Yuav siv cov tshuaj Lopirel li cas? > Kev khomob thiab kev tiv thaiv

Cov tshuaj tiv thaiv nquag xaiv xaiv inhibits cov ntawv cog lus molecule ADP nrog receptors nyob rau saum npoo platelet suavCov. Yog li, kev ua kom zoo ntawm lub complex GPIIb / IIIa thiab platelet aggregation ua tsis yooj yim sua. Ib yam ntxiv clopidogrel inhibits kev sib sau ua ke los ntawm lwm tus kev thaiv kevCov. Platelets tseem nyob puas thiab ua tsis tau txheej txheem kom txog rau thaum kawg ntawm lawv lub neej. kev sib sau ua ke.

Tom qab tau txais thawj cov tshuaj, cov tshuaj antithrombotic pib tshwm sim, theem ntawm leukocytes tau tsim los ntawm 3-7 hnub ntawm kev tswj hwm. Qhov nruab nrab, 5 hnub tom qab tsis ua tiav ntawm kev kho mob, platelet sib sau ua ke thiab lub sijhawm los ntshav rov qab los rau thawj qib.

Cov tshuaj yog zoo nkauj sai nkag rau hauv Kev kho mob txoj hnyuvCov. Txawm li cas los xij, cov concentration clopidogrelhauv ntshav muaj tsawg heev, nqus tau yog 50%. Cov tshuaj khi zoo rau cov ntshav plasma protein.

Clopidogrel yog metabolized hauv lub siab, txog 80% ntawm cov metabolites uas pom hauv plasma tsis tsaug zog. Nquag metabolite, uas muab qhov tsim nyog anti-aggregate kev txiav txim, tsim los ntawm kev tiv thaiv oxidation, cuam tshuam nrog isoenzyme ntawm cytochrome P450 - 2B6 thiab 3A4Cov. Lub metabolite nws tus kheej sai sai reacts nrog platelets thiab tsis kuaj pom nyob hauv cov ntshav ntshav.

Ib nrab-lub neej yog 6 teev rau cov tshuaj yeeb dej caw thiab 8 rau nws qhov nqus tsis tau. Cov khoom lag luam tsuas yog tso zis thiab quav.

Cov neeg uas raug mob los ntawm kev mob raum tsis ua haujlwm, txo qis hauv kev ua haujlwm ntawm cov tshuaj 25% piv nrog cov neeg muaj kev noj qab haus huv.

Kev taw qhia rau kev siv Lopirel

Cov tshuaj yog siv los tiv thaiv arterial thrombosis nyob rau hauv cov tib neeg kev txom nyem los ntawm mob huam:

Kuj qhia txog kev siv atherothrombotic cov nyom rau cov neeg mob uas tau ntsib myocardial infarction, mob strokemuaj peripheral arterial occlusion kab mobCov. Hauv qhov xwm txheej no, cov tshuaj siv tau los ua pov thawj.

Cov Yuav Tsum Muaj

Cov tshuaj tsis tau sau tseg:

nyob rau hauv loj daim siab ua hauj lwm,
poj niam cev xeeb tub thiab lactating,
ntawm hemorrhagic mob,
ntawm mob ntshav khov intracranial hemorrhage, mob rwjtsis-tshwj xeeb mob ncauj plab, mob ntsws hlav, tuberculosis thiab hyperfibrinolysis,
cov me nyuam hnub nyoog qis dua 18 xyoo
ntawm ua xua ntawm lub Cheebtsam ntawm cov tshuaj,
nrog intolerance galactose.

Ceev faj yuav tsum ua kom zoo thaum muaj sib xyaw nrog cov tshuaj acetylsalicylic acid, NSAIDs, heparin, thrombolytics, nrog lub raum thiab hepatic tsis txaus, ua ntej kev phais mob.

Lopirel, cov lus qhia rau kev siv (hom thiab qhov ntau npaum li cas)

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

Cov lus qhia rau kev siv Lopirel (75 mg)

Raws li txoj cai, nrog myocardial infarctionischemic mob stroke, cov neeg mob uas muaj mob ntshav tawm hauv cov qhov txhab nrog tshuaj yog 1 ntsiav tshuaj 1 zaug ib hnub.

Lub sijhawm nkag tom qab plawv nres - txij 1 mus rau 25 hnub, tom qab mob stroke - 7 hnub lossis 6 hli.

Yog tias tus neeg mobmob hlab ntsws txwv tsis pub rub tawm ST lossis tau tuav haujlwm mob ntshav cev, tom qab ntawd kev kho mob pib nrog ib koob tshuaj 300 mg, thiab tom qab ntawd 75 mg (ib ntsiav tshuaj) yog tshuaj ib hnub ib zaug rau 3 lub hlis (chav kawm yuav txuas ntxiv rau ib xyoos). Hauv cov kab mob zoo li no, raws li txoj cai, ntxiv rau tab siscetyl salicylic acidCov tshuaj pom zoo yog 100 mg.

Tso tawm daim ntawv thiab muaj pes tsawg leeg

Lopirel yog muaj nyob rau hauv daim ntawv ntawm cov ntsiav tshuaj hauv cov plhaub zaj duab xis: puag ncig, biconvex, paj yeeb, nrog ib qho "Kuv" sau rau ntawm ib sab (7 lossis 10 ntsiav tshuaj hauv cov hlwv pob: hauv pob ntawv los ntawm 1, 2, 4 lossis 8 hlwv, 7 ntsiav tshuaj lossis 1, 2, 3, 5, 6, 9 lossis 10 hlwv rau 10 ntsiav tshuaj, hauv ib pob ntawv cardboard rau lub tsev kho mob 10, 20, 30 lossis 40 lub hlwv).

1 ntsiav tshuaj ntawm Lopirel muaj:

cov tshuaj nquag: clopidogrel - 75 mg,
tus neeg mob: microcrystalline cellulose, lactose, talc, glyceryl dibehenate, crospovidone (hom A),
plhaub: Opadry II 85G34669 Paj yeeb talc, polyvinyl cawv, macrogol 3350, titanium dioxide (E171), zas hlau oxide liab (E172), lecithin (E322).

Mechanism ntawm kev ua

Clopidogrel belongs rau cov qeb ntawm prodrugs. Ib qho ntawm nws cov tshuaj tiv thaiv yog ib qho ua kom muaj zog ntawm cov platelet aggregation: inhibits qhov khi ntawm adenosine diphosphate (ADP) thiab P2Y₁₂platelet receptor ua raws li ADP-mediated kev ua haujlwm ntawm txoj haujlwm ntawm glycoprotein IIb / IIIa, uas ua rau kev saib tsis taus ntawm platelet sib sau ua ke. Ib qho tsis paub tseeb uas yuav tiv thaiv kab mob ua rau platelets yuav tsis muaj zog rau ADP kev xav thoob plaws hauv lawv lub neej (kwv yees li 7-10 hnub). Kev ua haujlwm qub ntawm platelets yog rov qab nyob ntawm qhov ceev ntawm lawv cov hloov kho tshiab.

Cov tshuaj kuj tseem txwv tsis pub platelet sib sau los ntawm agonists lwm yam tshaj li ADP. Kev tsim cov tshuaj metabolite nquag tshwm sim los ntawm kev ua ntawm isoenzymes ntawm system P₄₅₀, thiab vim tias qee qhov isoenzymes yuav txawv hauv polymorphism lossis raug txwv los ntawm lwm cov tshuaj, tsis yog txhua tus neeg mob muaj qhov txaus inhibition ntawm platelet aggregation.

Cov chaw muag tshuaj

Kev noj tshuaj txhua hnub ntawm clopidogrel ntawm koob tshuaj 75 mg muab qhov tseem ceeb ntawm ADP-ntxias cov platelet aggregation los ntawm thawj hnub ntawm kev tswj hwm. Maj mam, dhau ntawm 3-7 hnub, kev kawm paub txog kev tsim txom nce ntxiv, mus txog ib qib theem tom qab tau ncav cuag lub xeev qhov sib npaug. Thaum noj tshuaj rau txhua hnub ntawm 75 mg rau hauv kev sib npaug, platelet aggregation yog suppressed los ntawm 40-60%. Nyob rau ntawm 5 hnub tom qab txiav cov tshuaj, cov sijhawm los ntshav thiab platelet sib xyaw maj mam rov qab mus rau theem pib.

Clinical Efficiency / Safety

Clopidogrel tiv thaiv kev txhim kho ntawm atherothrombosis hauv txhua qhov chaw ntawm atherosclerotic vascular txhab (piv txwv li, nrog cov qhov txhab ntawm txoj hlab ntshav, hlab leeg lossis hlab hlwb).

Hauv ACTIVE-A cov chaw sim, nws tau qhia tias yog muaj atrial fibrillation hauv cov neeg mob uas muaj ib lossis ntau qhov kev pheej hmoo rau vascular mob tab sis tuaj yeem siv cov anticoagulants tsis ncaj, kev sib xyaw ntawm clopidogrel thiab acetylsalicylic acid (piv rau acetylsalicylic acid monotherapy) txo cov zaus ua ke coj myocardial infarction, mob hlab ntsha tawg, lub cev muaj zog thromboembolism sab nraum lub hauv nruab nrab lub paj hlwb lossis txoj hlab ntshav tuag, feem ntau vim yog qhov txo qis hauv kev pheej hmoo ntawm mob hlab ntsha tawg. Qhov ua tau zoo ntawm kev tswj hwm ntawm clopidogrel thiab acetylsalicylic acid tau qhia nws tus kheej thaum ntxov thiab mob siab rau 5 xyoo. Qhov kev txo qis ntawm qhov muaj feem yuav ua rau muaj kev mob ntshav siab ntau rau cov neeg mob noj acetylsalicylic acid thiab clopidogrel feem ntau yog muab los ntawm kev txo qis ntau zaus hauv cov cwj nrag. Thaum kho nrog cov tshuaj no, kev pheej hmoo ntawm mob hlab ntsha tawg ntawm txhua qhov hnyav tau raug txo qis, tseem muaj ib qho kev xav ntawm qhov tshwm sim ntawm myocardial infarction, tab sis tsis muaj qhov sib txawv ntawm qhov ntau zaus ntawm thromboembolism sab nraud lub hauv paus ntawm lub paj hlwb lossis vascular tuag. Nrog rau qhov no, noj clopidogrel thiab acetylsalicylic acid txo lub sijhawm pw hauv tsev kho mob tag nrho rau cov neeg mob uas muaj teeb meem ntawm cov hlab plawv.

Xuas

Xws li nrog ib zaug, thiab nrog ib chav kawm ntawm clopidogrel ntawm koob tshuaj ntawm 75 mg rau ib hnub, cov tshuaj quav tau nrawm heev. Hauv nruab nrab, qhov siab tshaj plaws ntawm kev hloov pauv tsis tau clopidogrel hauv cov ntshav ntshav tau mus txog kwv yees li 45 feeb tom qab kev tswj hwm qhov ncauj thiab thaj tsam li ntawm 2.2 txog 2.5 ng / ml. Qhov nqus ntawm clopidogrel los ntawm ob lub raum (raws li kev pom ntawm nws cov khoom noj khoom haus) muaj tsawg kawg yog 50%.

