me ka T max i hoʻonui ʻia e pili ana i nā hola he 4. ʻO ka hoʻokele ʻana o Bayeta® me nā HMG-CoA reductase inhibitors ʻaʻole i ukali ʻia e nā loli i ka hui lipid manu (HDL) -kolesterol, LDL-cholesterol, ka nui o ka kolamu a me TG).

I nā maʻi me ka hypertension arertial haʻahaʻa a maʻalahi paha, e kū nei i ka wā e lawe ana i ka lisinopril (5-20 mg / lā), ʻaʻole i hoʻololi ʻo Bayeta ® i ka AUC a me C max o lisinopril ma ka waiwai. ʻO T max o lisinopril ma ka kūlele he hoʻonui ma ka hakahaka 2. He mau loli i kēlā me kēia lā i loko o ke kaila systolic a me ka diastolic i ke koko.

Ua hōʻike ʻia me ka hoʻomaka ʻana o warfarin 30 mau minuke ma hope o ka mākaukau Baeta ® T max i hoʻonui ʻia e ka nui o nā hola 2. Ua nānā ʻia kahi hoʻololi koʻikoʻi ma C max a me AUC.

ʻO ka hoʻohana ʻana o Bayeta ® i hui pū me ka insulin, me ka ʻala o D-phenylalanine, ʻo meglitinide a i ʻole nā ​​alpha-glucosidase inhibitors i aʻo ʻole ʻia.

Mai alakaʻi i ka lāʻau lapaʻau ma hope o ka ʻaʻa ʻana. ʻAʻole ia i kāpae ʻia i loko / a i ʻole i ka mana m / i ka lāʻau lapaʻau.

ʻAʻole pono ke hoʻohana ʻo Bayeta ® inā ʻike ʻia nā ʻōpala i loko o ka hopena a inā palahā paha a he kala paha.

Ma muli o ka nui o ka immunogenicity o nā lāʻau lapaʻau e loaʻa ai nā protein a me nā peptides, hiki ke hoʻomohala ka hoʻomohala ʻana o nā antibodies e exenatide i ka wā o ka mālama ʻana me Bayeta ®. Ma ka hapa nui o nā poʻe maʻi e ʻike ʻia ai ka hana ʻana o ia mau ʻano antibodies, ua hoʻemi ʻia ka hapa o ko lākou titili ma muli o ka hoʻomau ʻia ʻana o ka lāʻau a hoʻomau ʻia ka liʻiliʻi no 82 mau pule. ʻAʻole ka hopena i ka hopena o nā antibodies i nā ʻano a me nā ʻano o nā hopena like ʻole i hōʻike ʻia.

Pono e hoʻomaopopo ʻia nā mea maʻi ʻo ka mālama ʻana me ka Bayeta ® hiki i ka hōʻemi i ka mea momona a me / a i ke kaumaha ʻana paha o ke kino, a ma muli o kēia mau hopena, ʻaʻohe mea e pono ke hoʻololi i ka noho aliʻi dosage.

Ma nā noi preclinical i loko o nā mehe a me nā kahe, ʻaʻole i ʻike ʻia ka hopena carcinogenic o exenatide. I ka wā e noi ʻia ai kahi hopena ma nā lālani 128 mau manawa i loko o nā kānaka, e loaʻa ana kahi helu helu C-cell thyroid adenomas me nā hōʻailona ʻole o ka malignancy, ka mea i hui pū ʻia me ka hoʻonui ʻana i nā lā o nā holoholona hoʻokolohua e loaʻa i ka exenatide.

Ua hōʻike ʻia nā hihia i ʻole o ka hana i ʻole ke ahonui a me ka hoʻonui ʻana i ka serum creatinine, ka ulu ʻana o ka pilikia o ka renal, ʻo ka hopohopo ʻana i ka papa o nā hana a me ke kūleʻa o ka renal o ka hana ʻole, a i kekahi manawa ua hemodialysis. Ua nānā ʻia kekahi mau mea e like me nā maʻi i loaʻa i nā lāʻau lapaʻau a ʻona paha e pili ana i ka hana renal / metabolism wai a me / a i ʻole e kūʻē i nā hanana ʻino ʻē aʻe e pili ana i ka hoʻoulu ʻia ʻana, e like me ka nausea, ka luaʻi a me / a me nā maʻi ʻana. ʻO nā lāʻau lapaʻau hoʻohui e pili ana i ka hana ACE inhibitors, NSAIDs, a me diuretics. Ke koho ʻana i ka maʻi hōʻailona a me ka hoʻokuʻu ʻana i ka lāʻau, hiki paha i ke kumu o nā loli pathological, ua hana hou ʻia ka hana renal impaired. I ka wā o nā noi preclinical a me ka lapaʻau o exenatide, ʻaʻole i loaʻa ka ʻike no ka nephrotoxicity pololei.

Ua hōʻike ʻia nā hihia pālua o ka pancreatitis hoʻonā e lawe ana iā Bayeta ®. Pono e hoʻomaopopo ʻia nā mea maʻi e pili ana i nā hōʻailona o ka maʻi o ka pancreatitis maʻa: mau loa ka maʻi ʻeha. I ka koho ʻana i ka therapyaticatic, nānā ʻia ka hopena o ka pancreatitis maʻa.

ʻO nā mea maʻi ma mua o ka hoʻomaka ʻana i ka mālama ʻana me ka Bayeta® pono e hoʻomaʻamaʻa iā lākou iho me ke "alakaʻi no ka hoʻohana ʻana i kahi peni ʻoi" i pili i ka lāʻau.

Papa inoa B. Pono e mālama i ka lāʻau lapaʻau ma ke mahana o 2 ° a 8 ° C. ʻO 2 mau makahiki kahi ola.

Pono ka mālama ʻana i kahi lāʻau lapaʻau i ka peni syringe ma kahi wela ʻaʻole eʻoi aku ma mua o 25 ° C no nā manawa 30 aku.

Pono ke mālama ʻia ka lāʻau i waho o ka hiki o nā keiki, pale ʻia mai ka ʻike i ka mālamalama, mai hoʻokaʻawale.