Cov tshuaj Clopidogrel C3: cov lus qhia rau kev siv

Kev piav qhia cuam tshuam rau 28.01.2015

Lub npe Latin: Clop>

Cov ntsiav tshuaj ntawm cov tshuaj Clopidogrel suav nrog 75 mg ntawm tib yam tshuaj ua tau zoo hauv daim ntawv ntawm hydrosulfate.

Cov tshuaj ntxiv: prosalv, lactose monohydrate, colloidal silicon dioxide, croscarmellose sodium, sodium fumarate.

Lub plhaub muaj pes tsawg leeg: paj yeeb opadray II (hypromellose, lactose monohydrate, titanium dioxide, carmine, zas xim daj hlau oxide, macrogol), silicone emulsion.

Daim ntawv tso tawm

Pink round coated ntsiav tshuaj yog biconvex zoo li, dawb-daj hauv seem.

14 ntsiav tshuaj rau ib pob, 1 lossis 2 ntim rau hauv ib pob ntawv.
7 lossis 10 ntsiav tshuaj rau ib pob, 1, 2, 3 lossis 4 ntim rau ib pob ntawv.
7 lossis 10 ntsiav tshuaj hauv ib lub hlwv; 1, 2, 3 lossis 4 blisters ua ib pob ntawv.
14 lossis 28 ntsiav tshuaj hauv lub raj mis polymer, 1 lub raj mis hauv ib pob ntawv.
14 lossis 28 ntsiav tshuaj hauv polymer tuaj yeem, 1 tuaj yeem nyob hauv ntim ntawv.

Pharmacodynamics thiab pharmacokinetics

Cov tshuaj siv tshuaj ua kom muaj zog platelet sib sau ua ke thiab xaiv txo qhov kev khi ntawm adenosine diphosphate (ADP) rau platelet receptors, thiab kuj txo lub peev xwm los ua kom glycoprotein receptors nyob rau hauv adenosine diphosphate nkaus. Cov tshuaj txo qis cov kev sib txuas ntawm platelets, uas yog tshwm sim los ntawm ib qho antagonists, inhibiting lawv kev ua haujlwm los ntawm kev tso tawm ADP. Cov tshuaj cov tshuaj molecules ua ke nrog platelet ADP receptors, tom qab ntawd platelets mus ib txhis plam lawv qhov tsis haum rau ADP stimulation.

Cov nyhuv ntawm inhibiting platelet aggregation tshwm sim ob teev tom qab txhaj thawj. Qib kev kev tsuj ntawm kev zaws nce ntxiv hauv 4-7 hnub thiab nce mus txog nws qhov siab kawg ntawm lub sijhawm kawg no. Hauv qhov no, kev noj tshuaj txhua hnub yuav tsum yog 50-100 mg rau ib hnub. Yog tias atherosclerotic vascular puas tsuaj tshwm sim, tom qab ntawd noj cov tshuaj tiv thaiv qhov kev vam meej ntawm tus kab mob.

Tom qab noj cov tshuaj nyob rau hauv ib lub sij hawm luv luv ntawm lub sij hawm yog nqus nyob rau hauv lub gastrointestinal ib ntsuj av. Lub bioavailability ntawm cov tshuaj yog 50%; kev noj zaub mov noj tsis cuam tshuam rau theem no. Cov metabolism ntawm cov tshuaj tshwm sim hauv lub siab. Hauv cov ntshav plasma, cov txiaj ntsig siab tshaj plaws tau mus txog ib teev tom qab siv tshuaj. Txoj kev tshem tawm ib nrab-lub neej yog yim teev, raug kho tawm ntawm lub raum thiab hauv cov hnyuv.

Cov lus qhia tshwj xeeb

Kev siv cov tshuaj muaj feem xyuam nrog kev xav tau tas li saib xyuas tus neeg mob tus mob. Cov lus hauv qab no muaj qee yam:

Hauv cov neeg mob uas lawv muaj hnub nyoog tshaj 75 xyoos, txoj cai ntawm thawj koob tshuaj yuav tsum tau muab tshem tawm.
Hauv cov txheej txheem ntawm txoj kev kho, koj yuav tsum ua raws li kev taw qhia ntawm cov kab mob siab tshaj plaws, los tshawb xyuas lub xeev kev ua haujlwm ntawm lub siab.
Siv nrog ceev faj hauv cov neeg mob uas muaj kev pheej hmoo ntawm ntshav ploj vim kev raug mob lossis lwm yam.
Nyob rau hauv muaj cov kab mob cuam tshuam nrog ntshav poob, nws yuav tsum tau nyob rau hauv lub siab hais tias cov tshuaj lengthens lub sijhawm los ntshav.
Thaum tsav tsheb, nco ntsoov tias clopidogrel tuaj yeem ua rau kiv taub hau.

Thaum cev xeeb tub

Txog hnub tim, tsis muaj kev tshawb fawb puv ntoob thiab ib qho kev sim rau kev ua haujlwm ntawm cov txiaj ntsig ntawm clopidogrel ntawm cev xeeb tub thiab kev loj hlob ntawm tus me nyuam hauv plab tsis tau loj hlob. Vim li no, cov tshuaj tsis raug txwv kom ua thaum cev xeeb tub. Tsis muaj pov thawj ntawm qhov kev cia siab hauv cov tshuaj no dhau mus rau niam mis, yog li kev noj Clopidogrel tsis pom zoo thaum pub mis.