Kev zom zaub mov

Cov tshuaj nquag muaj sia nyob hauv lub siab. Hauv vivo thiab hauv vitro, clopidogrel metabolized nyob rau hauv ob txoj kev: ntawm esterase ua raws li los ntawm hydrolysis, uas ua rau muaj kev tsim lub zog tsis ua haujlwm ntawm carboxylic acid (85%) los ntawm cov metabolites uas nthuav tawm hauv cov kev ncig mus rau hauv cytochrome P system₄₅₀.

Thaum pib theem, clopidogrel yog metabolized rau ib nrab metabolite - 2-oxoclopidogrel. Cov metabolism tom qab ntawm oxoclopidogrel ua rau pom kev ntawm lub cev metabolite, thiol derivative ntawm clopidogrel. Qhov no nyob rau hauv vitro metabolic pathway tshwm sim nrog kev koom tes ntawm isoenzymes CYP2C19, CYP3A4, CYP2B6, thiab CYP1A2. Lub nquag thiol metabolite cais nyob rau hauv vitro irreversibly thiab sai khi rau platelet receptors, inhibiting lawv cov kev sib sau tag.

Thaum muab ib zaug ntawm clopidogrel ntawm koob tshuaj 300 mg, qhov siab tshaj plaws ntawm lub cev cov metabolite yog ob zaug ntau dua li thaum noj cov tshuaj txij nkawm ntawm clopidogrel 75 mg rau 4 hnub. Qhov siab tshaj plaws ntawm kev nquag metabolite ntawm clopidogrel tau teev cia 0.5-1 teev tom qab noj tshuaj.

Hauv tib neeg, tom qab lub qhov ncauj tswj hwm ntawm 14 C-daim ntawv lo clopidogrel rau 120 teev, kwv yees li 46% ntawm lub xov tooj cua yog tawm los ntawm txoj hnyuv thiab kwv yees li 50% ntawm kev zom zaws yog tawm los ntawm ob lub raum. Tom qab txhaj ib zaug ntawm clopidogrel ntawm ib koob ntawm 75 mg, ib nrab-lub neej yog kwv yees li 6 teev. Nrog rau ib qho koob tshuaj thiab rov qab noj tshuaj ntau zaus, ib nrab-lub neej ntawm lub cev tsis muaj zog nyob rau hauv cov ntshav yog li 8 teev.

Cov Tshuaj Pharmacogenetics

Cov nquag metabolite ntawm clopidogrel thiab cov tshuaj nruab nrab ntawm lub cev 2-oxoclopidogrel tau tsim los siv isoenzyme CYP2C19. CYP2C19 isoenzyme genotype cuam tshuam rau cov nyhuv antiplatelet thiab pharmacokinetics ntawm lub zog nquag thaum lub sijhawm ua haujlwm ex vivo platelet aggregation kawm.

Tag nrho cov caj ces ntawm CYP2C19 * 1 lub cev sib raug rau cov roj ntsha uas ua haujlwm tau zoo, thiab cov pawg ntawm CYP2C19 * 3 thiab CYP2C19 * 2 noob tsis ua haujlwm thiab ua rau cov metabolism hauv feem ntau ntawm cov neeg sawv cev ntawm Mongoloid (99%) thiab Caucasoid (85%). Lwm cov alleles uas ua rau txo qis lossis tsis muaj metabolism (suav nrog tab sis tsis txwv rau txhua tus ntawm CYP2C19 * 4, * 5, * 6, * 7, * 8 noob) muaj tsawg dua. Cov neeg mob uas ua kom lub cev tsis muaj zog yuav tsum muaj ob qhov cim ntawm cov gene nrog poob haujlwm. Raws li cov ntaub ntawv luam tawm, ntau zaus ntawm phenotypes ntawm cov tsis muaj zog CYP2C19 metabolizers hauv cov tib neeg ntawm cov haiv neeg Negroid yog 4%, Caucasoid haiv neeg - 2%, thiab Suav - 14%.

Txheeb tshuaj pharmacokinetics thiab antiplatelet nyhuv thaum noj thawj zaug ntawm clopidogrel 300 mg thiab nws qhov kev noj tshuaj txuas ntxiv ntawm 75 mg rau ib hnub, zoo li thaum noj thawj zaug ntawm clopidogrel 600 mg thiab nws qhov kev noj tshuaj txuas ntxiv ntawm 150 mg rau ib hnub rau 5 hnub (kom txog thaum sib luag lawm ) ib qho kev tshawb nrhiav ntu tau koom nrog 40 tus neeg ua haujlwm pub dawb hauv 4 pab pawg ntawm 10 tus neeg nrog 4 pawg ntawm CYP2C19 isoenzyme (ultrafast, khaus, qaug zog lossis nruab nrab ntawm cov tshuaj tiv thaiv). Yog li ntawd, nyob rau hauv kev ua haujlwm ntev, nruab nrab, thiab ultrafast metabolizers, tsis muaj qhov sib txawv hauv kev cuam tshuam ntawm cov nquag metabolite, nrog rau cov txiaj ntsig nruab nrab ntawm kev txwv tsis pub platelet aggregation (ntxias cov ADP). Kev cuam tshuam ntawm cov metabolite nquag hauv cov tshuaj tiv thaiv kab mob uas tsis muaj zog hauv kev sib piv nrog cov tshuaj tiv thaiv kom hnyav dua li 63 decreased71%. Xws li 300 mg / 75 mg regimen, cov nyhuv antiplatelet ntawm cov tshuaj tiv thaiv tsis muaj zog poob qis nrog qhov nruab nrab platelet aggregation inhibition qhov tseem ceeb, uas tau yog 24% (tom qab 24 teev) thiab 37% (nyob rau hnub 5) piv nrog lub txiaj ntsig platelet aggregation inhibition nyob rau hauv kev siv zog (39% - tom qab 24 teev thiab 58% - nyob rau 5 hnub) thiab nruab nrab (37% - tom qab 24 teev thiab 60% - nyob rau hnub 5) metabolizers. Hauv kev siv cov phiaj xwm 600, CYP2C19 * 1 gene allele muab qhov ua haujlwm tag nrho mg / 150 mg metabolism, qhov kis tau ntawm cov nquag metabolite hauv cov tshuaj tiv thaiv kab mob uas tsis muaj zog tau siab dua nrog lub phiaj xwm 300 mg / 75 mg. Qhov txhais tau hais tias platelet aggregation inhibition yog 32% (tom qab 24 teev) thiab 61% (nyob rau hnub 5), uas ntau dua tus nqi rau 300 mg / 75 mg regimen, tab sis zoo li pawg neeg ntawm cov neeg mob uas tau nce CYP2C 19- cov metabolism, uas tau txais kev kho mob raws li cov txheej txheem 300 mg / 75 mg. Nws yuav tsum raug sau tseg tias hauv txoj kev tshawb fawb, suav txog qhov tshwm sim hauv tsev kho mob rau cov neeg mob ntawm pab pawg no, ntau npaum li cas cov tshuaj clopidogrel tsis tau tsim.

Kev tsom xam txog ntawm 6 qhov kev tshawb nrhiav, uas suav nrog cov ntaub ntawv los ntawm 335 tus neeg ua haujlwm pab dawb uas tau txais clopidogrel thiab tseem nyob hauv lub xeev kev sib npaug ntawm lub cev, qhia tau hais tias qhov kev cuam tshuam ntawm cov metabolite nquag nyob hauv cov roj ntsha tsis muaj zog tau txo 72%, thiab hauv nruab nrab lub cev sib xyaw - los ntawm 28%, txawm hais tias tus nqi nruab nrab ntawm kev cuam tshuam ntawm platelet aggregation tau txo qis hauv kev sib piv nrog cov tshuaj tiv thaiv zoo tshaj plaws los ntawm 21.4 thiab 5.9%, feem.

Cov kev sib raug zoo ntawm CYP2C19 lub cev thiab cov txiaj ntsig kev soj ntsuam hauv cov neeg mob tau txais clopidogrel tsis tau raug soj ntsuam hauv kev cia siab, tswj hwm, sim kev sim, txawm li cas los xij, los txog rau hnub no, muaj ntau yam kev tshuaj ntsuam yav dhau los. Cov ntaub ntawv tshaj tawm los ntawm ob peb qhov kev kawm ua ke, nrog rau cov txiaj ntsig ntawm genotyping hauv kev tshawb fawb soj ntsuam: CHARISMA (n = 2428), CURE (n = 2721), TRITON-TIMI 38 (n = 1477), KEV KAWM-TIMI 28 (n = 227), ACTIVE- A (n = 601).

Peb qhov kev kawm ua ke (Giusti, Collet, Sibbing) thiab kev tshawb nrhiav chaw kho mob TRITON-TIMI 38 hauv cov neeg mob ntawm cov pab pawg sib xyaw nrog cov tsis muaj zog thiab nruab nrab ntawm cov metabolism tau sau tseg tias muaj kev pheej hmoo ntawm cov hlab plawv (myocardial infarction, mob stroke, tuag) lossis stent thrombosis piv rau cov zoo sib xws cov ntaub ntawv hais txog cov tshuaj tiv thaiv lub cev muaj zog.

Hauv Simon txoj kev kawm cohort thiab CHARISMA txoj kev tshawb nrhiav, qhov muaj zog ntau dua ntawm cov kev mob plawv tau qhia tsuas yog hauv cov metabolizers tsis muaj zog (thaum piv nrog mob siab).

Hauv kev kawm txog Trenk cohort thiab qhov tsis paub tseeb, CURE, ACTIVE-A cov kev tshawb fawb, tsis muaj kev koom tes ntawm cov hlab plawv mob nrog qhov kev siv ntawm CYP2C19 metabolism.

Cov kev tshawb fawb soj ntsuam tau ua rau hnub tim muaj qhov piv txwv me me tsis txaus los tshawb xyuas qhov sib txawv hauv cov chaw kho mob hauv cov neeg mob uas tsis tshua muaj CYP2C19 isoenzyme kev ua si.

Chaw Kho Mob Tshwj Xeeb

Lub pharmacokinetics ntawm lub cev sib nqus ntawm clopidogrel rau cov pab pawg ib leeg tsis tau kawm.

Hauv cov kev tshawb fawb txog cov neeg laus tuaj pab dawb (tshaj 75 xyoo), piv nrog cov ntaub ntawv ntawm cov tub ntxhais hluas tuaj yeem pab dawb, qhov sib txawv ntawm cov sijhawm los ntshav thiab platelet sib xyaw tsis tau. Rau kev kho mob ntawm cov neeg laus laus, tsis tas yuav hloov kho Lopirel.

Lub chaw muag tshuaj ntawm clopidogrel hauv cov neeg mob hnub nyoog qis dua 18 xyoo tsis tau kawm.

Hauv lub raum ua puas (nrog creatinine tshem tawm ntawm 5 mus rau 15 ml / min) vim los ntawm kev rov qab siv clopidogrel ntawm ib koob tshuaj ntawm 75 mg rau ib hnub, qhov tseem ceeb ntawm pib ntawm ADP-ntxias cov platelet sib sau tau 25% qis dua qhov ntawd hauv cov neeg ua haujlwm noj qab haus huv, txawm li cas los xij, lub sijhawm los ntshav tseem nyob zoo ib yam li qhov ntsuas no rau cov neeg ua haujlwm noj qab haus huv uas tau txais koob tshuaj clopidogrel 75 mg ib hnub. Cov tshuaj tau pom zoo zoo los ntawm txhua tus neeg mob.

