Yuav ua li cas noj (haus dej) Zilt ntsiav tshuaj

Los ntawm kev txwv txoj hlua khi ntawm ADP rau cov neeg txais nyob rau sab platelets thiab kev ua haujlwm ntawm GP IIb / IIIa complex, clopidogrel inhibits ADP-dependant platelet aggregation. Clopidogrel tseem inhibits platelet aggregation los ntawm lwm yam. Cov nyhuv ntawm clopidogrel tseem muaj nyob thoob plaws lub neej ntawm platelets.
Nrog lub sijhawm ntev ntawm kev siv clopidogrel hauv kev kho tshuaj (75 mg / hnub), qhov cim tsis pom kev ntawm platelet kev sib xyaw tshwm sim twb tau dhau ntawm 1 hnub ntawm kev kho mob, tom qab ntawd cov nyhuv antiplatelet nce thiab nce mus txog qhov siab tshaj plaws tom qab 3-7 hnub ntawm kev siv tshuaj ib txwm muaj. Nrog lub sijhawm ntev ntawm kev siv clopidogrel hauv kev kho mob ntau npaum li cas, qhov nruab nrab inhibition ntawm platelet tag nrho yog 40-60%. Tom qab cessation ntawm kev kho mob, cov nyhuv ntawm clopidogrel ntawm cov kev sib sau ua ke thiab lub sijhawm ntawm los ntshav ploj, feem ntau yog tom qab 5 hnub.
Tom qab kev tswj hwm ntawm qhov ncauj, clopidogrel tau nrawm nrawm (lub sijhawm kom mus txog qhov siab tshaj plaws ntshav ntshav yog 0.7-0.8 teev). Tom qab 2 teev, cov tshuaj tsis kuaj pom nyob hauv cov ntshav ntshav. Kev tsis suav yog kwv yees li 50% thiab nws nyob ywj pheej ntawm qhov khoom noj. Lub hauv paus tseem ceeb ntawm clopidogrel thiab nws cov metabolite tseem ceeb (feem 98 thiab 94%) thim rov qab khi rau cov protein plasma.
Clopidogrel yog ib tug prodrug. Nws yog cov tshuaj tiv thaiv hauv lub siab, cov tshuaj metabolite tseem ceeb yog tshuaj muaj yees ntawm lub cev carboxylic acid. Nws cov peev xim hauv cov ntshav cov ntshav yog 85% ntawm tag nrho cov tshuaj. Qhov siab tshaj plaws hauv kev ntsuas ntshav yog mus txog kwv yees li 1 teev tom qab kev tswj hwm. Cov nquag metabolite - thiol derivative - yog tsim los ntawm oxidation ntawm clopidogrel rau 2 - oxoclopidogrel, tom qab los ntawm hydrolysis. Qhov oxidation no tshwm sim nrog kev koom tes ntawm cytochrome P450. Qhov kev nquag metabolite no uas tuaj yeem sib txawv hauv vitro, sai thiab irreversibly khi rau platelet receptors thiab inhibits lawv cov lus sib dhos. Nws tsis pom ntawm cov ntshav cov ntshav.
Tom qab ib zaug los yog rov ua dua nrog kev tso zis, 50% yog tawm, thiab nrog quav - 46% ntawm kev muab tshuaj ntawm clopidogrel. Ib nrab-lub neej ntawm lub ntsiab metabolite tom qab ib zaug los yog rov ua kom tswj tau cov tshuaj yog 8 teev.

Kev qhia rau kev siv tshuaj Zilt

Kev tiv thaiv ntawm cov hlab plawv tshwm sim (ischemic stroke, myocardial infarction thiab mob plawv tuag) hauv cov neeg mob uas muaj kev soj ntsuam cov kab mob atherosclerosis: nrog mob ntshav ischemic (los ntawm 7 hnub txog rau 6 lub hlis), myocardial infarction (los ntawm ob peb hnub mus rau 35 hnub tom qab lub plawv nres), nyob rau hauv muaj cov kab mob ntawm cov hlab ntsha peripheral.

Kev siv cov tshuaj Zilt

Cov koob tshuaj ib txwm rau cov neeg mob laus (suav nrog cov laus) yog 1 ntsiav tshuaj (75 mg) ib hnub. Cov tshuaj muaj peev xwm siv tau tsis hais txog kev noj zaub mov noj.
Lub sijhawm tiv thaiv kev kho tsis tau tsim, tab sis kev kho mob txog 12 lub hlis yog siv, cov txiaj ntsig siab tshaj plaws tau sau tseg tom qab 3 lub hlis ntawm kev siv tshuaj.

Txoj kev siv rau Zilt hauv ntsiav tshuaj daim ntawv

Sab hauv, tsis hais txog ntawm cov zaub mov noj, ib zaug ib hnub.

Cov neeg laus thiab cov neeg laus laus uas muaj CYP2C19 isoenzyme ib txwm ua

Myocardial infarction, ischemic stroke, lossis kuaj tus mob peripheral arterial occlusion.

Zilt® tau noj ntawm ib koob tshuaj 75 mg (1 ntsiav tshuaj) ib hnub ib zaug.

Mob mob caj dab mob yam tsis muaj ST ntu nce qib (tsis khov kho lub hlwb tsis khov lossis myocardial infarction tsis muaj yoj)

Kev kho mob nrog Zilt® yuav tsum tau pib nrog ib koob tshuaj ntawm lub ntsaws tshuaj tso tawm (300 mg), thiab tom qab ntawd txuas ntxiv nrog koob tshuaj 75 mg ib hnub ib zaug (ua ke nrog acetylsalicylic acid hauv koob tshuaj 75-325 mg ib hnub). Txij li thaum siv ntau dua ntawm cov tshuaj acetylsalicylic acid yog cuam tshuam nrog kev pheej hmoo los ntshav ntau dua, cov koob tshuaj pom zoo ntawm acetylsalicylic acid yuav tsum tsis pub ntau tshaj 100 mg. Qhov txiaj ntsig zoo tshaj plaws yog pom los ntawm 3 lub hlis ntawm kev kho mob. Cov sijhawm zoo tshaj plaws ntawm kev kho rau qhov ntsuas qhov no tsis tau txiav txim siab raws cai. Cov txiaj ntsig ntawm kev tshawb fawb soj ntsuam tshawb pom qhov ua tau ntawm kev noj clopidogrel txog 12 lub hlis tom qab kev txhim kho ntawm cov kev mob caj dab tsis mob nce qib ST ntu.

Cov mob ntxim ntxaug thaum lub caij ua haujlwm nrog ST ntu ntawm qhov siab (mob myocardial infarction) nrog kev kho mob tshuaj thiab muaj peev xwm kho tus mob thombolytic, ua ke nrog acetylsalicylic acid.

Zilt® yuav tsum tau noj nyob rau hauv ib koob tshuaj 75 mg (1 ntsiav tshuaj) ib hnub ib zaug, pib nrog kev txhaj tshuaj, nyob rau hauv sib xyaw nrog acetylsalicylic acid nrog lossis tsis muaj thrombolytics. Rau cov neeg mob uas laus dua 75 xyoo, kev kho mob nrog Zilt® yuav tsum tau nqa tawm yam tsis tas yuav siv cov tshuaj thauj khoom. Txoj kev kho ua ke yog pib kom sai li sai tau tom qab pib pom cov tsos mob thiab txuas ntxiv tsawg kawg 4 lis piam. Cov txiaj ntsig ntawm kev sib xyaw ua ke nrog kev kho mob nrog clopidogrel thiab acetylsalicylic acid ntev dua 4 lub lis piam tsis tau kawm txog cov neeg mob no.

Atrial fibrillation (ua rau atrial fibrillation)

Cov tshuaj Zilt® raug xaj nyob rau hauv ib koob ntawm 75 mg ib hnub ib zaug. Ua ke nrog clopidogrel, kev kho yuav tsum tau pib thiab tom qab ntawd kev noj cov tshuaj acetylsalicylic acid ntawm koob tshuaj 75-100 mg ib hnub yuav tsum txuas ntxiv.

Yog tias tus neeg mob tsis nco qab noj ntxiv lawm:

- yog tias tsawg dua 12 teev tau dhau mus tom qab hla lub koob tshuaj tom ntej, koj yuav tsum noj tam sim ntawd ntawm lub Zilt® uas ploj lawm, thiab tom qab ntawd rov qab noj dua tom qab lub sijhawm qub,

- Yog tias ntau dua 12 teev tau dhau mus tom qab dhau qhov kev siv tshuaj ntxiv, tom qab ntawd yuav tsum tau txais qhov koob tshuaj ntxiv nyob rau hauv lub sijhawm li ib txwm, thaum koob tshuaj yuav tsum tsis txhob suav ntxiv.

Cov neeg laus thiab cov neeg laus laus uas muaj lub zog txiav txim siab txo qis CYP2C19 isoenzyme

Qhov qis qis ntawm CYP2C19 isoenzyme cuam tshuam nrog kev txo qis hauv cov nyhuv antiplatelet ntawm clopidogrel. Kev siv cov Zilt® ntawm kev txhaj tshuaj ntau dua (kev thauj khoom ntawm 600 mg, tom qab ntawd 150 mg ib zaug ib hnub) hauv cov neeg mob uas tsis tshua muaj kev ua haujlwm ntawm CYP2C19 isoenzyme ua rau muaj kev cuam tshuam ntawm cov nyhuv antiplatelet ntawm clopidogrel (saib ntu "Pharmacokinetics"). Txawm li cas los xij, hauv kev kho mob hauv tsev kho mob los kawm txog cov txiaj ntsig kev soj ntsuam, kev noj tshuaj zoo tshaj plaws ntawm clopidogrel hauv cov neeg mob uas muaj cov metabolism txo vim qhov kev txiav txim siab caj ces qis ntawm CYP2C19 isoenzyme tsis tau tsim.

Cov pab pawg neeg tshwj xeeb

Cov neeg laus cov neeg mob

Hauv cov neeg laus tuaj yeem pab dawb (tshaj li 75 xyoo), thaum piv nrog cov tub ntxhais hluas tuaj yeem pab dawb, qhov sib txawv ntawm platelet sib sau thiab lub sijhawm ua kom ntshav tsis pom. Koob tshuaj hloov kho hauv cov neeg mob laus tsis tas yuav.

Lub raum khiav tsis zoo

Tom qab rov qab siv clopidogrel ntawm ib koob tshuaj ntawm 75 mg rau ib hnub hauv cov neeg mob uas lub raum tsis zoo (CC 5-15 ml / min), qhov kev txwv ntawm ADP-vim platelet aggregation yog 25% qis dua hauv cov neeg ua haujlwm noj qab haus huv. Txawm li cas los xij, qhov kev ntsuas lub sijhawm ncua ntev ntawm lub sijhawm los ntshav zoo ib yam li cov neeg tuaj yeem noj qab haus huv uas tau txais clopidogrel ntawm ib koob tshuaj ntawm 75 mg rau ib hnub. Kev zam rau cov tshuaj tau zoo hauv txhua tus neeg mob. Lub siab ua haujlwm tsis zoo

Tom qab siv clopidogrel ntawm koob tshuaj 75 mg rau ib hnub rau 10 hnub hauv cov neeg mob uas muaj lub siab tsis ua haujlwm siab, qib siab ntawm kev txwv tsis pub ADP-ua rau platelet sib xyaw thiab qhov nruab nrab ntawm lub sijhawm los ntshav elongation piv nrog cov neeg ua haujlwm noj qab haus huv.