Kev ntsuas rau siv

Kev tiv thaiv ntawm atherothrombotic cov xwm txheej hauv cov neeg mob tom qab myocardial infarction (los ntawm ob peb hnub mus rau 35 hnub), ischemic stroke (txij li 7 hnub txog rau 6 lub hlis) lossis cov uas muaj tus kab mob txha caj qaum txha caj qaum.

Kev tiv thaiv cov kab mob atherothrombotic (ua ke nrog acetylsalicylic acid) hauv cov neeg mob uas muaj mob rau txoj hlab ntshav siab:

- tsis muaj nce qib ST ntu (tsis khov kho lub hlwb pectoris lossis myocardial infarction tsis muaj Q yoj), suav nrog cov neeg mob uas tau ua stenting nrog percutaneous kev tiv thaiv kev mob,

- nrog kev sawv ntawm ST ntu (mob myocardial infarction) nrog kev kho tshuaj thiab qhov ua tau kom muaj tus mob thrombolysis.

Cov Yuav Tsum Tau Ua

- mob ntshav khov (piv txwv li, los ntshav los ntawm qhov mob peptic lossis mob ntshav sab hauv),

- tsis tshua muaj cov kab mob lactose tsis txaus ntseeg, lactase deficiency thiab glucose-galactose malabsorption,

- cov menyuam yaus thiab cov tub ntxhais hluas hnub nyoog qis dua 18 xyoo (kev nyab xeeb thiab kev ua tau zoo tsis tau tsim),

- Cawv lub cev tsis ua hauj lwm rau clopidogrel lossis ib yam dab tsi ua tsis zoo ntawm cov tshuaj.

- mob nyhav hauv daim siab, uas qhov xav tau ua rau los ntshav yog tau (muaj kev soj ntsuam tsawg)

- lub raum tsis ua hauj lwm (tsawg kho mob kev)

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

- tib lub sijhawm tswj hwm ntawm cov tshuaj tsis-tshuaj steroidal, suav nrog xaiv COX-2 inhibitors,

- kev siv tib lub sij hawm ntawm warfarin, heparin, glycoprotein IIb / IIIa inhibitors,

Yuav siv li cas: noj ntau thiab hom tshuaj kho

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

Clopidogrel-SZ yuav tsum tau noj qhov ncauj, tsis hais kev noj zaub mov.

Myocardial infarction, ischemic stroke, thiab kuaj tus mob peripheral arterial occlusion

Qhov tshuaj raug coj ntawm 75 mg 1 lub sijhawm / hnub.

Hauv cov neeg mob uas muaj myocardial infarction (MI), kev kho mob tuaj yeem pib txij thawj hnub mus txog 35 hnub ntawm MI, thiab hauv cov neeg mob ischemic stroke (II), txij li 7 hnub txog 6 hli tom qab MI.

Mob mob caj dab mob yam tsis muaj ST ntu kab mob siab (tsis khov kho lub hlwb tsis khov, myocardial infarction tsis muaj Q yoj)

Kev kho mob nrog Clopidogrel-SZ yuav tsum pib nrog ib koob txhaj tshuaj ntawm 300 mg, thiab tom qab ntawd txuas ntxiv ntawm koob tshuaj 75 mg 1 zaug / hnub (ua ke nrog acetylsalicylic acid ua tshuaj tiv thaiv antiplatelet ntawm koob tshuaj 75-325 mg / hnub). Txij li thaum siv cov tshuaj acetylsalicylic acid nyob rau hauv cov koob tshuaj ntau dua yog cuam tshuam nrog kev pheej hmoo ntawm ntshav los ntshav, qhov kev xav kom pom ntawm acetylsalicylic acid hauv qhov ntsuas no yuav tsum tsis pub ntau tshaj 100 mg. Qhov siab tshaj plaws kho tau tshwm sim los ntawm lub hlis thib 3 ntawm kev kho mob. Lub sij hawm ntawm kev kho mob yog txog 1 xyoos.

Mob mob caj dab mob syndrome nrog rau ST ntu ntu (mob myocardial infarction nrog ST ntu ntu)

Clopidogrel yog muaj kev noj tshuaj ntau npaum li 75 mg 1 zaug / hnub nrog thawj zaug ntawm kev thauj khoom hauv kev sib xyaw nrog Acetylsalicylic acid ua tshuaj antiplatelet thiab thrombolytics (lossis tsis muaj thrombolytics). 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. Hauv cov neeg mob uas muaj hnub nyoog tshaj 75 xyoos, kho nrog Clopidogrel-SZ yuav tsum pib tsis tas noj ib qho kev noj tshuaj.

Cov neeg mob Nrog Kev Caj Coob Coob CYP2C19 Isoenzyme Muaj nuj nqi

Kev tsis muaj zog ntawm cov metabolism hauv kev siv CYP2C19 isoenzyme tuaj yeem ua rau txo qis ntawm cov nyhuv antiplatelet ntawm clopidogrel. Cov koob tshuaj zoo tshaj plaws rau cov neeg mob uas tsis muaj zog txaus uas siv cov CYP2C19 isoenzyme tseem tsis tau tsim.

