Clopidogrel - nā ʻōlelo aʻoaʻo no ka hoʻohana ʻana i nā papa, nā hōʻailona, ka hana o ka hana, nā hopena ʻaoʻao a me ke kumukūʻai
ʻO ka wehewehe e pili ana i 28.01.2015
- Palapala Latin: Laka>
ʻO ka papa o ka lāʻau Clopidogrel ka hopena o 75 mg o nā mea hana like ma ka ʻano o ka hydrosulfate.
Nā kumuwaiwai hou: prosalv, lactose monohala, colloidal silicon dioxide, sodium croscarmellose, sodium fumarate.
Ka hana hui: pink opadray II (hypromellose, lactose monohydrate, titanium dioxide, carmine, dye yellow iron oxide, macrogol), silicone emulsion.
E hoʻokuʻu i ke ʻano
ʻO nā papa nā uhi poli a puni ke biconvex i ka like, keokeo-ʻeleʻele ma kahi ʻāpana.
- 14 papa no nā pākī, 1 a i ʻole 2 mau ʻāpana i kahi pā pepa.
- 7 a he 10 paha mau papa i ka pā, 1, 2, 3 a i ʻole 4 mau ʻāpana i kahi pā pepa.
- 7 a he 10 mau papa i loko o kahi pōpō; 1, 2, 3 a i ʻole 4 mau blisters i loko o kahi ʻāpana pepa.
- 14 a 28 mau papa i loko o kahi pahu polū, 1 pahu i loko o kahi pā.
- 14 a 28 mau papa i ke polū, hiki i 1 i loko o kahi pā.
Pharmacodynamics a me ka pharmacokinetics
Ua hoʻoikaika ikaika ʻia ka lāʻau lapaʻau i ka hoʻohui ʻana o platelet me ka hoʻokaʻawale mau i ka paʻa o ka adenosine diphosphate (ADP) i nā ʻāpana platelet, a he hōʻemi pū nō hoʻi i ka hiki ke hana i nā mea kūlike glycoprotein ma lalo o ka hana adenosine diphosphate. ʻO ka lāʻau lapaʻau e hōʻemi i ka pilina o nā platelets, ka mea i loaʻa e kekahi mau antagonist, ke kāohi nei i kā lākou hoʻoweliweli hou ʻia e ka ADP. Hoʻohui nā molekole o nā lāʻau me nā mea i hoʻonui ʻia i ka platelet ADP, ma hope o ka lilo ʻana o nā platelets mau loa i ko lākou manaʻo i ka hoʻoulu ʻana ADP.
Kūpono ka hopena o ka hoʻopili ʻana i ka palaki platelet i ʻelua mau hola ma hope o ke ʻano o ka ʻōlelo mua. ʻO ke kiʻekiʻe o ke pani ʻana o ka hoʻohui ʻana e hoʻonui i loko o 4-7 mau lā a hiki i kona kiʻekiʻe i ka hopena o kēia manawa. I kēia hihia, pono ke komo ʻana o ka lā i kēlā me kēia lā he 50-100 mg i kēlā me kēia lā. Inā loaʻa ka hōʻino o ka atherosclerotic vascular, a laila lawe i ka lāʻau lapaʻau e pale i ka holomua o ka maʻi.
Ma hope o ka lawe ʻana i ka lāʻau lapaʻau i kahi manawa pōkole e hoʻopili i ka gastrointestinal tract. ʻO ka bioavailability o ka lāʻau he 50%; ʻaʻole i pili ka ʻai i ka pae. Ka huelo o ka hana huakaʻi i loko o ke akea. I loko o ke kō koko, hiki ke loaʻa nā waiwai nui loa i hoʻokahi hola ma hope o ka lawe ʻana i ka lāʻau lapaʻau. ʻO ka pau ʻana o ka hapalua ola-ʻewalu mau hola, kahi i hoʻopā ʻia e nā keiki a ma o nā ʻāpana ʻole.
Nā ʻōlelo kikoʻī
Pili ka hoʻohana ʻana i ka lāʻau lapaʻau me ka pono o ka mālama mau ʻana i ke ʻano o ka mea maʻi. Loaʻa nā ʻano kikoʻī penei:
- I ka poʻe maʻi ʻoi aku ka nui o kona mau makahiki he 75 mau makahiki, e ʻoki ʻia ke kānāwai o ka nui o ka maʻi mua.
- I ke kaʻina o ka lāʻau, pono ʻoe e hahai i nā ʻōuli o ka ʻōnaehana kiʻekiʻe, e kaohi i ke ʻano hana o ke akea.
- Hoʻohana me ka mālama ʻana i nā maʻi i loaʻa i ka nui o ke neʻe o ke koko no ka hōʻeha ʻana a i nā kumu ʻē aʻe.
- Ma mua o nā maʻi e pili ana i ka nalowale o ke koko, pono ia e noʻonoʻo i ka lāʻau e hoʻolōʻihi i ka manawa koko.
- Ke hoʻokele nei i nā kaʻa, ʻike e hiki paha i ka clopidogrel ke hoʻohālikelike.
I ka wā hāpai
I kēia lā, ʻaʻohe kumu o nā noi holo piha a me ka papa hōʻike no ka hopena o ke clopidogrel i ka wā hāpai a me ka hoʻomohala ʻana i ka pūpū. No kēia kumu, ʻaʻole ke kuhikuhi ʻana i ka lāʻau i ka wā hāpai. ʻAʻohe mea hōʻike i ka hoʻoili ʻana i loko o ka lāʻau i loko o ka waiū umauma, no laila, ʻaʻole i ʻōlelo ʻia ʻo Clopidogrel i ka wā o ka ʻōpū.