Qhov dav dav ntawm cov CelP2C19 isoenzyme noob caj dab sib xyaw ua ke nrog cov kab nruab nrab lossis qis dua cov kab mob sib txawv ntawm cov neeg sawv cev ntawm ntau haiv neeg / pawg neeg sib txawv (saib Pharmacogenetics subsection). Cov ntaub ntawv tsis muaj ntawv tsawg tsawg los txhawm rau ntsuas qhov tseem ceeb ntawm kev hloov kho ntawm CYP2C19 isoenzyme rau kev soj ntsuam cov txiaj ntsig rau cov neeg mob ntawm haiv neeg Mongoloid.

Thaum piv lub pharmacodynamic zog ntawm clopidogrel nyob rau hauv cov txiv neej thiab poj niam, cov poj niam pom tsawg dua qhov tsis pom kev ntawm ADP-platelet aggregation, tab sis tsis muaj qhov sib txawv ntawm lub caij nyoog ntawm lub sijhawm los ntshav. Thaum piv clopidogrel nrog acetylsalicylic acid nyob rau hauv cov neeg mob uas muaj kev pheej hmoo ntawm kev tsim ischemic cov teeb meem, qhov tshwm sim ntawm cov chaw kuaj mob tshwm sim, lwm cov kev mob tshwm sim thiab kev hloov pauv los ntawm cov cai ntawm cov chaw kuaj mob thiab kuaj pom zoo ib yam rau txiv neej thiab poj niam.

Kev phiv tshuaj ntawm Zilt tshuaj

Kev tawm tsam: mob hauv siab, qaug zog, mob asthenia.
Los ntawm lub paj hlwb tawg: mob taub hau, kiv taub hau, mob caj dab, mob plab, sawv ntshav, mob hlwb, tsis nco qab.
Los ntawm cov hlab plawv system: peripheral edema, kub siab (mob hlab ntsha tawg), lub plawv tsis ua haujlwm, tachycardia.
Los ntawm cov mob hauv plab zom mov: mob plab, dyspepsia, raws plab, xeev siab, cem quav, ntuav, pom, saj txawv, perforation ntawm mob plab, hemorrhagic gastritis, plab hnyuv los ntshav.
Ntawm ib sab ntawm daim siab thiab cov hnyuv: nce kev ua si ntawm hepatic transaminases, hyperbilirubinemia, kab mob siab, mob siab steatosis.
Los ntawm cov ntshav system: thrombocytopenia, ua haujlwm ntshav (mob qog lossis hypochromic), agranulocytosis, granulocytopenia, leukocytosis, leukopenia, neutropenia.
Los ntawm cov ntshav kev coagulation system: mob ntswg, mob plab, los ntshav, ntshav tawm hauv lub qhov muag, hemothorax, ntshav tawm los ntawm txoj hlab ntuag, hemoptysis, mob ntshav tawm ntshav, mob ntshav txhaws, ntshav tawm los ntawm qhov txhab tom qab, mob ntshav hauv lub qhov muag, hemothorax, mob ntsws, mob rau lub cev, mob ntshav txhaws, mob ntshav txhaws.
Los ntawm cov leeg musculoskeletal: rov qab mob, mob caj dab, arthrosis.
Los ntawm sab ntawm lub hauv nruab nrab hauv lub paj hlwb: kev nyuaj siab
Los ntawm lub tshuab ua pa: cov pa ntawm txoj hlab ua pa ntev, ua tsis taus pa, rhinitis, mob ntsws, mob hnoos, mob ntsws, mob ntsws.
Daim tawv nqaij sab: pob khaus, khaus, eczema, mob tawv nqaij, tawv nqaij mob tawv nqaij, ua paug rau nqaij tawv, ua pob liab liab, ua pob ua pob ua paug, ua pob ua pob.
Los ntawm cov kabmob hauv nruab nrog: cataract, mob pob txha caj dab.
Los ntawm genitourinary system: mob txeeb zig, mob cystitis, hypermenorrhea, cais tus neeg mob hemolytic uremic syndrome thiab ua mob rau lub ntsws nephropathy.
Kev tsis haum tshuaj: raug cais tawm ntawm cov kev tiv thaiv tsis haum tus mob (angioedema, bronchospasm, anaphylaxis).

Cov lus qhia tshwj xeeb rau kev siv tshuaj Zilt

Hauv cov neeg mob myocardial infarction, nws tsis pom zoo kom pib kho nrog clopidogrel hauv thawj ob peb hnub tom qab kev mob plawv. Clopidogrel tsub kom ntshav ncua ntev. Cov tshuaj yuav tsum tau siv nrog ceev faj hauv cov neeg mob uas muaj kev pheej hmoo los ntshav vim los ntawm kev raug mob, kev phais mob lossis lwm yam kev mob, nrog rau cov neeg mob uas muaj lub cev tsis tuaj yeem los ntshav (txoj hnyuv los ntshav, qhov muag pom). Clopidogrel kev kho mob yuav tsum tau tsum tsis pub tsum tsawg kawg 7 hnub ua ntej npaj kev phais mob (suav nrog cov txheej txheem kho hniav).
Cov neeg mob yuav tsum tau ceeb toom tias thaum kho nrog clopidogrel, txoj kev pheej hmoo yuav los ntshav ntau ntxiv thiab qhov uas los ntshav yuav nyob ntev dua li niaj hnub, thiab tom qab ntawd tsum tsis nthawv. Nrog rau kev txiav me me (thaum shaving) lossis lwm yam kev raug mob hauv tsev, kev ntsuas tshwj xeeb kom tsis txhob los ntshav feem ntau tsis tas yuav tsum muaj. Yog tias muaj kev raug mob loj lossis raug mob, yuav tsum tau sab laj nrog tshuaj sai.
Vim tias tsis muaj kev paub zoo nrog clopidogrel hauv cov neeg mob uas lub raum tsis ua haujlwm, ceeb toom yuav tsum tau siv thaum siv cov tshuaj.
Nrog kev ua txhaum loj ntawm daim siab ua haujlwm, kev pheej hmoo ntawm los ntshav nce ntxiv, yog li ntawd, hauv cov neeg mob no, clopidogrel yuav tsum siv nrog ceev faj.
Kev nyab xeeb thiab ua haujlwm ntawm clopidogrel hauv cov menyuam yaus thiab cov hluas hauv qab 18 xyoo tseem tsis tau tsim, vim li no, cov tshuaj tsis raug txwv rau cov neeg mob ntawm cov pab pawg hnub nyoog no.
Vim tias cov ntaub ntawv tsis, clopidogrel tsis pom zoo rau siv thaum cev xeeb tub thiab lactation.
Cov tshuaj yeeb yaj kiab tuaj yeem cuam tshuam rau lub xeev psychophysical, uas yog pom los ntawm kev saib xyuas uas tsis muaj zog, ua rau qeeb ntawm psychomotor cov kev xav thiab xav kom ceev faj thaum tsav tsheb thiab ua haujlwm nrog cov phom sij txaus ntshai.

Kev sib cuam tshuam yeeb tshuaj Zilt

Vim tias qhov pheej hmoo txaus los ntshav, tsis tas li ntawd siv clopidogrel thiab warfarin tsis pom zoo. Nrog rau kev siv clopidogrel nrog heparin lossis lwm tus neeg mob thrombolytic, kev pheej hmoo los ntshav ntau ntxiv, yog li kev siv cov tshuaj no yuav tsum ceev faj. Kev siv tib lub sijhawm ntawm clopidogrel thiab NSAIDs ua rau muaj kev pheej hmoo ntawm kev ua haujlwm thiab kev txhim kho los ntshav los ntawm qhov txhab, yog li kev siv clopidogrel nrog NSAIDs yuav tsum ceev faj.
Nrog rau kev siv clopidogrel nrog atenolol, nifedipine, digoxin, phenobarbital, cimetidine, estrogen lossis theophylline, tsis muaj kev cuam tshuam tseem ceeb hauv chaw kho mob tau sau tseg. Muaj cov pov thawj ntawm kev nyab xeeb ntawm kev siv ib txhij ntawm clopidogrel nrog phenytoin thiab tobutamide.
Antacids tsis cuam tshuam rau kev nqus ntawm clopidogrel.

Kev noj ntau tshaj ntawm cov tshuaj Zilt, cov tsos mob thiab kev kho mob

1 qhov teeb meem ntawm kev txhob txwm tshaj tawm ntawm clopidogrel tau piav qhia thaum muaj hnub nyoog 34 xyoo tus poj niam nrog kev tua tus kheej siv 1050 mg (14 ntsiav tshuaj) ntawm clopidogrel. Tsis muaj cov tsos mob ntawm kev haus ntau dhau lossis teeb meem, tsis muaj kev kho tshwj xeeb.
Tom qab tau txais kev noj qab haus huv noj qab haus huv, 600 mg ntawm clopidogrel tsis tau muaj kev mob tshwm sim (tsuas yog zam ntawm 1.7 zaug ntawm lub sijhawm los ntshav).
Tsis muaj ib qho tshuaj tua kab mob tshwj xeeb. Qhov cuam tshuam ntawm clopidogrel tuaj yeem tshem tawm los ntawm kev hloov ntshav ntawm platelet pawg.

Daim ntawv noj tshuaj:

1 cov ntsiav tshuaj coated muaj:

tus tub ntxhais: cov tshuaj nquag: clopidogrel hydrosulfate 97.875 mg, suav raws li clopidogrel 75,000 mg, zam txim: lactose, anhydrous 108.125 mg, microcrystalline cellulose 30.00 mg, pregelatinized hmoov txhuv nplej 12.00 mg, macrogol 6000 8.00 mg, roj castor, hydrogenated 4.00 mg,

plhaub: hypromellose 6av 5.60 mg, titanium dioxide (E171) 1.46 mg, talc 0.50 mg, zas hlau oxide liab (E 172) 0.04 mg, propylene glycol 0.40 mg.

Hloov, me ntsis biconvex ntsiav tshuaj, coated nrog cov xim zaj duab xis txheej.

* Kev txiav kab-kev hla: qhov xim dawb los yog yuav luag dawb ntxhib nrog xim zaj duab xis sheath.

Kws tshuaj:

Clopidogrel yog prodrug, ib qho ntawm cov tshwj xeeb metabolites ntawm uas yog ib qho inhibitor ntawm platelet aggregation. Lub cev zom zaws metabolite ntawm clopidogrel xaiv kev tiv thaiv kev khi
adenosine diphosphate (ADP) nrog P2YI2 platelet receptors thiab tom qab ADP-mediated kev ua haujlwm ntawm glycoprotein GPIIb / IIIa complex, uas ua rau cov inhibition ntawm platelet sib txuas.

Kev tsuj ntawm cov platelet sib sau ua ke yog qhov tsis hloov thiab txuas ntxiv thoob plaws tag nrho lub neej ntawm cov hlwb (kwv yees li 7-10 hnub), yog li ntawd, tus nqi ntawm kev rov ua haujlwm ntawm platelet muaj nuj nqi sib luag nrog tus nqi ntawm lawv daim ntawv rov ntxiv. Platelet kev sib cais tsim los ntawm agonists dua li ADP kuj tseem raug txwv vim qhov kev thaiv ntawm cov platelet ua kom muaj zog los ntawm ADP.

Kev nquag metabolite yog tsim los ntawm kev ua ntawm CYP450 isoenzymes, qee qhov yuav txawv hauv polymorphism lossis yuav tiv thaiv tau los ntawm lwm cov tshuaj, yog li ntawd, tsis yog txhua tus neeg mob muaj kev txwv txaus ntawm platelet aggregation.

