Momwe mungagwiritsire ntchito mankhwala Zilt?

Mwa kuletsa kumangiriza kwa ADP ku ma receptor omwe ali pamwamba pamapulatelet ndi kuyambitsa kwa GP IIb / IIIa tata, clopidogrel imalepheretsa kuphatikiza kwa mapulani a ADP. Clopidogrel imalepheretsanso kuphatikiza kwa mapulateleti chifukwa cha zinthu zina. Mphamvu ya clopidogrel imapitilira mu moyo wonse wa mapulateleti.
Kugwiritsa ntchito clopidogrel nthawi yayitali (75 mg / tsiku), choletsa kuphatikizidwa kwa kupatsidwa zinthu za m'magazi kumachitika kale patsiku la 1 la chithandizo, ndiye kuti antiplatelet kwenikweni imayamba ndikufikirabe mpaka patatha masiku 3- 7 yogwiritsa ntchito mankhwalawa. Ndi nthawi yayitali yogwiritsa ntchito clopidogrel mu mankhwala othandizira, choletsa chophatikizira cha maselo ambiri ndi 40-60%. Pambuyo kutha kwa mankhwalawa, mphamvu ya kuphatikizika kwa magazi ndi kuchuluka kwa magazi kutha, nthawi zambiri pambuyo masiku 5.
Pambuyo pakukonzekera pakamwa, clopidogrel imatengedwa mwachangu (nthawi yofika ndende ya plasma yambiri ndi maola 0.7-0.8). Pambuyo maola 2, mankhwalawa samapezekanso m'madzi a m'magazi. Mafuta pafupifupi pafupifupi 50% ndipo alibe chakudya. Gawo lalikulu la clopidogrel ndi metabolite yake yayikulu (motero 98 ndi 94%) limasinthiratu kumapuloteni a plasma.
Clopidogrel ndi mankhwala osokoneza bongo. Amapukusidwa mu chiwindi, metabolite yayikulu imachokera ku carboxylic acid. Kuphatikizika kwake mu seramu yamagazi ndi 85% ya kuchuluka kwa mankhwalawo. Pazitali ndende yamagazi seramu imafikiridwa pafupifupi ola limodzi pambuyo pa kuperekedwa. Metabolite yogwira - thiol yotumphukira - imapangidwa ndi makutidwe ndi okosijeni a clopidogrel 2 - oxoclopidogrel, kenako hydrolysis. Oxidation iyi imachitika limodzi ndi cytochrome P450. Metabolite yogwira iyi yomwe ikhoza kusiyanitsidwa mu vitro, mwachangu komanso mosasinthika amamangirira ku ma cellulo othandizira ndikulepheretsa kuphatikizika kwawo. Sipezeka mu seramu yamagazi.
Pakapita kamodzi kapena mobwerezabwereza ndi mkodzo, 50% imachotsedwamo, ndipo ndowe - 46% ya mankhwala omwe amaperekedwa ndi clopidogrel. Hafu ya moyo wa metabolite yayikulu itangotha kamodzi kapena mobwerezabwereza kuyamwa kwa mankhwala ndi maola 8.

Zisonyezero zogwiritsira ntchito mankhwala Zilt

Kupewa kwa zochitika zamtima (ischemic stroke, myocardial infarction ndi mtima kufa) mwa odwala omwe ali ndi matenda a atherosulinosis: ndi stroke ya ischemic (kuyambira masiku 7 mpaka miyezi 6), kulowetsedwa kwa myocardial (kuyambira masiku angapo mpaka masiku 35 pambuyo pa vuto la mtima), pamaso pa matenda a zotumphukira mitsempha.

Kugwiritsa ntchito mankhwala Zilt

Mlingo wamba wa odwala akuluakulu (kuphatikizapo okalamba) ndi piritsi 1 (75 mg) patsiku. Mankhwalawa amatha kugwiritsidwa ntchito mosasamala zakudya.
Kutalika kwa mankhwalawa sichinakhazikitsidwe, koma mankhwalawa othandizira mpaka miyezi 12 amagwiritsidwa ntchito, zotsatira zake ndizowonekera pambuyo pa miyezi itatu itatha kumwa mankhwalawa.

Njira yogwiritsira ntchito Zilt piritsi

Mkati, ngakhale kudya zakudya, kamodzi patsiku.

Akuluakulu ndi odwala okalamba omwe ali ndi zochitika wamba za CYP2C19 isoenzyme

Myocardial infarction, ischemic stroke, kapena matenda ofunika a ochepa mwa njira ya occlusion.

Zilt® imatengedwa pa mlingo wa 75 mg (piritsi 1) kamodzi patsiku.

Acute coronary syndrome yopanda ST gawo kukweza (osakhazikika angina kapena myocardial infarction popanda Q wave)

Kuchiza ndi Zilt® kuyenera kuyambitsidwa ndi muyeso umodzi wa mlingo wobweza (300 mg), ndikupitilizidwa ndi mlingo wa 75 mg kamodzi patsiku (osakanikirana ndi acetylsalicylic acid mu Mlingo wa 75-325 mg patsiku. Popeza kugwiritsa ntchito milingo yapamwamba ya acetylsalicylic acid kumalumikizidwa ndi chiwopsezo chachikulu chokhetsa magazi, mlingo woyenera wa acetylsalicylic acid suyenera kupitirira 100 mg. Zopindulitsa kwambiri zimawonedwa ndi mwezi wachitatu wa chithandizo. Kutalika kwakanthawi kachipangizochi sikunatsimikizike mwatsatanetsatane. Zotsatira za kafukufuku wamankhwala zimatsimikizira kuthekera kwa kutenga clopidogrel mpaka miyezi 12 pambuyo pa chitukuko cha matenda a pachimake coronary popanda kukweza gawo la ST.

Pachimake coronary syndrome ndi ST gawo kukweza (pachimake myocardial infarction) ndi mankhwala ndi kuthekera kwa thrombolytic mankhwala, limodzi acetylsalicylic acid.

Zilt ® iyenera kumwedwa pamankhwala a 75 mg (piritsi 1) kamodzi patsiku, kuyambira ndi kuchuluka kwa gawo, limodzi ndi acetylsalicylic acid wokhala ndi kapena wopanda thrombolytics. Kwa odwala omwe ali ndi zaka zopitilira 75, chithandizo ndi Zilt® chiyenera kuchitika popanda kugwiritsa ntchito mlingo wokulitsa. Kuphatikiza mankhwala kumayambira posachedwa pambuyo pa kuyamba kwa zizindikiro ndikupitilira kwa milungu inayi. Kuchita bwino kwa mankhwala ophatikiza ndi clopidogrel ndi acetylsalicylic acid wopitilira masabata 4 sikunaphunzitsidwe mwa odwala.

Fibrillation ya atria

Mankhwala Zilt ® amatchulidwa muyezo wa 75 mg kamodzi patsiku. Kuphatikiza ndi clopidogrel, mankhwalawa amayenera kuyambitsidwa kenako kudya kwa acetylsalicylic acid pa mlingo wa 75-100 mg patsiku uyenera kupitilizidwa.

Ngati wodwala adaphonya wotsatira:

- ngati pasanathe maola 12 mutadumpha mlingo wotsatira, muyenera kumwa nthawi yomweyo Zamp®, ndiye kuti mukumwa mlingo wotsatira nthawi yomweyo.

- ngati maola opitilira 12 adatha kulumpha mlingo wotsatira, ndiye kuti mlingo wotsatira uyenera kumwedwa nthawi yokhayo, pomwe mankhwalawa sayenera kuwiriridwa kawiri.

Akuluakulu ndi odwala okalamba omwe ali ndi chibadwa chotsimikizika amachepetsa ntchito ya CYP2C19 isoenzyme

Ntchito yotsika ya CYP2C19 isoenzyme imalumikizidwa ndi kuchepa kwa mphamvu ya antiplatelet ya clopidogrel. Kugwiritsidwa ntchito kwa Zilt® pamlingo wapamwamba (kuthira mlingo wa 600 mg, ndiye 150 mg kamodzi patsiku) mwa odwala omwe ali ndi ntchito zochepa za CYP2C19 isoenzyme kumabweretsa kuwonjezeka kwa antiplatelet zotsatira za clopidogrel (onani gawo la Pharmacokinetics). Komabe, pakuyesa kwachipatala kuti muwerenge zotsatira zamankhwala, mulingo woyenera kwambiri wa clopidogrel mwa odwala omwe ali ndi metabolism yochepetsedwa chifukwa cha genetically otsimikiza zochitika za CYP2C19 isoenzyme sizinakhazikitsidwe.

Magulu apadera a odwala

Odwala okalamba

M'magulu odzipereka okalamba (zaka 75), poyerekeza ndi odzipereka achichepere, kusiyana kwa kuphatikizana kwa maplatelet ndi nthawi ya magazi sizinawululidwe. Kusintha kwa Mlingo kwa okalamba sikofunikira.