Hauv kev mob siab rau daim siab uas yog los ntawm kev noj clopidogrel ntawm ib koob tshuaj ntawm 75 mg rau ib hnub twg rau 10 hnub, qhov kev txiav txim siab ntawm ADP-pliaj platelet aggregation zoo ib yam li cov neeg ua haujlwm pab dawb noj qab haus huv.Ob pawg neeg ntawd kuj tau sib piv nyob rau lub sijhawm uas los ntshav.

Qhov dav dav ntawm cov tsiaj me ntawm CYP2C9 isoenzyme noob, uas yog lub luag haujlwm txo qis thiab nruab nrab ntawm cov metabolism, nws txawv ntawm cov neeg sawv cev ntawm ntau pawg sib txawv. Rau cov neeg sawv cev ntawm haiv neeg Mongoloid, muaj qhov tsawg tsawg ntawm cov ntaub ntawv keeb kwm uas tsis tso cai ntsuas kev ntsuas ntawm cov ntsiab lus tseem ceeb ntawm CYP2C19 isoenzyme txog kev txhim kho ischemic cov teeb meem.

Pharmacological kev txiav txim

Cov tshuaj sib xyaw ua ke ntawm cov tshuaj Lopirel xaiv yam tsis haum rau txoj hlua khi ntawm ADP molecule rau cov receptors nyob rau saum npoo ntawm platelets. Yog li, kev ua kom zoo ntawm GPIIb / IIIa complex thiab platelet aggregation ua tsis yooj yim sua. Clopidogrel tseem ua rau cov txheej txheem sib sau ua ke los ntawm lwm cov kev tawm tsam. Txog rau thaum xaus ntawm lub neej ua haujlwm, platelets tseem nyob puas thiab tsis muaj peev xwm ntawm kev sib sau ua ke.

Cov tshuaj yog yooj yim zoo nkauj nyob rau hauv lub plab zom mov. Txawm li cas los xij, kev mloog zoo ntawm clopidogrel hauv plasma tsawg heev, qhov nqus tau yog 50%. Cov tshuaj khi zoo rau cov ntshav plasma protein.

Clopidogrel yog metabolized hauv lub siab, txog 80% ntawm cov metabolites uas pom hauv plasma tsis tsaug zog. Kev nquag metabolite, uas muaj cov nyhuv tsim nyog antiaggregatory, yog tsim los ntawm cov tshuaj tiv thaiv oxidation, nrog kev koom tes ntawm cytochrome P450 isoenzyme 2B6 thiab 3A4. Lub metabolite nws tus kheej ceev nrooj nrog platelets thiab tsis pom muaj ntshav hauv cov ntshav ntshav.

Ib nrab-lub neej yog 6 teev rau cov tshuaj yeeb dej caw thiab 8 rau nws qhov nqus tsis tau. Cov khoom lag luam tsuas yog tso zis thiab quav.

Cov neeg uas raug mob los ntawm kev mob raum tsis ua haujlwm, txo qis hauv kev ua haujlwm ntawm cov tshuaj 25% piv nrog cov neeg muaj kev noj qab haus huv.

Cov lus qhia rau kev siv

Lopirel ntsiav tshuaj yuav tsum tau noj ntawm qhov ncauj, tsis hais txog kev noj zaub mov.

Cov neeg mob uas tau mob stroke ischemic / myocardial infarction lossis tus neeg mob peripheral leeg yuav tsum noj 75 mg ib hnub ib zaug. Tom qab lub plawv nres, txoj kev kho mob pib txij li thawj hnub thiab kav txog 35 hnub, thiab tom qab mob stroke - los ntawm 1 lub lis piam mus txog 6 hli.

Nyob rau ntawm qhov muaj mob voos mob hnyav yam tsis muaj ST ntu theem (nrog rau cov neeg mob stenting thaum mob sib luag nrog txoj kev cuam tshuam), txoj kev kho yog pib nrog kev thauj khoom ntawm 300 mg (siv ib zaug), thiab tom qab ntawd lawv hloov mus rau 75 mg ntawm 24 teev hauv 1 koob tshuaj (ua ke nrog acetylsalicylic acid hauv kev siv tsis tau saum toj no 100 mg). Txoj kev kawm ntev txog li 1 xyoos.

Hauv kev mob ntshav siab sai nrog tus kabmob ST ntu nce qib (hauv kev sib xyaw nrog tshuaj aspirin thiab thrombolytic), cov ntsiav tshuaj tau sau ib zaug hauv koob tshuaj 75 mg rau 24 teev rau 1 daim ntawv thov nrog kev siv thawj zaug thauj khoom (ib zaug, nrog thrombolytics thiab tshuaj aspirin). Txoj kev kho yuav pib sai li sai tau thiab txuas ntxiv rau 1 lub hlis tsawg kawg. Cov chaw thau khoom noj tom qab lub hnub nyoog 75 xyoo tsis siv.

Sab sij huam

lymphatic thiab circulatory systems: ua haujlwm tsis xws luag - eosinophilia, leukopenia, thrombocytopenia, tsis tshua muaj neutropenia (suav nrog neutropenia loj), mob tsis tshua muaj kab mob ntshav siab, ua tsis taus pa, thrombotic thrombocytopenic purpura, agranulocytosis, pancytopenia, mob ntshav qab zib ntau, mob txhab, mob ua ke
kev tiv thaiv kab mob: tsis tshua muaj tshwm sim - anaphylactoid kev tsis haum, mob ntshav siab, tsis paub ntau npaum li cas - kev loj hlob ntawm cov kev cuam tshuam ntawm hypersensitivity nrog thienopyridines (piv txwv li, nrog ticlopidine thiab prasugrel),
musculoskeletal thiab cov ntaub so ntswg mob sib txuas: tsis tshua muaj mob - mob caj dab, mob hemarthrosis (mob hauv cov leeg musculoskeletal), myalgia, arthralgia,
cov hlab ntsha hauv lub cev: tsis tuaj yeem - mob taub hau, mob ntshav khov (qee qhov mob yuav ua rau tuag taus), kiv taub hau, mob caj dab, tsis tshua muaj tshwm sim - saj tsis xis nyob,
daim tawv nqaij thiab cov nqaij mos subcutaneous: feem ntau - bruising, tsis xws luag - khaus, tawm pob, purpura, tsis tshua muaj tshwm sim - mob caj dab, mob nqaij daim tawv nqaij mob (erythema multiforme, Stevens-Johnson syndrome, tshuaj lom epidermal necrolysis), tshuaj tiv thaiv kab mob siab, mob caj dab lossis ua kom tawm pob. xoo pob mob nrog cov tsos mob ntawm lub cev thiab eosinophilia, urticaria, lichen planus, eczema,
lub zeem muag: ntuag - qhov muag pom kev tsis haum (hauv qhov nqaij ntawm lub qhov muag, pom, retina),
mob siab thiab mob txeeb zig: muaj tsawg kawg - kab mob siab, mob siab tsis ua hauj lwm, kuaj ntshav kuaj ntshav ntawm lub xeev kev ua haujlwm,
cov kev tshawb nrhiav khoom siv thiab kev kuaj sim: qog ua ntu zus - txo qis ntawm neutrophils, nce ntxiv hauv lub sijhawm los ntshav, txo qis hauv platelets,
kev cuam tshuam ntawm thaj chaw txhaj tshuaj thiab cov teeb meem dav dav: feem ntau - los ntshav los ntawm qhov chaw hno, tsis tshua muaj - kub taub hau,
hnov: tsis tshua muaj - vertigo,
psyche: tsis tshua muaj - tsis meej pem, pomzoo,
lub plab zom mov: feem ntau ua rau mob plab zom mov, plab zom mov los ntshav, dyspepsia, mob plab, mob plab hnyuv, mob plab thiab duodenal mob, xeev siab, ntuav, ua tsis taus pa, cem quav, tsis tshua muaj retroperitoneal los ntshav, tsis tshua muaj retroperitoneal thiab mob plab hnyuv. ua kom mob plab hnyuv tawm hauv plab, mob plab (suav nrog lymphocytic lossis mob ua paug), mob ua paug, mob plab,
cov kab mob ua pa: feem ntau - txhaws ntswg, tsis tshua muaj - bronchospasm, los ntshav los ntawm cov kab mob ua pa (mob ntsws, hemoptysis), mob ntsws o, mob ntsws, mob plab hnyuv pneumonitis,
ob lub raum thiab lub raum tso zis: tsis tu ncua - hematuria, tsis tshua muaj heev - kev nce siab hauv cov concentration ntawm creatinine hauv cov ntshav, glomerulonephritis,
cov hlab ntshav: feem ntau - hematomas, tsis tshua muaj tshwm sim - los ntshav los ntawm kev ua haujlwm zoo, los ntshav ntau, txo ntshav siab, vasculitis.

Cov lus qhia tshwj xeeb

Daim siab ua haujlwm: rau qib siab - nrog kev ceev faj, hauv qhov hnyav - nws yog contraindicated.

Kev overdose yog tus cwj pwm los ntawm kev nce rau hauv lub sijhawm los ntshav. Hauv cov mob no, kev kho mob muaj nyob rau ntawm qhov hloov ntshav ntawm platelet ntau, vim tias tsis muaj tshuaj los tiv thaiv.

Cov mob uas los ntshav ntau heev thaum lub sijhawm tib lub sijhawm siv nrog Lopirel acetylsalicylic acid, ntxiv rau heparin, tau sau tseg.
Raum tsis ua haujlwm: kev kho mob yog nqa tawm nrog ceev faj nrog mob pes tsawg.
Kev ceev faj yog qhov tseem ceeb hauv cov neeg mob uas muaj feem yuav muaj ntshav ntuav ntau yam los yog siv qee yam tshuaj kho.
Hauv cov txheej txheem phais mob, thaum siv tshuaj tiv thaiv antiplatelet tsis tsim nyog, qhov kev kawm raug tso tseg 1 lub lis piam ua ntej hnub kev phais.
Cov neeg mob yuav raug soj ntsuam tas mus li rau qhov uas los ntshav.
Tsav tsheb thauj khoom thiab cov cuab yeej siv: tsis cuam tshuam.
Clopidogrel muaj lub peev xwm los tiv thaiv kev ua si ntawm CYP2C9 isoenzyme, yog li muaj kev pheej hmoo hauv kev nce ntshav ntxiv ntawm tolbutamide thiab phenytoin. Ua ke cov thawj coj ntawm cov neeg sawv cev nrog Lopirel no nyab xeeb.
Tus neeg mob yuav tsum paub tias lub sijhawm ua haujlwm ntawm cov ntshav los ntau ntxiv, yog li tus kws kho mob yuav tsum paub txog kev kho.
Hauv cov mob ischemic stroke, cov tshuaj tsis pom zoo siv (tsawg dua 1 lub lim tiam).
Hnub nyoog qis dua 18 xyoo, txwv tsis pub siv tshuaj rau lwm tus.
Hauv kev kho mob ntawm cov neeg mob uas muaj tus kab mob myocardial infarction (nrog rau qhov nce hauv ntu ntawm ST), kev kho mob tsis pib hauv thawj ob peb hnub tom qab tau tsim myocardial infarction.

Nyob rau hauv kis ntawm los ntshav, ntshav thiab lub siab ua haujlwm saib xyuas.