Pharmacological kev txiav txim

Antiplatelet tus neeg sawv cev. Clopidogrel yog prodrug, ib qho ntawm cov tshwj xeeb metabolites ntawm uas yog ib qho inhibitor ntawm platelet aggregation. Lub zog ua haujlwm ntawm clopidogrel metabolite xaiv rau kev khuam khi ntawm adenosine diphosphate (ADP) rau P2Y12 platelet receptor thiab tom qab ADP-mediated kev ua haujlwm ntawm GPIIb / IIIa txoj hauv kev, ua rau muaj kev cuam tshuam ntawm platelet sib sau ua ke. Vim tias tsis to taub tau khi, platelets tseem muaj lub zog tiv thaiv ADP kev kho mob rau tas lawv lub neej (kwv yees li 7-10 hnub), thiab kev kho dua tshiab ntawm platelet muaj nuj nqi tshwm sim ntawm tus nqi sib xws rau lub platelet rov ua dua tshiab. Platelet kev sib cais los ntawm agonists dua li ADP kuj tseem raug thaiv los ntawm kev thaiv ntawm kev nce platelet ntau los ntawm ADP tso tawm. Vim hais tias kev tsim cov nquag metabolite tshwm sim siv P450 isoenzymes, qee qhov yuav txawv hauv polymorphism lossis yuav tiv thaiv los ntawm lwm cov tshuaj; tsis yog txhua tus neeg mob yuav muaj kev tiv thaiv platelet txaus.

Sab sij huam

Los ntawm lub hauv nruab nrab thiab lub paj hlwb ntawm lub paj hlwb: ua haujlwm tsis xws luag - mob taub hau, kiv taub hau thiab mob caj dab, tsis tshua muaj - vertigo, tsis tshua muaj heev - ua txhaum ntawm saj hnov.

Nyob rau ib feem ntawm cov hlab plawv: muaj tsawg kawg - vasculitis, cim txo qis ntshav siab, mob ntshav tawm ntshav, mob ntshav tawm (ua mob rau hauv cov nqaij mos thiab retina), hematoma, ntswg, los ntshav los ntawm txoj hlab pa, txoj hnyuv los ntshav, mob ntshav tawm los ntshav qhov tshwm sim, hemorrhages hauv cov leeg thiab pob qij txha, hematuria.

Los ntawm cov kab mob ua pa: tsis tshua muaj mob - bronchospasm, interstitial pneumonitis.

Los ntawm cov txheej txheem plab zom mov: feem ntau - raws plab, mob plab, dyspepsia, tso tsis tau - mob plab thiab mob plab, mob plab, ntuav, xeev siab, cem quav, mob plab, tsis tshua mob heev - pancreatitis, mob plab (suav nrog rau ulcerative lossis lymphocytic colitis), stomatitis, mob siab ua haujlwm nrawm, kab mob siab.

Los ntawm cov kab mob ntawm lub tso zis: tsis tshua muaj - glomerulonephritis.

Los ntawm cov ntshav kev coagulation system: ncus - lengthening ntawm lub sijhawm los ntshav.

Los ntawm cov kab mob hemopoietic: ua tsis xws luag - thrombocytopenia, leukopenia, neutropenia thiab eosinophilia, muaj tsawg kawg - thrombocytopenic thrombohemolytic purpura, mob hnyav thrombocytopenia (platelet suav tsawg dua los sis sib npaug li 30 × 109 / l), agranulocytosis, granululocytosis, granulia.

Nyob rau ntawm daim tawv nqaij thiab subcutaneous cov ntaub so ntswg: ntxiag dhau - tawv nqaij ua pob khaus thiab khaus, tsis tshua muaj tshwm sim - angioedema, urticaria, erythematous pob (cuam tshuam nrog clopidogrel lossis acetylsalicylic acid), tsis tshua muaj - kev ua rau mob tawv nqaij (erythema multiforme, Stevens-Johnson syndrome), lom, lom ), eczema thiab lichen planus.

Los ntawm cov leeg musculoskeletal: tsis tshua muaj tshwm sim - mob caj dab, mob caj dab, mob myalgia.

Ntawm ib feem ntawm lub cev tiv thaiv kab mob: tsis tshua muaj tshwm sim - anaphylactoid kev tsis haum, ntshiab ntshav mob.

Kev sib txuam

Ib txhij tswj hwm nrog clopidogrel tuaj yeem ntxiv qhov ntshav khov ntau ntxiv, yog li kev siv ntawm kev sib xyaw no tsis pom zoo.

Kev siv IIb / IIIa receptor blockers nrog clopidogrel yuav tsum ceeb toom rau cov neeg mob uas muaj kev pheej hmoo los ntshav ntau ntxiv (nrog kev raug mob thiab kev phais mob lossis lwm yam mob pathological).

Acetylsalicylic acid tsis hloov pauv cov nyhuv ntawm clopidogrel, uas inhibits ADP-vim platelet aggregation, tab sis clopidogrel potentiates cov nyhuv ntawm acetylsalicylic acid ntawm collagen-ntxias platelet aggregation. Txawm li cas los xij, kev siv tib lub sijhawm ntawm acetylsalicylic acid nrog clopidogrel yog cov tshuaj tiv thaiv kab mob ntawm 500 mg 2 zaug / hnub rau 1 hnub tsis ua rau muaj teeb meem loj ntxiv rau lub sijhawm los ntshav los ntawm clopidogrel cov thawj coj. Nruab nrab ntawm clopidogrel thiab acetylsalicylic acid, kev sib txuam ntawm pharmacodynamic yog ua tau, uas ua rau muaj kev pheej hmoo ntxiv los ntshav. Yog li ntawd, nrog lawv siv tib lub sijhawm, kev ceev faj yuav tsum siv, txawm hais tias hauv kev tshawb fawb soj ntsuam, cov neeg mob tau txais kev kho ua ke nrog clopidogrel thiab acetylsalicylic acid txog li ib xyoos.