Matenda aimpso

Pambuyo kugwiritsidwa ntchito mobwerezabwereza kwa clopidogrel pa mlingo wa 75 mg patsiku kwa odwala omwe ali ndi vuto laimpso (CC 5-15 ml / min), kuchuluka kwa zoletsa za kuphatikizidwa kwa mapulani a ADP ndi 25% kutsika kuposa odzipereka athanzi. Komabe, kuchuluka kwa kutalika kwa magazi nthawi yayitali kunali kofanana ndi kwa odzipereka athanzi omwe amalandila clopidogrel pa mlingo wa 75 mg patsiku. Kulekerera kwa mankhwalawa kunali kwabwino mwa odwala onse. Kuwonongeka kwa chiwindi

Pambuyo kugwiritsa ntchito clopidogrel pa mlingo wa 75 mg patsiku kwa masiku 10 kwa odwala omwe ali ndi vuto lalikulu la chiwindi, kuchuluka kwa zoletsa zam'magazi a ADP komanso kuchuluka kwa magazi nthawi yayitali kunali kufananizidwa ndi odzipereka athanzi.

Kukula kwa mitundu ya CYP2C19 isoenzyme yomwe imagwirizanitsidwa ndi sing'anga kapena kuchepa kwa kagayidwe kosiyanasiyana kumasiyana pakati pa oimira amitundu / mafuko osiyanasiyana (onani mafotokozedwe a Pharmacogenetics). Zambiri zowerengeka zamabuku zimapezeka kuti ziwunikire kufunika kwa kusintha kwa mtundu wa CYP2C19 isoenzyme pazotsatira zamankhwala kwa odwala a liwiro la Mongoloid.

Poyerekeza pharmacodynamic katundu wa clopidogrel mwa amuna ndi akazi, azimayi adawonetsa kuletsa kwapadera kwa kuphatikiza kuphatikizira kwa mapulani a ADP, koma palibe kusiyana pakutalika kwa magazi nthawi. Poyerekeza clopidogrel ndi acetylsalicylic acid mwa odwala omwe ali pachiwopsezo chokhala ndi zovuta za ischemic, pafupipafupi pazotsatira zamankhwala, zotsatira zina komanso kupatuka kuzungulira kwazomwe zimachitika kuchipatala ndi ma labotale omwe anali ofanana mwa amuna ndi akazi.

Zotsatira zoyipa za mankhwala Zilt

Zotsatira zambiri: kupweteka pachifuwa, kutopa, asthenia.
Kuchokera ku dongosolo lamanjenje: mutu, chizungulire, paresthesia, miyendo kukokana, Hypesthesia, neuralgia, kulephera kudziwa.
Kuchokera pamtima: zotumphukira edema, matenda oopsa (ochepa matenda oopsa), mtima kulephera, tachycardia.
Kuchokera m'mimba thirakiti: kupweteka kwam'mimba, kukomoka, kutsegula m'mimba, mseru, kudzimbidwa, kusanza, kugona, kusokonezeka kwa magazi, zilonda zam'mimba, hemorrhagic gastritis, magazi am'mimba.
Pa mbali ya chiwindi ndi biliary thirakiti: kuchuluka kwa kwa chiwindi transaminases, hyperbilirubinemia, hepatitis, chiwindi steatosis.
Kuchokera ku magazi: thrombocytopenia, magazi m'thupi (aplastic kapena hypochromic), agranulocytosis, granulocytopenia, leukocytosis, leukopenia, neutropenia.
Kuchokera pamagazi othandizira magazi: nosebleeds, m'mimba magazi, hemarthrosis, magazi kuchokera kwamkodzo thirakiti, hemoptysis, intracranial hemorrhage, kutuluka kwa magazi, kutuluka magazi kuchokera pachilonda cha postoperative, hemorrhage m'maso, hemothorax, pulmonary hemorrhage, allergic purpura.
Kuchokera ku minculoskeletal system: kupweteka kumbuyo, nyamakazi, arthrosis.
Kuchokera kumbali yamanjenje yapakati: kukhumudwa
Kuchokera ku kupuma: chapamwamba kupuma thirakiti kutupa, kufupika, rhinitis, bronchitis, chifuwa, chibayo, sinusitis.
Khungu mbali: zotupa, kuyabwa, chikanga, zilonda za pakhungu, zotupa zamkaka, zotupa za erythematous, zotupa za maculopapular, urticaria.
Kuchokera kumankhwala akumva: cataract, conjunctivitis.
Kuchokera ku genitourinary system: kwamikodzo thirakiti matenda, cystitis, hypermenorrhea, okhawo milandu hemolytic uremic syndrome ndi nembanemba nephropathy.
Zotsatira zoyipa: okhawo milandu hypersensitivity zimachitika (angioedema, bronchospasm, anaphylaxis).

Malangizo apadera ogwiritsira ntchito mankhwala Zilt

Odwala omwe ali ndi myocardial infarction, osavomerezeka kuti ayambe kulandira mankhwala a clopidogrel masiku angapo atadwala matenda a mtima. Clopidogrel imawonjezera nthawi yotaya magazi. Mankhwalawa ayenera kugwiritsidwa ntchito mosamala odwala omwe ali ndi chiopsezo chowonjezereka cha magazi chifukwa cha kuvulala, maopaleshoni kapena zochitika zina zam'mitsempha, komanso kwa odwala omwe ali ndi magazi. Chithandizo cha Clopidogrel ziyenera kuletsedwa osachepera masiku 7 musanachitike opaleshoni yokonzekera (kuphatikizapo njira zamano).
Odwala ayenera kuchenjezedwa kuti pochiza matenda a clopidogrel, kuopsa kwa magazi kumawonjezeka komanso kuti magazi atha kukhala nthawi yayitali kuposa masiku onse, kenako nkumangoyimitsa. Ndi mabala ang'onoang'ono (pometa) kapena kuvulala kwanyumba, njira zapadera zothetsera magazi sizimafunikira kwenikweni. Pothetsa kapena kuvulala kwakukulu, kufunsa achipatala ndikofunikira.
Chifukwa chosakwanira ndi clopidogrel odwala omwe ali ndi vuto laimpso, muyenera kusamala mukamagwiritsa ntchito mankhwalawa.
Ndi kuphwanya kwakukulu kwa ntchito ya chiwindi, chiopsezo cha kukwera magazi chikuwonjezereka, chifukwa chake, mwa odwalawa, clopidogrel ayenera kugwiritsidwa ntchito mosamala.
Chitetezo ndi kugwira ntchito kwa clopidogrel mwa ana ndi achinyamata ochepera zaka 18 sizinakhazikitsidwe, chifukwa chake, mankhwalawa saikidwa kwa odwala a m'badwo uno.
Chifukwa cha kusowa kwa deta, clopidogrel siyikulimbikitsidwa kuti mugwiritse ntchito panthawi yomwe muli ndi pakati komanso mkaka wa m`mawere.
Mankhwalawa amatha kusokoneza chikhalidwe cha psychophysical, chomwe chimawonetsedwa ndikuchepetsa chidwi, kutsika pang'ono mu psychomotor reaction ndipo kumafunikira kusamala poyendetsa magalimoto ndikugwiritsa ntchito njira zowopsa.

Zochita Zokhudzana ndi Mankhwala

Chifukwa cha kuchuluka kwa magazi, nthawi yomweyo kugwiritsa ntchito clopidogrel ndi warfarin sikulimbikitsidwa. Pogwiritsa ntchito nthawi yomweyo clopidogrel ndi heparin kapena othandizira ena a thrombolytic, chiopsezo chotulutsa magazi chitha kuchuluka, chifukwa chake kugwiritsa ntchito mankhwalawa kumafunikira kusamala. Kugwiritsa ntchito nthawi yomweyo clopidogrel ndi NSAIDs kumawonjezera chiopsezo cha ulcerogenic kanthu ndi kukula kwa magazi kuchokera ku zilonda, kotero kugwiritsa ntchito clopidogrel ndi NSAIDs kumafuna kusamala.
Ndi munthawi yomweyo kugwiritsa ntchito clopidogrel ndi atenolol, nifedipine, digoxin, phenobarbital, cimetidine, estrogen kapena theophylline, palibe mgwirizano wachipatala womwe unadziwika. Pali umboni wa chitetezo cha munthawi yomweyo kugwiritsa ntchito clopidogrel ndi phenytoin ndi tobutamide.
Maantacid sichikhudza mayamwidwe a clopidogrel.

Mankhwala osokoneza bongo Zilt, zizindikiro ndi mankhwala

Mlandu wina wokhudza kuphatikiza kwa dongo wa clopidogrel akufotokozedwa pamene mayi wazaka 34 wazaka zodzipha adatenga 1050 mg (mapiritsi 14) a clopidogrel. Panalibe zizindikiro za bongo kapena zovuta zina, palibe chithandizo chapadera chomwe chinachitika.
Atalandira odzipereka athanzi, 600 mg ya clopidogrel sanawonetse mavuto (kupatula kuwonjezeka kwa 1.7 nthawi kutalika kwa magazi).
Palibe mankhwala enieni. Zotsatira za clopidogrel zimatha kuthetsedwa mwa kuikidwa kwa maselo ambiri.