Nā hōʻailona no ka hoʻohana ʻana
Kāohi i nā hanana atherothrombotic ma hope o nā maʻi ma hope o ka maʻi myocardial (mai ka lā mai a hiki i 35 mau lā), he ischemic stroke (mai 7 mau lā a hiki i 6 mau makahiki ka nui) a i ka poʻe paha i kahi maʻi peripheral arterial occlusion maʻi.
Kāohi i nā hanana atherothrombotic (i hui pū me ka acetylsalicylic acid) i nā mea maʻi me ka maʻi coronary syndrome:
- me ka hōʻea ʻole o ka māhele ST (neʻe ʻole aina ʻole a myocardial infarction me ka Q wave), me ka poʻe maʻi e hoʻomau ana me ka ʻanā e pili ana i ka interutan coronary.
- me ka piʻi ʻana o ka ʻāhai ST (ʻoiʻi myocardial infarction) me ka loaʻa ʻana o ka lāʻau lapaʻau a me ka hiki ʻana o thrombolysis.
Nā Hoʻohui
- ka huhū maʻi (no ka laʻana, kahe koko mai i ka uluna peptic a i ʻole hemorrhage intracranial).
- ka lahui lactose lula, lactase ka hapa lactase a me ka malabsorption glucose-galactose,
- nā keiki a me nā ʻōpio ma lalo o 18 makahiki o ka makahiki (ʻaʻole i hoʻokumu ʻia ka palekana a me ka pono),
- Hypersensitivity i clopidogrel a i ʻole nā mea hoʻohiki o ka lāʻau lapaʻau.
- ka huakaʻi kaoole maʻa mau, kahi e hopohopo ai ke koko i hiki ke ʻokoʻa (ʻokoʻa i ka ʻike mākia)
- ka maʻi hakahaka (maopopo i ka ʻike kikī)
- nā maʻi i loaʻa ka predisposition i ka hoʻomohala ʻana i ke koko (e pili ana i ka gastrointestinal a i ʻole intraocular).
- ka hui pū ʻana o nā lāʻau non-steroidal non-inflammatory, komo koho koho COX-2
- ka hoʻohana like o warfarin, heparin, glycoprotein IIb / IIIa inhibitors,
Pehea e hoʻohana ai: dosis a me ke ʻano o ka mālama ʻana
ʻO nā poʻeʻelemakule a me nā mea maʻi maʻi me ka hana maʻamau o ka CYP2C19 isoenzyme
Pono e lawe ʻia i Clopidogrel-SZ ma ke ʻano pono, me ke ʻano o ka kō ʻana o ka meaʻai.
ʻO ka maʻi Myocardial infarction, ka maʻi ischemic, a hōʻike i ke maʻi peripheral arterial occlusion maʻi
Lawe ʻia ka lāʻau lapaʻau ma 75 mg 1 mau lā / lā.
I ka poʻe maʻi me ka myocardial infarction (MI), hiki ke mālama ʻia ka mālama ʻana mai nā lā mua a hiki i ka lā 35 o MI, a me nā mea maʻi me ka ischemic stroke (II) - mai 7 mau lā a hiki i 6 mau mahina ma hope o MI.
Ka maʻi coronary eʻae me ka ʻole o ka paukū st (kahi paʻa, ka myocardial infarction a ʻole Q wave)
Pono e mālama ʻia me ka Clopidogrel-SZ me hoʻokahi dosis o ka hoʻouka ʻana o 300 mg, a laila hoʻomau ʻia ma kahi pākeke o 75 mg 1 manawa / lā (i hui pū me ka acetylsalicylic acid ma ke ʻano he antiplatelet agent ma nā inika o 75-325 mg / lā). Mai ka hoʻohana ʻana o ka acetylsalicylic acid ma nā koina nui e pili ana i ka nui o ka pohō o ke koko, ʻo ka nui o ke ʻano o ka acetylsalicylic acid e pono e nui aku i ka 100 mg. ʻO ka hopena therapeutic kiʻekiʻe e nānā ʻia e ke kolu o ka malama o ka mālama ʻana. ʻO ka papa aʻo o ka mālamaʻana a hiki i ka 1 makahiki.
Ka maʻi coronary e pili ana i ka pae kiʻekiʻe ST
Ua koho ʻia ʻo Clopidogrel ma kahi mahele o 75 mg 1 mau lā / lā me kahi pākaukau hoʻokahi o ka hoʻouka ʻai ʻana i ka hui pū me ka acetylsalicylic acid ma ke ʻano he antiplatelet agent a me ka thrombolytics (a i ʻole thrombolytics). Hoʻomaka ka lāʻau hoʻohui i ka manawa like ma hope o ka hoʻomaka ʻana o nā hōʻailona a hoʻomau mau no ka liʻiliʻi o 4 mau hebedoma. I nā mea maʻi ma luna o ka makahiki 75, pono e hoʻomaka ʻia ke mālama ʻana me Clopidogrel-SZ me ka ʻole o ka lawe ʻana i kahi poka.
ʻO nā maʻi me ka genetically hoʻemi ʻia CYP2C19 Isoenzyme function
ʻO ka nāwaliwali o ka hana metabolism e hoʻohana ana i ka isoenzyme CYP2C19 hiki ke alakaʻi i ka hoʻohemo ʻana i ka hopena antiplatelet o clopidogrel. ʻO ka regimen dosage kiʻekiʻe loa no nā maʻi me ka nāwaliwali nāwaliwali me ka hoʻohana ʻana i ka isoenzyme CYP2C19.
