Clopidogrel thiab Ticagrelor yog P2Y12 receptor antagonists uas inhibit plateboard adenosine diphosphate (ADP) los ntawm kev xaiv inhibiting kev khi ntawm adenosine diphosphate (ADP) rau nws plateboard P2Y12 receptor thiab kev ua haujlwm ntawm theem nrab ADP-mediated glycoprotein GPa complex.b/III.

Ob leeg yog cov kws kho mob feem ntau siv cov tshuaj antiplatellers, uas tuaj yeem siv los tiv thaiv thrombosis hauv cov neeg mob uas muaj mob angina, mob hlab ntsha tawg, thiab ischemic stroke.Yog li qhov txawv li cas?

1, Lub sijhawm pib

Ticagrelor muaj txiaj ntsig zoo dua, thiab rau cov neeg mob uas mob hlab ntsha tawg, nws tuaj yeem ua sai sai rau inhibit plateplate aggregation, thaum Clopidogrel tsis zoo.

2, Siv cov koob tshuaj ntau zaus

Ib nrab-lub neej ntawm Clopidogrel yog 6 teev, thaum ib nrab-lub neej ntawm Ticagrelor yog 7.2 teev.

Txawm li cas los xij, cov metabolites nquag ntawm Clopidogrel yog irreversibly khi rau P2Y12 kev kawm, thaum lub ntsiab lus Ticagrelor thiab P2Y12 yog thim rov qab.

Yog li ntawd, Clopidogrel tau noj ib hnub ib zaug, thaum Ticagrelor muab ob zaug ib hnub.

3, Antiplatelet kev ua haujlwm

Ticagrelor's antiplatelets muaj txiaj ntsig zoo dua, thiab kev tshawb fawb pom tias Ticagrelor tsis muaj qhov sib txawv hauv kev txo qis kev tuag ntawm cov hlab plawv thiab myocardial infarction, uas siab dua hauv pawg Clopidogrel, thiab mob stroke.

Raws li cov txiaj ntsig ntawm kev kho mob Ticagrelor rau cov neeg mob uas muaj tus mob coronary syndrome (ACS), cov lus qhia tseem ceeb hauv tsev thiab txawv teb chaws pom zoo tias Ticagrelor yuav siv tau rau kev kho mob antiplatelet phaj hauv ACS cov neeg mob.Hauv ob txoj kev cai lij choj los ntawm European Heart Association (ESC NSTE-ACS Guidelines 2011 thiab STEMI Guidelines 2012), Clopidogrel tsuas yog siv tau rau cov neeg mob uas tsis tuaj yeem kho nrog Ticagrelor.

4, Kev pheej hmoo los ntshav

Qhov kev pheej hmoo ntawm los ntshav los ntawm kev siv mus sij hawm ntev ntawm Ticagrelor yog me ntsis siab dua li Clopidogrel, tab sis qhov kev pheej hmoo ntawm los ntshav zoo ib yam li siv sijhawm luv.

Kev tshawb fawb los ntawm KAMIR-NIH raws li cov neeg Esxias sab hnub tuaj qhia tau hais tias qhov kev pheej hmoo ntawm TIMI haemorrhage muaj ntau dua rau cov neeg mob hnub nyoog ≥ 75 xyoo dua li Clopidogrel.Yog li, rau cov neeg mob acS ≥ 75 xyoo, nws raug nquahu kom xaiv Clopidogrete raws li qhov nyiam P2Y12 inhibitor raws li cov tshuaj aspirin.

Antiplate platepett txoj kev kho rau cov neeg mob uas tsis tshua muaj cov phaj me me yuav tsum zam kev xaiv ntawm Ticagrelor.

5 、 Lwm yam tsis zoo tshwm sim

Feem ntau tshaj tawm cov kev phiv tshwm sim nyob rau hauv cov neeg mob kho nrog Ticagrelor yog ua pa nyuaj, bruising thiab nosebleeds, uas tshwm sim ntawm tus nqi siab tshaj nyob rau hauv cov pab pawg neeg Clopidogrel.