Hauv kev kho mob nrog clopidogrel ntawm koob tshuaj 75 mg rau ib hnub los ntawm thawj hnub ntawm kev kho, muaj qhov tseem ceeb ntawm ADP-ntxias cov platelet sib xyaw, uas maj mam nce dhau 3-7 hnub thiab tom qab ntawd mus txog qhov theem tsis tu ncua (thaum nce mus txog qhov sib npaug). Hauv lub xeev qhov sib npaug, cov neeg kawm ntawv ntawm kev txwv tsis pub platelet sib xyaw thaum siv clopidogrel ntawm koob tshuaj 75 mg rau ib hnub, qhov nruab nrab, thaj tsam li 40% txog 60%. Tom qab siv ceev xwmphem clopidogrel, platelet sib sau thiab lub sijhawm los ntshav maj mam rov qab los rau lawv thawj qhov tseem ceeb, qhov nruab nrab, dhau 5 hnub.
Clopidogrel tuaj yeem tiv thaiv kev txhim kho atherothrombotic cov teeb meem hauv cov neeg mob nrog atherosclerotic vascular txhab ntawm txhua qhov chaw, tshwj xeeb tshaj yog cov uas muaj hlwb, mob hlab ntshav tes lossis hlab ntsha txhaws.

Kws tshuaj:

Tom qab ib zaug thiab rov ua dua qhov ncauj ntawm kev noj tshuaj ntawm 75 koob tshuaj rau ib hnub
clopidogrel tso tawm sai heev. Cov nqi nruab nrab ntawm qhov siab tshaj plaws (Cmah) kev hloov pauv clopidogrel hauv cov ntshav plasma (2.2-2.5 ng / ml tom qab noj ib koob ntawm 75 mg) tau tiav tom qab 45 feeb. Raws li kev tshawb nrhiav ntawm lub raum tsis tuaj yeem ua tiav ntawm clopidogrel metabolites, cov neeg nqus tau yog kwv yees li 50%.

Clopidogrel thiab nws lub ntsiab tsis tseem ceeb metabolite ncig hauv cov ntshav ntshav reversibly khi rau tib neeg cov ntshav protein nyob hauv cov xwm txheej hauv vitro (98% thiab 94%, feem). Qhov kev sib khi no yog qhov tsis tau txais nyob rau ntau qhov ntau.

Clopidogrel nquag plias hauv daim siab. Hauv cov xwm txheej hauv vitro thiab hauv vivo
clopidogrel yog metabolized nyob rau hauv ob txoj kev: thawj zaug yog kho kom haum xeeb los ntawm esterases thiab ua rau hydrolysis nrog kev tsim cov tshuaj tiv thaiv metabolite - lub zog ntawm carboxylic acid (85% ntawm circulating metabolites), thiab lwm yam yog catalyzed los ntawm ntau isoenzymes ntawm cytochrome P450. Thaum hauv paus
clopidogrel yog hloov mus rau qhov nruab nrab ntawm cov tshuaj metabolite - 2-oxo-clopidogrel. Cov metabolism tom qab ntawm 2-oxo-clopidogrel ua rau kev tsim cov kev siv dag zog ntawm clopidogrel - thiol derivative ntawm clopidogrel. Hauv vitro, txoj hauv kev no tau sib kho los ntawm isoenzymes CYP3A4, CYP2C19, CYP1A2 thiab CYP2B6. Nquag thiol metabolite ntawm clopidogrel cais raws li cov xwm txheej hauv vitro, sai thiab irreversibly cuam tshuam nrog platelet receptors, thaiv lawv cov kev sib sau.

Nrogmah cov nquag metabolite hauv cov ntshav ntshav tom qab noj cov tshuaj thawb tawm (300 mg) ntawm clopidogrel yog ob zaug ntau dua Cmah tom qab 4 hnub ntawm kev siv clopidogrel hauv kev tswj kev noj tshuaj (75 mg / hnub). Nrogmah hauv cov ntshav ntshav yog tiav kwv yees li 30-60 feeb tom qab siv cov tshuaj.

Tom qab kev noj ntawm 14 C-daim ntawv lo clopidogrel, kwv yees li 50% ntawm tag nrho cov tshuaj xov hluav taws xob ua rau lub raum thiab kwv yees li 46% los ntawm txoj hnyuv hauv 120 teev tom qab noj tshuaj. Tom qab ib qho kev noj tshuaj ntawm qhov ncauj ntawm clopidogrel ntawm ib koob ntawm 75 mg, ib nrab-lub neej (T1/2) yog kwv yees li 6 teev. T1/2 lub ntsiab tsis muaj zog metabolite ncig hauv cov ntshav ntshav tom qab ib zaug thiab siv tas li yog 8 teev.

Lub isoenzyme CYP2C19 koom nrog kev tsim ob qho tib si ntawm kev siv hluav taws xob thiab qhov nruab nrab ntawm lub cev (metabolite) - 2-oxo-clopidogrel. Cov tshuaj pharmacokinetics thiab antiplatelet nyhuv ntawm lub nquag clopidogrel metabolite, nrog rau cov txiaj ntsig ntawm kev soj ntsuam ntawm platelet kev sib xyaw hauv qab vivo tej yam kev mob, txawv nyob ntawm lub cim ntawm CYP2C19 isoenzyme.

The allele ntawm CYP2C19 * 1 isoenzyme noob sib raug zoo rau cov khoom siv roj ntsha ua haujlwm, thaum lub sijhawm tagnrho ntawm CYP2C19 * 2 thiab CYP2C19 * 3 isoenzyme noob tsis ua haujlwm. Alleles ntawm CYP2C19 * 2 thiab CYP2C19 * 3 isoenzyme noob yog lub luag haujlwm rau kev txo qis hauv cov metabolism hauv feem ntau cov neeg sawv cev ntawm Caucasoid (85%) thiab Mongoloid (99%) haiv neeg. Lwm qhov chaw sib koom ua ke nrog qhov tsis txaus los yog txo qis hauv cov metabolism yog qhov tsawg dua thiab suav nrog, tab sis tsis tas rau, cov kab mob ntawm CYP2C19 * 4, * 5, * 6, * 7 thiab * 8 isoenzyme noob.

Cov neeg mob uas tsis tshua muaj CYP2C19 isoenzyme kev ua si yuav tsum muaj ob qho kev ua haujlwm tau hais los saum toj no nrog kev ploj haujlwm. Raws li kev tshawb fawb luam tawm, ntau zaus ntawm genotypes nrog kev ua haujlwm tsawg ntawm CYP2C19 isoenzyme, nrog rau kev txo qis hauv cov metabolism, yog kwv yees li 2% hauv cov neeg sawv cev ntawm Caucasoid haiv neeg, 4% hauv cov neeg ntawm cov haiv neeg Negroid thiab 14% hauv cov neeg ntawm haiv neeg Mongoloid. Muaj kev ntsuam xyuas los txiav txim rau lub caj dab ntawm CYP2C19 isoenzyme. Raws li kev tshawb nrhiav thiab meta-tsom xam, uas suav nrog cov neeg muaj ntau, siab, nruab nrab thiab qis kev ua haujlwm ntawm CYP2C19 isoenzyme, qhov sib txawv ntawm kev cuam tshuam ntawm cov nquag metabolite thiab qhov nruab nrab ntawm kev tsis sib xyaw ntawm ADP-ntxias platelet aggregation hauv cov neeg ua haujlwm pab dawb nrog qhov siab, siab thiab nruab nrab isoenzyme kev ua si. CYP2C19 tsis tuaj. Hauv cov neeg ua haujlwm pab dawb uas tsis tshua muaj isoenzyme, qhov kev cuam tshuam ntawm cov metabolite nquag txo qis piv rau cov neeg tuaj yeem nrog cov kev ua haujlwm siab ntawm isoenzyme CYP2C19.

Thaum siv clopidogrel nyob rau hauv koob tshuaj 600 mg, lub chaw thau khoom koob / 150 mg txij nkawm koob tshuaj (600 mg / 150 mg) hauv cov neeg mob uas muaj cov metabolism tsawg, kev sib kis ntawm cov tshuaj tiv thaiv metabolite tau siab dua nrog kev kho 300 mg / 75 mg kev kho mob. Tsis tas li ntawd, cov neeg kawm ntawv qib siab ntawm kev txwv tsis pub platelet tau zoo ib yam li cov pawg hauv cov neeg mob uas muaj kev ua haujlwm siab ntawm CYP2C19 isoenzyme tau txais
clopidogrel raws li cov txheej txheem ntawm 300 mg / 75 mg. Txawm li cas los xij, kev noj tshuaj ntau npaum li cas ntawm clopidogrel hauv ib pawg ntawm cov neeg mob uas tsis tshua muaj kev ua haujlwm ntawm CYP2C19 isoenzyme tsis tau txiav txim siab hauv kev tshawb fawb uas cuam tshuam nrog kev kawm txog kev soj ntsuam. Kev soj ntsuam sim ua rau hnub tim muaj tsis txaus coj mus kuaj kom pom qhov sib txawv hauv cov chaw kho mob hauv cov neeg mob uas tsis muaj CYP2C19 isoenzyme kev ua ub no.

Pharmacokinetics ntawm cov neeg mob tshwj xeeb

Lub pharmacokinetics ntawm lub cev sib xyaw ua ke ntawm clopidogrel hauv cov pab pawg tshwj xeeb ntawm cov neeg mob (cov neeg laus laus, cov menyuam yaus, cov neeg mob tsis zoo lub raum thiab hepatic muaj nuj nqi) tsis tau kawm.

Cov neeg laus cov neeg mob

Hauv cov neeg laus tuaj yeem pab dawb (tshaj li 75 xyoo), thaum piv nrog cov tub ntxhais hluas tuaj yeem pab dawb, qhov sib txawv ntawm platelet sib sau thiab lub sijhawm ua kom ntshav tsis pom. Koob tshuaj hloov kho hauv cov neeg mob laus tsis tas yuav.

Lub raum khiav tsis zoo

Tom qab rov qab siv clopidogrel ntawm ib koob tshuaj ntawm 75 mg rau ib hnub hauv cov neeg mob uas lub raum tsis zoo (CC 5-15 ml / min), qhov kev txwv ntawm ADP-vim platelet aggregation yog 25% qis dua hauv cov neeg ua haujlwm noj qab haus huv. Txawm li cas los xij, cov neeg kawm tiav qib ntev los ntshav lub sijhawm zoo ib yam li cov neeg tuaj yeem noj qab haus huv tau txais
clopidogrel ntawm koob tshuaj 75 mg rau ib hnub.

Lub siab ua haujlwm tsis zoo

Tom qab siv clopidogrel ntawm koob tshuaj 75 mg rau ib hnub rau 10 hnub hauv cov neeg mob uas muaj lub siab tsis ua haujlwm siab, qib siab ntawm kev txwv tsis pub ADP-ua rau platelet sib xyaw thiab qhov nruab nrab ntawm lub sijhawm los ntshav elongation piv nrog cov neeg ua haujlwm noj qab haus huv.

Qhov dav dav ntawm cov CelP2C19 isoenzyme noob caj dab sib xyaw ua ke nrog cov kab nruab nrab lossis qis dua cov kab mob sib txawv ntawm cov neeg sawv cev ntawm ntau haiv neeg / pawg neeg sib txawv (saib Pharmacogenetics subsection). Cov ntaub ntawv tsis muaj ntawv tsawg tsawg los txhawm rau ntsuas qhov tseem ceeb ntawm kev hloov kho ntawm CYP2C19 isoenzyme rau kev soj ntsuam cov txiaj ntsig rau cov neeg mob ntawm haiv neeg Mongoloid.