Raws li kev tshawb fawb soj ntsuam ua nrog cov neeg ua haujlwm noj qab haus huv, thaum noj clopidogrel, tsis tas yuav hloov pauv cov tshuaj heparin thiab nws cov nyhuv anticoagulant tsis hloov pauv. Kev siv txhij ib txhij ntawm heparin tsis hloov pauv antiplatelet nyhuv ntawm clopidogrel. Nruab nrab ntawm clopidogrel thiab heparin, kev sib txuam pharmacodynamic yog ua tau, uas tuaj yeem ua rau muaj kev pheej hmoo los ntshav, yog li ntawd siv cov tshuaj no ua ke kom ceev faj.

Cov lus qhia rau kev siv

Clopidogrel yog siv rau hauv cov neeg mob cov neeg laus 1 zaug nyob rau ib hnub (ua ntej noj su, tom qab noj su), tsis hais zaub mov dab tsi. Lub ntsiav tshuaj yuav tsum tsis txhob txhaws. Haus dej kom ntau (yam tsawg kawg nkaus 70 ml). Qhov pom zoo kho kom zoo ntawm cov tshuaj yog 75 mg rau ib hnub (ib ntsiav tshuaj).

Cov txheej txheem ntawm kev thov rau kev mob plawv hauv lub plawv: cov neeg laus hauv chav kho plawv hauv kev saib xyuas kev kho mob yog ib zaug sau 300 mg ntawm clopidogrel. Tom qab, kev kho mob txuas ntxiv nyob rau hauv kev saib xyuas kev noj qab haus huv ntawm 75 mg, ntau zaus nyob rau hauv kev sib txuas nrog acetylsalicylic acid hauv kev siv tshuaj ntawm 0.075 txog 0.325 g.

Tseem Ceeb! Txhawm rau kom tsis txhob los ntshav, tsis txhob siv ntau tshaj 100 mg ntawm acetylsalicylic acid.

Lub sijhawm sijhawm ntawm kev pub nkag yog tsis paub tseeb. Kev noj cov tshuaj mus txuas ntxiv kom txog thaum tus neeg mob lub cev rov qab zoo li qub ntawm kev txiav txim ntawm tus kws kho mob.

Lub sijhawm ntawm kev kho mob thaum lub sij hawm mob siab ceev ntawm lub plawv nres: ntau npaum ntawm clopidogrel yog 75 mg rau ib hnub, suav nrog thawj zaug kev thauj khoom ntawm 300 mg nyob rau hauv ua ke nrog acetylsalicylic acid thiab tshuaj thombolytic.

Tseem Ceeb! Nws yog ib qho tseem ceeb rau cov neeg mob tom qab 75 xyoo uas yuav tsum tsis suav siv kev siv khoom thauj khoom ntawm cov tshuaj.

Lub sijhawm tiv thaiv yog tsawg kawg ib hlis.

Thaum muaj kev tshem tawm, hauv qab no yuav tsum tau ua:

Yog tias ntau dua 12 teev tso rau ua ntej noj cov ntsiav tshuaj txuas ntxiv, haus tshuaj tam sim ntawd.
Yog tias ua ntej thov kev noj tshuaj ntxiv ntawm clopidogrel tsawg dua 12 teev - noj dua lwm lub sijhawm thaum lub sijhawm (tsis txhob nce lub koob).

Nws yog txwv tsis pub rau nws tus kheej thiab sai txwv tsis pub siv clopidogrel, vim tias tus neeg mob tus mob yuav loj tuaj, kev rov kis tus kab mob hauv qab yuav tshwm sim.

Noj ntau dhau

Kev ua txhaum kev siv ntawm kev txhaj tshuaj siab ntawm clopidogrel tuaj yeem nrog cov kev cuam tshuam no:

los ntshav
ntxiv sijhawm ntawm los ntshav.

Kev noj tshuaj ntau dhau yog mob. Kev ua tau zoo dua yog kev hloov ntshav ntawm cov tshuaj raws platelet mass.

Nrog cawv

Thaum muaj kev cuam tshuam nrog kev haus cawv, qhov ntxim nyiam ua rau lub cev ntawm lub plab thiab cov hnyuv nce ntxiv, vim cov ntshav tawm tuaj. Yog li ntawd, kev sib xyaw ntawm clopidogrel thiab cawv yuav tsum tau muab cais tawm vim yog kev sib txuam tsawg heev.