Yeeb tshuaj sib cuam tshuam

Cov tshuaj tuaj yeem ua ke nrog atenolol, phenobarbital, estrogens, cimetidine lossis nifedipine.

Nws ua pov thawj tias kev noj tshuaj Acetylsalicylic acid txhua hnub (txog 1000 mg rau ib hnub) thiab clopidogrel tsis cuam tshuam rau qhov zoo ntawm cov tshuaj no. Txawm li cas los xij, lub sijhawm ua haujlwm ntawm kev tswj hwm ntawm cov tshuaj no yuav tsum tsis pub ntau dua 1 xyoos (kev saib xyuas yuav tsum tau noj).

Thaum ua ke nrog cov tshuaj tiv thaiv kab mob hauv qhov ncauj, tshwj xeeb yog cov tshuaj warfarin, qhov ntxim nyiam tshwm sim thiab lub sijhawm ntshav los ntau dua.
Kev sib xyaw ntawm cov tshuaj nrog thrombolytics kuj tsis pom zoo, vim tias kev nyab xeeb ntawm kev sib txuam no tsis tau tsim tshwj xeeb.
Txawm hais tias muaj txiaj ntsig zoo ntawm kev tshawb fawb soj ntsuam ntawm kev sib cuam tshuam ntawm cov tshuaj nrog heparin, ceev faj yuav tsum tau siv thaum coj lawv ib txhij.
Hauv cov tib neeg muaj kev pheej hmoo los ntshav ntau thiab noj Lopirel, nws tsis pom zoo ntxiv rau kev noj ntshav glycoprotein IIb / IIaa inhibitors.
Tej zaum ua ke ntawm cov tshuaj nrog digoxin, theophylline, antacids.

Cov tshuaj inhibits cov metabolism hauv cov tshuaj uas nws cov pharmacokinetic tsis haum nyob rau CYP2C9 isoenzyme. Hauv qee yam, ib qho tshuaj yuav ua rau lub plasma concentration ntawm phenytoin thiab tolbutamide ntxiv. Kev saib xyuas yuav tsum ua.

Nws yog qhov tseeb tias kev sib xyaw ntawm clopidogrel - naproxen ntau qhov kev pheej hmoo ntawm kev txhim kho latent gastrointestinal los ntshav. Txawm li cas los xij, nyob rau hauv cov ntaub ntawv ntawm lwm tus NSAIDs, cov qauv no tsis tau muab pov thawj. Hauv qhov no, nrog kev sib txuam ntawm cov tshuaj no yuav tsum tau ceev faj.

Cov tshuaj ntawm cov tshuaj Lopirel

Tus qauv txiav txim siab pom cov qauv analogues:

Plavix,
Aggregal
Sylt,
Fluder,
Fagot,
Rhuav tshem
Deplatt 75,
Thromborel,
Detrombe
Plaglir,
Cardutol,
Lub Hom Phiaj
Klopilet,
Clapitax
Clopidogrel,
Lirta
Sauab 75,
Egithromb,
Cardogrel
Lopirel
Tus npau taws,
Klopirel.

Cov pab pawg ntawm cov neeg ua haujlwm antiplatelet suav nrog analogues:

Phasostable
Aggregal
Pentilin
Agrenox
Ayferol
Thromborel,
Clopidogrel,
Clapitax
Cardutol,
Parsedil
Tshuaj Hlawv
Lirta
Agrilin,
Lopirel
Tiklo
Aklotin,
Curantyl
Rhuav tshem
Pentomere
Pawxia
Methylethylpyridinol,
Klopilet,
TXHEEJ TXHEEM
Radomin
Brilinta
Fluder,
Lub Hom Phiaj
Cardiomagnyl
Thromboreductin,
Cardioxypine
Eifitol
Acetylsalicylic acid
Trental
Coplavix,
Vixipin
Agapurin
Doksilek,
Akonol,
Mob siab
Emoxibel
Klopirel,
Alprostan,
Kev tsis meej pem
Ginkio
Aspinat
Colpharite
Ginos
Emoxipin
Ibustrin
Tiklid,
Mikristin
Fagot,
Pentoxifylline
Tagren
Plavix,
Cilostazol
Sauab 75,
Monafram
Vajtswv
Muse
Laspalas
Ticagrelor,
Xanthinol Nicotinate,
Pentamon
Ralofect,
Cardogrel
Thrombital
Ventavis.

Noj ntau dhau

Nrog kev siv tshuaj ntau dhau, qhov nce ntawm lub sijhawm los ntshav thiab txuas ntxiv rau lub dag zog yog qhov muaj peev xwm ua tau.

Kev Kho - raws li cov tsos mob.

Tshwj xeeb tshuaj tiv thaiv kab mob cov tshuaj tsis muaj. Hauv cov xwm txheej hnyav, kev txiav tawm cov tshuaj los ntawm kev hloov ntshav rau tus neeg raug mob yog ua tau. platelet pawg.

Kev sib txuam

Thaum muab sib xyaw nrog tshuaj tiv thaiv qhov ncaujhauv tshwj xeeb warfarin, qhov ntxim nyiam tshwm sim thiab lub sijhawm los ntshav ntxiv.

Hauv cov neeg uas muaj kev pheej hmoo ntshav los ntshav ntau dua thiab noj Lopirel, nws tsis pom zoo kom noj ntxiv glycoprotein IIb / IIІa inhibitors.

Pov thawj ua ke clopidogrel – naproxen nce txoj kev pheej hmoo ntawm mob ntshav tawm hauv plab tsis txaus. Txawm li cas los xij, hauv rooj plaub ntawm lwm tus NSAIDs xws li tus qauv tsis tau muab pov thawj. Hauv qhov no, nrog kev sib txuam ntawm cov tshuaj no yuav tsum tau ceev faj.

Txawm tias muaj txiaj ntsig zoo ntawm kev tshawb fawb tshawb fawb txog kev cuam tshuam tshuaj nrog heparin, thaum lawv txais tos ib txhij nws yog qhov tsim nyog yuav tsum tau ceev faj.

Kev sib xyaw ntawm cov tshuaj nrog thrombolytics, txij li kev nyab xeeb ntawm kev sib koom ua ke no tsis tau tsim tsa.

Ua pov thawj txhua hnub acetylsalicylic acid(txog 1000 mg ib hnub twg) thiab clopidogrel tsis cuam tshuam dabtsi aggregate cov khoom ntawm cov tshuaj. Txawm li cas los xij, lub sijhawm ua haujlwm ntawm kev tswj hwm ntawm cov tshuaj no yuav tsum tsis pub ntau dua 1 xyoos (kev saib xyuas yuav tsum tau noj).

Cov tshuaj inhibits cov metabolism hauv tshuaj, pharmacokinetic ntsuas uas vam khom isoenzyme CYP2C9Cov. Hauv qee, cov tshuaj yuav nce ntshav plasma concentration phenytoin thiab tolbutamideCov. Kev saib xyuas yuav tsum ua.

Tej zaum muaj cuab yeej ua ke nrog digoxin, theophylline, tshuaj tua kab mob.

Cov Ntawv Lopirela

Cov tshuaj tiv thaiv: Clopidogrel, Avix, Atrogrel, Deplat, Zilt, Karum Sanovel, Clopidale, Klopikor, Lopigrol, Orogrel, Plavigrel, Plagril, Reodar, Tessiron, Trombone, Flamogrel 75, Aterocardium, Gridoklein, Deplatt, Cardogrelog, Medrogrel, Medogrel Krel Neo, Plavix, Platogril, Reomax, Lub Sijhawm.

Tsuas tshuaj thiab tswj hwm

Txog kev tiv thaiv ischemic kev tsis sib haum xeeb hauv cov neeg mob tom qab myocardial infarction, ischemic stroke thiab tsis ntev los no kuaj mob peripheral leeg mob, cov neeg laus (suav nrog cov neeg laus laus) tau txhaj tshuaj 75 mg 1 zaug / hnub, tsis hais noj zaub mov noj. Kev kho yuav tsum pib nyob rau hauv lub sijhawm txij li ob peb hnub mus rau 35 hnub tom qab myocardial infarction nrog kev tsim ntawm pathological Q yoj thiab txij li 7 hnub txog rau 6 hli tom qab muaj mob stroke ischemic.

Siv rau cov neeg laus thiab cov neeg laus laus uas muaj kev ua haujlwm tsis tu ncua ntawm CYP2C19 isoenzyme

Nrog myocardial infarction, ischemic stroke thiab kuaj cov kab mob txhaws kab mob txha caj qaum, 75 mg ntawm Lopirel yog kho ib hnub ib zaug.

Hauv cov mob hlab ntsha hlwb tsis muaj ST ntu kab mob siab (myocardial infarction tsis muaj Q yoj, tsis khov lub siab), kev kho mob yuav tsum pib nrog ib qho kev txhaj tshuaj ib zaug (300 mg), tom qab uas 75 mg tau sau tseg ib hnub ib zaug (ua ke nrog txhua hnub ntawm 75-325 mg acetylsalicylic acid ) Txij li thaum siv ntau dua ntawm cov tshuaj acetylsalicylic acid ua rau muaj kev pheej hmoo los ntshav, koob tshuaj acetylsalicylic acid pom zoo rau qhov ntsuas no yuav tsum tsis pub ntau tshaj 100 mg. Qhov zoo siab kawg ntawm kev kho mob tsis tau txiav txim siab raws cai. Raws li kev tshawb fawb hauv kev tshawb fawb, cov tshuaj yuav tsum noj ntev txog 1 xyoos. Qhov txiaj ntsig zoo tshaj plaws pom tau los ntawm 3 lub hlis ntawm kev kho mob.

Hauv kev muaj mob ntawm cov leeg mob nrog rau ST-ntu ntu nce siab (mob myocardial infarction los ntawm ST-ntu nce), ib qho kev thauj khoom ntawm 300 mg yog kho ib zaug, tom qab 75 mg ib hnub ib zaug ua ke nrog acetylsalicylic acid (ua ke nrog lossis tsis muaj thrombolytics). Thaum kho cov neeg mob hnub nyoog 75 xyoo thiab laus dua, Lopirel txoj kev kho yuav tsum raug tswj hwm yam tsis muaj chaw thau khoom. Kev sib xyaw ua ke yuav pib tam sim ntawd tom qab pib qhov tsos mob thiab kav rau 4 lub lis piam. Cov txiaj ntsig ntawm kev sib xyaw ntawm acetylsalicylic acid thiab clopidogrel nrog cov kev ntsuas no dhau 4 lub lis piam tsis tau kawm.

Nrog cov tshuaj atrial fibrillation (atrial fibrillation), 75 mg ntawm Lopirel tau sau tseg ib hnub ib zaug. Ua ke nrog clopidogrel, kev siv cov tshuaj acetylsalicylic acid yuav tsum tau pib thiab txuas ntxiv (txhua hnub ntawm 75-100 mg).

Yog tias koj tsis nco qab noj Lopirel ntxiv, koj yuav tsum ua raws li cov lus pom zoo hauv qab no:

yog tias tsawg dua 12 teev tau dhau mus tom qab hla lub koob tshuaj, koj yuav tsum tau noj Lopirel tam sim ntawd, thiab noj lwm cov koob tshuaj txuas ntxiv li niaj zaus,
yog tias ntau dua 12 teev tau dhau mus tom qab hla lub koob tshuaj, koob tshuaj Lopirel ntxiv yuav tsum noj ib txwm muaj (txwv ob koob).