Cov Yuav Tsum Muaj

- Ua haujlwm siab rau clopidogrel lossis lwm tus ua rau muaj tshuaj,

- Kev mob siab ua rau mob siab,

- mob ntshav qis, xws li los ntshav los ntawm mob tawm ntawm plab lossis tso ntshav khov,

- lactase deficiency, lactose intolerance, qabzib-galactose malabsorption syndrome,

- cev xeeb tub thiab lub sijhawm pub mis niam,

- Cov menyuam yaus hnub nyoog qis dua 18 xyoo (tsis muaj kev nyab xeeb thiab ua tau zoo).

Nrog saib xyuas:

- Qog ua haujlwm hauv lub siab tsis zoo nrog lub siab xav kom los ntshav (kev paub tsawg)

- Lub raum khiav tsis zoo (muaj kev paub tsawg)

- pathological tej yam kev mob uas ua rau muaj feem los ntshav (nrog rau kev raug mob, kev phais mob (saib ntu "Cov lus qhia tshwj xeeb")),

- kab mob nyob rau hauv uas muaj ib tug predisposition rau kev loj hlob ntawm los ntshav (tshwj xeeb tshaj yog gastrointestinal thiab intraocular),

- tib lub sijhawm siv nrog cov tshuaj tsis muaj tshuaj steroidal (NSAIDs), suav nrog cyclooxygenase-2 inhibitors (COX-2),

- tib lub sijhawm siv cov tshuaj warfarin, heparin lossis glycoprotein IIb / IIIa inhibitors,

- cov neeg mob uas tsis tshua muaj kev ua haujlwm ntawm CYP2C19 isoenzyme (thaum siv clopidogrel hauv kev txhaj tshuaj pom zoo, kev tsis tshua muaj metabolite ntawm clopidogrel tau tsim thiab nws cov nyhuv antiplatelet tsawg dua, yog li ntawd, thaum siv clopidogrel hauv kev pom zoo rau cov mob txha caj qaum los yog kev cuam tshuam ntawm cov hlab ntshav txhaws, yuav muaj lub plawv dhia. ntau dua nyob hauv cov neeg mob uas muaj kev ua haujlwm ntawm isoenzyme CYP2C19),

muaj qhov tsis haum rau lwm thienopyridines (piv txwv li
ticlopidine, prasugrel) (saib ntu "Cov lus qhia tshwj xeeb").

Cev xeeb tub thiab lactation:

Txij li thaum tsis muaj cov ntaub ntawv tshawb fawb txog kev siv clopidogrel thaum cev xeeb tub, cov tshuaj tsis pom zoo rau siv thaum cev xeeb tub. Cov kev tshawb fawb tsiaj tsis tau qhia tawm qhov cuam tshuam ncaj qha los yog tsis ncaj rau kev xeeb tub, kev loj hlob ntawm cov embryo / fetus, chav kawm ntawm kev mob plab lossis yug menyuam tom qab.

Cov kev tshawb fawb tsiaj pom tau hais tias
clopidogrel thiab / lossis nws cov khoom noj ua ke tau tawm hauv cov kua mis. Yog li ntawd, yog tias tsim nyog, txoj kev kho
clopidogrel om pom zoo kom tsis txhob pub mis niam.

Tsuas tshuaj thiab tswj hwm

Sab hauv, tsis hais txog ntawm cov zaub mov noj, ib zaug ib hnub.

Cov neeg laus thiab cov neeg laus laus uas muaj CYP2C19 isoenzyme ib txwm ua

Myocardial infarction, ischemic stroke, lossis kuaj tus mob peripheral arterial occlusion.

Zilt® tau noj ntawm ib koob tshuaj 75 mg (1 ntsiav tshuaj) ib hnub ib zaug.

Mob mob caj dab mob yam tsis muaj ST ntu nce qib (tsis khov kho lub hlwb tsis khov lossis myocardial infarction tsis muaj yoj)

Kev kho mob nrog Zilt® yuav tsum tau pib nrog ib koob tshuaj ntawm lub ntsaws tshuaj tso tawm (300 mg), thiab tom qab ntawd txuas ntxiv nrog koob tshuaj 75 mg ib hnub ib zaug (ua ke nrog acetylsalicylic acid hauv koob tshuaj 75-325 mg ib hnub). Txij li thaum siv ntau dua ntawm cov tshuaj acetylsalicylic acid yog cuam tshuam nrog kev pheej hmoo los ntshav ntau dua, cov koob tshuaj pom zoo ntawm acetylsalicylic acid yuav tsum tsis pub ntau tshaj 100 mg. Qhov txiaj ntsig zoo tshaj plaws yog pom los ntawm 3 lub hlis ntawm kev kho mob. Cov sijhawm zoo tshaj plaws ntawm kev kho rau qhov ntsuas qhov no tsis tau txiav txim siab raws cai. Cov txiaj ntsig ntawm kev tshawb fawb soj ntsuam tshawb pom qhov ua tau ntawm kev noj clopidogrel txog 12 lub hlis tom qab kev txhim kho ntawm cov kev mob caj dab tsis mob nce qib ST ntu.

Cov mob ntxim ntxaug thaum lub caij ua haujlwm nrog ST ntu ntawm qhov siab (mob myocardial infarction) nrog kev kho mob tshuaj thiab muaj peev xwm kho tus mob thombolytic, ua ke nrog acetylsalicylic acid.

Zilt® yuav tsum tau noj nyob rau hauv ib koob tshuaj 75 mg (1 ntsiav tshuaj) ib hnub ib zaug, pib nrog kev txhaj tshuaj, nyob rau hauv sib xyaw nrog acetylsalicylic acid nrog lossis tsis muaj thrombolytics. Rau cov neeg mob uas laus dua 75 xyoo, kev kho mob nrog Zilt® yuav tsum tau nqa tawm yam tsis tas yuav siv cov tshuaj thauj khoom. Txoj kev kho ua ke yog pib kom sai li sai tau tom qab pib pom cov tsos mob thiab txuas ntxiv tsawg kawg 4 lis piam. Cov txiaj ntsig ntawm kev sib xyaw ua ke nrog kev kho mob nrog clopidogrel thiab acetylsalicylic acid ntev dua 4 lub lis piam tsis tau kawm txog cov neeg mob no.

Atrial fibrillation (ua rau atrial fibrillation)

Cov tshuaj Zilt® raug xaj nyob rau hauv ib koob ntawm 75 mg ib hnub ib zaug. Ua ke nrog clopidogrel, kev kho yuav tsum tau pib thiab tom qab ntawd kev noj cov tshuaj acetylsalicylic acid ntawm koob tshuaj 75-100 mg ib hnub yuav tsum txuas ntxiv.

Yog tias tus neeg mob tsis nco qab noj ntxiv lawm:

- yog tias tsawg dua 12 teev tau dhau mus tom qab hla lub koob tshuaj tom ntej, koj yuav tsum noj tam sim ntawd ntawm lub Zilt® uas ploj lawm, thiab tom qab ntawd rov qab noj dua tom qab lub sijhawm qub,

- Yog tias ntau dua 12 teev tau dhau mus tom qab dhau qhov kev siv tshuaj ntxiv, tom qab ntawd yuav tsum tau txais qhov koob tshuaj ntxiv nyob rau hauv lub sijhawm li ib txwm, thaum koob tshuaj yuav tsum tsis txhob suav ntxiv.

Cov neeg laus thiab cov neeg laus laus uas muaj lub zog txiav txim siab txo qis CYP2C19 isoenzyme

Qhov qis qis ntawm CYP2C19 isoenzyme cuam tshuam nrog kev txo qis hauv cov nyhuv antiplatelet ntawm clopidogrel. Kev siv cov Zilt® ntawm kev txhaj tshuaj ntau dua (kev thauj khoom ntawm 600 mg, tom qab ntawd 150 mg ib zaug ib hnub) hauv cov neeg mob uas tsis tshua muaj kev ua haujlwm ntawm CYP2C19 isoenzyme ua rau muaj kev cuam tshuam ntawm cov nyhuv antiplatelet ntawm clopidogrel (saib ntu "Pharmacokinetics"). Txawm li cas los xij, hauv kev kho mob hauv tsev kho mob los kawm txog cov txiaj ntsig kev soj ntsuam, kev noj tshuaj zoo tshaj plaws ntawm clopidogrel hauv cov neeg mob uas muaj cov metabolism txo vim qhov kev txiav txim siab caj ces qis ntawm CYP2C19 isoenzyme tsis tau tsim.

Cov pab pawg neeg tshwj xeeb

Cov neeg laus cov neeg mob

Hauv cov neeg laus tuaj yeem pab dawb (tshaj li 75 xyoo), thaum piv nrog cov tub ntxhais hluas tuaj yeem pab dawb, qhov sib txawv ntawm platelet sib sau thiab lub sijhawm ua kom ntshav tsis pom. Koob tshuaj hloov kho hauv cov neeg mob laus tsis tas yuav.

Lub raum khiav tsis zoo

Tom qab rov qab siv clopidogrel ntawm ib koob tshuaj ntawm 75 mg rau ib hnub hauv cov neeg mob uas lub raum tsis zoo (CC 5-15 ml / min), qhov kev txwv ntawm ADP-vim platelet aggregation yog 25% qis dua hauv cov neeg ua haujlwm noj qab haus huv. Txawm li cas los xij, cov neeg kawm tiav qib ntev los ntshav lub sijhawm zoo ib yam li cov neeg tuaj yeem noj qab haus huv tau txais
clopidogrel ntawm koob tshuaj 75 mg rau ib hnub. Kev zam rau cov tshuaj tau zoo hauv txhua tus neeg mob. Lub siab ua haujlwm tsis zoo

Tom qab siv clopidogrel ntawm koob tshuaj 75 mg rau ib hnub rau 10 hnub hauv cov neeg mob uas muaj lub siab tsis ua haujlwm siab, qib siab ntawm kev txwv tsis pub ADP-ua rau platelet sib xyaw thiab qhov nruab nrab ntawm lub sijhawm los ntshav elongation piv nrog cov neeg ua haujlwm noj qab haus huv.

Qhov dav dav ntawm cov CelP2C19 isoenzyme noob caj dab sib xyaw ua ke nrog cov kab nruab nrab lossis qis dua cov kab mob sib txawv ntawm cov neeg sawv cev ntawm ntau haiv neeg / pawg neeg sib txawv (saib Pharmacogenetics subsection). Cov ntaub ntawv tsis muaj ntawv tsawg tsawg los txhawm rau ntsuas qhov tseem ceeb ntawm kev hloov kho ntawm CYP2C19 isoenzyme rau kev soj ntsuam cov txiaj ntsig rau cov neeg mob ntawm haiv neeg Mongoloid.

Thaum piv lub pharmacodynamic zog ntawm clopidogrel nyob rau hauv cov txiv neej thiab poj niam, cov poj niam pom tsawg dua qhov tsis pom kev ntawm ADP-platelet aggregation, tab sis tsis muaj qhov sib txawv ntawm lub caij nyoog ntawm lub sijhawm los ntshav. Thaum piv clopidogrel nrog acetylsalicylic acid nyob rau hauv cov neeg mob uas muaj kev pheej hmoo ntawm kev tsim ischemic cov teeb meem, qhov tshwm sim ntawm cov chaw kuaj mob tshwm sim, lwm cov kev mob tshwm sim thiab kev hloov pauv los ntawm cov cai ntawm cov chaw kuaj mob thiab kuaj pom zoo ib yam rau txiv neej thiab poj niam.