Cov chaw tsim tshuaj tsim cov tshuaj xws li Clopidogrel hloov chaw:

Nkauj Mim,
Gridoklein,
Atherocard,
Avwmx,
Clopidogrel ntawm ntau cov tuam ntxhab - Izvarino, Tatkhimpharmpreparaty, Canon Pharma, Severnaya Zvezda (SZ), Biocom (analogues Lavxias ntawm Clopidogrel), Teva, Gideon Richter, Ratiopharm, Zentiva,
Atrogrel
Cardogrel
Diloxol
Sylt,
Chaw,
Deplatt
Noclot,
Clopact,
Clorelo
Clopix
Clopid
Lodigrel,
Orogrel
Thromborel,
Qhov chaw
Lopirel
Plavix,
Reodar,
Trombix,
Plaglir,
Sibhawm,
Platogril
Ntxhw
Reomax
Pob Tsuas,
Clopidex
Plavigrel
Flamogrel.

Tag nrho cov tshuaj no tsis muaj qhov sib txawv hauv qhov muaj pes tsawg leeg thiab ntau npaum li cas ntawm cov tshuaj nquag. Qhov txawv yog tsuas yog hauv cov tuam ntxhab thiab nqi.

Cov Tshuaj Pharmacokinetics

Kev Tsis Txaus Siab Tom qab ib zaug thiab rov tso qhov ncauj ntawm 75 mg rau ib hnub, clopidogrel yog nqus tau sai. Qhov nruab nrab ntshav ntau tshaj plaws ntawm qhov kev sib xyaw loj (kwv yees li 2.2-2.5 ng / ml tom qab noj ib zaug ntawm 75 mg) tau pom thaj tsam li 45 feeb tom qab kev tswj hwm.Raws li clopidogrel metabolites ua tawm hauv cov zis, nqus tsawg kawg yog 50%.

Kev xa Khoom. Clopidogrel thiab qhov tseem ceeb (tsis voos) circulating metabolite reversibly khi rau cov protein ntshav hauvvitro (98 thiab 94%, feem). Daim ntawv cog lus no tseem nyob tsis ruaj khov. hauvvitro dhau ntawm ntau qhov ntau.

Kev zom zaub mov. Clopidogrel sai sai hauv daim siab. Hauvvitro thiab hauvvivo clopidogrel metabolized nyob rau hauv ob txoj kev loj: ib qho yog kev kho kom haum xeeb los ntawm esterases thiab ua rau hydrolysis rau ib qho kev tsis sib haum xeeb ntawm carboxylic acid (85% ntawm metabolites circulating hauv cov hlab ntsha), lwm qhov (15%) yog kev kho kom haum xeeb los ntawm ntau P450 cytochromes. Ua ntej, clopidogrel yog metabolized rau nruab nrab metabolite, 2-oxo-clopidogrel. Tom qab cov metabolism ntawm cov tshuaj nruab nrab ntawm 2-oxo-clopidogrel ua rau kev tsim cov khoom noj rau lub cev, cov thiol derivative ntawm clopidogrel. Hauvvitro cov metabolic pathway no tau sib kho los ntawm CYP3A4, CYP2C19, CYP1A2 thiab CYP2B6. Lub zog thiol metabolite uas tau muab cais tawm hauvvitro sai thiab irreversibly, nws nkag mus rau hauv kev sib cuag nrog platelet receptors, yog li inhibiting platelet aggregation.

Nrog_max cov nquag metabolite yog ob zaug ntau dua tom qab txhaj ib zaug ntawm kev txhaj tshuaj ntawm 300 mg ntawm clopidogrel dua tom qab plaub hnub ntawm kev saib xyuas txij nkawm ntawm 75 mg. Nrog_max cai hauv lub sijhawm 30-60 feeb tom qab siv cov tshuaj.

Kev Ntaus Tawm. Li 50% ntawm cov tshuaj tau tawm hauv cov zis thiab kwv yees li 46% nrog quav hauv lub sijhawm 120 teev tom qab kev tswj hwm. Tom qab ib qho qhov ncauj ntawm 75 mg, tshem tawm ib nrab-lub neej ntawm clopidogrel yog 6 teev. Ib nrab-lub neej ntawm cov tshuaj tseem ceeb hauv lub cev yog 8 teev tom qab ib zaug thiab rov ua dua.

Cov Tshuaj Pharmacogenetics. CYP2C19 yog kev koom tes hauv kev tsim cov tshuaj metabolite thiab nruab nrab metabolite, 2-oxo-clopidogrel. Pharmacokinetics thiab antiplatelet cuam tshuam ntawm cov nquag metabolite ntawm clopidogrel raws li ntsuas hauv platelet aggregation test exvivo, sib txawv raws qhov sib txawv ntawm CYP2C19.

CYP2C19 * 1 allele sib raug rau cov roj ntsha uas ua haujlwm tau zoo, thaum lub CYP2C19 * 2 thiab CYP2C19 * 3 alleles tsis ua haujlwm. Alleles CYP2C19 * 2 thiab CYP2C19 * 3 tus lej feem ntau rau cov alleles nrog kev txo qis hauv cov tawv nqaij dawb (85%) thiab Asians (99%) nrog cov metabolism hauv tsis txaus. Lwm cov alleles nrog ploj lossis txo qhov muaj nuj nqi suav nrog, ntawm lwm tus, CYP2C19 * 4, * 5, * 6, * 7 thiab * 8. Cov neeg mob uas ua rau lub cev qhov tsis ua haujlwm zoo yog cov nqa khoom ntawm ob lub cev tsis ua haujlwm. Raws li cov ntaub ntawv tshaj tawm, qhov ntau zaus ntawm qhov tshwm sim ntawm cov noob caj dab nrog qhov kev ua kom muaj cov metabolism tsawg ntawm CYP2C19 yog kwv yees li 2% hauv Caucasoid haiv neeg, 4% hauv haiv neeg Negroid thiab 14% hauv haiv neeg Mongoloid.