Fomu ya Mlingo:

Piritsi 1 yokhala ndi:

pachimake: chinthu yogwira: clopidogrel hydrosulfate 97.875 mg, yowerengedwa ngati clopidogrel 75,000 mg, obwera: lactose, anhydrous 108.125 mg, microcrystalline cellulose 30.00 mg, pregelatinized wowuma 12.00 mg, macrogol 6000 8.00 mg, mafuta a castor, hydrogenated 4.00 mg,

chipolopolo: hypromellose 6av 5.60 mg, titanium dioxide (E171) 1.46 mg, talc 0,50 mg, utoto wa iron utoto wofiira (E 172) 0.04 mg, propylene glycol 0,40 mg.

Zozungulira, mapiritsi a biconvex pang'ono, ophimbidwa ndi utoto wofiirira.

* Kuwona kwapakati: kuyera koyera kapena pafupifupi koyera ndi mbewa yapinki ya pinki.

Mankhwala:

Clopidogrel ndi mankhwala osokoneza bongo, amodzi mwa metabolites yogwira yomwe imalepheretsa kuphatikizana kwa maselo ambiri. Yogwira metabolite ya clopidogrel kusankha zoletsa zomangira
adenosine diphosphate (ADP) yokhala ndi P2Y_I2 mapuloteni othandizira ndi kupatsidwa mphamvu kwa ADP-mediation ya glycoprotein GPIIb / IIIa, komwe kumabweretsa zoletsa zophatikizana za mapulateleti.

Kupsinjika kwa kuphatikiza kwa maselo a cellplation sikungasinthe ndipo kumapitilira m'masiku onse a moyo (pafupifupi masiku 7-10), motero, kubwezeretsedwa kwa ntchito yothandizirana ndi mapuloteni kumafanana ndi kuchuluka kwa kukonzanso kwawo. Kuphatikiza kwa mapulateleti oyambitsidwa ndi agonists ena kupatula ADP kumalepheretsanso chifukwa chakutseka kwa kuchuluka kwa mapulateleti ndi ADP.

Metabolite yogwira imapangidwa ndi zochita za CYP450 isoenzymes, zina zomwe zingasiyane ndi polymorphism kapena zitha kuphatikizidwa ndi mankhwala ena, chifukwa chake, si odwala onse omwe ali ndi zoletsa zokwanira za kuphatikizana kwa maselo.

Mankhwalawa ndi clopidogrel pa mlingo wa 75 mg patsiku kuyambira tsiku loyamba la chithandizo, pali kuponderezedwa kwakukulu kwa kuphatikizana kwa mapulani a ADP, omwe pang'onopang'ono amawonjezeka masiku 3-7 kenako amafika pamlingo wokhazikika (pofika kufanana. Mu boma lofanana, kuchuluka kwa zoletsa zamagulu ophatikizika pogwiritsa ntchito clopidogrel pa mlingo wa 75 mg patsiku, pafupifupi, kuyambira 40% mpaka 60%. Atayimitsa clopidogrel, kuphatikizika kwa mapulosi ndi nthawi ya kukhetsa magazi pang'onopang'ono kunabwereranso kuzikhalidwe zawo zoyambirira, pafupifupi, masiku opitilira 5.
Clopidogrel imalepheretsa kukula kwa zovuta za atherothrombotic kwa odwala atherosulinotic zotupa za malo aliwonse, makamaka omwe ali ndi mitsempha ya m'mimba, yamitsempha yamagazi.

Pharmacokinetics:

Pambuyo pakamwa kamodzi mobwerezabwereza makonzedwe a 75 mg patsiku
clopidogrel imalowa mwachangu. Mitengo yapakati pazomwe zimapangitsa ndende (C_m_Ah) clopidogrel yosasinthika m'madzi am'magazi (2.2-2.5 ng / ml atatha kumwa kamodzi kwa 75 mg) imatheka pambuyo pa mphindi 45. Malinga ndi kafukufuku wa impretion wa impopidogrel metabolites, kuchuluka kwa mayamwidwe kuli pafupifupi 50%.

Clopidogrel ndi metabolite wake wambiri wosagwira mu plasma umasinthidwa kumapuloteni a plasma aumunthu pamikhalidwe mu vitro (98% ndi 94%, motsatana). Chomangira ichi sichimalumikizika m'njira zosiyanasiyana.

Clopidogrel imapukusidwa mwachangu mu chiwindi. M'mikhalidwe mu vitro ndi mu vivo
clopidogrel imapukusidwa m'njira ziwiri: yoyamba imayang'aniridwa ndi ma esterases ndipo imatsogolera ku hydrolysis ndikupanga metabolite yosagwira - kuchokera kwa carboxylic acid (85% ya metabolites yozungulira), ndipo inayo imayambitsa ma isoenzymes osiyanasiyana a cytochrome P450. Pa chiyambi
clopidogrel imasinthidwa kukhala yapakatikati metabolite - 2-oxo-clopidogrel. Pambuyo kagayidwe ka 2-oxo-clopidogrel kumabweretsa mapangidwe yogwira metabolite ya clopidogrel - thiol yotengera Clopidogrel. Mu vitro, njirayi imalumikizidwa ndi isoenzymes CYP3A4, CYP2C19, CYP1A2 ndi CYP2B6. Yogwira thiol metabolite wa clopidogrel olekanitsidwa pansi pamikhalidwe mu vitro, mwachangu komanso mosagwirizana amalumikizana ndi mapulateleti, kuti atsekere.

Ndi_m_Ah yogwira metabolite m'magazi am'magazi mutamwa mankhwala othamanga (300 mg) ya clopidogrel ndi okwanira kuchulukana ndi C_m_Ah Pambuyo 4 masiku ntchito clopidogrel mu yokonza mlingo (75 mg / tsiku). Ndi_m_Ah mu madzi a m'magazi zimatheka pafupifupi mphindi 30-60 mutamwa mankhwalawa.

Pambuyo pakukulitsa 14 C-cholembedwa clopidogrel, pafupifupi 50% ya ma radioac yonse amatulutsidwa ndi impso ndipo pafupifupi 46% ndi matumbo mkati mwa maola 120 atangomaliza kuchita. Pambuyo pakamwa limodzi makonzedwe a clopidogrel pa 75 mg, theka-moyo (T_1/2) ndi pafupifupi maora 6. T_1/2 chachikulu chosagwira metabolite kuzungulira mu madzi am`magazi pambuyo kamodzi ndi mobwerezabwereza ntchito ndi 8 maola.

Isoenzyme CYP2C19 imatenga nawo mbali pakapangidwe ka metabolite yogwira komanso yapakatikati ya metabolite - 2-oxo-clopidogrel. The pharmacokinetics ndi antiplatelet zotsatira za yogwira clopidogrel metabolite, komanso zotsatira za kuwunika kwa kupatsidwa zinthu za m'magazi pansi pa v vivo, zimasiyana kutengera mtundu wa CYP2C19 isoenzyme.

Khungu la CYP2C19 * 1 isoenzyme gene limafanana ndi kagayidwe kogwira mokwanira, pomwe ma genulo a CYP2C19 * 2 ndi CYP2C19 * 3 isoenzyme sagwira ntchito. Alleles a CYP2C19 * 2 ndi CYP2C19 * 3 isoenzyme amachititsa kuchepa kwa metabolism m'mayimidwe ambiri amtundu wa Caucasoid (85%) ndi Mongoloid (99%). Zotsatira zina zomwe zimagwirizanitsidwa ndi kuchepa kapena kuchepa kwa kagayidwe kachilengedwe sizachilendo ndipo zimaphatikizapo, koma sizingokhala, ma gens a CYP2C19 * 4, * 5, * 6, * 7 ndi * 8 isoenzyme.

Odwala omwe ali ndi CYP2C19 isoenzyme yotsika ntchito ayenera kukhala ndi magwiridwe antchito awiri omwe atchulidwa pamwambapa ndi kuwonongeka kwa ntchito. Malinga ndi kafukufuku wosindikizidwa, kuchuluka kwa ma genotypes okhala ndi ntchito zochepa za CYP2C19 isoenzyme, limodzi ndi kuchepa kwa metabolism, ali pafupifupi 2% mwa oimira mpikisano wa Caucasoid, 4% mwa anthu a liwiro la Negroid ndi 14% mwa anthu a mtundu wa Mongoloid. Pali mayeso oti adziwe mtundu wa CYP2C19 isoenzyme. Malinga ndi kafukufuku komanso kusanthula kwa meta, komwe kunaphatikizapo anthu omwe ali ndi ntchito zapamwamba kwambiri, zapamwamba, zapakati komanso zochepa za CYP2C19 isoenzyme, kusiyana kwakukulu pakuwonekera kwa metabolite yogwira ntchito komanso kuchuluka kwa zoletsa za kuphatikizira kwa mapulateleti a ADP-odzipereka omwe ali ndi ntchito zapamwamba kwambiri, zapamwamba komanso zapakati pa isoenzyme CYP2C19 kunalibe. Odzipereka omwe ali ndi ntchito yochepa ya isoenzyme iyi, kuwonetsa kwa metabolite yogwira kunachepa poyerekeza ndi odzipereka omwe ali ndi ntchito yayikulu ya isoenzyme CYP2C19.