Sab sij huam

Kev nyab xeeb ntawm clopidogrel tau tshawb pom hauv cov neeg mob uas tau txais kev kho clopidogrel rau 1 xyoo lossis ntau dua. Kev nyab xeeb ntawm clopidogrel ntawm koob tshuaj 75 mg rau ib hnub tau muab piv rau cov acetylsalicylic acid ntawm ib koob ntawm 325 mg rau ib hnub, tsis hais hnub nyoog li cas, poj niam txiv neej thiab haiv neeg. Cov kev tshwm sim tsis zoo uas tau pom hauv kev kuaj mob hauv qab no tau teev tseg hauv qab no. Ntxiv rau, cov lus ceeb toom tshwm sim ntawm qhov tshwm sim tsis zoo yog qhia.

Hauv cov kev tshawb fawb soj ntsuam thiab tom qab kev soj ntsuam ntawm clopidogrel, kev txhim kho los ntshav feem ntau tau tshaj tawm, feem ntau thaum thawj lub hli ntawm kev kho.

Kev faib tawm ntawm qhov tshwm sim ntawm cov kev mob tshwm sim ntawm Lub Koom Haum Ntiaj Teb Kev Noj Qab Haus Huv (WHO): feem ntau? 1/10, feem ntau los ntawm 1/ 1/100 txog 1/10000

Tso tawm daim ntawv thiab muaj pes tsawg leeg

Daim ntawv txiav tshuaj - cov yeeb yaj kiab-cov ntsiav tshuaj: puag ncig, me ntsis biconvex, paj yeeb, cov ntsiav tshuaj tub ntxhais muaj qhov xim dawb los yog yuav luag tsis muaj xim tawv (7 hauv cov hlwv, hauv pob ntawv los ntawm 2, 4 lossis 12 hlwv).

Cov tshuaj phiv yog clopidogrel hydrosulfate, hauv 1 ntsiav tshuaj - 97.875 mg, lossis clopidogrel - 75 mg.

Ntu cov khoom siv: microcrystalline cellulose, anhydrous lactose, pregelatinized starch, hydrogenated castor roj, macrogol 6000.

Cov sib xyaw ua ke ntawm cov zaj duab xis plhaub: propylene glycol, hypromellose 6cp, talc, titanium dioxide (E171), zas hlau oxide liab (E172).

Chaw tsim tshuaj paus thiab nqe

Lub tuam txhab kws kho mob koom nrog kev tsim cov tshuaj Zilt hauv tebchaws Russia KRKA. Tsis tas li, ntawm kev lag luam hauv tsev neeg, qee zaum koj tuaj yeem nrhiav pom ib qho tshuaj txawv teb tuaj ntawm Slovenia.

Nws yog "Zilt", hmoov tsis, tsis tshua kim. Tus nqi ntawm cov tshuaj no nyob ntawm, ua ntej ntawm txhua tus, ntawm tus naj npawb ntawm cov hlwv ntim hauv ib lub thawv. Piv txwv li, 14 ntsiav tshuaj ntawm cov khoom no raug nqi li 500-600 r, nyob ntawm tus xa khoom. Rau 12 lub blisters, koj yuav tsum them ntau dua 2000 p. Txawm li cas los xij, cov tshuaj no tau faib rau hauv cov khw muag tshuaj nkaus xwb los ntawm cov tshuaj noj.

Pharmacological kev txiav txim

Hauv qhov chaw vascular puas tsuaj hauv tib neeg lub cev, platelets ib txwm pib sib zog. Nyob rau tib lub sijhawm, lawv lo ua ke nrog txhua tus thiab ua raws li cov ntaub so ntswg. Tus txheej txheem no xaus rau qhov tsim ntawm ntshav txhaws.

Cov tshuaj "Zilt", cov lus qhia rau kev siv uas yooj yim heev, pib ua qhov zoo rau tus neeg mob tau nrawm dua - txog 30 feeb tom qab kev tswj hwm. Thaum nws nkag mus rau hauv tib neeg lub cev, kev txwv tsis pub platelet tshwm sim. Nrog kev siv cov tshuaj no tsis tu ncua tom qab txog 4-7 hnub, qhov siab tshaj plaws kho tau tshwm sim.

Qhov siab tshaj plaws ntawm cov tshuaj no hauv lub cev tshwm sim ob peb teev tom qab kev tswj hwm. Ntxiv mus, nws cov ntsiab lus hauv cov ntshav txawm tias lub sijhawm no feem ntau tsis tshua muaj.

Cov tshuaj no tawm ntawm lub cev los ntawm ob lub raum thiab txoj hnyuv. Ib nrab-lub neej tom qab siv ib zaug xwb yog kwv yees li 6-8 teev.

Cov tshuaj "Zilt": cov lus qhia rau kev siv

Cov tshuaj no yog muaj, raws li twb tau hais, tsuas yog nyob rau hauv daim ntawv ntawm cov ntsiav tshuaj. Raws li, lawv coj nws tsuas yog hais lus. Haus cov ntsiav tshuaj 75 mg "Zilt" cov lus qhia rau kev siv tso cai ob qho ua ntej noj mov, thiab tom qab lossis thaum nws. Cov hau kev ntawm kev noj cov tshuaj no nyob ntawm seb tus mob tshwj xeeb.

Ib tus neeg mob uas muaj myocardial infarction feem ntau yog hais kom noj ib ntsiav tshuaj 75 mg ib hnub twg. Kev muab tshuaj rau tib cov tshuaj rau cov neeg mob ischemic cerebrovascular kev sib tsoo thiab cov leeg ntshav occlusion. Hauv qhov no, rau cov neeg mob myocardial infarction, cov tshuaj no tuaj yeem raug kho nyob rau lub sijhawm 1 txog 35 hnub ntawm kev txhim kho kabmob. Cov neeg mob uas muaj ischemic stroke "Zilt" feem ntau yog tsim los ntawm 7 hnub mus rau rau lub hlis.

Hauv kev mob plawv nrog cov leeg hauv ntu ntshav ST, qhov tshuaj no kuj tau sau tseg hauv 75 mg rau ib hnub. Tab sis nyob rau hauv cov ntaub ntawv no, tus neeg mob yav dhau los yuav siv ib zaug coj mus txhaj rau cov tshuaj aspirin thiab thrombolytics.

Hauv cov roj ntsha ntawm lub cev tsis muaj qhov siab ST, kev siv tshuaj kho mob txawv me ntsis. Hauv qhov no, cov tshuaj feem ntau npaum li cas raws li hauv qab no:

haus ib qho chaw thau khoom ntawm 300 mg ib zaug

noj cov tshuaj txhua hnub ntawm 1 ntsiav tshuaj hauv ib hnub.

Ntxiv mus, kev sib xyaw nrog kev noj tshuaj nrog cov tshuaj aspirin hauv qhov ntau npaum li 75-325 mg, koob tshuaj txhua hnub ntawm Zilt yuav tsum yog 100 mg. Nrog txoj kev tswj hwm no, cov txiaj ntsig siab tshaj plaws hauv cov neeg mob yog feem ntau pom tom qab peb lub hlis. Lub chav ntawm kev kho mob feem ntau yog 12 lub hlis.

Kev kho zoo li no tau teev tseg hauv feem ntau tsuas yog rau cov neeg mob laus hauv qab lub hnub nyoog 75 xyoo.

Cov lus qhia rau kev siv tshuaj "Zilt": contraindications

Cov tub ntxhais hluas hnub nyoog qis dua 18 xyoo "Zilt" rau kev tiv thaiv tus mob thrombosis tsis tau sau tseg. Nws kuj tseem tsis pom zoo kom noj cov tshuaj no rau lactating thiab cov poj niam cev xeeb tub. Clopidogrel tuaj yeem txeem tau, suav nrog, mus rau hauv niam mis.

Yog lawm, koj tsis tuaj yeem siv cov tshuaj no thiab cov neeg uas tuaj yeem tsim kev fab tshuaj rau ib qho ntawm cov khoom siv. Puas yog qhov tsis haum rau siv "Zilt":

Raws li cov lus qhia rau kev siv, "Zilt" yuav tsum tau ua nrog ceev faj thaum muaj teeb meem xws li:

hypersensitivity rau thienopyridines,

qis kev ua haujlwm ntawm CYP2C19,

lub siab thiab lub raum khiav tsis zoo,

kab mob nyob rau hauv uas los ntshav yog ua tau,

phais kev phais thiab raug mob uas tuaj yeem ua rau ntshav tsis los ntshav.

Kev sib txuam

Ib qho ntxiv, nrog ceev faj yuav tsum ua, raws li cov lus qhia rau kev siv, "Zilt" 75 mg ib txhij nrog rau cov kev txhais tau tias:

Tib yam siv rau cov kev kho mob nyuaj nrog Zilt thiab tshuaj tsis-steroidal anti-inflammatory tshuaj.

Cov txiaj ntsig ntawm kev noj cov tshuaj no tuaj yeem txo qis yog tias tus neeg mob tau txais kev kho mob siv:

"Ticlopidine" thiab qee yam tshuaj ntxiv.

Dab tsi cov neeg mob yuav tsum paub

Cov neeg mob uas tau noj Zilt yuav tsum ua raws li cov lus qhia hauv qab no:

cov xwm txheej txawv txav txawv hauv cheeb tsam lossis lub sijhawm los ntshav yuav tsum qhia rau tus kws kho mob,

cov kws kho kaus hniav thiab kws phais mob yuav tsum raug ceeb toom txog chav kho mob nrog Zilt yog lawv tau ntsib.

Yam tshwm sim yuav tshwm sim

Zoo li lwm yam tshuaj, Zilt tuaj yeem muaj kev cuam tshuam tsis zoo rau tus neeg mob lub cev. Feem ntau, thaum huas chav kawm siv cov tshuaj no, cov kev mob tshwm sim hauv qab no raug pom nyob hauv cov neeg mob:

mob plab thiab raws plab,

Qee zaum, cov uas noj cov tshuaj no kuj tuaj yeem ua rau lawv tus kheej pom:

khaus lossis purpura

hemorrhages nyob rau hauv lub qhov muag,

Hauv kev kuaj ntshav hauv lub chaw kuaj ntshav, qee zaum muaj cov platelets thiab neutrophils txo qis hauv qee cov neeg mob.

Muaj, yog li ntawd, qee qhov kev phiv rau cov tshuaj no. Yog li no, cov lus qhia rau kev siv "Zilt" 75 mg yuav tsum tau pom zoo yam tsis poob. Kev noj tshuaj ntau dhau ntawm cov tshuaj no, tsis tuaj yeem zam tsis tau. Yog tias tus neeg mob nco qab hnov ​​qab noj ib hnub ib hnub, haus ib qho tshuaj noj ob hnub txuas rau hnub tom qab tsis pom zoo rau qee kis.

Raws li cov lus qhia rau kev siv, Zilt ntsiav tshuaj, zoo li lwm qhov, yuav tsum tsis txhob haus cawv yog tias koj muaj kev fab tshuaj rau ib qho ntawm lawv cov khoom. Cov kev xav zoo li no thaum siv cov tshuaj no tsis tshua muaj. Tab sis qee zaum kev fab tshuaj rau cov neeg mob raug kho siv cov tshuaj no tseem tuaj yeem pom. Cov kev nquag tshwm sim feem ntau yog:

kev tso ntshav tawm thienopyridines.

