I-Clopidogrel kunye ne-Ticagrelor yi-P2Y12 i-receptor antagonists evimbela i-plateboard adenosine diphosphate (ADP) ngokuthintela ngokufanelekileyo ukubopha i-adenosine diphosphate (ADP) kwi-plateboard yayo ye-P2Y12 receptor kunye nomsebenzi wesibini se-ADP-mediated glycoprotein GPII.b/III.

Zombini zii-antiplatellers ezisetyenziswa ngokweklinikhi, ezinokuthi zisetyenziswe ukukhusela i-thrombosis kwizigulane ezine-angina engapheliyo, i-acute coronary artery syndrome, kunye ne-ischemic stroke.Ngoko ke yintoni umahluko?

1, Ixesha lokuqala

I-Ticagrelor iyasebenza ngakumbi, kwaye izigulane ezine-acute coronary artery syndrome, zinokusebenza ngokukhawuleza ukuvimbela ukuhlanganiswa kweplateplate, ngelixa i-Clopidogrel ingasebenzi kakuhle.

2, Thatha umthamo wethamo

Ubomi besiqingatha seClopidogrel ziiyure ze-6, ngelixa i-half-life ye-Ticagrelor yi-7.2 iiyure.

Nangona kunjalo, i-metabolites esebenzayo yeClopidogrel ibophelela ngokungenakuguquleka kwisifundo se-P2Y12, ngelixa i-Ticagrelor kunye ne-P2Y12 isifundo sibuyiselwa umva.

Ngoko ke, i-Clopidogrel ithathwa kanye ngosuku, ngelixa i-Ticagrelor inikezelwa kabini ngosuku.

3, Antiplatelet isenzo

I-antiplatelet ye-Ticagrelor yayisebenza ngakumbi, kwaye izifundo zibonise ukuba i-Ticagrelor ayinayo umehluko ekunciphiseni ukufa kwe-cardiovascular death and myocardial infarction, eyayiphezulu kuneqela le-Clopidogrel, kunye ne-stroke.

Ngokusekelwe kwiinzuzo zonyango lwe-Ticagrelor kwizigulane ezine-acute coronary syndrome (ACS), izikhokelo ezifanelekileyo ekhaya nakwamanye amazwe zincoma ukuba i-Ticagrelor isetyenziswe unyango lwe-antiplatelet plate kwizigulane ze-ACS.Kwizikhokelo ezibini ezigunyazisiweyo ezivela kwi-European Heart Association (ESC NSTE-ACS Guidelines 2011 kunye ne-STEMI Guidelines 2012), i-Clopidogrel inokusetyenziswa kuphela kwizigulane ezingenakuphathwa ngeTicagrelor.

4,Ingozi yokopha

Umngcipheko wokuphuma kwegazi kwisicelo sexesha elide leTicagrelor wawuphezulu kancinci kuneClopidogrel, kodwa umngcipheko wokuphuma kwegazi wawufana nokusetyenziswa kwexesha elifutshane.

Uphononongo olwenziwe yi-KAMIR-NIH olusekwe kubemi baseMpuma Asia lubonisa ukuba umngcipheko we-TIMI ukopha ubephezulu kakhulu kwizigulane ezineminyaka yobudala ≥ 75 kuneClopidogrel.Ngoko ke, kwizigulane ze-acS ≥ iminyaka eyi-75 ubudala, kucetyiswa ukuba ukhethe i-Clopidogrete njenge-inhibitor ekhethiweyo ye-P2Y12 ngesiseko se-aspirin.

Unyango lwe-Antiplate platepett kwizigulane ezineeplati eziphantsi zokubala iiplate ezincinci kufuneka ziphephe kwakhona ukhetho lweTicagrelor.

5. Ezinye iziphumo ezibi

Iimpendulo ezixhaphakileyo ezichazwe ngokuqhelekileyo kwizigulane eziphathwe nge-Ticagrelor zazinzima ukuphefumla, ukubetha kunye ne-nosebleeds, eyenzeka kwizinga eliphezulu kuneqela le-Clopidogrel.