Mukamagwiritsa ntchito clopidogrel muyezo wa 600 mg, muyezo wokweza / 150 mg yokonza mlingo (600 mg / 150 mg) mwa odwala omwe ali ndi kagayidwe kochepa, chiwonetsero cha metabolite chogwira ntchito chinali chokwera kuposa njira ya mankhwala ya 300 mg / 75 mg. Kuphatikiza apo, kuchuluka kwa zoletsa za kuphatikizana kwa mapulateleti kunali kofanana ndi komwe kumachitika m'magulu a odwala omwe ali ndi ntchito yayikulu ya CYP2C19 isoenzyme
Clopidogrel malinga ndi pulani ya 300 mg / 75 mg. Komabe, mlingo wa clopidogrel mu gulu la odwala omwe ali ndi ntchito zochepa za CYP2C19 isoenzyme sizinatsimikizidwe mu maphunziro omwe amaphatikizapo kafukufuku wazotsatira zamankhwala. Zoyesa zamankhwala zomwe zachitika mpaka pano zilibe zitsanzo zosakwanira kuti muzindikire kusiyana kwa zotsatira zamankhwala kwa odwala omwe ali ndi CYP2C19 isoenzyme yotsika.

Pharmacokinetics yamagulu apadera a odwala

The pharmacokinetics ya yogwira metabolite ya clopidogrel m'magulu apadera a odwala (okalamba, ana, odwala omwe ali ndi vuto laimpso ndi kwa chiwindi) sanaphunzire.

Odwala okalamba

Matenda aimpso

Pambuyo kugwiritsidwa ntchito mobwerezabwereza kwa clopidogrel pa mlingo wa 75 mg patsiku kwa odwala omwe ali ndi vuto laimpso (CC 5-15 ml / min), kuchuluka kwa zoletsa za kuphatikizidwa kwa mapulani a ADP ndi 25% kutsika kuposa odzipereka athanzi. Komabe, kuchuluka kwa kutalika kwa nthawi yotuluka magazi kunali kofanana ndi komwe odzipereka athanzi omwe adalandira
clopidogrel pa mlingo wa 75 mg patsiku.

Kuwonongeka kwa chiwindi

Contraindication

- Hypersensitivity to clopidogrel kapena aliyense wakupanga yemwe amapanga mankhwalawa,

- kukanika kwambiri kwa chiwindi,

- kutuluka magazi kwambiri, monga magazi ochokera ku zilonda zam'mimba kapena zotupa za m'mimba,

- kuchepa kwa lactase, tsankho lactose, shuga-galactose malabsorption syndrome,

- mimba ndi nthawi yoyamwitsa,

- Ana ochepera zaka 18 (chitetezo ndi kuchita bwino osakhazikitsidwa).

Ndi chisamaliro:

- Kuchepa mphamvu kwa chiwindi ndi vuto la kukhetsa magazi (zochitika zochepa)

- matenda aimpso

- matenda omwe amachulukitsa magazi (kuphatikizapo zoopsa, opaleshoni (onani gawo "Malangizo apadera"),

- matenda omwe ali ndi chiyembekezo cha chitukuko cha magazi (makamaka m'mimba ndi ma intraocular),

- kugwiritsa ntchito nthawi imodzi ndi mankhwala osapinga a antiidal (NSAIDs) kuphatikizapo cycloo oxygenase-2 inhibitors (COX-2),

- kugwiritsa ntchito munthawi yomweyo warfarin, heparin kapena glycoprotein IIb / IIIa zoletsa,

- odwala omwe ali ndi vuto lochepa la CYP2C19 isoenzyme (mutagwiritsa ntchito clopidogrel mu Mlingo wolimbikitsidwa, metabolite yochepa kwambiri ya clopidogrel imapangika ndipo mphamvu yake ya antiplatelet imakhala yochepa kwambiri chifukwa chake, mukamagwiritsa ntchito clopidogrel mu Mlingo wovomerezeka wa coronary syndrome kapena kulowerera kwamitsempha yama coronary, pamakhala kugunda kwa mtima. apamwamba kuposa odwala omwe ali ndi zochitika wamba za isoenzyme CYP2C19),

Hypersensitivity kwa thienopyridines ena (i.e.
ticlopidine, prasugrel) (onani gawo "Malangizo apadera").

Mimba ndi kuyamwa:

Popeza palibe deta yakuchipatala pakugwiritsa ntchito clopidogrel pa nthawi yomwe muli ndi pakati, mankhwalawa ali osavomerezeka kuti mugwiritse ntchito panthawi yomwe mukukhala ndi pakati. Kafukufuku wazinyama sanawonetse chofooka chachindunji kapena chosakhudza pakubala, kukula kwa mluza / mwana wosabadwayo, njira ya kubereka kapena kubereka.

Kafukufuku wazinyama wasonyeza kuti
clopidogrel ndi / kapena ma metabolites ake amuchotseredwa mkaka wa m'mawere. Chifukwa chake, ngati kuli kotheka, chithandizo
Clopidogrel om analimbikitsa kuti ayamwe kuyamwitsa.

Mlingo ndi makonzedwe

Mkati, ngakhale kudya zakudya, kamodzi patsiku.

Akuluakulu ndi odwala okalamba omwe ali ndi zochitika wamba za CYP2C19 isoenzyme

Myocardial infarction, ischemic stroke, kapena matenda ofunika a ochepa mwa njira ya occlusion.

Zilt® imatengedwa pa mlingo wa 75 mg (piritsi 1) kamodzi patsiku.

Acute coronary syndrome yopanda ST gawo kukweza (osakhazikika angina kapena myocardial infarction popanda Q wave)

Pachimake coronary syndrome ndi ST gawo kukweza (pachimake myocardial infarction) ndi mankhwala ndi kuthekera kwa thrombolytic mankhwala, limodzi acetylsalicylic acid.

Fibrillation ya atria

Ngati wodwala adaphonya wotsatira:

- ngati pasanathe maola 12 mutadumpha mlingo wotsatira, muyenera kumwa nthawi yomweyo Zamp®, ndiye kuti mukumwa mlingo wotsatira nthawi yomweyo.

- ngati maola opitilira 12 adatha kulumpha mlingo wotsatira, ndiye kuti mlingo wotsatira uyenera kumwedwa nthawi yokhayo, pomwe mankhwalawa sayenera kuwiriridwa kawiri.

Akuluakulu ndi odwala okalamba omwe ali ndi chibadwa chotsimikizika amachepetsa ntchito ya CYP2C19 isoenzyme

Magulu apadera a odwala

Odwala okalamba

Matenda aimpso

Pambuyo kugwiritsidwa ntchito mobwerezabwereza kwa clopidogrel pa mlingo wa 75 mg patsiku kwa odwala omwe ali ndi vuto laimpso (CC 5-15 ml / min), kuchuluka kwa zoletsa za kuphatikizidwa kwa mapulani a ADP ndi 25% kutsika kuposa odzipereka athanzi. Komabe, kuchuluka kwa kutalika kwa nthawi yotuluka magazi kunali kofanana ndi komwe odzipereka athanzi omwe adalandira
clopidogrel pa mlingo wa 75 mg patsiku. Kulekerera kwa mankhwalawa kunali kwabwino mwa odwala onse. Kuwonongeka kwa chiwindi

Zotsatira zoyipa

Chitetezo cha clopidogrel chakhala chikufufuzidwa mwa odwala omwe adalandira chithandizo cha clopidogrel 1 chaka kapena kuposerapo. Chitetezo cha clopidogrel pa mlingo wa 75 mg patsiku chinali chofanana ndi cha acetylsalicylic acid pa mlingo wa 325 mg patsiku, mosaganizira zaka, jenda komanso mtundu. Zoyipa zomwe zimawonedwa m'mayesero azachipatala zalembedwa pansipa. Kuphatikiza apo, malipoti osinthasintha amasonyezedwa.

M'maphunziro azachipatala ndi kuwunika kwakumbuyo kwa clopidogrel, kutulutsa magazi nthawi zambiri kumanenedwa, makamaka m'mwezi woyamba wamankhwala.

Kugawidwa kwa zotsatira zoyipa za World Health Organisation (WHO): pafupipafupi? 1/10, nthawi zambiri kuchokera pa 1/100 mpaka 1/10000 kupita

Kutulutsa mawonekedwe ndi kapangidwe kake

Fomu ya Mlingo - mapiritsi okhala ndi filimu: ozungulira, pang'ono ndi biconvex, pinki, piritsi imakhala ndi yoyera kapena pafupi yoyera (7 m'matumba, m'matupa a 2, 4 kapena 12 matuza).