Ka hana lāʻau lapaʻau
Hoʻopiha āpau Antiplatelet. ʻO Clopidogrel he prodrug, kekahi o nā metabolite ikaika o ia ka mea pale i ka hui platelet. ʻO ka clopidogrel metabolite ikaika e kāohi i ka paʻa ʻana o ka adenosine diphosphate (ADP) i ka pīpī ʻeke o ka P2Y12 a ma hope o ka hoʻōla ʻana o ADP-mediated o ka pūlea GPIIb / IIIa, e alakaʻi ana i ka hoʻopaʻa ʻana i ka hoʻohui platelet. Ma muli o ke kau palena ʻole ʻia, mālama ʻia nā platelets i ka hoʻoulu ʻana o ka ADP no ke koena o ko lākou ola (ma kahi o 7-10 lā), a me ka hoʻoulu hou ʻana o ka hana platelet maʻamau i kahi wikiwiki e like me ka hōʻano hou o ka platelet. ʻO ka hui platelet i hoʻoulu ʻia e nā agonist e ʻokoʻa i ka ADP ke kī ʻia ʻia hoʻi e ka blockade o ka hoʻonui ʻana o ka platelet i hoʻonui ʻia e ADP. No ka mea ka hana ʻana i kahi metabolite ikaika me ka hoʻohana ʻana i ka isoenzymes P450, a ʻokoʻa paha kekahi o ka polymorphism a i hoʻopaʻa ʻia paha e nā lāʻau lapaʻau ʻē aʻe; ʻaʻole paha i nā maʻi āpau i loaʻa nā kīkala platelet.
Nā hopena hopena
Mai ke kikowaena waena a me ka peripheral nervous system: pinepine - i ka ʻeha, ka maʻi ʻana a me ka paresthesia, ʻaʻole aneane - vertigo, aneane ʻole - ka pale hewa ʻana i ke ʻano o ka naʻau.
Ma ka ʻāpana o ka ʻōnaehana cardiovascular: ka liʻiliʻi loa - vasculitis, hōʻailona i ka hoʻokaʻina ʻana o ke koko, ka hemorrhage intracranial, hemorrhage ocular (conjunctival, i ka iwi a me ka retina), hematoma, nosebleeds, ka huhū mai ka ʻōpū o ka ʻōpū, ka hoʻokaʻa ʻana o gastrointestinal, hemorrhage retroperitoneal me ka ʻeha. ka hopena, hemorrhages ma nā ʻeha a me nā ʻāpana, hematuria.
Mai ka pūnaehana hanu: ākea loa - bronchospasm, perstonitis interstitial.
Mai ka papa hana ʻana: pinepine - ka ʻeha, ka ʻeha o ka ʻōpū, ka ʻōpū, ka maʻi maʻamau - he ʻōpū o ka ʻōpū a me ka ʻōpio duodenal, gastritis, maʻiʻa, luaʻi, constipation, flatulence, ʻokoʻa loa - pancreatitis, colitis (me ka ulcerative a i ʻole lymphocytic colitis). stomatitis, waha o ka ate ole, hepatitis.
Mai ka ʻōnaehana urinary: jarang loa - glomerulonephritis.
Mai ke ʻano piʻipiʻi koko: pinepine - hoʻonui i ke kahe koko.
Mai ka ʻōnaehana hemopoietic: pinepine - thrombocytopenia, leukopenia, neutropenia a eosinophilia, loa jarang - thrombocytopenic thrombohemolytic purpura, thrombocytopenia nui (platelet counts a ʻoi paha ma kahi o 30 × 109 / l), agranulocytosis, granulocytopenia,
Ma ka ʻāpana o ka ʻili a me nā kiko o ka subcutaneous: pinepine - maʻamau ka ʻili o ke kino a me ka ʻeha, ʻike pinepine loa - angioedema, urticaria, erythematous rash (pili me ka clopidogrel a i acetylsalicylic acid), i aneane loa - dermatitis bullous (erythema multiforme, Stevens-Johnson syndrome, ʻonaʻawa, ka ʻona ), eczema a me ka licus planus.
Mai ka ʻōnaehana musculoskeletal: loa loa - arthralgia, arthritis, myalgia.
Ma ka ʻāpana o ka ʻōnaehana pale: ākea loa - kūʻai i ka anaphylactoid, maʻi serum.
Hoʻohui
Hiki i ka lawelawe ʻana me ka clopidogrel ke hoʻonui i ka nui o ke koko, no laila ʻaʻole ʻae ʻia ka hoʻohana ʻana o kēia hui.
Hoʻohana ʻia ka hoʻohana ʻana o nā blockers receptor IIb / IIIa i hui pū me ka clopidogrel e makaʻala i nā poʻe maʻi e loaʻa ka nui o ke kahe koko (me nā hōʻeha a me nā hana hōʻemi a me nā kūlana pathological paha).