Qhov ntim ntawm cov kev tshawb fawb tau ua tsis txaus los tshawb pom qhov sib txawv hauv cov txiaj ntsig tau rau cov neeg mob uas tsis muaj cov kabmob clopidogrel metabolism.

Lub raum khiav tsis zoo. Qhov siab ntawm lub cev tseem ceeb ntawm cov ntshav sib xyaw ua ke hauv cov ntshav plasma thaum noj 75 mg ntawm clopidogrel ib hnub tau qis dua hauv cov neeg mob mob raum (tsim kom muaj kev tshem tawm ntawm 5 mus rau 15 ml / min) piv nrog cov neeg mob uas muaj creatinine tshem yog 30-60 ml / min thiab cov tib neeg noj qab nyob zoo. Nyob rau tib lub sijhawm, qhov cuam tshuam rau ADP-ua rau platelet sib sau ua ke rau cov neeg mob uas muaj lub raum mob siab tau raug txo qis (25%) piv nrog cov txiaj ntsig zoo hauv cov tib neeg muaj kev noj qab haus huv, lub sijhawm ntshav tau lengthened tib yam li cov neeg noj qab haus huv uas tau txais 75 mg clopidogrel ib hnub. Ib qho ntxiv, kev kuaj mob thev taus zoo rau txhua tus neeg mob.

Lub siab ua haujlwm tsis zoo. Hauv cov neeg mob uas muaj qhov tsis txaus siab hepatic txaus, thaum noj ib koob tshuaj txhua txhua hnub ntawm 75 ml ntawm clopidogrel rau 10 hnub, qhov ADP-vim kev tsim txom cov platelet aggregation zoo ib yam li cov neeg muaj kev noj qab haus huv. Qhov txhais tau tias nce rau hauv lub sijhawm los ntshav kuj tseem zoo sib xws ntawm ob pawg.

Kwv Txhiaj. Cov tshwm sim dhau los ntawm CYP2C19 alleles, uas ua rau muaj kev cuam tshuam hauv nruab nrab thiab cov metabolism tsis zoo uas cuam tshuam nrog CYP2C19, nws txawv ntawm cov haiv neeg lossis haiv neeg. Tsuas yog cov ntaub ntawv txwv txog cov neeg Asian tau muaj nyob rau hauv cov ntaub ntawv los txhawm rau soj ntsuam qhov tseem ceeb ntawm CYP caj ces rau cov txiaj ntsig kev soj ntsuam.

Cev xeeb tub thiab lactation

Cov kev tshawb fawb txog kev cuam tshuam ntawm clopidogrel ntawm kev xeeb tub hauv tsiaj txhu tsis muaj kev cuam tshuam tsis zoo rau kev xeeb tub, kev loj hlob ntawm tus menyuam / tus menyuam hauv plab, kev ua haujlwm thiab kev loj hlob tom qab.

Kev pub niam mis. Kuj tsis paub meej tias clopidogrel kis mus rau leej niam cov kua mis tau li cas. Kev tshawb fawb tsiaj muaj pov thawj tias cov tshuaj kis tau rau niam mis. Raws li kev ceev faj, kev pub mis niam yuav tsum tau tsum txiav thaum kho mob clopidogrel.

Txij li feem ntau cov tshuaj tau tawm hauv niam cov kua mis, thiab kuj tseem vim tias muaj peev xwm tsim cov kev tsis haum xeeb hauv cov menyuam mos uas noj niam mis, kev txiav txim siab kom tsis txhob siv cov tshuaj lossis tsis pub niam mis rau menyuam noj, muab qhov xav tau kho clopidogrel kev kho mob hauv leej niam.

Kev muaj me nyuam muaj nuj nqi. Hauv kev tshawb fawb tsiaj, clopidogrel tsis cuam tshuam rau kev ua me nyuam.

Tsuas tshuaj thiab tswj hwm

Clopidogrel yog npaj rau kev tswj hwm qhov ncauj ib hnub ib zaug, tsis hais txog ntawm cov khoom noj.

Koob tshuaj

Cov muaj hnub nyoog thiab cov neeg laus

Cov tshuaj ib txwm ib txwm noj yog 75 mg rau lub qhov ncauj ib hnub ib zaug.

Mob ntsws mob ntsws kas cees:

- mob hlab ntsha hlwb tsis muaj ntu nceST(tsis khov kho lub pob ntseg tsis khov los yog myocardial infarction tsis muaj ib qho hniav)Q): Clopidogrel kev kho mob yuav tsum tau pib nrog kev txhaj tshuaj ib zaug ntawm 300 mg, thiab tom qab ntawd txuas ntxiv nrog koob tshuaj 75 mg ib hnub ib zaug (nrog rau acetylsalicylic acid ntawm koob tshuaj 75-325 mg ib hnub). Nws tsis raug nquahu kom dhau ib koob tshuaj acetylsalicylic acid ntawm 100 mg, vim tias cov tshuaj ASA ntau dua yog cuam tshuam nrog kev pheej hmoo ntshav los ntshav. Qhov zoo tshaj plaws sijhawm ntawm kev kho mob tsis tau pom tseeb lub cev. Cov ntaub ntawv sim hauv tsev kho mob paub meej txog kev siv cov tshuaj rau 12 lub hlis, thiab cov txiaj ntsig siab tshaj plaws tau pom tom qab 3 lub hlis.