The yogwira ndi clopidogrel hydrosulfate, piritsi limodzi - 97.875 mg, kapena clopidogrel - 75 mg.

Zothandiza: microcrystalline cellulose, anactrous lactose, pregelatinized starch, hydrogenated castor mafuta, macrogol 6000.

Mapangidwe a chipolopolo cha filimuyi: propylene glycol, hypromellose 6cp, talc, titanium dioxide (E171), utoto wa iron utayidi wofiira (E172).

Wopanga ndi mtengo

Kampani yopanga zamankhwala yopanga mankhwala a Zilt ku Russia KRKA. Komanso pamsika wapakhomo, nthawi zina mungapeze mankhwala ochokera kunja ochokera ku Slovenia.

Ndi "Zilt", mwatsoka, yotsika mtengo. Mtengo wa mankhwalawa umadalira, choyamba, pa kuchuluka kwa matuza omwe amapakidwa m'bokosi. Mwachitsanzo, mapiritsi 14 a ichi chida pafupifupi 500-600 r, kutengera wothandizira. Kwa matuza 12, muyenera kulipira kuposa 2000 p. Mulimonsemo, mankhwalawa amagawidwa m'mafakisoni pokhapokha ngati mwalandira mankhwala.

Zotsatira za pharmacological

Mu malo owonongeka a mtima mthupi la munthu, maplatelet nthawi zonse amayamba kudziunjikira. Nthawi yomweyo, amamatira limodzi komanso amatsatira minofu. Izi zimatha ndikupanga magazi.

Mankhwala "Zilt", malangizo ogwiritsira ntchito omwe ndi osavuta, amayamba kuchita bwino kwa wodwala mwachangu kwambiri - pafupifupi mphindi 30 pambuyo pa kuperekedwa. Pamene ilowa mthupi laumunthu, chopinga cha kuphatikizana kwa maplatelet chimachitika. Kugwiritsa ntchito mankhwalawa pafupipafupi pakatha masiku 4-7, pazotheka kwambiri pochizira.

Kuchuluka kwa mankhwalawa kwa mankhwalawa m'thupi kumachitika patatha maola angapo mutakhazikitsa. Komanso, zomwe zimapezeka m'magazi ngakhale nthawi imeneyi nthawi zambiri zimakhala zochepa.

Mankhwalawa amachotsedwa m'thupi ndi impso komanso matumbo ake. Hafu ya moyo pambuyo pa limodzi mlingo pafupifupi maola 6-8.

Mankhwala "Zilt": malangizo ogwiritsira ntchito

Mankhwalawa amapezeka, monga tanenera kale, mwa mapiritsi okha. Mogwirizana, amatenga kokha pakamwa. Imwani mapiritsi a 75 mg "Zilt" omwe amagwiritsidwa ntchito amalola zonse musanadye, komanso mukatha kudya kapena mkati mwake. Njira zoyenera kumwa mankhwalawa zimadalira nthendayi.

Wodwala yemwe ali ndi vuto la m'mnyewa wamtima nthawi zambiri amapatsidwa piritsi limodzi 75 mg patsiku. Mlingo womwewo umaperekedwa kwa odwala omwe ali ndi ischemic cerebrovascular ngozi ndi ochepa occlusion. Pankhaniyi, kwa odwala omwe ali ndi myocardial infarction, mankhwalawa amatha kuikidwa panthawiyi kuyambira masiku 1 mpaka 35 chitukuko cha matendawa. Odwala omwe ali ndi ischemic stroke "Zilt" nthawi zambiri amalembedwa kuyambira masiku 7 mpaka miyezi isanu ndi umodzi.

Mu coronary syndrome yokhala ndi gawo lama ST, mankhwalawa amadziwikanso kuchuluka kwa 75 mg patsiku. Koma pankhaniyi, wodwalayo kale amatenga muyeso umodzi wokweza limodzi ndi aspirin ndi thrombolytics.

Mu coronary syndrome popanda kukwezedwa kwa ST, njira ina yosiyanasiyana ya mankhwala imagwiritsidwa ntchito. Pankhaniyi, mankhwalawa nthawi zambiri amatengedwa motere:

kumwa kumwa kwa 300 mg kamodzi

kumwa mankhwala tsiku lililonse piritsi 1 patsiku.

Kuphatikiza apo, kuphatikiza ndimankhwala omwe amapezeka ndi aspirin mu 75-325 mg, tsiku lililonse la Zilt liyenera kukhala 100 mg. Ndi regimen iyi, zotsatira zabwino kwambiri mwa odwala zimawonedwa pambuyo pa miyezi itatu. Njira ya mankhwala nthawi zambiri ndi miyezi 12.

Mankhwala oterewa amaperekedwa nthawi zambiri kwa odwala akuluakulu osakwana zaka 75.

Ntchito malangizo "Zilt": contraindication

Kwa achinyamata ochepera zaka 18, "Zilt" sinafotokozeredwe kupewa matenda a thrombosis. Sitikulimbikitsidwanso kumwa mankhwalawa kwa amayi apakati ndi amayi apakati. Clopidogrel amatha kulowa, kuphatikiza, mkaka wa m'mawere.

Zachidziwikire, simungathe kumwa mankhwalawa komanso anthu omwe angayambitse zovuta zake pazigawo zake zilizonse. Kodi contraindication pa ntchito "Zilt":

Malinga ndi malangizo ogwiritsira ntchito, "Zilt" iyenera kumwedwa mosamala pakakhala zovuta monga:

Hypersensitivity to thienopyridines,

zochitika zochepa za CYP2C19,

chiwindi ndi impso ntchito.

Matenda omwe magazi amatuluka,

opareshoni ndi kuvulala komwe kumayambitsa magazi.

Kuchita

Kuphatikiza apo, mosamala muyenera kutengedwa, mogwirizana ndi malangizo ogwiritsira ntchito, "Zilt" 75 mg imodzi mwanjira zina monga:

Zomwezi zimagwiranso ntchito pa chithandizo chovuta cha mankhwala a Zilt komanso sanali antiidal.

Zotheka kumwa mankhwalawa zitha kuchepa ngati wodwala walandira chithandizo:

"Ticlopidine" ndi mankhwala ena.

Zomwe odwala ayenera kudziwa

Odwala omwe akutenga Zilt ayenera kutsatira malangizo otsatirawa:

milandu yachilendo zachilendo kapena kutuluka kwa magazi kuyenera kuuzidwa kwa dotolo,

madokotala a mano ndi madokotala a opaleshoni ayenera kudziwitsidwa za njira ya chithandizo ndi Zilt ngati alumikizidwa.

Zotsatira zoyipa zomwe zingachitike

Monga mankhwala ena aliwonse, Zilt ikhoza kukhala ndi zotsutsana ndi thupi la wodwalayo. Nthawi zambiri, mukadutsa maphunziro pogwiritsa ntchito mankhwalawa, zotsatirazi zoyipa zimawonedwa mwa odwala:

kupweteka kwam'mimba ndi m'mimba,

Nthawi zina, omwe amamwa mankhwalawa amatha kudziwonetsanso:

kuyabwa kapena kupindika

zotupa m'maso,

Pakayezetsa magazi a labotale, kuchepa kwamapulatifomu ndi ma neutrophils nthawi zina kumatha kupezeka mwa odwala.

Pali zovuta zingapo za mankhwalawa. Chifukwa chake, malangizo ogwiritsira ntchito "Zilt" 75 mg ayenera kuyang'aniridwa mosalephera. Mankhwala ochulukirapo a mankhwalawa, omwe, sangathe kulekerera. Ngati wodwalayo angaiwale mwadzidzidzi kumwa mapiritsi tsiku lina, kumwa kawiri tsiku lotsatira sikulimbikitsidwa mulimonse.

Malinga ndi malangizo ogwiritsira ntchito, mapiritsi a Zilt, monga ena onse, sayenera kuledzera ngati mukusowa mtundu uliwonse wa zigawo zake. Kusintha kotereku mukamagwiritsa ntchito mankhwalawa nkosowa. Koma nthawi zina odwala omwe akumwa mankhwala pogwiritsa ntchito mankhwalawa amatha kuonedwa. Ambiri zimachitika ndi:

Hypersensitivity kuti thienopyridines.

Zoyenera kuchita vuto la bongo

Kugwiritsa ntchito mankhwala mosemphana ndi malangizo ogwiritsira ntchito "Zilt" kumapangitsa kuti mavuto abwere motere:

magazi amtundu wina,

kuchuluka kwa magazi.

Chithandizo cha mankhwala osokoneza bongo omwe ali ndi mankhwalawa ndi chizindikiro. Odwala nthawi zambiri amathiridwa magazi ndi mapulatele.