ʻAʻole ka hoʻololi o ka acetylsalicylic i ka hopena o ka clopidogrel, ka mea e pale ai i ka hui platelet ADP-induced, akā ʻo ka clopidogrel potentiates ka hopena o ka acetylsalicylic acid ma ka collelet-induced platelet aggregation. Eia nō naʻe, ʻaʻole i hoʻopiʻi nui ka hoʻohana ʻana i ka acetylsalicylic acid me ka clopidogrel e lilo i mea antipyretic mākaʻi o 500 mg 2 mau manawa / lā no 1 lā ʻaʻole i hoʻoulu nui i ka wā koko i hoʻoneʻe ʻia e ka ʻoihana clopidogrel. Ma waena o ka clopidogrel a me ka acetylsalicylic acid, hiki ke hoʻokūkū pharmacodynamic, kahi e hiki ai ke hoʻonui i ka pohō. No laila, me kā lākou hana like ʻana, pono e mālama ʻia, ʻoiai ma nā noiʻi haumania, ua loaʻa i nā mea maʻi ke ʻano hui me clopidogrel a me ka acetylsalicylic acid a hiki i hoʻokahi makahiki.
Wahi a kahi haʻawina hōʻike i mālama ʻia me nā mea hana olakino olakino, i ka wā e lawe ai i ka clopidogrel, ʻaʻohe pono e loli i ka nui o ka heparin a me kāna hopena anticoagulant, ʻaʻole i loli. ʻO ka hoʻohana like ʻana o ka heparin i hoʻololi i ka hopena antiplatelet o ka clopidogrel. Ma waena o ka clopidogrel a me ka heparin, hiki i kahi hoʻopihapiha pharmacodynamic hiki ke hoʻonui i ka hōʻalo o ke kahe, no laila ʻo ka hoʻohana like ʻana i kēia mau lāʻau e pono ai ka makaʻala.
Nā ʻōkuhi no ka hoʻohana
Hoʻohana ʻia ka Clopidogrel i nā maʻi pākeke 1 mau manawa i ka lā (ma mua o ka ʻaina awakea, ma hope o ka ʻaina awakea), ʻaʻohe o ka meaʻai. ʻAʻole hoʻi e ʻawa ʻia ka papa papa. E inu i ka wai o ka wai (palena liʻiliʻi maʻa 70 ml). ʻO ka laʻana e hōʻike ʻia ai e ka hopena o ka lāʻau lapaʻau ʻo 75 mg i kēlā me kēia lā.
Ka hana noi no ka maʻi naʻau puʻuwai: nā pākeke ma ke keʻena cardiology ma lalo o ka mālama ʻana i nā maʻi lapaʻau i kuhikuhi mua ʻia he 300 mg o clopidogrel. Ma hope aku, hoʻomau ʻia ka hoʻomau i ke kahu mālama ʻana o ka 75 mg, ʻoi aku ka pinepine i nā hui pū ʻana me ka acetylsalicylic acid i loko o nā huina mai 0,075 a 0.325 g.
Nui! No ka pale ʻana i ke kahe, lawe hou aku i ka 100 mg o ka acetylsalicylic acid.
ʻAʻole maopopo ia ka lōʻihi o ke komo ʻana. Ke hoʻomau nei ka lāʻau lapaʻau a hiki i ke ʻano o ka mea maʻi i ka maʻamau i ke ʻano o ke kauka e hele ana.
ʻO ke papa o ka mālama ʻana i ka wā o ka hopena o ka hōʻeha ʻana o ka puʻuwai: ʻo ke kumu o ka clopidogrel he 75 mg i kēlā me kēia lā, ʻoiai ka hoʻomaka ʻana o ka haʻahaʻa o 300 mg i hui pū me nā acetylsalicylic acid a me nā lāʻau thrombolytic.
Nui! He mea nui ia no nā poʻe maʻi ma hope o ko 75 mau makahiki o ka makahiki e wehe i ka hoʻohana ʻana i ke kaomi ʻana i nā helu ʻana o ka lāʻau.
ʻO ka lōʻihi ma hoʻokahi mahina.
I kahi o ka pauku ole, penei e hana ia:
- Ināʻoi aku ma mua o 12 mau hola i waiho ʻia ma mua o ka lawe ʻana i ka pōkole hou, inu koke i ka paila.
- Inā ma mua o ka noi ʻana i ka hopena hou o clopidogrel e emi iho ma mua o 12 mau hola - e lawe i ka maʻi aʻe ma hope i ka manawa kūpono (ʻaʻole e hoʻonui i ka nui).
Ka pāpā ʻia i ke kuʻikahi a me ka hoʻokau ʻana i ka hoʻohana ʻana i ka clopidogrel, no ka mea e iʻoi aku ka weliweli o ke ʻano o ka mea maʻi.
Ke keu
ʻO ka hoʻohana hewa ʻana o nā palapala kiʻekiʻe o clopidogrel hiki ke hele pū me nā hopena like ʻole:
- kahe koko
- hoʻonui hoʻonui koko.
Hoʻomaʻamaʻa ka hoʻomaʻemaʻe overdose. ʻOi aku ka maikaʻi o ka hoʻololi ʻana o nā lāʻau lapaʻau e pili ana i ka hāliʻiliʻi platelet.
Me ka waiʻona
I ka pili o ka launa pū me ka waiʻona, hiki i ka ʻeha o ka ʻāʻī ʻana o ka ʻōpū a me nā ʻōpū, e like hoʻi me ke ʻano o ke koko e ulu ai. No laila, pono e hoʻokaʻawale ʻia ka hui ʻana o ke clopidogrel a me ka waiʻona no ka hoʻopulapula haʻahaʻa loa.