Daim ntawv thov nta

Kev kuaj ntshav yuav tsum tau ua nyob rau thawj lub lim tiam ntawm kev kho mob thaum muaj kev sib xyaw ntawm clopidogrel nrog acetylsalicylic acid, NSAIDs, heparin, IIb / IIIa glycoprotein inhibitors lossis fibrinolytics, nrog rau cov neeg mob uas muaj kev pheej hmoo los ntshav (kev raug mob, kev phais mob lossis lwm yam mob pathological).

Vim tias txoj kev pheej hmoo ntawm los ntshav thiab hematological tshwm sim, yog tias cov tsos mob hauv tsev kho mob pom tias qhov no tshwm sim thaum kho mob, kuaj ntshav (APTT, platelet suav, platelet ua haujlwm) thiab daim siab kev ua haujlwm hauv lub siab yuav tsum tau ua tam sim ntawd.

Yog hais tias ntawm kev phais mob, yog tias muaj cov nyhuv los tiv thaiv kev tsis sib haum, tsis muaj qhov xav tau, clopidogrel yuav tsum tau tsum txiav 7 hnub ua ntej kev phais mob.

Clopidogrel yuav tsum tau siv nrog ceev faj hauv cov neeg mob uas muaj kev pheej hmoo los ntshav (tshwj xeeb tshaj yog lub plab hnyuv plab thiab pob txha).

Cov neeg mob yuav tsum tau ceeb toom tias lawv yuav tsum qhia tus kws kho mob txog txhua kis ntawm los ntshav.

Vim tias cov ntaub ntawv tsis txaus, clopidogrel yuav tsum tsis txhob raug tshuaj rau lub sijhawm mob sai ischemic stroke (hauv thawj 7 hnub).

Kev tiv thaiv kev nyab xeeb

Nws yog cov ntawv ceeb toom nrog ceev faj rau cov neeg mob uas muaj kev pheej hmoo los ntshav (kev raug mob, kev phais mob, thiab lwm yam) thiab nrog lub raum thiab cov ntshav tsis zoo ua haujlwm (hemorrhagic diathesis yuav tshwm sim).

Kev nyab xeeb thiab ua tau zoo rau cov neeg mob hnub nyoog qis dua 18 xyoo tsis tau teeb tsa.

Cov tshuaj muaj lactose, yog li nws yuav tsum tsis txhob coj los ntawm cov neeg uas muaj kev mob caj dab tsis txaus ntseeg.

Clopidogrel yog ib qho prodrug uas tau yauv hloov pauv metabolic koom nrog ntau lub siab enzymes. Kev tswj hwm tib lub sijhawm ua haujlwm ntawm cov tshuaj uas cuam tshuam cov kev ua haujlwm ntawm lub siab enzyme CYP2C19 tuaj yeem ua rau muaj kev hloov pauv ntawm kev tsim cov nquag metabolite thiab, yog li, txo qis hauv cov nyhuv kho. Txais tos ntawm clopidogrel thiab proton twj tso kua mis thaiv cov khoom sib txawv ntawm cov sij hawm ntawm lub hnub tsis cuam tshuam rau kev txhim kho cov tshuaj tiv thaiv ntawm kev sib cuam tshuam.

Kev tswj hwm tib lub sijhawm ntawm clopidogrel nrog proton twj tso kua mis blockers yuav tsum raug txiav txim siab, rau cov uas muaj pov thawj ntawm lawv lub peev xwm los ua kom zoo tshaj qhov ua tau zoo ntawm clopidogrel, piv txwv li, omeprazole.

Yog tias tus neeg mob xav tau noj cov tshuaj tiv thaiv proton twj tso kua mis thaum noj clopidogrel, cov tshuaj ntawm pawg no uas muaj peev xwm tsawg tshaj plaws los cuam tshuam yuav tsum yog cov kws kho mob. Ib qho ntawm cov tshuaj no yog pantoprazole.

Tso cov ntaub ntawv thiab cov nyob ua ke

Cov tshuaj muaj nyob rau hauv cov ntsiav tshuaj uas muaj 1 cov khoom tivthaiv (clopidogrel hydrosulfate) thiab cov neeg tsis muaj zog uas tsis muaj cov teebmeem antiplatelet. Qhov siab ntawm cov kab xev theem pib yog 97.87 mg. Tus nqi no sib raug rau 75 mg ntawm clopidogrel. Cov ntsiav tshuaj muaj lub plhaub tshwj xeeb, vim tias cov nyhuv ntawm cov tshuaj mos muag. Hauv qhov no, cov tshuaj nquag yuav tso tawm maj, kev nqus tau tshwm sim hauv txoj hnyuv. Me me:

crospovidone
lactose
microcrystalline cellulose,
glyceryl dibehenate
Opadry II 85 G34669 paj yeeb,
talcum hmoov.

Cov pob muaj 14, 28 lossis 100 ntsiav tshuaj.

Cov tshuaj muaj nyob hauv cov ntsiav tshuaj uas muaj 1 cov khoom xyaw dhia.

Cov Tshuaj Pharmacokinetics

Cov tshuaj pib tshwm sim tam sim ntawd ntawm txoj haujlwm ntawm kev tswj hwm - tom qab 2 teev muaj qhov txo qis ntawm kev siv ntawm platelet txuas. Qhov loj dua cov koob tshuaj, qhov kev txhim kho nrawm dua. Thaum cov tsos mob ntawm tus mob tshem tawm, qhov ntau ntawm cov tshuaj txo qis. Yog li ntawd, tom qab noj cov tshuaj txij nkawm ntawm Lopirel rau 4-7 hnub, kev pom zoo siab ntawm cov tshuaj yeeb dej caw. Cov txiaj ntsig tau txais yog tswj nyob rau lub sijhawm ntawm kev siv ntshav ntawm ntshav (5-7 hnub).

Qhov nqus ntawm clopidogrel tau nrawm, thaum txoj hlua khi rau cov ntshav cov ntshav muaj protein ntau heev (98%). Kev hloov pauv ntawm cov tshuaj no tshwm sim hauv lub siab. Nws pom tau hais hauv 2 txoj hauv kev: los ntawm esterases nrog kev tshaj tawm ntawm carboxylic acid (tsis qhia kev ua haujlwm), nrog kev koom tes ntawm cytochrome P450. Cov txheej txheem ntawm txoj hlua khi rau platelet receptors tshwm sim nyob rau hauv kev cuam tshuam ntawm metabolites.

Nws yuav tsum tau yug los rau hauv lub siab tias kev noj cov tshuaj hauv qhov loj (300 mg ib zaug) ua rau muaj kev nce siab hauv qhov siab tshaj plaws. Tus nqi ntawm qhov ntsuas no yog 2 zaug siab dua qhov siab tshaj plaws ntawm cov neeg mob thaum cov koob tshuaj txij nkawm (75 mg) tau noj rau 4 hnub.

Kev nthuav tawm ntawm cov tshuaj muaj nyob rau hauv qhov muaj pes tsawg leeg ntawm cov tshuaj tshwm sim dhau los ntawm ob lub raum.

Kev nthuav tawm ntawm cov tshuaj muaj nyob rau hauv cov tshuaj muaj pes tsawg leeg tshwm sim los ntawm lub raum thiab hnyuv (hauv cov sib npaug ntawm cov sib npaug). Txoj kev no qeeb. Kev ua tiav kev tshem tawm ntawm cov tshuaj yeeb dej caw feem ntau tshwm sim rau hnub thib 5 tom qab noj Lopirel kawg.

Nrog saib xyuas

Yog hais tias npaj qhov kev phais mob, cov tshuaj tsis raug txiav txim vim qhov txaus ntshai los ntshav. Lwm yam mob pathological uas muaj nyob hauv pawg ntawm cov txheeb ze contraindications:

cov kab mob uas yuav ua rau los ntshav heev, piv txwv, nrog kev puas tsuaj rau cov plab hnyuv siab raum tsis pom kev lossis txoj hnyuv,
keeb kwm ua xua rau thienopyridines.

Txog rau cov hlab ntsha hemorrhage, noj Lopirel yog contraindicated.
Lopirel txwv tsis pub hauv exacerbation ntawm peptic mob.
Nrog kev puas tsuaj ntawm cov hnyuv, Lopirel yuav tsum tau ua nrog ceev faj.

Yuav ua li cas kom noj Lopirel

Feem ntau, 0.075 g yog tshuaj ib hnub ib zaug. Cov lus qhia rau kev siv cov tshuaj hauv lwm qhov xwm txheej:

mob ntsig txog tus mob nrog rau kev nce siab hauv ST: ntawm 0.075 g ib hnub los ntawm hnub thib ob, thawj koob tshuaj yog 0.3 g ib zaug, lub sijhawm kho tsis ntev dua 4 lub lis piam, qhov kev soj ntsuam kev kho mob ntev dua tsis tau tsim,
mob caj dab tsis muaj cov cim ntawm qib siab: tus qauv zoo li qub, tab sis lub sijhawm ntawm chav kawm tuaj yeem ntev dua (txog 12 lub hlis),
Atrial fibrillation: 0.075 g ib hnub.

Hauv txhua kis, kev siv ntawm ASA raug pom zoo. Txawm li cas los xij, muaj cov kev txwv: tsis pub ntau tshaj 0.1 mg ib hnub.

Noj cov tshuaj rau ntshav qab zib

Nws raug pom zoo los siv tshuaj kho rau tus mob zoo li no, tab sis ceev faj yuav tsum tau siv vim tias lactose uas yog ib feem ntawm nws. Tsis tas li ntawd, tawm tsam keeb kwm ntawm cov ntshav qab zib, qhov kev pheej hmoo ntawm kev tsim mob stroke, myocardial infarction nce. Antiplatelet txoj kev kho yog cov kauj ruam tseem ceeb hauv kev kho tus mob no, tsuas yog tsuas tshuaj yog txiav txim siab ib tus zuj zus, txiav txim siab lub xeev ntawm lub cev.

Nws raug tso cai siv tshuaj rau mob ntshav qab zib, tab sis ceev faj yuav tsum tau siv thaum noj nws.

Lub plab zom mov

Kev zom zom, mob hauv plab, hloov pauv tus qauv ntawm cov quav yog pom ntau zaus, xeev siab yuav tshwm sim. Tsawg tsawg zaus, qhov kev txhim kho ntawm yaig nyob rau hauv lub plab yog sau tseg, kev tso quav tawm los yog qhov nyuaj, kev tsim muaj roj nyob ze. Qee zaum kuaj pom tias qhov kiav txhab ua paug. Mob raws plab thiab pancreatitis yog yam tsawg dua.

Nruab nrab hauv lub paj hlwb

Kiv taub hau, mob taub hau, saj yam ntxwv, nws ua tiav. Kev ua dej siab tus neeg xav tau. Tsis meej pem yog sau tseg.

Thaum kho mob Lopirel, xeev siab thiab ntuav tej zaum yuav tshwm sim.
Kiv taub hau yog phiv cov tshuaj Lopirel.
Lopirel tuaj yeem ua rau mob taub hau.
Thaum noj Lopirel, qhov mob ntawm plab yuav tshwm sim.
Ib qho kev cuam tshuam ntawm cov tshuaj Lopirel yog qhov tshwm sim ntawm tus kab mob siab.
Cov tawv nqaij khaus khaus yog qhov tshwm sim ntawm lub tshuaj Lopirel.
Kev ua qhov chaw nyob thaj yeeb yuav tshwm sim thaum kho nrog Lopirel.