Mitu ya mankhwalawa

Zimawononga "Zilt", monga tanena kale, mtengo wokwera mtengo. Chifukwa chake, odwala ambiri, ali ndi chidwi ndi zomwe mtengo wotsika mtengo ungalowe m'malo mwa mankhwalawa ngati pakufunika.

Mgwirizano wama mankhwala "Zilt" ndi: mwachitsanzo:

Ndalamazi zonse m'mapangidwe ake zimakhala ndi zinthu zofanana ndi Zilt. Ngati angafune, mankhwalawa amatha kusintha nthawi iliyonse ndi imodzi mwazofanana pamndandanda. Malangizo ogwiritsira ntchito ndi Zilt ndi maulumikizidwe ake pafupifupi amafanana. Mankhwalawa amachepetsa magazi kuundika. Komabe, imaloledwa kusintha Zilt kukhala ina iliyonse mwa mawonekedwe awa pokhapokha atakambirana ndi adokotala.

Zomwe zimapangidwira ku Zilt ndi mankhwala Clopidogrel (mtengo wa 190 p. Kwa ma PC 14) ndi Clopidogrel Richter (292 p).

Mankhwala a mankhwalawa, komanso kupewa magazi kukokana, ali motere:

"Phenilin" amawonetsedwa kwa odwala pa 0,025-0.1 g katatu patsiku. Odwala amatha kumwa Dicumarin mu Mlingo kuchokera 0,05 mpaka 0,1 g katatu patsiku. Madokotala amapereka Heparin kwa odwala mozungulira, kudzera m'mitsempha kapena m'mitsempha.

Komanso, mankhwala "Plavix" amatanthauza fanizo la mankhwalawa. "Zilt", malangizo ogwiritsira ntchito omwe tidawunikiranso pamwambapa, nawokha, ndiwotsika mtengo pamalonda awa. Odwala ambiri, opatsidwa ndalama zokwanira, amalangizidwa kuti asankhe Plavix popewa thrombosis. Pakugwiritsa ntchito bwino, Zilt imakhala yotsika pang'ono pamankhwala opangidwa ngati awa.

Malo osungira

Inde, kuti muteteze magazi kuundana uyenera kukhala wopanda mankhwala kwa "Zilt". Ndikulimbikitsidwa kusunga mankhwalawa pamtunda wotsika mpaka +25 ° C. Ndiye kuti, m'chilimwe ndikofunikira kuyika mapiritsi awa mufiriji. Alumali moyo wa mankhwala osindikizidwa omata ndi zaka zitatu.

Ndemanga za chithandizo kuchokera kwa odwala

Odwala ali ndi lingaliro labwino kwambiri za mankhwalawa. Odwala amagwirizana ndi zabwino zake:

kusowa kwa zoyipa pamimba.

Mankhwalawa amathandizira magazi, malinga ndi odwala ambiri, abwino kwambiri kuposa aspirin yemweyo. Ndiye kuti, chiwopsezo cha kubwereza kwa mtima kawiri kapena kugunda kwa mtima ngati mugwiritsidwa ntchito mosamala mogwirizana ndi malangizo ogwiritsira ntchito, Zilt, ndemanga zake pankhaniyi ndizabwino zokhazokha, zimachepetsa.

Zina mwa zovuta za mankhwalawa, odwala amaganiza:

osakwanira kwambiri ma CD.

Matenda a mtima ndi stroko zimachitika, mwachidziwikire, mwa anthu azaka zapakati. Koma nthawi zambiri, anthu okalamba amakumana ndi vutoli. Ndipo zowonadi, kugula mtengo wotsikirira woterewu nthawi zambiri kumakhala kovuta.

Mapiritsi okhala ndi mapaketi amapakidwa m'matumba omwe amawonongeka m'manja. Mwina wopanga motero amafuna kuti kugwiritsa ntchito mankhwalawa tsiku lililonse kukhala kosavuta. Komabe, malinga ndi odwala ambiri, zingakhale bwino kutulutsa mapiritsiwo m'matenthe olimba motsatira mzere wotumphuka.

Chovuta china cha mankhwala a Zilt ndichakuti odwala ambiri amachiona kuti chimakhudza chiwindi. Odwala ambiri amalangizidwa kumwa mankhwalawa moyang'aniridwa ndi dokotala.

Kodi madokotala amaganiza chiyani za mankhwalawa?

Madokotala nawonso amawona kuti Zilt ndi njira yabwino yochepetsera kusokonekera kwa magazi. Zovuta za mankhwalawa, madokotala amati makamaka zimathandizidwa ndi odwala ambiri. Poyerekeza ndi ndemanga, kutaya magazi pakamagwiritsidwa ntchito ndikosowa kwambiri.

Maziko a umboni pokhudzana ndi chitetezo ndi kufunika kwa mankhwalawa, monga momwe madokotala ambiri amanenera, ndizabwino kwambiri. Komabe, amakhulupirira kuti mankhwalawo ali mulingo woyenera kwambiri. Madokotala amadziyambitsa okha kuti asamayanjane ndi kugwiritsa ntchito kwake.

Malangizo ogwiritsira ntchito Zilt: Njira ndi mlingo

Mapiritsi amatengedwa pakamwa, ngakhale chakudyacho.

Mlingo wovomerezeka wa odwala omwe ali ndi zochitika za CYP2C19 isoenzyme, kuphatikizapo odwala okalamba:

Myocardial infarction, ischemic stroke kapena matenda opatsirana a minyewa a occlusion: 75 mg kamodzi patsiku,
Acute coronary syndrome yopanda ST gawo kukweza (osakhazikika angina ndi myocardial infarction popanda Q wave): kuchuluka kwa mankhwala - kamodzi 300 mg, ndiye 75 mg kamodzi patsiku palimodzi ndi acetylsalicylic acid pa 75 mg wa 75 pa tsiku. Mukapereka mankhwala, ziyenera kukumbukiridwa kuti milingo ya acetylsalicylic acid pamwamba pa 100 mg imayanjana ndi chiwopsezo chotaya magazi. Zotsatira zakuchizira zimachitika mwezi wachitatu wamankhwala, pazotsatira zoyenera, ndikofunika kupitiliza kugwiritsa ntchito clopidogrel kwa miyezi 12,
Pachimake myocardial infarction (pachimake coronary syndrome ndi ST gawo kukweza): limodzi loading mlingo, ndiye 75 mg kamodzi patsiku osakaniza kapena wopanda acetylsalicylic acid ndi thrombolytics. Iwo ali osavomerezeka kugwiritsa ntchito Mlingo wa mankhwala othandizira odwala omwe ali ndi zaka zopitilira 75. Kuchiza kuyenera kuyambitsidwa pamene zizindikiro zoyambirira za matendawo ziwoneka ndipo zipitilira pafupifupi milungu 4,
Atrial fibrillation (atration fibrillation): 75 mg kamodzi patsiku osakanikirana ndi acetylsalicylic acid pa mlingo wa 75-100 mg tsiku lililonse.

Ndikulimbikitsidwa kumwa mapiritsi nthawi yomweyo, ngati mwachedwa kwa maola osakwana 12, muyenera kumwa mlingo womwe mwasowa ndi wotsatira panthawi yokhazikika, ndikutalikirana kwa nthawi yopitilira maola 12 - mlingo wotsatira umatengedwa osanenanso.

Odwala ndi chibadwa kutsimikiza anachepetsa ntchito ya CYP2C19 isoenzyme pamene Zilt mu analimbikitsa Mlingo, mapangidwe yogwira metabolite wa clopidogrel kumachitika zochepa ndipo antiplatelet kwenikweni sanena. Mlingo woyenera kwambiri wa odwala omwe ali m'gulu lino silinakhazikitsidwe, nthawi zambiri, mankhwalawa amadziwitsidwa muyezo waukulu ndi muyeso umodzi wa muyeso wa 600 mg ndi 150 mg kamodzi patsiku.

Odwala okalamba safuna kusintha kwa mlingo.