Hoʻopuka nā lāʻau lapaʻau i nā pono Clopidogrel:
- ʻAno,
- Gridoklein,
- Ather,
- Avix,
- Clopidogrel o nā mea hana like - Izvarino, Tatkhimpharmpreparaty, Canon Pharma, Severnaya Zvezda (SZ), Biocom (Rūkīlani Mīkini Clopidogrel), Teva, Gideon Richter, Ratiopharm, Zentiva,
- Atrogrel
- Kāleka
- Diloxol
- Sylt,
- Holoi,
- Deplatt
- Noclot,
- Kiʻi,
- Clorelo
- Clopix
- Clopidal
- Lodigrel,
- Orogrel
- Helina,
- Kūkulu
- Lopirel
- Plavix,
- Reodar,
- Trombix,
- Plaglir,
- Trombeks,
- Nā Pūnaewele
- Kāleka
- Reomax
- Trombone,
- Clopidex
- Plavigrel
- Flamogrel.
ʻAʻole like nā loli a pau o kēia mau lāʻau i ka hoʻopili ʻana a me ka hewa o ka mea ikaika. Aia ka hoʻokoʻa ma nā mea hana a me nā kumu kūʻai.
Lapaʻau lāʻau
Hoʻopau Ma hope o kēlā me kēia kīnā waha a 75 a i kēlā me kēia lā, hopu koke ke kelepona i ka clopidogrel. Ka awelika ʻana ka nui o ka plasma kiʻekiʻe o ka pūhui nui (ma kahi o 2.2-2.5 ng / ml ma hope o hoʻokahi kiʻi waha o 75 mg) i nānā ʻia ma kahi o 45 mau minuke ma hope o ka lawelawe ʻana.Hoʻokumu ʻia i nā metabolite clopidogrel i hoʻopuka ʻia i loko o ka urine, aia ka liʻiliʻi ma kahi o 50%.
Kahele. ʻO Clopidogrel a me ka nui (hana ʻole) ka lihilihi i ka metabolite hoʻi e hōʻole hou i nā protein plasma i lokovitro (98 a me 94%, kekona). Ke paʻa nei kēia paʻa paʻa. i lokovitro maluna o nā wahi he nui.
Hāpai. Hoʻopili koke ʻo Clopidogrel i loko o ka ate. Ivitro a i lokovivo Hoʻopili ʻia ka clopidogrel i ʻelua mau ala nui: ka mea i palahalaha ʻia e nā esterases a alakaʻi i ka hydrolysis i kahi kumulāʻau ʻano o kahi waikawa carboxylic. ʻO ka mea, hoʻopili ʻia ka clopidogrel i kahi metabolite waena, 2-oxo-clopidogrel. ʻO ka hoʻololiʻana o ka metabolite ka hopena o ka metabolite waena o 2-oxo-clopidogrel e alakaʻi i ka hoʻokumuʻana o kahi metabolite ikaika, kahi derivative thiol o clopidogrel. Ivitro ʻO kēia ala metabolic i hoʻomāhele ʻia e CYP3A4, CYP2C19, CYP1A2 a me CYP2B6. ʻO ka thiol metabolite kaawale i hoʻokaʻawale i lokovitro wikiwiki a hiki ʻole ke hoʻopili pono ʻia, e hoʻopili me ka hoʻopili ʻia o nā platelet receptors, me ka pale ʻana i ka platelet aggregation.
Me kamax ʻoi aku ka nui o ka metabolite maʻa ʻelua mau manawa kiʻekiʻe ma hope o hoʻokahi ka manawa o ka hoʻouka ʻana o 300 mg o clopidogrel ma mua o ʻehā mau lā o kahi mālama mālama ʻo 75 mg. Me kamax nānā i ka manawa 30-60 mau minuke ma hope o ka lawe ʻana i ka lāʻau lapaʻau.
Hoʻopau. Ma kahi o 50% o ka lāʻau lapaʻau e kāpae ʻia i loko o ka pāʻai a ma kahi o 46% me nā feces i nā hola 120 ma hope o ka hoʻokō ʻana. Ma hope o hoʻokahi kahe waha waha o 75 mg, ʻo ia ka hapalua o ka hapalua o ke ola o ka clopidogrel he 6 mau hola. ʻO ka hapalua ola o ka metabolite koʻikoʻi nui he 8 mau hola ma hope o ke ʻano hoʻokahi a hoʻokahi.
Lapaʻau lāʻau. Hoʻololi ʻo CYP2C19 i ka hoʻokumu ʻana i kahi metabolite ikaika a me kahi metabolite waena waena, 2-oxo-clopidogrel. ʻO ka hopena Pharmacokinetics a me nā hopena antiplatelet o ka metabolite ikaika o ka clopidogrel e like me ke ana ma ka hōʻike ʻana o ke ʻano platelet exvivo, kūlike ia i ka genotype o CYP2C19.
ʻO ka CYP2C19 * 1 allele e pili ana i kahi metabolism holoʻokoʻa holoʻokoʻa, aʻo CYP2C19 * 2 a me CYP2C19 * 3 alleles i ʻole hana. ʻO ka account alleles CYP2C19 * 2 a me CYP2C19 * 3 ka helu no ka hapa nui o nā alleles me ka hōʻemi ʻana i ka hana ma ke keʻokeʻo keʻokeʻo (85%) a me nā poʻe ʻAmelika (99%) me ka lawa ʻole o ka metabolism. ʻO nā mea āpau ʻē aʻe me ka hana a i ʻole ka hoʻemi ʻana i ka lawelawe, i waena pū me CYP2C19 * 4, * 5, * 6, * 7 a me 8 ʻO nā mea maʻi me ka hoʻohaʻahaʻa metabolic function he mau halihali ʻelua o nā alleles pono ʻole. Wahi a nā hōʻike i paʻi ʻia, ʻo ka pinepine o ka hanana o ka genotype me ka hana haʻahaʻa haʻahaʻa o CYP2C19 ma kahi o 2% i ka lāhui Caucasoid, 4% i ka lāhui Negroid a me 14% i ka lāhui Mongoloid.