- mob myocardial infarction nrog ntu nceST: clopidogrel yog tshuaj ib hnub ib zaug ntawm kev txhaj tshuaj ntawm 75 mg siv kev pib thauj khoom ntawm 300 mg rau hauv kev sib xyaw nrog acetylsalicylic acid ua ke nrog lossis tsis muaj lwm yam thrombolytics. Rau cov neeg mob uas muaj hnub nyoog tshaj li 75 xyoos, kev kho tus mob clopidogrel 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 mob thiab pib tsawg kawg plaub lub lis piam. Cov txiaj ntsig ntawm kev sib xyaw ntawm clopidogrel nrog ASA tom qab plaub lub lis piam tsis tau kawm txog qhov no.

Atrial fibrillation: 75 mg clopidogrel ib hnub ib zaug. Txheeb ASA (75-100 mg / hnub) thiab txuas ntxiv noj nrog clopidogrel.

Thaum twg tsis txhaj koob tshuaj:

- tsawg dua 12 teev tom qab lub sijhawm niaj hnub ntawm kev tuaj yeem nkag: nws yog ib qho tsim nyog yuav tsum tau noj lub sijhawm tam sim ntawd, qhov tshuaj ntxiv yuav tsum noj nyob rau lub sijhawm sijhawm,

- Ntau dua 12 teev tom qab lub sijhawm dhau los ntawm kev txais neeg mob: koob tshuaj ntxiv yuav tsum noj nyob rau lub sijhawm teem sijhawm, yam tsis muaj ob zaug.

Menyuam yaus thiab tub ntxhais hluas

Kev nyab xeeb thiab ua tau ntawm clopidogrel nyob rau hauv cov pej xeem cov me nyuam yaus tseem tsis tau tsim.

Cov neeg mob uas lub raum tsis ua hauj lwm zoo

Cov kev paub ntawm kev kho cov neeg mob uas lub raum lub raum tsis ua haujlwm me me.

Cov neeg mob uas muaj lub siab ua haujlwm tsis zoo

Cov kev paub ntawm kev kho cov neeg mob uas muaj kab mob hauv lub siab nyob rau hauv uas hemorrhagic diathesis yog tau me me.

Kev tiv thaiv kev nyab xeeb

Kev los ntshav thiab hematologic phiv

Yog tias cov tsos mob hauv tsev kho mob tau tshwm sim thaum kev kho mob uas qhia pom kev txhim kho kev los ntshav thiab hematological, yuav tsum kuaj ntshav sai sai. Vim tias txoj kev pheej hmoo los ntshav ntau, yuav tsum ceev faj thaum ua haujlwm ntawm clopidogrel nrog warfarin.

Clopidogrel yuav tsum siv nrog ceev faj hauv cov neeg mob uas muaj feem yuav los ntshav txuam nrog kev raug mob, phais lossis lwm yam kab mob, nrog rau kev sib xyaw ntawm clopidogrel nrog acetylsalicylic acid, tsis-tshuaj steroidal anti-inflammatory tshuaj, suav nrog COX-2 inhibitors, heparin, glycoprotein inhibitors IIb / IIIa, xaiv serotonin reuptake inhibitors (SSRIs) lossis lwm yam tshuaj cuam tshuam nrog kev pheej hmoo los ntshav, xws li pentoxifylline. Ua tib zoo saib xyuas qhov tseeb ntawm cov tsos mob los ntshav, suav nrog kev tsis tau txog caij, yog tshwj xeeb tshaj yog nyob rau thawj lub limtiam ntawm kev kho thiab / lossis tom qab tus txheej txheem mob plawv lossis phais. Kev siv ua ke ntawm clopidogrel nrog tshuaj tiv thaiv qhov ncauj tsis pom zoo, vim tias qhov kev sib koom ua ke no tuaj yeem ua rau kom muaj ntshav ntau dua.

Yog hais tias muaj kev phais mob, yog tias siv tshuaj antiplatelet tsis tsim nyog, txoj kev kho mob nrog clopidogrel yuav tsum tau tsum tsis pub dhau 7 hnub ua ntej kev phais mob. Nws yog qhov yuav tsum tau qhia rau tus kws kho mob uas tuaj kawm thiab kws kho hniav txog kev noj cov tshuaj yog tias tus neeg mob yuav tsum tau mus phais lossis yog tus kws kho mob tau sau ntawv rau cov tshuaj tshiab rau tus neeg mob.

Clopidogrel yuav tsum siv nrog ceev faj hauv cov neeg mob uas muaj kev pheej hmoo los ntshav (tshwj xeeb tshaj tawm txoj hnyuv thiab lub plab). Thaum noj cov tshuaj clopidogrel, siv kev ceev faj txog kev siv tshuaj uas tuaj yeem ua rau muaj kab mob ntawm txoj hnyuv (piv txwv, acetylsalicylic acid thiab NSAIDs).

Koj yuav tsum nco ntsoov tias txij li txwv tsis pub los ntshav thaum noj clopidogrel (ib leeg lossis ua ke nrog ASA) yuav tsum muaj sijhawm ntxiv, koj yuav tsum qhia koj tus kws kho mob txog txhua kis tsis txawv (hauv thaj chaw thiab / lossis sijhawm) los ntshav.