Kev phiv tshuaj

Raws li cov lus qhia, Lopirel 75 mg muaj qee qhov kev txwv tsis pub noj:

Eosinophilia (ib yam kabmob uas muaj ntau ntxiv rau eosinophils).
Leukopenia (txo qis cov qe ntshav dawb hauv cov ntshav).
Thrombocytopenia (ib qho mob uas tau pom los ntawm kev txo ntshav hauv qab qis dua ib txwm, uas nrog los ntawm los ntshav thiab teeb meem nrog cheem los ntshav).
Neutropenia (qib qis hauv neutrophilic granulocytes hauv cov ntshav).
Keeb kwm lossis nrhiav ntshav pathology vim muaj kev puas tsuaj rau cov hlwb pob txha hlwb.
Thrombotic thrombocytopenic purpura (ib qho mob loj heev uas ua rau microangiopathic hemolytic anemia).
Kiv taub hau
Granulocytopenia (muaj cov qe ntshav dawb tsawg).
Mob Kev Plab
Intracranial hemorrhage.
Nrhiav Hemophilia (ib qho mob tsis tshua muaj kab mob txuam nrog kev tsis taus coagulation).
Anaphylactoid kev tsis haum.
Tsis meej pem.
Kev Ua Si.
Mob taub hau
Paresthesia (ib qho kev tsis haum ntawm lub siab, uas yog tus kheej los ntawm qhov tshwm sim pom ntawm qhov hnov ntawm hlawv thiab nkag mus ntawm goosebumps).
Ua txhaum ntawm saj.
Qhov muag hemorrhage.
Hematomas.
Kev los ntshav hnyav.
Txo cov ntshav siab.
Vasculitis (ib pawg kab mob raws li immunopathological vascular voos).
Epistaxis.
Bronchospasm (ib qho pathology uas tshwm sim thaum cov leeg nqaij ntawm txoj hlab ntsws sib kis tau thiab lawv cov lumen txo qis).
Lub plawv mob ntsws.

Raws li cov lus qhia rau Lopirel, nws paub tias, ntxiv rau cov kev phiv uas tau piav qhia saum toj no, cov tshuaj tuaj yeem ua rau cov kev tsis zoo hauv qab no:

Eosinophilic mob ntsws (ib tug kab mob uas eosinophils ntau ntxiv nyob rau hauv pulmonary alveoli).
Mob plab zawv (txoj kev mob uas tus neeg ua kom sai, thaum tso quav ua dej).
Interstitial pneumonitis (mob ntsws, uas txoj kev cuam tshuam ua rau mob interstitium).
Duodenal rwj (kev ua haujlwm los ntawm kev ua ntawm cov kua qaub thiab pepsin rau ntawm cov leeg mos ntawm duodenum hauv cov neeg muaj acidity ntau).
Los ntshav.
Gastritis (mob ntev ntev uas yog tus cwj pwm los ntawm dystrophic thiab inflammatory hloov ntawm lub plab hnyuv, tau nce nrog kev ua txhaum ntawm kev tsim dua tshiab).
Cov hnyuv ob leeg.
Retroperitoneal los ntshav.
Cov mob o ntawm qhov hnyuv mucosa.
Pancreatitis (ib tug kab mob nyob rau hauv uas txiav ntawm daim tawv nqaij txiav).
Angioedema (ib qho mob uas pom muaj los ntawm kev hloov sai ntawm lub zos ntawm cov leeg nqaij, nrog rau cov nqaij mos thiab nqaij tawv).
Nettle pob.
Mob caj dab (mob kab mob ntawm pob qij txha, nrog mob o).
Hemarthrosis (hemorrhage hauv cov leeg kab noj hniav).
Arthralgia (mob pob qij txha).
Hematuria (kev muaj ntshav nyob hauv cov zis).
Glomerulonephritis (mob raum ua cim los ntawm lub qhov txhab ntawm glomeruli).

Kuv puas tuaj yeem siv cov tshuaj thaum cev xeeb tub?

Raws li kev tshuaj xyuas ntawm Lopirel, nws paub tias clopidogrel tsis tau pom tias muaj qhov tsis zoo rau kev xeeb tub thiab kev yug menyuam, tab sis vim tsis muaj cov ntaub ntawv tshawb fawb, cov tshuaj yog contraindicated rau cov poj niam cev xeeb tub.

Hauv chav kawm ntawm cov kev tshawb fawb, nws tau pom tias cov tshuaj ua kom nquag plias thiab nws cov metabolites kis mus rau niam mis, yog li lactation yuav tsum nres thaum kho cov tshuaj. Tsis muaj ntaub ntawv qhia txog kev rho tawm clopidogrel nrog niam lub mis. "Lopirel" yog sib kis rau cov menyuam yaus hnub nyoog qis dua kaum yim xyoo.

Lopirel muaj qee yam tshuaj hloov:

"Plagril."
Egithromb.
Plavix.
"Deplatt 75".
Detrombe.
Clapitax.
"Teev Npe 75".
Zauv.
Avwmx.
"Orogrel".
Brilinta.
"Platogril."
Reomax.
"Medogrel".
Cardogrel.
Tessiron.
"Clorelo."
Klopikor.
Claridol
Gridoklein.

Ua ntej hloov daim qub nrog ib qho tshuaj pleev ib ce, sab laj nrog tus kws kho mob.

Cov tshuaj muaj nyob rau hauv daim ntawv ntawm ntsiav tshuaj, uas yog coated nrog ib zaj duab xis txheej. Lawv muaj puag ncig, biconvex duab, paj yeeb hauv xim. Cov ntsiav tshuaj tau ntim rau hauv blisters ntawm kaum daim. "Plagril" cov lus piav qhia ntawm "Lopirel".

Ob teev tom qab noj thawj zaug tshuaj - plaub puas milligrams - qhov kev txwv tsis pub platelet yog sib xyaw. Qhov siab tshaj plaws ua tiav tau tom qab xya hnub, nrog kev siv tshuaj ib txwm nyob rau hauv ntau npaum ntawm tsib caug mus rau ib puas milligrams ib hnub.

Raws li cov lus qhia rau kev siv nrog Lopirel analogue 75 mg, nws paub tias cov nyhuv ntawm cov tshuaj siv tau ntev txog kaum hnub. Tom qab qhov kev txiav tawm ntawm txoj kev kho nrog "Plagril" rau 5 hnub, lub sijhawm los ntshav thiab kev sib xyaw ntawm cov platelets rov qab mus rau lawv qib qub. Cov tshuaj txwv tsis pub cov tsos mob atherothrombosis hauv cov neeg muaj mob atherosclerotic vascular.

Kev siv tshuaj kho mob yuav tsum tau txiav xya hnub ua ntej kev phais mob, uas qhov ua tau zoo antiplatelet yog qhov tsis xav tau. Hauv qhov no, tus neeg yuav tsum qhia tus kws kho mob tshwj xeeb txog ib qho kev los ntshav thaum siv Plagril. Tsis tas li ntawd, yog tias ib tus neeg yuav tsum tau mus phais lossis lwm yam tshuaj noj, tus neeg mob yuav tsum qhia tus kws kho mob txog kev siv Plagril. Thaum lub sijhawm kho, nws yog ib qho tsim nyog los saib xyuas lub cev ua haujlwm.

Cov tshuaj pab txo cov pas dej platelet, uas yog kev npau taws los ntawm lwm cov agonists, inhibiting lawv kev ua haujlwm los ntawm kev tso tawm adenosine diphosphate.

Raws li cov lus qhia, Lopirel analogue yog siv rau cov txheej txheem prophylactic los tiv thaiv qhov tshwm sim ntawm atherothrombosis:

Hauv cov neeg uas tau raug mob myocardial infarction, nrog rau ischemic mob hlab ntsha tawg nrog kev kuaj mob txhab ntawm cov hlab ntsha txhaws.
Hauv cov neeg uas muaj mob vwm ua mob hlab ntsha tawg.
Hauv cov neeg mob uas tau raug mob thaum lub sijhawm ua cov hlab ntshav hlab plawv angioplasty.

Tsis tas li ntawd, Klopikor pom zoo rau lub hom phiaj prophylactic ntawm thromboembolic, atherothrombotic cov xwm txheej nrog atrial fibrillation.

Thaum noj tshuaj rau hauv qhov ntau npaum ntawm xya caum-tsib milligrams ib hnub twg, kev txwv tsis pub platelet ntau rau ntawm thawj hnub ntawm txoj kev kho. Hauv xya hnub tom ntej, qhov kev txiav txim no nce.

Kev txhawb nqa ntawm platelet tsim nyob rau hauv kev sib npaug yog qhov nruab nrab ntawm plaub caug mus txog rau caum feem pua (thaum noj tshuaj ntawm lub siab ntawm xya caum tsib milligrams ib hnub). Tom qab kev kaw ntshav los ntshav, qhov ntsuas ntawm koom nrog platelets rov qab mus rau theem pib ntawm tsib hnub.

Raws li kev txheeb xyuas, cov tshuaj nyob ntawm Lopirel 75 mg - Zilt pab tiv thaiv qhov tshwm sim ntawm lub plawv nres lossis mob stroke hauv cov neeg mob vascular atherosclerosis.

Cov tshuaj nquag muaj peev xwm nqus tau nrawm tom qab kev tswj hwm qhov ncauj. Cov ntsiab lus siab tshaj plaws ntawm clopidogrel qhov nruab nrab 2.2-2.5 nanograms ib milliliter (tom qab noj xya caum-tsib milligrams ntawm cov tshuaj). Lub sijhawm kom mus txog qhov siab tshaj plaws yog txog plaub caug-tsib feeb. Qhov ntsuas ntawm kev nqus ntawm cov nquag tivthaiv, raws li cov ntaub ntawv ntawm kev nthuav tawm ntawm cov khoom lag luam metabolic ntawm cov tshuaj los ntawm ob lub raum, yog tsib caug feem pua.

Nws tsis pom zoo kom muab tshuaj rau cov neeg rau mob vwm ischemic stroke nrog cov tshuaj tsawg dua li ib lub lim tiam. "Zilt" rub lub sijhawm ntev los ntshav, qhov no yuav tsum raug coj los siv thaum siv ib txhij nrog "Aspirin", tsis siv tshuaj tiv thaiv tsis haum tshuaj, "Heparin" thiab "Warfarin". Cov neeg mob zoo li no yuav tsum tau kuaj xyuas seb puas muaj kev cuam tshuam ntau ntxiv rau ticlopidine, prazogrel thiab lwm yam thienopyridines, vim tias qhov tshuaj tiv thaiv kab mob tau nce siab los ntawm cov tshuaj ntawm cov pab pawg no tau.

Thaum qhia hauv tus neeg mob lub keeb kwm kho mob txog kev raug mob siab rau lwm tus mob thienopyridines, nws yuav tsum ua tib zoo saib xyuas lub sijhawm kho mob txhawm rau txheeb xyuas cov cim kev tiv thaiv qhov mob siab rau qhov sib txuas. Thaum npaj tus neeg mob rau lub sijhawm npaj ua haujlwm, kev siv cov tshuaj yuav tsum nres rau tsib mus rau xya hnub.