ʻAʻole lawa ka nui o nā haʻawina e ʻike i nā ʻokoʻa i nā hopena no nā poʻe maʻi me ka lawaʻole o ka clopidogrel metabolism.
Hola paʻa kino hana. ʻO ka ʻai ʻana o ka metabolite nui i ka plasma koko i ka wā e lawe ai i ka 75 mg o ka clopidogrel i kēlā me kēia lā ka haʻahaʻa loa i nā mea maʻi me ka maʻi ʻehaʻeha (ʻo ka cleinine clearance mai 5 a 15 ml / min) hoʻohālikelike ʻia me nā mea maʻi ʻo kā cleinine clearance he 30-60 ml / min a oleio oleio. I ka manawa like, ʻo ka hopena pale i ka hoʻohui ʻana o ka platelet ADP-induction i loko o nā mea maʻi me ka maʻi maʻi o ka maʻi ua hōʻemi ʻia (25%) i hoʻohālikelike ʻia me nā hopena like ʻole i nā kānaka olakino, ua hoʻolōʻihi ʻia ka manawa koko i ka hopena like ma nā poʻe olakino i loaʻa i ka 75 mg clopidogrel i kēlā me kēia lā. Eia kekahi, ʻoi ka maikaʻi o ka pale ʻana ma nā maʻi āpau.
Hōʻeha ka naʻau ʻili. I ka poʻe maʻi me ka maʻi hepatic koʻikoʻi, i ka wā e lawe ai i ka pākahi i kēlā lā i kēia lā he 75 ml o clopidogrel no 10 mau lā, ʻo ka ADP-induction suppression o platelet aggregation i like pū me i ka poʻe olakino. ʻO ka like me ka hoʻonui ʻana i ka manawa koko ua like nō hoʻi ma nā hui ʻelua.
Kāhea. ʻO ka nui o ka alleles CYP2C19, e hoʻohālikelike i ka hōʻuluʻulu waena a me ka metabolism maikaʻi e pili ana CYP2C19, ʻokoʻa i ka lāhui a me ke ʻano ʻē aʻe. Loaʻa wale nā ʻikepili i ka lehulehu ma Asia i loaʻa i ka puke e loiloi i ke ʻano kino o kēia genieype CYP no nā hopena olakino.
ʻŌpū a me ka lactation
ʻO nā haʻawina e pili ana i nā hopena o clopidogrel i ka wā hāpai i mālama ʻia i nā holoholona, ʻaʻole i hōʻike i ka hopena maikaʻi ʻole i ka hapai ʻana, ka hoʻomohala ʻana o ka embryo / fetus, hana a me ka hoʻomohala postnatal.
Haumakua. ʻAʻole i ʻike ʻia inā hoʻopili ʻia ka clopidogrel i loko o ka umauma wai kanaka. Ua hōʻike ʻia nā haʻawina holoholona holoholona i ka lāʻau i loko o ka waiū umauma. E like me ka mua o ka mālama ʻana, pono ka hōʻuluʻulu o ka umauma i ka wā o ka mālama ʻana me ka clopidogrel.
No ka mea nui ka nui o nā lāʻau lapaʻau i loko o ka waiū umauma, a no ka hiki ke hoʻomohala i nā hopena ʻino i nā keiki hānai hānai, ʻoi ka hoʻoholo e hoʻolei i ka lāʻau a hōʻoki paha i ka uwē ʻana, e hana ʻia, hāʻawi ʻia i ka pono no ka clopidogrel therapy i ka makuahine hānai.
Hopu hana. I nā haʻawina holoholona, ʻaʻole i pili ka clopidogrel i ka hana hānau.
ʻLoe a me ke kākele
Kuhi ʻia ʻo Clopidogrel no ka hoʻoponopono waha i kēlā me kēia lā, me kaʻole o ka meaʻai.
Nā ʻōpala
ʻO nā pākeke a me nā poʻe kahiko
ʻO ka paona maʻamau ʻo kēlā me kēia lā he 75 mg maʻamau ma ka lā.
ʻO ka maʻi coronary ʻeha:
- ka maʻi coronary ʻokoʻa ʻole o ka pae kiʻekiʻeST(uniana paʻa indina ʻole myocardial infarction me ka mea ʻole o ka nihoQ): Hoʻomaka ʻia ka lāʻau Clopidogrel me kahi pahu hoʻokahi ʻana o 300 mg, a hoʻomau ʻia me ka houluana o 75 mg hoʻokahi i hoʻokahi lā (me ka acetylsalicylic acid ma kahi kikoʻī o 75-325 mg i hoʻokahi lā). ʻAʻole ia e uku i kahi ʻoi aku o ka acetylsalicylic acid o 100 mg, no ka mea e pili ana nā dosis kiʻekiʻe o ASA me ka nui o ke kahe. ʻAʻole paʻa i ka lōʻihi o ka mālama ʻana. Hoʻopili ka data hoʻokolohua maʻi lapaʻau i ka hoʻohana ʻana o ka hoʻoponopono no nā mahina 12, a ʻo ka nui o ka pōmaikaʻi e nānā ʻia ma hope o 3 mau mahina.