6 、 Kev sib cuam tshuam yeeb tshuaj

Clopidogrel yog cov tshuaj presuperial, uas yog metabolized nyob rau hauv ib feem los ntawm CYP2C19 raws li nws cov nquag metabolite, thiab noj cov tshuaj uas inhibits qhov kev ua ntawm cov enzyme no yuav txo tau cov theem uas Clopidogrel hloov mus rau hauv ib tug nquag metabolite.Yog li, kev siv cov tshuaj muaj zog lossis nruab nrab CYP2C19 inhibitors xws li omeprazole, Esomeprazole, fluoronazole, voliconazole, fluoxetine, fluorovolsamine, cycloproxacin, camasi tsis pom zoo.

Ticagrelor feem ntau yog metabolized los ntawm CYP3A4, thiab ib feem me me yog metabolized los ntawm CYP3A5.Combined siv CYP3A inhibitors tuaj yeem nce Cmax thiab AUC ntawm ticagrelor.Yog li ntawd, kev sib xyaw ua ke ntawm ticagrelor nrog cov muaj zog CYP3A inhibitors xws li ketoconazole, itraconazole, voriconazole, clarithromycin, thiab lwm yam, yuav tsum tau zam.Txawm li cas los xij, kev sib xyaw ua ke ntawm CYP3A inducer tuaj yeem txo Cmax thiab AUC ntawm ticagrelor, raws li.Yog li ntawd, kev sib xyaw ua ke ntawm CYP3A muaj zog inducer, xws li dexamethasone, phenytoin sodium, phenobarbital thiab carbamazepine, yuav tsum zam.

7. Kev kho Antiplatelet hauv cov neeg mob lub raum tsis txaus

PLATO, hauv kev tshawb fawb ntawm cov neeg mob uas muaj mob plawv nrog lub raum tsis ua haujlwm, pom tias muaj kev nce ntxiv hauv cov ntshav creatinine hauv pawg ticagrelor piv nrog clopidogrel; Kev tshuaj xyuas ntxiv ntawm cov neeg mob kho nrog ARB pom tias nce 50% hauv cov ntshav creatinine>, raum cuam tshuam txog qhov tsis zoo. Cov xwm txheej, thiab lub raum ua haujlwm cuam tshuam txog cov xwm txheej tsis zoo hauv pawg ticagrelor ntau dua li hauv pawg clopidogrel.Yog li ntawd, clopidogrel + aspirin yuav tsum yog thawj qhov kev xaiv rau cov neeg mob lub raum tsis ua haujlwm.

8 、 Kev kho Antiplatelet rau cov neeg mob gout / hyperuricemia

Kev siv ntev ntev ntawm ticagrelor tau pom tias yuav ua rau muaj kev pheej hmoo ntawm gout.Gout yog qhov tshwm sim tsis zoo ntawm kev kho mob ticagrelor, uas tej zaum yuav cuam tshuam rau cov nyhuv metabolites ntawm ticagrelor ntawm uric acid metabolism. Yog li ntawd clopidogrel yog qhov zoo tshaj plaws antiplatelet kho rau gout. / cov neeg mob hyperuricemia.

9 、 Kev kho Antiplatelet ua ntej CABG (coronary artery bypass grafting)

Cov neeg mob tau teem caij rau CABG uas tau noj cov tshuaj aspirin qis (75 txog 100 mg) tsis tas yuav tsum nres ua ntej; Cov neeg mob uas tau txais P2Y12 inhibitor yuav tsum txiav txim siab txiav ticagrelor tsawg kawg 3 hnub thiab clopidogrel tsawg kawg 5 hnub ua ntej.

10, Tsawg reactivity ntawm clopidogrel

Qhov qis qis ntawm platelets rau clopidogrel tuaj yeem ua rau lub sijhawm ischemia.Txhawm rau kom kov yeej qhov tsis tshua muaj tshwm sim ntawm clopidogrel, nce koob tshuaj clopidogrel lossis hloov nrog ticagrelor yog cov kev xaiv ntau.

Hauv kev xaus, ticagrelor ua sai sai thiab muaj zog inhibitory nyhuv phaj.Hauv kev kho mob ntawm cov kab mob plawv, ticagrelor muaj cov nyhuv antithrombotic zoo dua, uas tuaj yeem txo qis kev tuag ntxiv, tab sis nws muaj kev pheej hmoo los ntshav ntau dua, thiab muaj kev cuam tshuam ntau dua xws li ua tsis taus pa, contusion, bradycardia, gout thiab lwm yam tshaj li clopidogrel.