Ib tug neeg yuav tsum raug ceeb toom txog qhov ua tau los ntshav ntxiv ntev heev thaum kho thiab qhov yuav tsum tau qhia tus kws kho mob tshwj xeeb txog txhua qhov teeb meem los ntshav. Thaum sab laj nrog lwm tus kws kho mob, koj yuav tsum qhia qhov kev siv "Zilt" tas li, cov ntaub ntawv no tseem ceeb heev thaum sau tshuaj tshiab, thiab thaum mus ntsib kws kho hniav.

Qhov no yog cov tshuaj antithrombotic uas cuam tshuam rau cov koom haum platelet, thaiv cov txheej txheem ntawm kev sib txuas ntawm adenosine diphosphate nrog receptors uas nyob rau ntawm lub platelet membrane, thiab tseem ua kom cov glycoprotein receptors. "Reomax" pab txo cov platelet sib sau, uas yog kev npau taws los ntawm lwm tus agonists, inhibiting lawv kev ua haujlwm los ntawm kev tso tawm adenosine diphosphate.

Cov tshuaj muaj zog (clopidogrel) xaiv txoj hlua khi adenosine diphosphate nrog platelet receptors, inhibiting lawv lub koom haum. Irreversibly txuas nrog cov hlab ntsha kawg, ua rau cov ntshav ua haujlwm thoob lawv "tag nrho" lub voj voog. Egithromb yog ib qho tshuaj noj ntawm Lopirel ntsiav tshuaj.

Kev txhawb nqa los ntawm cov neeg koom tes yog sau tseg tom qab ob teev, thiab cov txiaj ntsig siab tshaj plaws yog pom tom qab tsib rau xya hnub. Nws tsis muaj dab tsi cuam tshuam rau kev ua haujlwm ntawm cov pab pawg ntawm cov enzymes uas hydrolyze phosphodiester bond.

Nyob rau hauv muaj cov kab mob hlwb ntev, uas cov roj cholesterol thiab lwm yam cov rog tau muab tso rau sab hauv phab ntsa ntawm cov hlab ntsha hauv daim ntawv thiab cov plaques, thiab cov phab ntsa lawv tus kheej ua denser thiab poob lawv qhov elasticity, cov tshuaj pab tiv thaiv kom tsis txhob mob thrombosis.

Cov tshuaj sawv cev rau ib pawg pharmacological ntawm cov tshuaj - cov neeg sawv cev antiplatelet. Nws yog siv los tiv thaiv atherothrombotic cov teeb meem hauv ntau cov txheej txheem pathological ntawm kab mob plawv.

Tus nquag muaj txiaj ntsig hauv Plavix ntsiav tshuaj yog clopidogrel. Nws inhibits qhov txheej txheem ntawm gluing platelets. Qhov kev siv roj ntsha no tshwm sim vim yog kev xaiv ntawm kev tsim cov txheej txheem ntawm cov ntawv txuas ntawm adenosine diphosphoric acid rau qee qhov kawg ntawm cov leeg platelets thiab kev ua kom txuas ntxiv ntawm cov txheej txheem ntawm lawv cov txuas. Cov nyhuv no tshwm sim thoob plaws hauv lub neej ntawm platelet (xya mus rau kaum hnub), yog li muaj peev xwm rov ua dua ib pawg tshwm sim tsuas yog tom qab kev tsim kho cell.

Cov nyhuv pharmacological ntawm Plavix tshwm sim tom qab kev sib hloov ntawm clopidogrel hauv lub siab, thiab ib qho kev ua haujlwm ntawm cov khoom lag luam metabolic tau tsim, uas inhibits cov txheej txheem ntawm platelet adhesion. Tom qab pib siv Plavix, qhov kev siv ntawm kev tawm tsam kev ua ub ua no tau coj mus rau ob rau peb hnub thiab tom qab ntawd mus txog qib tas li.

Tom qab tsis ua tiav ntawm Plavix txoj kev kho, platelet kev ua si rov qab rau tsib mus rau xya hnub. Siv cov tshuaj noj kom tsawg tuaj yeem txo txoj kev pheej hmoo ntawm kev txhim kho cerebral ischemia, nrog rau myocardial infarction nyob rau hauv ntau yam pathologies ntawm lub plawv thiab cov hlab ntsha, nrog rau kev nce ntxiv ntawm atrial contractions, uas ua rau muaj feem ntau ntawm cov ntshav txhaws hauv lawv kab noj hniav.

Cov tshuaj yog mus rau pab pawg kho mob ntawm cov tshuaj - cov neeg sawv cev antiplatelet thiab anticoagulants. Brilinta tau siv rau hauv kev kho mob nyuaj rau cov kab mob plawv, uas muaj kev pheej hmoo ntawm cov ntshav txhaws hauv cov hlab ntsha, uas tuaj yeem ua rau cov hlab hlwb txhaws lossis myocardial infarction.

Tom qab siv cov tshuaj, cov tshuaj tiv thaiv qhov ncauj ntawm qhov tshuaj txuam rau cov ntshav los ntawm cov hnyuv me. Cov ntsiab lus pharmacological hauv cov ntshav tau tiav nees nkaum mus rau peb caug feeb tom qab siv tshuaj, qhov siab tshaj plaws tau tiav tom qab ib thiab ib nrab teev.

Cov khoom sib xyaw ua haujlwm kom sib kis thoob plaws cov ntaub so ntswg ntawm tag nrho lub cev, hla ntawm qhov teeb meem rau hauv lub hlwb cov ntaub so ntswg thiab los ntawm qhov chaw tiv thaiv kab mob rau hauv cov me nyuam hauv plab thiab mis thaum lub sijhawm lactation. Cov tshuaj nquag (ticagrelor) raug sib pauv hauv cov qog ntawm daim siab, nws cov khoom lwj ua kom yuag hauv cov kua tsib. Qhov kev tshem tawm ib nrab-lub neej yog li xya teev.

Siv rau hauv cov neeg mob uas tau txiav txim siab txo cov kev ua haujlwm ntawm CYP2C19 isoenzyme

Nrog qis kev ua haujlwm ntawm CYP2C19 isoenzyme, cov nyhuv antiplatelet ntawm clopidogrel txo qis. Thaum siv cov koob tshuaj loj (qhov kev thauj khoom ntawm 600 mg, thiab tom qab ntawd 150 mg rau ib hnub ib hnub), cov nyhuv antiplatelet ntawm clopidogrel nce ntxiv. Kev xav txog cov txiaj ntsig kev soj ntsuam hauv txoj kev tshawb fawb, nws tsis tuaj yeem tsim kom tau cov tshuaj zoo tshaj plaws rau cov neeg mob uas txo qis metabolism vim cov haujlwm tsawg ntawm CYP2C19 isoenzyme.

Siv rau hauv cov neeg mob ntawm ntau haiv neeg

Rau cov neeg sawv cev ntawm cov pab pawg neeg sib txawv, nthuav dav ntawm cov khoom siv ntawm cov CYP2C19 isoenzyme noob caj noob ces, uas yog lub luag haujlwm rau qhov txo qis thiab nruab nrab ntawm cov metabolism ntawm clopidogrel rau lub zog metabolite, sib txawv. Tsuas yog cov ntaub ntawv muaj tsawg tsawg ntawm cov neeg sawv cev ntawm haiv neeg ntawm Mongoloid hais txog kev txheeb xyuas kev sib raug zoo ntawm CYP2C19 isoenzyme genotype thiab cov txiaj ntsig soj ntsuam.

Siv rau hauv cov txiv neej thiab poj niam

Ib qho kev tshawb nrhiav me me sib piv cov pharmacodynamic zog ntawm Lopirel hauv ob hom kev sib deev pom tias muaj qis dua qhov kev txwv ntawm ADP-vim platelet sib xyaw rau cov poj niam, tab sis tsis muaj qhov sib txawv ntawm lub sijhawm los ntshav. Hauv kev tshawb nrhiav loj ntawm CAPRIE (kev sib xyaw ntawm clopidogrel thiab acetylsalicylic acid nyob rau hauv cov neeg mob uas muaj qhov ua tau ntau ntawm kev txhim kho ischemic muaj teeb meem) rau cov poj niam thiab tus txiv neej, qhov ntau zaus ntawm cov kev soj ntsuam, kev kuaj mob thiab kuaj qhov txawv ntawm qhov feem cuam, thiab lwm cov kev mob tshwm sim tau zoo ib yam.

Sab sij huam

Kev tshawb fawb txog kev nyab xeeb tau koom nrog ntau dua 44,000 tus neeg mob, suav nrog ntau dua 12,000 cov neeg mob uas tau kho nyob rau tsawg kawg 1 xyoos. Kev zam dav dav ntawm clopidogrel zoo ib yam li kev mob siab rau ntawm acetylsalicylic acid, tsis hais haiv neeg twg, poj niam txiv neej thiab hnub nyoog ntawm cov neeg mob. Ib tug xov tooj ntawm cov kev tshawb fawb soj ntsuam (CURE, CAPRIE, KEV SIB THAM, KEV SIB HLUB, KEV UA SI A) tau tshawb pom muaj kev cuam tshuam loj hauv kev mob tshwm sim hauv qab no.

Hauv CAPRIE cov kev sim siab, kev zam ntawm clopidogrel (koob tshuaj txhua hnub ntawm 75 mg) sib haum rau qhov ntawd rau acetylsalicylic acid (koob tshuaj txhua hnub ntawm 325 mg). Xov tshwm sim muaj cov lus qhia txog kev phiv tshuaj.

Hauv kev sim tshuaj thiab tom qab kev siv khoom lag luam ntawm clopidogrel, qhov feem ntau los ntshav ntau dhau los (tshwj xeeb tshaj yog nyob rau thawj lub hlis ntawm kev kho mob) tau sau tseg.

Hauv CAPRIE cov ntaub ntawv sim, tag nrho cov ntshav los nrog sib cais siv clopidogrel lossis acetylsalicylic acid yog 9.3%. Kev los ntshav ntau nrog clopidogrel tau sau nrog tib zaus uas nrog acetylsalicylic acid.

Hauv kev soj ntsuam kab mob CURE siv cov tshuaj acetylsalicylic acid thiab clopidogrel rau 7 hnub tom qab txoj hlab ntshav o hla kev txhim kho hauv cov neeg mob uas tau tso tseg kev kho mob ntau dua 5 hnub ua ntej kev phais mob, qhov nce ntawm cov zaus los ntshav ntau heev tsis pom. Hauv cov neeg mob uas txuas ntxiv noj cov tshuaj ntawm cov tshuaj rau 5 hnub ua ntej pib lub cev ntawm txoj hlab ntshav o hla kev sib tsoo, kev los ntshav hnyav tau pom nrog ntau zaus ntawm 9.6% (rau kev sib xyaw ntawm acetylsalicylic acid + clopidogrel) thiab 6.3% (rau kev sib xyaw ntawm acetylsalicylic acid + placebo).