Zotsatira zoyipa

Kuchokera pamtima dongosolo: Nthawi zambiri - hematoma, osowa - ochepa hypotension, vasculitis,
Kuchokera hematopoietic dongosolo: infrequecent - leukopenia, thrombocytopenia, eosinophilia, kawirikawiri neutropenia, kuphatikizapo mitundu yoopsa, kawirikawiri aplastic anemia, thrombotic thrombocytopenic purpura (TTP), pancytopenia, strombocytopenia, agranulocytosis, aganocytosis
Kuchokera pamatumbo am'mimba: pafupipafupi - kupweteka kwam'mimba, magazi am'mimba, kutsekula m'mimba, dyspepsia, pafupipafupi - nseru, kusanza, kudzimbidwa, gastritis, kuchepa kwa zilonda zam'mimba komanso / kapena zilonda zam'mimba, kawirikawiri - kuchepa kwa zotupa m'mimba, kawirikawiri - pancreatitis, kutuluka kwa magazi ndi chifuwa cham'mimba (kuphatikizapo kufera), colitis (kuphatikiza zam'mimba), kuperewera kwa chiwindi, hepatitis, matenda amtundu wa chiwindi, stomatitis,
Kuchokera kumbali yamanjenje: pafupipafupi - kupweteka mutu, kukhathamiritsa kwamkati (kuphatikiza zotsatira zakupha), chizungulire, paresthesia, kawirikawiri - chisokonezo, kuyerekezera zinthu m'maganizo,
Kuchokera ku minculoskeletal system: kawirikawiri - hemarthrosis, zotupa za m'mimba, nyamakazi, myalgia, arthralgia,
Kuchokera kupuma dongosolo: Nthawi zambiri - nosebleeds, kawirikawiri - bronchospasm, magazi ochokera kupuma thirakiti (pulmonary hemorrhage, hemoptysis), interstitial pneumonitis,
Kuchokera ku genitourinary system: pafupipafupi - hematuria, osowa - glomerulonephritis, kuchuluka kwa serum creatinine ndende,
Pa khungu: pafupipafupi - subcutaneous hematomas, pafupipafupi - khungu kuyabwa, zotupa, zotupa za pakhungu (purpura), osowa kwambiri - bulous dermatitis (Stevens-Johnson syndrome, poyizoni epermermosis, erythema multiforme), uritisaria, zotupa za erythematous, lichen planus, chikanga
Kuchokera ku ziwalo zam'maganizo: kawirikawiri - zotupa kapena zotupa zam'mimba, kawirikawiri - vertigo, kawirikawiri - kulawa kwa pathologies,
Zizindikiro zasayansi: kawirikawiri - kuchepa kwamapulatifomu ndi ma neutrophils, kukulitsa nthawi yotuluka magazi,
Thupi lawo siligwirizana: kawirikawiri - eczema, angioedema, anaphylactoid zimachitika, seramu matenda, pafupipafupi - mankhwala zidzolo ndi zokhudza zonse zizindikiro za DRESS matenda ndi eosinophilia, mtanda-yogwira hypersensitivity kwa thienopyridines, mankhwala ochititsa hypersensitivity syndrome,
Zina: pafupipafupi - kutulutsa kwamitsempha pamalo opumira, osowa kwambiri - magazi kwambiri kuchokera ku bala la opaleshoni, malungo.

Mimba komanso kuyamwa

Malinga ndi malangizo, Zilt siyikulimbikitsidwa kuti mugwiritse ntchito panthawi yomwe muli ndi pakati, popeza palibe zambiri zakuchipatala pakugwiritsa ntchito kwa clopidogrel mwa amayi apakati. Kafukufuku wazinyama sanawonetse mavuto alionse mwachindunji kapena osakhudzana ndi mankhwalawa pamimba, kukula kwa mwana wosabadwa, kubadwa kwa mwana, kapena kukula kwa mwana pambuyo pake.

M'maphunziro oyesera a nyama, zidapezeka kuti clopidogrel ndi metabolites ake amalowa mkaka wa m'mawere, chifukwa chake, ngati pakufunika kugwiritsa ntchito Zilt mwa amayi oyamwitsa, kuyamwitsa kuyenera kuyimitsidwa.

Mu vuto laimpso

Pogwiritsa ntchito mobwerezabwereza Zeke pa mlingo wa 75 mg patsiku kwa odwala omwe ali ndi vuto la impso (creatinine chilolezo - 5-15 ml / min), kuchuluka kwa kuponderezedwa kwa kupatsidwa kwa zinthu zam'magazi kunali 25% kutsika kuposa kuchuluka kwa zoletsa za kupatsidwa zinthu za m'magazi poyerekeza ndi odzipereka athanzi. Komabe, kuchuluka kwa nthawi yotuluka magazi kunali kofanana ndi komwe odzipereka athanzi omwe amalandira mankhwalawa pa 75 mg tsiku lililonse. Kulekerera kwa Zilt kulinso bwino kwa odwala onse.

Kuyanjana kwa mankhwala osokoneza bongo

Chifukwa cha kuchuluka kwa magazi, osavomerezeka kupereka mankhwalawa nthawi imodzi ndi warfarin, ndipo akaphatikizidwa ndi heparin ndi othandizira ena a thrombolytic, chisamaliro chapadera chiyenera kumwedwa.

NSAIDs imawonjezera chiopsezo cha zilonda zam'mimba komanso zotupa m'matumbo am'mimba.

Palibe kulumikizana kwakukulu mwachipatala komwe kunapezeka ndi ntchito imodzi ndi atenolol, ma inhibitors a angiotensin (ACE), mankhwala omwe amachepetsa magazi a cholesterol, digoxin, nifedipine, phenobarbital, estrogens, cimetidine, theophylline.

Clopidogrel imatha kuwonjezera kuchuluka kwa acetylsalicylic acid pa collagen-inachititsa kuphatikiza kupatsidwa zinthu za m'magazi. Kulumikizana kwa mankhwalawa kwa mankhwalawa ndi acetylsalicylic acid kumawonjezera mwayi wokhetsa magazi, kotero kugwiritsa ntchito kuphatikiza uku ndikotheka chaka chimodzi chokha.

Mafuta a clopidogrel samakhudzidwa ndi maantacid.

Kuphatikiza ndi tolbutamide, phenytoin imawonjezera kuchuluka kwa kutsekeka kwa plasma yamagazi.

Zifanizo za Zilt ndi: Lopirel, Clopidogrel, Clopidogrel-SZ, Plavix, Aggregal, Detromb, Cardutol, Clopidex, Clopilet, Listab 75, Deplatt-75, Cardogrel, Clopigrant, Lirta, Targetek, Plagril, Egithrombrel, Troken.

Ndemanga za Zilt

Odwala amalabadira bwino mankhwalawo, osangogwira ntchito, komanso mtengo wovomerezeka (poyerekeza ndi anzawo ena okwera mtengo). Malinga ndi ndemanga, Zilt imagwira mtima pambuyo pa vuto la mtima ndi njira yoluma. Odwala adawona kusintha kwamtundu wonse, kuchepa kwa ziwopsezo za angina, komanso kusakhalapo kwa arterial and vein thrombosis.

Nthawi zina odwala amadandaula za kubwera kwa zotsatira zoyipa (urticaria, kupuma movutikira), koma ngati mupitiliza chithandizo, ndiye kuti zotsatirapo zake zoyipa zimasowa mwaokha pakapita kanthawi.

Mtengo wa Zilt m'mafakitale

Mpaka pano, mitengo yolingana ndi Zilt m'mafakitore ndi iyi:

mapiritsi okhala ndi filimu, 75 mg (14 ma PC. pakiti iliyonse) - 470-530 rubles,
mapiritsi okhala ndi filimu, 75 mg (28 ma PC. pakiti iliyonse) - 830-1200 rubles,
mapiritsi okhala ndi filimu, 75 mg (84 zidutswa pa paketi) - 1875-2030 rubles.

Zogulitsa

Pambuyo pakamwa kamodzi komanso mobwerezabwereza pakamwa pa 75 mg patsiku, clopidogrel imatengedwa mwachangu. Mitundu yayitali ya kuchuluka kwambiri kwa ndende (Cmax) yosasinthika ya clopidogrel m'madzi am'magazi (2.2-2.5 ng / ml atatha kumwa kamodzi kwa 75 mg) imatheka pambuyo pa mphindi pafupifupi 45. Malinga ndi kafukufuku wa impretion wa impopidogrel metabolites, kuchuluka kwa mayamwidwe kuli pafupifupi 50%.

Kupenda

Clopidogrel imapukusidwa mwachangu mu chiwindi. In vitro ndi vivo, clopidogrel imapukusidwa m'njira ziwiri: yoyamba imayang'aniridwa ndi ma esterases ndipo imayambitsa hydrolysis ndikupanga metabolite yosagwira - kotengera carboxylic acid (85% ya metabolites yozungulira), ndipo inayo imagwidwa ndi ma isoenzymes osiyanasiyana a cytochrome P450. Poyamba, clopidogrel imasinthidwa kukhala yapakatikati metabolite - 2-oxo-clopidogrel. Pambuyo kagayidwe ka 2-oxo-clopidogrel kumabweretsa mapangidwe yogwira metabolite ya clopidogrel - thiol yotengera Clopidogrel. Mu vitro, njirayi imalumikizidwa ndi isoenzymes CYP3A4, CYP2C19, CYP1A2 ndi CYP2B6. The thiol metabolite yogwira ya clopidogrel, yokhayokha mu vitro, mwachangu komanso mosasinthika imalumikizana ndi mapuloteni othandizira, ndikuletsa kuphatikizika kwawo.

Cmax ya yogwira metabolite m'magazi am'magazi atamwa mankhwala okweza (300 mg) ya clopidogrel ndiwokwera kwambiri kuposa Cmax pambuyo masiku 4 akugwiritsa ntchito clopidogrel pa kashiamu wokonza (75 mg / tsiku). Cmax mu madzi am'magazi amafikira pafupifupi mphindi 30-60 atatha kumwa mankhwalawa.