- myocardial hoʻonā ʻia me ka kiʻekiʻe kiʻekiʻeST: Ua kau ʻia ka clopidogrel i hoʻokahi manawa i ka lā ma kahi o ka 75 mg e hoʻohana ana i kahi pākaukau mua o 300 mg i hui pū ʻia me ka acetylsalicylic acid i hui pū ʻia a i ʻole me nā thrombolytics ʻē aʻe. No nā mea maʻi i ʻoi aku ma mua o 75 mau makahiki o ka makahiki, pono e mālama ʻia ka lāʻau clopidogrel me ka ʻole o ka hoʻohana ʻana i kahi pāʻālua. Hoʻomaka ka lāʻau hoʻohui me ka hiki ke hoʻomaka ma hope o ka hoʻomaka ʻana o nā hōʻailona a hoʻomau mau no ka liʻiliʻi o nā hebedoma ʻehā. Loaʻa nā pōmaikaʻi o ka hui pū ʻana o clopidogrel me ASA ma hope o nā hebedoma ʻehā i aʻo ʻia i kēia hihia.
Hoʻopili ʻo Atrial: 75 mg clopidogrel hoʻokahi lā i ka lā. Hāʻawi iā ASA (75-100 mg / lā) a hoʻomau i ka lawe pū ʻana me clopidogrel.
Ma ka ʻae ʻana o ke kākā:
- e emi iho ma mua o 12 mau hola ma hope o ka manawa maʻamau o ka hoʻokomo: pono e lawe koke i ka dosis, pono nā lāʻau hou aʻe i ka manawa i hoʻonohonoho ʻia.
- Ponoʻoi aku ma mua o 12 mau hola ma hope o ka manawa maʻamau o ka hoʻokomo ʻana: pono e lawe ʻia ka lāʻau hou aʻe i ka manawa i hoʻonohonoho ʻia, me ke kānalua ʻole.
Na keiki a ʻōpio
ʻAʻole paʻa i ka palekana a me ka hana o ka clopidogrel i ka lahui pediatric.
ʻO ka maʻi me ka hana renal impaired
He liʻiliʻi ka ʻike no ka hoʻomaʻamaʻa ʻana i nā mea maʻi me nā mahi ʻole a pau ʻole.
ʻO nā mea maʻi me ka hana pūlima hemahema
ʻO ka ʻike pono i ka mālama ʻana i nā maʻi me nā maʻi maʻi palupalu i hiki ai i ka hemorrhagic diathesis ka mea liʻiliʻi.
ʻO nā mea mālama palekana
Hoʻolaha a me nā hopena hematologic
Inā hele mai nā ʻōleʻa lapaʻau i ka wā o ka mālama ʻana e hōʻike ana i ka hoʻomohala ʻana o ke koko a me nā hopena hematological, pono ke hana i kahi hōʻike koko. Ma muli o ka piʻi nui o ka huhū, pono e hoʻohana ʻia ka makaʻala i ka wā e hoʻopili pū ai ʻo clopidogrel me warfarin.
Pono e hoʻohana ʻo Clopidogrel me ka makaʻala i nā mea maʻi i ka piʻi nui o ke koko e pili ana i ka trauma, i ka hana ʻana a i ʻole nā kūlana pathological, aia hoʻi i ka hui pū ʻana o ka clopidogrel me ka acetylsalicylic acid, nā lāʻau lapaʻau anti-inflammatory non-steroidal, me nā haukole COX-2, heparin, glycoprotein inhibitors. IIb / IIIa, selotonin reuptake inhibitors (SSRIs) a i nā mea ola ʻē aʻe e pili ana i ka hopena o ke koko, e like me pentoxifylline. Pono ka nānā pono ʻana o ka hōʻike ʻana o nā hōʻailona o ka huhū, me ke komo ʻana i ka pehu latene, e pono no i nā hebedoma mua o ka mālama ʻana a / ai ʻole ma hope o nā hanana cardiac invasse a i ʻole maʻa. ʻAʻole i ʻōlelo ʻia ka hoʻohana pū ʻana o ka clopidogrel me nā anticoagulants waha, no ka mea, he hiki ke hui pū ʻia e hoʻonui i ka nui o ke kahe.
Ma ka hihia o nā mea hōʻiliʻili o ka hopena, inā he hopena antiplatelet e hikiʻole, e hoʻokaʻawale ʻia ke ʻano o ka mālama ʻana me clopidogrel i nā lā 7 ma mua o ka hoʻomaʻemaʻe ʻana. Pono e hōʻike i ke kauka hele ʻana a me nā mea lapaʻau e pili ana i ka lawe ʻana i ka lāʻau lapaʻau inā e hoʻomaʻamaʻa ka mea maʻi a i ʻole ke kuhikuhi ke kauka i kahi lāʻau hou no ka mea maʻi.
Pono e hoʻohana ʻia ka Clopidogrel me ka makaʻala i nā mea maʻi i ka hopena o ke koko (ʻoi loa ka gastrointestinal a me ka intraocular). Ke lawe nei i ka clopidogrel, e hoʻohana akahele i ka hoʻohana ʻana i nā lāʻau hōʻeha e hiki ai i nā maʻi o ke ake o ka ʻokiʻoki (e.g., acetylsalicylic acid a me nā NSAID).
E makaʻala ʻoe no ka mea e hoʻohiolo i ke koko i ka wā e lawe ana i ka clopidogrel (ʻo ia wale nō a i hui pū paha me ASA) pono nui ka manawa, pono ʻoe e hoʻomaopopo i kāu kauka e pili ana i kēlā me kēia hihia o ka maʻamau (ma ke ʻano o ka wahi a me / a lōʻihi paha) koko.