Dab tsi yog qhov ua txhaum cai dhau

Siv cov tshuaj nrog kev ua txhaum cov lus qhia rau kev siv "Zilt" ua rau qhov tshwm sim ntawm cov teeb meem zoo li no:

los ntshav ntawm qhov sib txawv,

ntxiv sijhawm ntawm los ntshav.

Kev kho mob overdoses nrog cov tshuaj no yog cov tsos mob. Cov neeg mob feem ntau yog txhab nrog platelet pawg.

Analogues ntawm cov tshuaj

Nws raug nqi "Zilt", raws li twb tau hais los, nws kim heev. Yog li, ntau tus neeg mob, yog lawm, xav paub txog dab tsi cov tshuaj pheej yig dua tuaj yeem hloov cov tshuaj no yog tias tsim nyog.

Txhais ntawm cov tshuaj "Zilt" yog, piv txwv li:

Tag nrho cov nyiaj no hauv lawv cov kev sib xyaw muaj cov tshuaj qub zoo ib yam li Zilt. Yog tias xav tau, cov tshuaj no tuaj yeem hloov lub sijhawm twg los tau nrog ib qho ntawm cov analogues ntawm cov npe. Cov lus qhia rau kev siv nrog Zilt thiab nws cov lus ua yuav luag zoo ib yam. Cov tshuaj no txo ​​cov ntshav txhaws khov kho tau zoo. Txawm li cas los xij, nws tseem raug tso cai hloov Zilt rau ib qho ntawm cov analogues no tsuas yog tom qab kev sab laj ua ntej nrog tus kws kho mob.

Cov generics ntawm Zilt yog cov tshuaj Clopidogrel (tus nqi 190 p. Rau 14 pcs) thiab Clopidogrel Richter (292 p).

Cov tshuaj analogues ntawm cov tshuaj no, tseem tiv thaiv ntshav coagulation, yog li hauv qab no:

"Phenilin" yog tshaj tawm rau cov neeg mob ntawm 0.025-0.1 g 1-3 zaug hauv ib hnub. Cov neeg mob yuav noj Dicumarin hauv kev noj tshuaj ntau npaum li cas ntawm 0.05 txog 0.1 g 2-3 zaug ib hnub. Cov kws kho mob muab tshuaj rau Heparin rau cov neeg mob subcutaneously, tso ntshav los yog intramuscularly.

Tsis tas li ntawd, cov tshuaj "Plavix" yog hais txog cov analogues ntawm cov tshuaj no. "Zilt", cov lus qhia rau kev siv uas peb tau saib saum toj no, qhov tseeb, nws tus kheej yog qhov pheej yig hloov rau cov tshuaj no. Ntau tus neeg mob, uas tau them nyiaj txaus, tau hais qhia kom xaiv Plavix rau kev tiv thaiv ntawm thrombosis. Hais txog qhov ua tau zoo, Zilt yog me ntsis qis dua ntawm cov tshuaj muaj npe no.

Cia rau cov neeg mob

Ntawm chav kawm, kom coj kev tiv thaiv ntawm cov ntshav txhaws yuav tsum tshwj rau cov tshuaj tsis tau pom zoo "Zilt". Nws raug nquahu kom khaws cov tshuaj no ntawm qhov kub txog +25 ° C. Ntawd yog, nyob rau lub caij ntuj sov nws yog ntshaw kom tso cov ntsiav tshuaj no rau hauv tub yees. Lub txee lub neej ntawm cov tshuaj hauv cov ntim ntim yog 3 xyoos.

Kev tshuaj xyuas txog txoj kev kho mob los ntawm cov neeg mob

Cov neeg mob muaj lub tswv yim zoo txog cov tshuaj no. Cov neeg mob muaj feem cuam tshuam nrog nws qhov zoo:

tsis muaj qhov tsis zoo ntawm lub plab.

Cov tshuaj no dilutes cov ntshav, raws li feem ntau ntawm cov neeg mob, zoo dua li cov tshuaj aspirin tib yam. Ntawd yog, txoj kev pheej hmoo ntawm kev rov ua dua lub plawv lossis mob stroke thaum siv nruj me ntsis raws li cov lus qhia rau kev siv, Zilt, kev tshuaj xyuas ntawm qhov uas hais txog qhov no tsuas yog qhov zoo xwb, txo qis.

Qee qhov tsis zoo ntawm cov tshuaj no, cov neeg mob xav txog:

tsis ntim yooj yim heev.

Kev tawm tsam thiab mob ntshav nrag tshwm sim, ntawm cov neeg muaj hnub nyoog ib nrab. Tab sis ntau zaus ntau dua tsis, cov neeg laus tseem ntsib cov teeb meem no. Thiab ntawm chav kawm, yuav zoo li no ib qho kev hloov pauv tshuaj kim yog feem ntau nyuaj.

Cov ntsiav tshuaj Zilt raug ntim rau hauv cov hlwv uas cia sib nrug hauv txhais tes. Tej zaum cov chaw tsim khoom lag luam xav kom ua qhov niaj hnub siv cov tshuaj no yooj yim dua. Txawm li cas los xij, raws li feem ntau ntawm cov neeg mob, nws yuav zoo dua yog tias tso cov tshuaj no hauv cov hlwv muaj zog dua raws txoj kab ntawm kev sib tw.

Lwm qhov kev tsis zoo ntawm cov tshuaj Zilt yog tias ntau tus neeg mob xav txog nws kom muaj cov nyhuv zoo rau daim siab. Cov neeg mob feem ntau qhia txoj kev noj tshuaj no tshwj xeeb los ntawm kev saib xyuas ntawm kws kho mob.

Cov kws kho mob xav li cas txog cov tshuaj

Cov kws kho mob lawv tus kheej kuj txiav txim siab Zilt yog txoj hauv kev zoo rau txo ntshav coagulation. Lub pluses ntawm cov tshuaj no, cov kws kho mob ntaus nqi feem ntau rau qhov tseeb tias nws muaj kev tiv thaiv zoo los ntawm cov neeg mob feem ntau. Kev txiav txim los ntawm kev txheeb xyuas, hemorrhages thaum nws siv tsis tshua muaj.

Cov ntaub ntawv pov thawj hauv cov ntsiab lus ntawm kev nyab xeeb thiab ua tau ntawm cov tshuaj no, raws li ntau tus kws kho mob nco tau, zoo heev. Txawm li cas los xij, lawv ntseeg hais tias qhov tshuaj nyob hauv txhua kis loj. Cov kws kho mob tus kheej pom zoo kom tsis txhob muab tshuaj rau nws tus kheej nrog nws siv.

Cov lus qhia rau siv Zilt: txoj kev thiab ntau npaum li cas

Cov ntsiav tshuaj yog noj ntawm qhov ncauj, tsis hais txog kev noj mov.

Kev noj tshuaj pom zoo rau cov neeg mob uas muaj kev ua haujlwm tsis tu ncua ntawm CYP2C19 isoenzyme, suav nrog cov neeg mob laus:

  • Myocardial infarction, ischemic stroke lossis kuaj tus mob peripheral arterial occlusion: 75 mg ib hnub ib zaug,
  • Mob puas hlwb uas tsis muaj ST ntu kab mob siab (tsis khov kho lub hlwb thiab myocardial infarction yam tsis muaj yoj): kev txhaj tshuaj - ib zaug 300 mg, tom qab ntawv 75 mg ib hnub ib zaug ua ke nrog acetylsalicylic acid ntawm koob tshuaj 75-325 mg ib hnub. Thaum sau tshuaj, nws yuav tsum tau yug los rau hauv lub siab tias kev noj tshuaj ntawm acetylsalicylic acid saum 100 mg yog txuam nrog qhov kev pheej hmoo siab los ntshav. Kev kho mob tshwm sim nyob rau ntawm 3 lub hlis ntawm kev kho mob, rau cov txiaj ntsig zoo, nws raug nquahu kom txuas ntxiv siv clopidogrel mus txog 12 lub hlis,
  • Mob myocardial infarction mob (mob vwm nrog cov leeg hauv qib): ib zaug txhaj, ces 75 mg ib hnub ib zaug ua ke nrog lossis tsis muaj acetylsalicylic acid thiab thrombolytics. Nws tsis pom zoo kom siv cov koob tshuaj txhaj hauv kev kho mob rau cov neeg mob hnub nyoog tshaj 75 xyoo. Txoj kev kho yuav tsum tau pib thaum thawj cov tsos mob tshwm sim thiab txuas ntxiv tsawg kawg 4 asthiv,
  • Atrial fibrillation (atrial fibrillation): 75 mg ib hnub ib zaug nyob rau hauv kev sib xyaw nrog acetylsalicylic acid ntawm koob tshuaj 75-100 mg rau ib hnub.

Nws raug nquahu kom noj cov ntsiav tshuaj tib lub sijhawm, yog tias koj tuaj txog tsawg dua 12 teev, koj yuav tsum noj tsis nco qab thiab lub sijhawm ntxiv nyob rau tib lub sijhawm, nrog ncua sijhawm nruab nrab ntawm ntau dua 12 teev - koob tshuaj ntxiv raug noj yam tsis muaj ob npaug.

Hauv cov neeg mob uas tau txiav txim siab txo cov kev ua haujlwm ntawm CYP2C19 isoenzyme thaum noj Zilt hauv cov koob tshuaj pom zoo, kev tsim cov nquag metabolite ntawm clopidogrel tshwm sim tsawg dua thiab nws cov nyhuv antiplatelet tsawg dua. Cov koob tshuaj zoo tshaj plaws rau cov neeg mob ntawm pawg no tsis tau tsim, feem ntau, cov tshuaj tau sau rau hauv cov koob tshuaj ntau dua nrog ib zaug ntawm kev thauj khoom ntawm 600 mg thiab tom qab ntawd 150 mg ib hnub ib zaug.

Cov neeg laus yog cov tsis xav tau kev hloov kho koob.