6. Ukusebenzisana kweziyobisi

I-Clopidogrel lichiza le-presuperial, elenziwe ngokuyinxenye yiCYP2C19 njengemetabolite esebenzayo, kwaye ukuthatha ichiza elithintela umsebenzi wale enzyme kunokunciphisa inqanaba apho iClopidogrel iguqulwa ibe yimetabolite esebenzayo.Ngoko ke, ukusetyenziswa okudibeneyo kwe-CYP2C19 inhibitors eqinile okanye ephakathi njenge-omeprazole, i-Esomeprazole, i-fluoronazole, i-volconazole, i-fluoxetine, i-fluorovolsamine, i-cycloproxacin, i-camasi ayikhuthazwa.

I-Ticagrelor i-metabolized ikakhulu yi-CYP3A4, kwaye inxalenye encinci i-metabolized yi-CYP3A5.Ukusetyenziswa okudibeneyo kwe-CYP3A inhibitors kunokunyusa i-Cmax kunye ne-AUC ye-ticagrelor.Ngoko ke, ukusetyenziswa okudibeneyo kwe-ticagrelor kunye ne-CYP3A inhibitors enamandla njenge-ketoconazole, i-itraconazole, i-voriconazole, i-clarithromycin, njl., kufuneka igwenywe.Nangona kunjalo, ukusetyenziswa okudibeneyo kwe-CYP3A inducer kunokunciphisa i-Cmax kunye ne-AUC ye-ticagrelor, ngokulandelanayo.Ngoko ke, ukusetyenziswa okudibeneyo kwe-CYP3A inducer enamandla, njenge-dexamethasone, i-phenytoin sodium, i-phenobarbital kunye ne-carbamazepine, kufuneka igwenywe.

7, Unyango lwe-Antiplatelet kwizigulana ezinokusilela kwezintso

I-PLATO, kuphononongo lwezigulane ezine-acute coronary syndrome kunye nokusilela kwezintso, ibonise ukwanda okukhulu kwe-serum creatinine kwiqela le-ticagrelor xa kuthelekiswa ne-clopidogrel;Uhlalutyo olongezelelweyo lwezigulane eziphathwe nge-ARB lubonise ukwanda kwe-serum creatinine nge-50% iziganeko, kunye neziganeko ezimbi ezinxulumene nomsebenzi we-renal ziphezulu kakhulu kwiqela le-ticagrelor kuneqela le-clopidogrel.Ngoko ke, i-clopidogrel + i-aspirin kufuneka ibe yinto yokuqala yokukhetha izigulane ezine-renal insufficiency.

8, unyango lwe-Antiplatelet kwizigulane ezine-gout / hyperuricemia

Ukusetyenziswa kwexesha elide le-ticagrelor kubonakaliswe ukunyusa umngcipheko we-gout.I-Gout yinto exhaphakileyo yokuchasa unyango lwe-ticagrelor, enokuthi ihambelane nefuthe le-metabolites esebenzayo ye-ticagrelor kwi-uric acid metabolism.Ngoko ke i-clopidogrel yonyango oluchanekileyo lwe-antiplatelet ye-gout. / izigulane ze-hyperuricemia.

9, unyango lwe-Antiplatelet phambi kwe-CABG (i-coronary artery bypass grafting)

Izigulane ezicwangciselwe i-CABG ezithatha i-aspirin ye-dose ephantsi (i-75 ukuya kwi-100 mg) ayifuni ukuyeka kwangaphambili; Izigulane ezifumana i-P2Y12 inhibitor kufuneka ziqwalasele ukuyeka i-ticagrelor ubuncinane iintsuku ze-3 kunye ne-clopidogrel ubuncinane iintsuku ze-5 kwangaphambili.

10, Ukusebenza okuphantsi kwe-clopidogrel

Ukusebenza okuphantsi kweeplatelet kwi-clopidogrel kunokukhokelela kwixesha le-ischemia.Ukuze unqobe i-reactivity ephantsi ye-clopidogrel, ukwandisa umthamo we-clopidogrel okanye ukutshintshwa kwe-ticagrelor zikhetho eziqhelekileyo.

Ukuqukumbela, i-ticagrelor yenza ngokukhawuleza kwaye ine-plate ye-inhibitory effect eqinile.Kunyango lwe-acute coronary syndrome, i-ticagrelor inempembelelo engcono ye-antithrombotic, enokunciphisa ngakumbi ukufa, kodwa inomngcipheko ophezulu wokuphuma kwegazi, kwaye ineempembelelo eziphezulu ezinobungozi ezifana ne-dyspnea, i-contusion, i-bradycardia, i-gout kunye nokunye ngaphezu kwe-clopidogrel.