Thrombocytopenic Purpura (TTP)
ʻAʻole loaʻa nā hihia nui o ka thrombocytopenic purpura (TTP) ma hope o ka clopidogrel. Hōʻike ʻia kēia i ka thrombocytopenia a me microangiopathic anemia hemolytic i hui pū ʻia me nā ʻōlima a neurological, ʻokiʻoki a me ke ake maʻi. Hiki i ka hoʻomohala ʻana o TTP ke ola hoʻoweliweli a koi i kahi hana wikiwiki, e komo pū me ka plasmapheresis.
ʻO nā hihia o ka hoʻomohala ʻana i loaʻa ka hemophilia i loaʻa ma hope o ka lawe ʻana i ka clopidogrel. I ka hihia o kahi hoʻonui i hōʻoia ʻia i ka manawa thromboplastin hoʻolaʻa hoʻolaʻa i hoʻolaʻa me ka ʻole ʻole o ke kahe, ke noʻonoʻo pono ʻia ka loaʻa ʻana o ka hemophilia i loaʻa. ʻO ka poʻe maʻi me ka maʻi hōʻoia i hōʻoia ʻia i ka hemophilia i loaʻa ʻia, pono e nānā a mālama ʻia e nā loea, ʻoi aku ka lāʻau clopidogrel.
Ma muli o ka lawa ʻole o ka ʻike, ʻaʻole pono e kuhikuhi ʻia nā clopidogrel i nā lā 7 mua o ka maʻi o ka ischemic stroke.
I ka poʻe maʻi me ka hoʻohaʻahaʻa metabola hana o CYP2C19, ʻo ka clopidogrel i loko o nā koina i ʻōlelo ʻia ai e hāʻawi i kahi hapa liʻiliʻi o ka metabolite ikaika o ka clopidogrel a me ka hopena antiplatelet i haʻahaʻa. ʻO nā mea maʻi me ka hoʻohaʻahaʻa metabola ma ka maʻi coronary syndrome a i ʻole ka mea i loaʻa i ka hoʻoneʻe coronary percutaneous a ke loaʻa nei ka hopena clopidogrel i nā ʻōkena i ʻōlelo ʻia ai, e piʻi paha ka nui o ka hoʻomohala ʻana i nā hoʻopiʻi cardiovascular ma mua o nā mea maʻi me ka hana hana maʻamau o CYP2C19.
No ka mea ka hoʻokaʻina clopidogrel i kahi metabolite ikaika ma kekahi ma o CYP2C19, e manaʻo ʻia e nā lāʻau lapaʻau e ʻoki ana i ka hana o kēia enzyme e alakaʻi ai i ka emi ʻana o ka hōʻalo o ka lāʻau o ka metabolite clopidogrel aktif. ʻAʻole i aʻo ʻia ka maʻi koʻikoʻi o kēia pilina. ʻO ka hoʻohana ʻana i ka ʻōmole mākeke ikaika ʻole CYP2C19 i hoʻopau ʻia.
Pono ʻia ka mālama ʻana i nā mea maʻi e loaʻa pū ana me nā lāʻau clopidogrel - nā kānana o ka isoenzyme CYP2C8.
Allergic cross-reactivity
Pono ka mea maʻi i kekahi mōʻaukala o ka hypersensitivity i nā thienopyridines ʻē aʻe (e.g. ticlopidine, prasugrel), no ka mea aia nā hihia i ka maʻi al-crossactactivity me nā thienopyridines. ʻO nā mea maʻi me ka mōʻaukala o ka hypersensitivity i nā thienopyridines ʻē aʻe e mālama pono ʻia i ka wā o ka mālama ʻana no nā hōʻailona o ka hypersensitivity i clopidogrel. Hiki i nā Thienopyridines ke alakaʻi i ka hoʻomohala ʻana i nā hopena kūlohelohe o nā ʻano paʻakikī, e like me ka pāheʻe ʻana, ka edema o Quincke, a i ʻole hematological cross-reaksi, e like me thrombocytopenia a me neutropenia. ʻO nā mea maʻi i loaʻa i ka mōʻaukala o nā hopena alaka a me / a he hematological paha i hoʻokahi thienopyridine i nui ka piʻi o ka ulu ʻana i like ʻole a i ʻole nā ʻano like ʻole ʻē aʻe i kekahi thienopyridine.
ʻO ka pūnaina o ka lāʻau lapaʻau ka loko o ka waʻa karmuazin (E-122), hiki i nā mea kūlohelohe.
Hola paʻa kino hana
Hoʻohālikelike ka hopena therapeutic me clopidogrel i nā maʻi me nā maʻi renal impaired. Pono e hoʻohana ʻia ka lāʻau i loko o nā mea maʻi me ka akahele.
Hōʻeha ka hana ʻoluʻolu
Pono e hoʻohana i ka Clopidogrel me ka makaʻala i nā mea maʻi me ka hana o ka puʻuwai maʻi i hōʻemi ʻia, ka mea e hōʻeha ai i ka hemorrhagic diathesis.
Hoʻokomo i ka hiki ke lawe i nā kaʻa a me nā mīkini ʻē aʻe e weliweli hou ʻia. ʻAʻole pili a Clopidogrel a i ʻole he hopena iki no ka hiki ke alakaʻi i nā kaʻa a me nā mīkini ʻē aʻe.