Lub Tuam Txhab Ua Yeeb Yam (Thrombocytopenic Purpura)

Cov xwm txheej tsis tshua muaj mob ntawm thrombotic thrombocytopenic purpura (TTP) tom qab clopidogrel tau tshaj tawm. Qhov no tau pom los ntawm thrombocytopenia thiab microangiopathic hemolytic anemia ua ke nrog cov tsos mob ntawm lub paj hlwb, lub raum tsis ua haujlwm, lossis ua npaws. Kev loj hlob ntawm TTP tuaj yeem tsim kev puas tsuaj rau lub neej thiab tej zaum yuav tsum tau nqis tes ua haujlwm sai, suav nrog plasmapheresis.

Cov kab mob ntawm kev txhim kho cov neeg muaj kabmob hemophilia tau tshaj tawm tom qab noj clopidogrel. Nyob rau hauv rooj plaub ntawm kev pom zoo nce nyob rau hauv raug rho tawm ib feem thromboplastin lub sijhawm nrog lossis tsis los ntshav, qhov ntxim nyiam ntawm kev txhim kho cov neeg mob hemophilia yuav tsum raug txiav txim siab. Cov neeg mob uas tau kuaj pom tias muaj tus mob hemophilia yuav tsum tau saib xyuas thiab kho mob los ntawm cov kws tshaj lij, kev kho clopidogrel yuav tsum tsis ua ntxiv.

Vim tias cov ntaub ntawv tsis txaus, clopidogrel yuav tsum tsis txhob muab tshuaj rau thawj 7 hnub tom qab muaj mob ischemic mob stroke.

Hauv cov neeg mob uas txo qis kev ua haujlwm ntawm CYP2C19, clopidogrel hauv cov koob tshuaj pom zoo muab ib qho me me ntawm cov kev siv metabolite ntawm clopidogrel thiab muaj cov nyhuv antiplatelet qis dua. Cov neeg mob uas siv cov kev ua rau lub cev tsawg dua los ntawm kev muaj mob hlab ntsha hlwb lossis tus neeg uas tau ua haujlwm rau lub plawv thiab tau txais kev kho mob clopidogrel ntawm cov koob tshuaj pom zoo tej zaum yuav muaj kev pheej hmoo loj dua ntawm kev mob plawv dua li cov neeg mob uas ua haujlwm ntawm CYP2C19.

Txij li thaum clopidogrel metabolized rau cov tshuaj metabolite nyob rau ib feem los ntawm CYP2C19, nws cia siab tias cov tshuaj noj uas txwv qhov kev ua haujlwm ntawm enzyme no yuav ua rau txo qis tshuaj ntau ntxiv ntawm lub cev metabolite ntawm clopidogrel. Cov kab mob tseem ceeb ntawm qhov kev sib txuam no tsis tau kawm. Kev siv tib lub zog lossis hnyav CYP2C19 yuav tsum muab pov tseg.

Ceev faj yog yuav tsum muaj nyob rau hauv cov neeg mob uas tau txais concomitantly nrog clopidogrel tshuaj - substrates ntawm CYP2C8 isoenzyme.

Ua xua khaub lig-ua xua

Tus neeg mob yuav tsum muaj keeb kwm kev tiv thaiv tsis haum rau lwm cov thienopyridines (piv txwv li ticlopidine, prasugrel), vim tias muaj cov neeg paub txog kev ua xua cuam tshuam nrog thienopyridines. Cov neeg mob uas muaj keeb kwm kev tiv thaiv tsis haum rau lwm cov thienopyridines yuav tsum ua tib zoo saib thaum kho mob rau cov tsos mob ntawm tus mob hypersensitivity rau clopidogrel. Thienopyridines tuaj yeem ua rau txoj kev txhim kho ntawm kev ua xua ntawm kev ua kom txawv txav, xws li pob xoo, Quincke's edema, lossis rau hematological cross-reaction, xws li thrombocytopenia thiab neutropenia. Cov neeg mob uas muaj keeb kwm ua xua thiab / lossis hematological tsis haum rau ib qho thienopyridine yuav muaj kev pheej hmoo ntawm kev tsim kom zoo ib yam lossis txawv dua lwm tus thienopyridine.

Cov tshuaj muaj pes tsawg leeg suav nrog zas xim karmuazin (E-122), uas tuaj yeem ua rau muaj kev tsis haum.

Lub raum khiav tsis zoo

Txoj kev kho mob nrog clopidogrel hauv cov neeg mob uas lub raum lub raum tsis ua hauj lwm tsawg. Cov tshuaj yuav tsum tau siv hauv cov neeg mob nrog ceev faj.

Lub siab ua haujlwm tsis zoo

Clopidogrel yuav tsum tau siv nrog ceev faj hauv cov neeg mob uas muaj lub cev tsis txaus ua haujlwm, uas yuav ua rau hemorrhagic diathesis.

Cuam tshuam rau lub peev xwm tsav tsheb thiab lwm yam uas muaj peev xwm txaus ntshai. Clopidogrel tsis cuam tshuam lossis muaj qhov cuam tshuam me ntsis ntawm kev muaj peev xwm tsav tsheb thiab lwm yam txheej txheem.