Sab sij huam

  • Los ntawm cov hlab plawv system: feem ntau - hematoma, tsis tshua muaj tshwm sim - txoj hlab ntshav hypotension, vasculitis,
  • Los ntawm cov kab mob hematopoietic: ua haujlwm tsis zoo - leukopenia, thrombocytopenia, eosinophilia, tsis tshua muaj neutropenia, suav nrog rau cov ntawv hnyav, tsis tshua muaj neeg mob ntshav liab, ua kom mob ntshav txhaws, mob plab, mob ntshav, mob txhawm, mob ntshav nkees;
  • Los ntawm cov txheej txheem plab zom mov: feem ntau - mob plab, mob plab zom mov, mob plab zawv plab, dyspepsia, ua tsis xws luag - xeev siab, ntuav, cem quav, mob plab, plab zom mov, mob plab thiab / lossis mob plab, mob tsis tshua - kab mob retroperitoneal hemorrhage, tsis tshua muaj - kab mob txham, retroperitoneal thiab mob plab hnyuv los ntshav (nrog rau kev ua rau lub cev tuag), colitis (suav nrog lymphocytic), mob siab ua haujlwm rau lub siab, mob siab, ua haujlwm ntawm lub siab, mob plab,
  • Los ntawm sab hauv ntawm cov hlab ntsha: tsis xws luag - mob taub hau, mob ntshav khov (nrog rau kev mob tshwm sim), kiv taub hau, mob plab, tsis tshua muaj tshwm sim - tsis meej pem, pom kev tsis meej,
  • Los ntawm cov leeg musculoskeletal: tsis tshua muaj - hemarthrosis, mob leeg ntshav, mob caj dab, myalgia, mob pob txha,
  • Los ntawm cov kab mob ua pa: feem ntau - txhaws ntswg, tsis tshua muaj - bronchospasm, los ntshav los ntawm txoj hlab pa hauv lub ntsws (mob ntsws, hemoptysis), interstitial pneumonitis,
  • Los ntawm cov kab ke genitourinary: ua haujlwm tsis xws luag - hematuria, tsis tshua muaj tshwm sim - glomerulonephritis, muaj cov ntshav creatinine ntau zuj zus,
  • Ntawm ib feem ntawm daim tawv nqaij: feem ntau - subcutaneous hematomas, infrequently - khaus ntawm daim tawv nqaij, tawm pob, ua pob ntawm daim tawv nqaij (purpura), tsis tshua muaj tshwm - tawv nqaij dermatitis (Stevens-Johnson syndrome, tshuaj lom epidermal necrolysis, erythema multiforme), urticaria, erythematous pob, ua pob khaus daj, eczema
  • Los ntawm cov kab mob hauv lub cev: hnov ​​nrog sab hauv - rov qab los yog ua rau cov leeg ntshav, tsis tshua muaj - ntsug, tsis tshua muaj - saj cov pathologies,
  • Kev ntsuas ntsuas: feem ntau - txo qis ntawm cov platelets thiab neutrophils, txuas ntxiv lub sijhawm los ntshav,
  • Kev tsis haum tshuaj: muaj mob tsawg kawg - eczema, angioedema, anaphylactoid kev tsis haum tshuaj, kev mob hnyav, tsis paub ntau npaum li cas - tshuaj mob pob khaus nrog cov tsos mob ntawm DRESS syndrome thiab eosinophilia, tiv thaiv kev tiv thaiv kab mob siab rau thienopyridines, kev cuam tshuam los ntawm kev siv tshuaj yeeb hypersensitivity syndrome,
  • Lwm yam: feem ntau - mob ntshav los ntshav ntawm thaj chaw hno, tsis tshua muaj heev - los ntshav ntau los ntawm qhov txhab phais, kub taub hau.

Cev xeeb tub thiab lactation

Raws li cov lus qhia, Zilt tsis pom zoo rau siv thaum cev xeeb tub, txij li tsis muaj cov ntaub ntawv tshawb fawb txog kev siv clopidogrel hauv cov poj niam cev xeeb tub. Cov kev tshawb fawb tsiaj tseem tsis tau qhia tawm qhov tshwm sim ncaj qha lossis tsis ncaj los ntawm cov tshuaj rau kev xeeb tub, kev xeeb menyuam, yug menyuam, lossis kev loj hlob tom qab yug menyuam.

Hauv kev sim tsiaj, nws tau pom tias clopidogrel thiab nws cov metabolites nkag mus rau hauv niam mis, yog li ntawd, yog tias nws yuav tsum siv Zilt hauv cov poj niam laus, kev pub mis niam yuav tsum tau nres.

Nrog lub raum tsis ua haujlwm

Nrog kev siv dua Zilt ntawm ib koob tshuaj ntawm 75 mg rau ib hnub hauv cov neeg mob uas muaj mob tsis zoo hauv lub raum (kev tsim kho lub peev xwm - 5-15 ml / min), qhov kev ntsuas ntawm kev txo cov platelet suav yog 25% qis dua qib siab ntawm kev txwv tsis pub platelet sib piv nrog cov neeg ua haujlwm noj qab haus huv. Txawm li cas los xij, lub sijhawm ntev ntawm lub sijhawm los ntshav zoo ib yam li cov neeg tuaj yeem noj qab haus huv tau txais cov tshuaj ntawm koob tshuaj 75 mg rau ib hnub. Zilt kam rau ua yog sib luag rau txhua tus neeg mob.

Yeeb tshuaj sib cuam tshuam

Vim tias qhov kev pheej hmoo siab los ntshav, nws tsis pom zoo kom sau ntawv tshuaj ib txhij nrog warfarin, thiab thaum sib xyaw nrog heparin thiab lwm yam kab mob thrombolytic, yuav tsum tau saib xyuas tshwj xeeb.

NSAIDs ua rau muaj kev pheej hmoo ntawm mob thiab txhab ntshav tawm hauv lub plab zom mov.

Tsis muaj kev sib cuam tshuam hauv chaw kho mob tau pom nrog kev siv tib lub sijhawm nrog atenolol, angiotensin-hloov pauv enzyme (ACE) inhibitors, cov tshuaj uas txo cov roj cholesterol, digoxin, nifedipine, phenobarbital, estrogens, cimetidine, theophylline.

Clopidogrel tuaj yeem nce cov txiaj ntsig ntawm acetylsalicylic acid ntawm collagen-hle platelet aggregation. Cov chaw muag tshuaj sib xyaw nrog cov tshuaj uas muaj acetylsalicylic acid tsub kom muaj feem los ntshav ntau, yog li siv cov tshuaj sib txuam no tsuas ua tau rau 1 xyoo xwb.

Qhov nqus ntawm clopidogrel tsis cuam tshuam los ntawm antacids.

Kev sib xyaw nrog tolbutamide, phenytoin nce qib ntawm lawv cov peev xwm hauv cov ntshav ntshav.

Zilt cov duab ntxiv yog: Lopirel, Clopidogrel, Clopidogrel-SZ, Plavix, Aggregal, Detromb, Cardutol, Clopidex, Clopilet, Listab 75, Deplatt-75, Cardogrel, Clopigrant, Lirta, Targetek, Plagril, Egithrombrel, Troken.

Kev txheeb xyuas txog Zilt

Cov neeg mob teb tau zoo rau cov tshuaj, tsis tsuas yog nws cov txiaj ntsig, tab sis kuj tsim nyog tus nqi (piv rau qee tus nqi kim dua. Raws li kev txheeb xyuas, Zilt muaj txiaj ntsig tom qab kev mob plawv thiab cov txheej txheem stenting. Cov neeg mob tau sau tseg tias muaj kev txhim kho kom zoo rau tag nrho lub dag zog, qhov kev xaus ntawm lub plawv nres, zoo li tsis muaj txoj hlab ntshav thiab txoj hlab ntshav.

Qee zaum cov neeg mob yws ntawm qhov tshwm sim ntawm kev mob tshwm sim (urticaria, ua tsis taus pa hnyav), tab sis yog tias koj tseem kho mob ntxiv, tom qab ntawd qhov tsis xav hnov ​​tshwm sim ploj ntawm lawv tus kheej tom qab ib pliag.

Tus nqi them nyob rau hauv cov khw muag tshuaj

Txog hnub, kwv yees tus nqi rau Zilt hauv cov khw muag tshuaj muaj raws li hauv qab no:

  • cov ntsiav tshuaj zaj duab xis, 75 mg (14 pcs. ib pob) - 470-530 rubles,
  • cov ntsiav tshuaj zaj duab xis, 75 mg (28 pcs. ib pob) - 830-1200 rubles,
  • cov ntsiav tshuaj zaj duab xis, 75 mg (84 pieces rau ib pob) - 1875-2030 rubles.

Xuas

Tom qab ib zaug thiab rov ua dua qhov ncauj ntawm qhov ncauj ntawm ib koob tshuaj 75 mg rau ib hnub, clopidogrel yog nqus tau sai. Cov nqi nruab nrab ntawm qhov siab tshaj plaws (Cmax) ntawm tsis hloov pauv clopidogrel hauv cov ntshav plasma (2.2-2.5 ng / ml tom qab noj ib koob ntawm 75 mg) tau mus txog tom qab li 45 feeb. Raws li kev tshawb nrhiav ntawm lub raum tsis tuaj yeem ua tiav ntawm clopidogrel metabolites, cov neeg nqus tau yog kwv yees li 50%.

Kev zom zaub mov

Clopidogrel nquag plias hauv daim siab. Nyob rau hauv vitro thiab hauv vivo, clopidogrel metabolized nyob rau hauv ob txoj kev: thawj yog sib kho los ntawm esterases thiab ua rau hydrolysis nrog kev tsim cov tshuaj tiv thaiv metabolite - lub zog ntawm carboxylic acid (85% ntawm circulating metabolites), thiab lwm yam yog catalyzed los ntawm ntau isoenzymes ntawm cytochrome P450. Thaum pib, clopidogrel tau hloov mus rau qhov nruab nrab ntawm cov tshuaj metabolite - 2-oxo-clopidogrel. Cov metabolism tom qab ntawm 2-oxo-clopidogrel ua rau kev tsim cov kev siv dag zog ntawm clopidogrel - thiol derivative ntawm clopidogrel. Hauv vitro, txoj hauv kev no tau sib kho los ntawm isoenzymes CYP3A4, CYP2C19, CYP1A2 thiab CYP2B6. Lub nquag thiol metabolite ntawm clopidogrel, cais tawm hauv vitro, sai thiab tsis tuaj yeem cuam tshuam nrog platelet receptors, thaiv lawv cov kev sib sau.

Cmax ntawm lub cev sib xyaw ua ke nyob rau hauv cov ntshav plasma tom qab noj cov tshuaj thawb tawm (300 mg) ntawm clopidogrel yog ob zaug ntau dua Cmax tom qab 4 hnub ntawm siv clopidogrel hauv kev saib xyuas txij nkawm (75 mg / hnub). Cmax hauv cov ntshav ntshav tau kwv yees li 30-60 feeb tom qab siv cov tshuaj.

Tom qab kev noj ntawm 14C-daim ntawv lo ntawm clopidogrel, kwv yees li 50% ntawm tag nrho cov tshuaj xov hluav taws xob raug tso tawm los ntawm lub raum thiab kwv yees li 46% los ntawm txoj hnyuv hauv 120 teev tom qab noj tshuaj. Tom qab ib qho kev noj tshuaj ntawm qhov ncauj ntawm clopidogrel ntawm ib koob tshuaj 75 mg, ib nrab ntawm lub neej (T1 / 2) yog kwv yees li 6 teev. T1 / 2 ntawm lub ntsiab tsis muaj zog metabolite ncig hauv cov ntshav ntshav tom qab ib zaug thiab rov siv tau yog 8 teev.

Kev tiv thaiv ntawm cov quav atherothrombotic:

  • hauv cov neeg mob cov neeg mob myocardial infarction (los ntawm ob peb hnub mus rau 35 hnub), nrog mob hlab ntsha ischemic (txij li 7 hnub txog rau 6 lub hlis), lossis nrog kev kuaj mob ntawm tus kabmob hnoos qeev txha caj qaum,
  • nyob rau hauv cov neeg mob cov neeg mob loj uas tsis muaj mob: tsis muaj ST ntu ntu (tsis khov lub siab los yog myocardial infarction tsis muaj Q yoj), suav nrog cov neeg mob uas tau stenting nrog percutaneous coronary cuam tshuam, hauv kev sib xyaw nrog acetylsalicylic acid, nrog ST ntu ntu (mob myocardial infarction) nrog kev siv tshuaj kho mob thiab qhov ua tau ntawm kev kho thrombolytic, ua ke nrog acetylsalicylic acid.

Kev tiv thaiv ntawm atherothrombotic thiab thromboembolic muaj teeb meem, suav nrog mob stroke, nrog atrial fibrillation (atrial fibrillation)

Cov neeg laus uas mob atrial fibrillation (atrial fibrillation), uas muaj tsawg kawg yog ib qho kev pheej hmoo rau kev txhim kho vascular teebmeem, tsis tuaj yeem siv cov anticoagulants tsis ncaj thiab muaj kev pheej hmoo los ntshav tsawg (nrog rau acetylsalicylic acid).