Pambuyo pomeza 14C yolembedwa clopidogrel, pafupifupi 50% ya ma radioac yonse amatsitsidwa ndi impso ndipo pafupifupi 46% ndi matumbo mkati mwa maola 120 atangomaliza kuchita. Pambuyo pakamwa limodzi lokhazikika la clopidogrel pa 75 mg, theka la moyo (T1 / 2) ndi pafupifupi maola 6. T1 / 2 ya metabolite yayikulu yosagwira mu plasma pambuyo pokhapokha kamodzi ndi maola 8.

Kupewa kwa mavuto atherothrombotic:

Odwala achikulire omwe ali ndi vuto la myocardial infarction (kuyambira masiku ochepa mpaka masiku 35), ali ndi vuto la ischemic (kuyambira masiku 7 mpaka miyezi 6), kapena atapezeka ndi matenda amitsempha yamagazi yotupa.
Odwala akuluakulu omwe ali ndi vuto la pachimake coronary syndrome: popanda kukwera kwa STina (angina osakhazikika kapena kutsika kwa myocardial popanda Q wave), kuphatikiza odwala omwe adayamba kununkha ndi kulowererapo kwa coronary, osakanikirana ndi acetylsalicylic acid, ndi ST segment election mankhwala a mankhwala ndi kuthekera kwa thrombolytic mankhwala, kuphatikiza acetylsalicylic acid.

Kupewa kwa atherothrombotic ndi thromboembolic, kuphatikiza stroko, ndi atraya fibrillation (atria fibrillation)

Odwala achikulire omwe ali ndi atrill fibrillation (atria fibrillation), omwe ali ndi vuto limodzi la chiwopsezo cha mtima, sangatenge anticoagulants osagwirizana komanso amakhala ndi chiopsezo chochepa kutaya magazi (kuphatikiza ndi acetylsalicylic acid).

Acute coronary syndrome yopanda gawo la ST

Pachimake coronary syndrome ndi ST gawo kukweza

Fibrillation ya atria

Ngati wodwala adaphonya wotsatira:

Ngati maola ochepera 12 apita mutatha kulumpha mlingo wotsatira, muyenera kumwa nthawi yomweyo Zost®, kenako ndi kumwa nthawi yotsatira.
Ngati maola opitilira 12 adatha kulumpha mlingo wotsatira, ndiye kuti mlingo wotsatira uyenera kumwedwa nthawi yokhayo, pomwe mlingowo suyenera kuwiriridwa kawiri.

Matenda aimpso

Gwiritsani ntchito pa nthawi yoyembekezera komanso mkaka wa m`mawere

Kafukufuku wazinyama awonetsa kuti clopidogrel ndi / kapena ma metabolites ake amachotsedwa mkaka wa m'mawere. Chifukwa chake, ngati mankhwala a clopidogrel ndi ofunika, tikulimbikitsidwa kusiya kuyamwitsa.

Ma anticoagulants pakamwa

Kugwiritsa ntchito nthawi yomweyo kwa clopidogrel ndi anticoagulants pakamwa kungathe kuwonjezera kuchuluka kwa magazi, chifukwa chake, kuphatikiza uku sikulimbikitsidwa.

Kugwiritsidwa ntchito kwa clopidogrel pa mlingo wa 75 mg patsiku sikusintha pharmacokinetics ya warfarin (gawo lapansi la CYP2C9 isoenzyme) kapena kuchuluka kwa mayiko wamba (INR) mwa odwala omwe amalandila chithandizo cha nthawi yayitali ndi warfarin. Komabe, kugwiritsa ntchito nthawi imodzi ndi warfarin kumawonjezera ngozi ya kutuluka magazi chifukwa chakuwonjezera kowonjezera pakubwera magazi. Chifukwa chake, kusamala kuyenera kugwiritsidwa ntchito mukamagwiritsa ntchito warfarin ndi clopidogrel.

Acetylsalicylic acid

Acetylsalicylic acid sikukhudza chopinga cha kuphatikiza kwa kupatsidwa zinthu za m'magazi kochokera ku ADP, koma Clopidogrel amachititsa zotsatira za acetylsalicylic acid pa collagen-ikiwayambitsa kupatsidwa zinthu zamagulu. Komabe, kugwiritsa ntchito munthawi yomweyo 500 mg ya acetylsalicylic acid kawiri pa tsiku limodzi, sikuwonjezera kwambiri nthawi yotaya magazi chifukwa cha clopidogrel. Kulumikizana kwa pharmacodynamic pakati pa clopidogrel ndi acetylsalicylic acid mwina kumawonjezera mwayi wotulutsa magazi. Popeza izi, kusamala kuyenera kuchitika pakumwa mankhwalawa, ngakhale mu maphunziro azachipatala, odwala adatenga mankhwala ophatikizana ndi clopidogrel ndi acetylsalicylic acid chaka chimodzi.

Malinga ndi kafukufuku wazachipatala mwa anthu athanzi, akamamwa clopidogrel, panalibe chifukwa chosinthira heparin, ndipo zotsatira za heparin sizinasinthe. Kugwiritsidwa ntchito kwa nthawi imodzi kwa heparin sikunakhudze kuponderezedwa kwa kuphatikizana kwa maselo ndi clopidogrel. Mwinanso kukhudzana kwa pharmacodynamic pakati pa clopidogrel ndi heparin, zomwe zimayambitsa chiopsezo chotaya magazi. Chifukwa chake, kugwiritsa ntchito mankhwalawa munthawi yomweyo pamafunika kusamala.

Maulonda

Chitetezo pakugwiritsa ntchito munthawi yomweyo clopidogrel, fibrin-eni kapena fibrin-enieni a thrombolytics ndi heparin adayesedwa mwa odwala omwe ali ndi infralate ya myocardial infaration. Kuchuluka kwa magazi kwakanthawi kochepa kunali kofanana ndi kugwiritsidwa ntchito nthawi imodzi kwa thrombolytics, heparin wokhala ndi acetylsalicylic acid.

Mankhwala omwe amaletsa kutupa (NSAIDs)

Malinga ndi kafukufuku wachipatala wodzipereka ogwira ntchito zathanzi, kugwiritsa ntchito nthawi yomweyo Clopidogrel ndi naproxen kumawonjezera magazi am'mimba am'mimba. Komabe, chifukwa cha kuchepa kwa maphunziro pokhudzana ndi ma NSAID ena pakadali pano, sizikudziwika ngati chiopsezo chotenga magazi m'matumbo chikuwonjezeka mukamagwiritsa ntchito limodzi ndi ma NSAID ena. Chifukwa chake, chithandizo cha munthawi yomweyo cha NSAIDs, kuphatikiza COX-2 zoletsa, ndi clopidogrel ziyenera kuchitika mosamala (onani gawo "Malangizo apadera").

CYP2C19 Isoenzyme Inhibitors

Clopidogrel imapangidwa kuti ipangike metabolite yake yogwira, pang'ono pang'ono motsogozedwa ndi CYP2C19 isoenzyme. Chifukwa chake, mankhwala omwe amalepheretsa iyi isoenzyme angayambitse kuchepa kwa anthu omwe ali ndi metabolite ya clopidogrel. Kukula kwakukhudzana kwa matendawa sikudziwika. Kugwiritsa ntchito moyenera ndi zoletsa zamphamvu kapena zowonjezera za CYP2C19 isoenzyme ziyenera kupewedwa. Zoletsa za CYP2C19 isoenzyme zimaphatikizapo omeprazole ndi esomeprazole, fluvoxamine, fluoxetine, moclobemide, voriconazole, fluconazole, ticlopidine, ciprofloxacin, cimetidine, carbamazepine, oxcarbazepine ndi chloramphenicol.

Proton pump zoletsa

Kugwiritsira ntchito omeprazole muyezo wa 80 mg kamodzi patsiku nthawi imodzi ndi clopidogrel kapena kupuma kwa maola 12 pakati pa kumwa mankhwala awiriwa kumachepetsa kukhudzana (AUC) kwa metabolite yogwira ya Clopidogrel ndi 45% (mutatha kumwa mankhwalawa a clopidogrel) ndi 40% (mutatha kumwa mlingo wokonzanso Mlingo wa clopidogrel). Kuchepa kwa AUC kwa metabolite yogwira ya clopidogrel kumalumikizidwa ndi kuchepa kwa kuchuluka kwa zoletsa zamagulu ambiri (39% mutatenga mlingo wa clopidogrel ndi 21% mutamwa mlingo wa clopidogrel). Kugwirizana kwofanananso kwa Clopidogrel ndi esomeprazole kukusonyezedwa. Pazowonera komanso zamankhwala, zambiri zotsutsana pazokhudzana ndi zamatenda pazokhudzana ndi kuphatikizana kwa pharmacokinetic / pharmacodynamic zalembedwa. Kugwiritsa ntchito limodzi ndi omeprazole kapena esomeprazole kuyenera kupewedwa.