Lub chaw soj ntsuam CLARITY tau qhia pom dav dav nce ntxiv rau hauv kev tso ntshav ntau rau cov neeg muaj acetylsalicylic acid + pawg clopidogrel piv nrog cov acetylsalicylic acid + cov pawg placebo. Hauv ob pawg, ntau zaus ntawm kev los ntshav hnyav tau zoo sib xws thiab yuav luag ywj siab ntawm hom kev kho mob heparin lossis fibrinolytic thiab cov yam ntxwv thaum pib ntawm cov neeg mob.

Hauv kev sim tshuaj COMMIT, tag nrho cov teeb meem ntawm txoj hlab ntshav khov lossis ntshav tsis ua mob rau lub hlwb tsis tshua muaj thiab tsis txawv rau ob pawg.

Hauv ACTIVE-A qhov kev sim tshuaj, qhov tshwm sim ntawm los ntshav loj dua rau cov pawg acetylsalicylic acid + clopidogrel pawg dua rau cov acetylsalicylic acid + placebo pawg (6.7% thiab 4.3%, feem). Feem ntau, los ntshav loj hauv ob pawg yog extracranial (5.3% thiab 3.5%, feem), feem ntau feem ntau mob plab hnyuv los ntshav tau tsim (3.5% thiab 1.8%, feem). Hauv cov tshuaj acetylsalicylic acid + pawg clopidogrel, cov kabmob sib xyaw ua haujlwm tau ntau dua thaum piv nrog cov acetylsalicylic acid + placebo pawg (1.4% thiab 0.8%, feem). Kuj tseem tsis pom muaj qhov sib txawv ntawm cov kev sib txawv ntawm cov pawg no hauv kev tshwm sim ntshav tawm (0.8% thiab 0.6%, feem) thiab tuag taus los ntshav (1.1% thiab 0.7%, feem).

Hauv cov kev tshawb fawb soj ntsuam thiab nrog cov ntawv tshaj tawm tshwm sim, cov kev mob tshwm sim tom qab tau sau tseg:

lymphatic thiab circulatory systems: ua haujlwm tsis xws luag - eosinophilia, leukopenia, thrombocytopenia, tsis tshua muaj neutropenia (suav nrog neutropenia loj), mob tsis tshua muaj kab mob ntshav siab, ua tsis taus pa, thrombotic thrombocytopenic purpura, agranulocytosis, pancytopenia, mob ntshav qab zib ntau, mob txhab, mob ua ke
kev tiv thaiv kab mob: tsis tshua muaj tshwm sim - anaphylactoid kev tsis haum, mob ntshav siab, tsis paub ntau npaum li cas - kev loj hlob ntawm cov kev cuam tshuam ntawm hypersensitivity nrog thienopyridines (piv txwv li, nrog ticlopidine thiab prasugrel),
psyche: tsis tshua muaj - tsis meej pem, pomzoo,
cov hlab ntsha hauv lub cev: tsis tuaj yeem - mob taub hau, mob ntshav khov (qee qhov mob yuav ua rau tuag taus), kiv taub hau, mob caj dab, tsis tshua muaj tshwm sim - saj tsis xis nyob,
lub zeem muag: ntuag - qhov muag pom kev tsis haum (hauv qhov nqaij ntawm lub qhov muag, pom, retina),
hnov: tsis tshua muaj - vertigo,
cov hlab ntshav: feem ntau - hematomas, tsis tshua muaj tshwm sim - los ntshav los ntawm kev ua haujlwm zoo, los ntshav ntau, txo ntshav siab, vasculitis,
cov kab mob ua pa: feem ntau - txhaws ntswg, tsis tshua muaj - bronchospasm, los ntshav los ntawm cov kab mob ua pa (mob ntsws, hemoptysis), mob ntsws o, mob ntsws, mob plab hnyuv pneumonitis,
lub plab zom mov: feem ntau ua rau mob plab zom mov, plab zom mov los ntshav, dyspepsia, mob plab, mob plab hnyuv, mob plab thiab duodenal mob, xeev siab, ntuav, ua tsis taus pa, cem quav, tsis tshua muaj retroperitoneal los ntshav, tsis tshua muaj retroperitoneal thiab mob plab hnyuv. ua kom mob plab hnyuv tawm hauv plab, mob plab (suav nrog lymphocytic lossis mob ua paug), mob ua paug, mob plab,
mob siab thiab mob txeeb zig: muaj tsawg kawg - kab mob siab, mob siab tsis ua hauj lwm, kuaj ntshav kuaj ntshav ntawm lub xeev kev ua haujlwm,
daim tawv nqaij thiab cov nqaij mos subcutaneous: feem ntau - bruising, tsis xws luag - khaus, tawm pob, purpura, tsis tshua muaj tshwm sim - mob caj dab, mob nqaij daim tawv nqaij mob (erythema multiforme, Stevens-Johnson syndrome, tshuaj lom epidermal necrolysis), tshuaj tiv thaiv kab mob siab, mob caj dab lossis ua kom tawm pob. xoo pob mob nrog cov tsos mob ntawm lub cev thiab eosinophilia, urticaria, lichen planus, eczema,
musculoskeletal thiab cov ntaub so ntswg mob sib txuas: tsis tshua muaj mob - mob caj dab, mob hemarthrosis (mob hauv cov leeg musculoskeletal), myalgia, arthralgia,
ob lub raum thiab lub raum tso zis: tsis tu ncua - hematuria, tsis tshua muaj heev - kev nce siab hauv cov concentration ntawm creatinine hauv cov ntshav, glomerulonephritis,
cov kev tshawb nrhiav khoom siv thiab kev kuaj sim: qog ua ntu zus - txo qis ntawm neutrophils, nce ntxiv hauv lub sijhawm los ntshav, txo qis hauv platelets,
mob cuam tshuam ntawm thaj chaw txhaj tshuaj thiab cov teeb meem dav dav: feem ntau - los ntshav los ntawm qhov chaw hno, feem ntau tsis tshua muaj - ua npaws.

Los ntshav, mob ntshav tsis txaus

Thaum cov tsos mob hauv tsev kho mob tau tshwm sim qhia tias qhov tshwm sim ntawm los ntshav thiab qhov kev pheej hmoo ntawm kev tsim cov txiaj ntsig tsis tsim nyog, nws yog qhov yuav tsum tau ua qhov kev kuaj ntshav sai sai, txiav txim siab qhib cov ntu thromboplastin lub sijhawm, platelet suav, platelet ua haujlwm, thiab lwm yam kev kawm tsim nyog.

Lopirel yuav tsum siv nrog ceev faj hauv cov neeg mob uas muaj kev pheej hmoo los ntshav txuam nrog kev phais mob, kev raug mob, lwm yam kab mob, thiab hauv cov neeg mob tau txais cov tshuaj tsis-steroidal anti-inflammatory (tshwj xeeb, acetylsalicylic acid, heparin, COX-2 inhibitors, glycoprotein IIb / IIb / inhibitors) IIIa lossis xaiv serotonin reuptake inhibitors).

Thawj thawj lub lim tiam ntawm Lopirel txoj kev kho thiab / lossis tom qab ib qho kev kho mob kom zoo nkauj lossis kev phais mob, ua tib zoo saib xyuas cov cim los ntshav, suav nrog latent, yuav tsum tau nqa tawm.

Vim tias qhov ua tau nce ntxiv ntawm kev siv khov kho ntau dua los ntshav, kev siv tshuaj Lopirel thiab warfarin tsis pom zoo. Qhov zam tshwj xeeb yog qee yam kev mob tshwm sim tsawg tsawg: muaj nyob rau ntawm sab laug ventricle ntawm lub plab hnyuv thiav, stenting hauv cov neeg mob atrial fibrillation, thiab lwm yam.

Thaum yuav los tom ntej ua haujlwm phais thiab tsis muaj qhov xav tau los ua kom lub cev tiv thaiv kev mob, Lopirel thawj coj yuav tsum nres 7 hnub ua ntej kev cuam tshuam.

Ua ntej pib siv cov tshuaj tshiab thiab ua ntej kev phais mob tom ntej, tus neeg mob yuav tsum qhia rau tus kws kho mob (suav nrog tus kws kho hniav) txog kev noj Lopirel.

Cov tshuaj lengthens lub sijhawm los ntshav, yog li ntawd, nws yuav tsum tau siv nrog ceev faj nyob rau hauv cov neeg mob uas muaj kab mob predisposing los ntshav (tshwj xeeb tshaj yog intraocular thiab gastrointestinal).

Tus neeg mob yuav tsum tau ceeb toom tias thaum noj Lopirel (hauv kev kho mob monotherapy lossis hauv kev sib xyaw nrog acetylsalicylic acid), cheem los ntshav yuav tsum siv sijhawm ntau. Yog tias muaj ntshav txawv txawv tshwm sim (los ntawm sijhawm lossis hauv ib cheeb tsam), koj yuav tsum sab laj nrog koj tus kws kho mob.

Lub Tuam Txhab Ua Yeeb Yam (Thrombocytopenic Purpura)

Txawm hais tias tom qab luv luv ntawm clopidogrel, kuj tsis tshua muaj tus neeg muaj mob thrombocytopenic purpura, uas muaj cov kabmob thrombocytopenia, microangiopathic hemolytic anemia, nrog los ntawm kev ua haujlwm tsis zoo hauv lub raum, ua npaws, mob hlab ntsha hlwb. TTP yog suav tias yog qhov muaj feem yuav txo tau txoj sia uas yuav tsum tau kho tam sim ntawd, suav nrog plasmapheresis.

Nrhiav Hemophilia

Thaum kho nrog clopidogrel, cov neeg uas tau kis mob hemophilia tau muab sau cia. Thaum paub tseeb tias elongation ntawm qhib ib feem thromboplastin lub sijhawm tsis muaj kev tsim los ntshav lossis nrog nws, koj yuav tsum xav txog qhov yuav ua rau mob hemophilia, thiab yog tias muaj kev kuaj mob tsim nyog, tsum tsis txhob noj Lopirel thiab pib kho kom tsim nyog.

Tsis ntev los no ischemic mob stroke

Lopirel tsis pom zoo thaum sau tshuaj rau ischemic mob hnyav txog 7 hnub dhau los vim tsis muaj cov ntaub ntawv hais txog kev siv nws hauv cov xwm txheej no.Kev sib xyaw ua ke nrog cov tshuaj acetylsalicylic acid thiab clopidogrel hauv cov neeg mob uas tsis ntev los no ischemic nres lossis ischemic stroke thiab muaj qhov tshwm sim siab dua ntawm kev tshwm sim atherothrombotic tsis zoo dua li kev kho mob monotherapy nrog clopidogrel, tab sis muaj kev pheej hmoo ntawm kev los ntshav ntau dua.

Cev xeeb tub thiab lactation

Cov kev tshawb fawb tsiaj tsis tau qhia qhov tseeb thiab tsis ncaj rau ntawm clopidogrel ntawm kev txhim kho embryonic, kev xeeb tub, kev yug menyuam, kev loj hlob tom qab, tab sis vim tsis muaj cov ntaub ntawv soj ntsuam uas cuam tshuam, kev siv Lopirel yog contraindicated rau cov neeg mob cev xeeb tub.

Hauv kev tshawb fawb ntawm cov nas, nws tau pom tias clopidogrel thiab nws cov metabolites kis mus rau niam mis, yog li ntawd, kev kho Lopirel, kev pub mis niam yuav tsum tsis tsum. Cov ntaub ntawv hais txog kev tso tawm clopidogrel nrog tib neeg cov kua mis niam tsis muaj.