Mob mob caj dab mob plawv yam tsis muaj txoj cai ST ntu nce

Kev kho mob nrog Zilt® yuav tsum tau pib nrog ib koob tshuaj ntawm lub ntsaws tshuaj tso tawm (300 mg), thiab tom qab ntawd txuas ntxiv nrog koob tshuaj 75 mg ib hnub ib zaug (ua ke nrog acetylsalicylic acid hauv koob tshuaj 75-325 mg ib hnub). Txij li thaum siv ntau dua ntawm cov tshuaj acetylsalicylic acid yog cuam tshuam nrog kev pheej hmoo los ntshav ntau dua, cov koob tshuaj pom zoo ntawm acetylsalicylic acid yuav tsum tsis pub ntau tshaj 100 mg. Qhov txiaj ntsig zoo tshaj plaws yog pom los ntawm 3 lub hlis ntawm kev kho mob. Cov sijhawm zoo tshaj plaws ntawm kev kho rau qhov ntsuas qhov no tsis tau txiav txim siab raws cai. Cov txiaj ntsig ntawm kev tshawb fawb soj ntsuam tshawb pom qhov ua tau ntawm kev noj clopidogrel txog 12 lub hlis tom qab kev txhim kho ntawm cov kev mob caj dab tsis mob nce qib ST ntu.

Mob pob txha taub hau mob kas cees nrog ST ntu theem

Zilt® yuav tsum tau noj nyob rau hauv ib koob tshuaj 75 mg (1 ntsiav tshuaj) ib hnub ib zaug, pib nrog kev txhaj tshuaj, nyob rau hauv sib xyaw nrog acetylsalicylic acid nrog lossis tsis muaj thrombolytics. Rau cov neeg mob uas laus dua 75 xyoo, kev kho mob nrog Zilt® yuav tsum tau nqa tawm yam tsis tas yuav siv cov tshuaj thauj khoom. Txoj kev kho ua ke yog pib kom sai li sai tau tom qab pib pom cov tsos mob thiab txuas ntxiv tsawg kawg 4 lis piam. Cov txiaj ntsig ntawm kev sib xyaw ua ke nrog kev kho mob nrog clopidogrel thiab acetylsalicylic acid ntev dua 4 lub lis piam tsis tau kawm txog cov neeg mob no.

Atrial fibrillation (ua rau atrial fibrillation)

Cov tshuaj Zilt® raug xaj nyob rau hauv ib koob ntawm 75 mg ib hnub ib zaug. Ua ke nrog clopidogrel, kev kho yuav tsum tau pib thiab tom qab ntawd kev noj cov tshuaj acetylsalicylic acid ntawm koob tshuaj 75-100 mg ib hnub yuav tsum txuas ntxiv.

Yog tias tus neeg mob tsis nco qab noj ntxiv lawm:

  • yog tias tsawg dua 12 teev tau dhau mus tom qab hla lub koob tshuaj tom ntej, koj yuav tsum noj tam sim ntawd ntawm lub Zilt® uas ploj lawm, thiab tom qab ntawd noj cov koob tshuaj ntxiv rau lub sijhawm ib txwm,
  • yog tias ntau dua 12 teev tau dhau mus tom qab dhau lub koob tshuaj ntxiv, tom qab ntawd cov koob tshuaj yuav tsum noj nyob rau lub sijhawm ib txwm, thaum koob tshuaj yuav tsum tsis txhob suav ntxiv.

Lub raum khiav tsis zoo

Tom qab rov qab siv clopidogrel ntawm ib koob tshuaj ntawm 75 mg rau ib hnub hauv cov neeg mob uas lub raum tsis zoo (CC 5-15 ml / min), qhov kev txwv ntawm ADP-vim platelet aggregation yog 25% qis dua hauv cov neeg ua haujlwm noj qab haus huv. Txawm li cas los xij, qhov kev ntsuas lub sijhawm ncua ntev ntawm lub sijhawm los ntshav zoo ib yam li cov neeg tuaj yeem noj qab haus huv uas tau txais clopidogrel ntawm ib koob tshuaj ntawm 75 mg rau ib hnub. Kev zam rau cov tshuaj tau zoo hauv txhua tus neeg mob.

Siv thaum cev xeeb tub thiab lactation

Txij li thaum tsis muaj cov ntaub ntawv tshawb fawb txog kev siv clopidogrel thaum cev xeeb tub, cov tshuaj tsis pom zoo rau siv thaum cev xeeb tub. Cov kev tshawb fawb tsiaj tsis tau qhia tawm qhov cuam tshuam ncaj qha los yog tsis ncaj rau kev xeeb tub, kev loj hlob ntawm cov embryo / fetus, chav kawm ntawm kev mob plab lossis yug menyuam tom qab.

Cov kev tshawb fawb tsiaj tau pom tias clopidogrel thiab / lossis nws cov khoom noj tiv thaiv tau tawm hauv cov kua mis. Yog li, yog tias kho nrog clopidogrel yog qhov tsim nyog, nws raug nquahu kom tsis pub mis niam.

Anticoagulants rau kev tswj hwm qhov ncauj

Kev siv tib txhij ntawm clopidogrel thiab anticoagulants rau kev tswj hwm qhov ncauj tuaj yeem nce qhov hnyav ntawm los ntshav, thiab yog li ntawd, kev siv ntawm kev sib xyaw no tsis pom zoo.

Kev siv clopidogrel ntawm koob tshuaj ntawm 75 mg rau ib hnub tsis pauv pauv pharmacokinetics ntawm warfarin (qhov tsis sib xws ntawm CYP2C9 isoenzyme) lossis thoob ntiaj teb li qub piv (INR) hauv cov neeg mob tau txais kev kho mob ntev nrog warfarin. Txawm li cas los xij, kev siv tib lub sijhawm nrog warfarin ua rau muaj kev pheej hmoo los ntshav vim nws txoj kev ywj pheej ntxiv rau ntshav coagulation. Yog li, ceev faj yuav tsum tau siv thaum siv warfarin thiab clopidogrel.

Acetylsalicylic acid

Acetylsalicylic acid tsis cuam tshuam rau inhibition of platelet aggregation ntxias los ntawm clopidogrel ntxias los ntawm ADP, tab sis clopidogrel potentiates cov nyhuv ntawm acetylsalicylic acid ntawm collagen-ntxias platelet aggregation. Txawm li cas los xij, kev tswj hwm ib txhij ntawm 500 mg ntawm acetylsalicylic acid ob zaug hauv ib hnub rau ib hnub tsis ntau ncua sij hawm los ntshav los ntawm clopidogrel. Txoj kev sib txuam pharmacodynamic ntawm clopidogrel thiab acetylsalicylic acid tej zaum yuav ua rau muaj kev pheej hmoo los ntshav. Muab qhov no, ceev faj yuav tsum tawm dag zog thaum noj cov tshuaj no, txawm hais tias nyob rau hauv kev tshawb fawb soj ntsuam, cov neeg mob tau siv tshuaj ua ke nrog clopidogrel thiab acetylsalicylic acid rau ib xyoos.

Raws li kev tshawb fawb soj ntsuam hauv cov tib neeg muaj kev noj qab haus huv, thaum noj clopidogrel, tsis tas yuav hloov pauv cov tshuaj heparin, thiab cov nyhuv anticoagulant ntawm heparin tsis hloov. Kev siv heparin ib txhij tsis cuam tshuam rau kev cuam tshuam ntawm platelet aggregation los ntawm clopidogrel. Tej zaum qhov pharmacodynamic sib cuam tshuam ntawm clopidogrel thiab heparin, ua rau muaj kev pheej hmoo ntxiv los ntshav. Yog li, kev siv ua ke ntawm cov tshuaj no yuav tsum ceeb toom.

Thrombolytics

Kev nyab xeeb ntawm kev siv tib txhij ntawm clopidogrel, fibrin-specific los yog fibrin-specific thrombolytics thiab heparin raug soj ntsuam hauv cov neeg mob uas muaj myocardial infarction. Qhov tshwm sim ntawm qhov tseem ceeb ntawm kev tso ntshav tau los piv nrog qhov kev siv tib lub sij hawm ntawm thrombolytics, heparin nrog acetylsalicylic acid.

Nonsteroidal anti-inflammatory tshuaj (NSAIDs)

Raws li kev tshawb fawb soj ntsuam nrog cov neeg ua haujlwm noj qab haus huv, kev siv tib txhij ntawm clopidogrel thiab naproxen nce latent gastrointestinal los ntshav. Txawm li cas los xij, vim tias tsis muaj kev kawm txog kev cuam tshuam nrog lwm tus NSAIDs tam sim no, nws tseem tsis tau paub meej tias qhov kev pheej hmoo ntawm kev txhim kho txoj hnyuv ntshav yuav nce ntxiv thaum siv ua ke nrog lwm cov NSAIDs. Yog li, kev kho tib lub sijhawm ntawm NSAIDs, suav nrog COX-2 inhibitors, thiab clopidogrel yuav tsum tau ua nrog ceev faj (saib ntu "Cov lus qhia tshwj xeeb").

CYP2C19 Isoenzyme Tus Neeg Txom Nyem

Clopidogrel yog metabolized rau qhov tsim ntawm nws cov metabolite nquag, ib feem nyob hauv qab ntawm CYP2C19 isoenzyme. Yog li, cov tshuaj noj uas txwv qhov isoenzyme no tuaj yeem ua rau txo qis hauv kev ua kom muaj zog ntawm cov tshuaj metabolite ntawm clopidogrel. Cov kab mob tseem ceeb ntawm cov kev sib txuam no tsis muaj leej twg paub. Siv nrog rau cov muaj zog los yog siv tshuaj tiv thaiv kab mob CYP2C19 isoenzyme yuav tsum tau zam. Cov tshuaj tiv thaiv ntawm CYP2C19 isoenzyme suav nrog omeprazole thiab esomeprazole, fluvoxamine, fluoxetine, moclobemide, voriconazole, fluconazole, ticlopidine, ciprofloxacin, cimetidine, carbamazepine, oxcarbazepine thiab chloramphen.

Proton twj tso kua mis inhibitors

Kev siv omeprazole hauv ib koob ntawm 80 mg ib zaug ib hnub ib zaug nrog clopidogrel lossis nrog 12-teev so ntawm kev noj ob yam tshuaj txo tus kabmob sib kis (AUC) ntawm cov metabolite ntawm clopidogrel los ntawm 45% (tom qab noj tshuaj pab rau ntawm clopidogrel) thiab 40% (tom qab noj cov tshuaj txij nkawm. txhaj tshuaj ntawm clopidogrel). Qhov kev txo qis hauv AUC ntawm cov tshuaj metabolite ntawm clopidogrel yog txuam nrog qhov kev txo qis ntawm kev txwv tsis pub platelet sib cais (39% tom qab noj cov tshuaj ntawm clopidogrel thiab 21% tom qab noj cov tshuaj txij nkawm ntawm clopidogrel). Ib qho kev sib cuam tshuam zoo sib xws ntawm clopidogrel nrog esomeprazole tau pom zoo. Hauv kev soj ntsuam thiab kev soj ntsuam, cov ntaub ntawv tsis sib haum txog cov chaw kho mob ntawm cov hlab plawv hais txog qhov chaw muag tshuaj / chaw muag tshuaj sib cuam tshuam tau sau tseg. Kev siv tib lub sijhawm omeprazole lossis esomeprazole yuav tsum zam.

Cia Koj Saib