I-Clopidogrel ne-Ticagrelor yi-P2Y12 receptor antagonists evimbela i-plateboard adenosine diphosphate (ADP) ngokuvimbela ngokukhetha ukubopha i-adenosine diphosphate (ADP) ku-plateboard yayo ye-P2Y12 receptor kanye nomsebenzi wesibili we-ADP-mediated glycoprotein GPII.b/III.

Zombili zingama-antiplateller asetshenziswa kakhulu emtholampilo, angasetshenziswa ukuvimbela i-thrombosis ezigulini ezine-angina ezinzile engapheli, i-acute coronary artery syndrome, kanye ne-ischemic stroke.Uyini-ke umehluko?

1, Isikhathi sokuqala

I-Ticagrelor iphumelela kakhulu, futhi ezigulini ezine-acute coronary artery syndrome, ingakwazi ukwenza ngokushesha ukuvimbela ukuhlanganiswa kweplateplate, kuyilapho i-Clopidogrel ingasebenzi kahle.

2, Thatha imvamisa umthamo

I-half-life ye-Clopidogrel amahora angu-6, kanti i-half-life ye-Ticagrelor ingamahora angu-7.2.

Kodwa-ke, ama-metabolites asebenzayo e-Clopidogrel abophezela ngendlela engenakuhlehliswa esihlokweni se-P2Y12, kuyilapho isihloko se-Ticagrelor ne-P2Y12 zibuyiselwa emuva.

Ngakho-ke, i-Clopidogrel ithathwa kanye ngosuku, kuyilapho i-Ticagrelor inikezwa kabili ngosuku.

3, isenzo se-Antiplatelet

I-antiplatelet ye-Ticagrelor yayiphumelela kakhulu, futhi izifundo zibonise ukuthi i-Ticagrelor yayingenalo umehluko ekunciphiseni ukufa kwenhliziyo ne-myocardial infarction, eyayiphakeme kuneqembu le-Clopidogrel, kanye ne-stroke.

Ngokusekelwe ezinzuzweni zokwelashwa kwe-Ticagrelor ezigulini ezine-acute coronary syndrome (ACS), iziqondiso ezifanele ekhaya nakwamanye amazwe zincoma ukuthi i-Ticagrelor isetshenziselwe ukwelashwa kwe-antiplatelet plate ezigulini ze-ACS.Eziqondisweni ezimbili ezigunyaziwe ezivela ku-European Heart Association (ESC NSTE-ACS Guidelines 2011 kanye ne-STEMI Guidelines 2012), i-Clopidogrel ingasetshenziswa kuphela ezigulini ezingakwazi ukuphathwa nge-Ticagrelor.

4,Ingozi yokopha

Ingozi yokuphuma kwegazi kusukela ekusetshenzisweni kwesikhathi eside kwe-Ticagrelor yayiphakeme kancane kune-Clopidogrel, kodwa ingozi yokuphuma kwegazi yayifana nokusetshenziswa kwesikhashana.

Ucwaningo lwe-KAMIR-NIH olusekelwe kubantu baseMpumalanga Asia lubonisa ukuthi ingozi yokopha kwe-TIMI yayiphezulu kakhulu ezigulini ezineminyaka engu-≥ 75 kunakwi-Clopidogrel.Ngakho-ke, ezigulini ze-acS ezineminyaka engu-≥ engu-75 ubudala, kunconywa ukuthi ukhethe i-Clopidogrete njenge-P2Y12 inhibitor ekhethwayo ngesisekelo se-aspirin.

I-Antiplate platepett therapy yeziguli ezinepuleti ephansi yokubala ipuleti encane kufanele futhi igweme inketho ye-Ticagrelor.

5. Okunye ukusabela okungekuhle

Ukusabela okubi okuvame ukubikwa ezigulini eziphathwe nge-Ticagrelor kwakunzima ukuphefumula, ukulimaza kanye ne-nosebleeds, okwenzeka ngenani eliphakeme kuneqembu le-Clopidogrel.

6, Ukusebenzisana kwezidakamizwa

I-Clopidogrel iyisidakamizwa se-presuperial, esakhiwe ngokwengxenye yi-CYP2C19 njenge-metabolite esebenzayo, futhi ukuthatha umuthi ovimbela umsebenzi wale enzyme kunganciphisa izinga lapho i-Clopidogrel iguqulwa ibe yi-metabolite esebenzayo.Ngakho-ke, ukusetshenziswa okuhlangene kwe-CYP2C19 inhibitors eqinile noma elinganiselwe njenge-omeprazole, i-Esomeprazole, i-fluoronazole, i-volconazole, i-fluoxetine, i-fluorovolsamine, i-cycloproxacin, i-camasi ayinconywa.

I-Ticagrelor i-metabolized ikakhulukazi yi-CYP3A4, futhi ingxenye encane isetshenziselwa i-CYP3A5.Ukusetshenziswa okuhlangene kwe-CYP3A inhibitors kungandisa i-Cmax ne-AUC ye-ticagrelor.Ngakho-ke, ukusetshenziswa okuhlangene kwe-ticagrelor nge-CYP3A inhibitors enamandla njenge-ketoconazole, i-itraconazole, i-voriconazole, i-clarithromycin, njll., kufanele kugwenywe.Nokho, ukusetshenziswa okuhlangene kwe-CYP3A inducer kunganciphisa i-Cmax ne-AUC ye-ticagrelor, ngokulandelana.Ngakho-ke, ukusetshenziswa okuhlangene kwe-CYP3A inducer enamandla, njenge-dexamethasone, i-phenytoin sodium, i-phenobarbital ne-carbamazepine, kufanele kugwenywe.

7, Ukwelashwa kwe-Antiplatelet ezigulini ezinokwehluleka kwezinso

I-PLATO, ekucwaningweni kweziguli ezine-acute coronary syndrome engasebenzi kahle, ibonise ukwanda okukhulu kwe-serum creatinine eqenjini le-ticagrelor uma kuqhathaniswa ne-clopidogrel; Ukuhlaziywa okwengeziwe kweziguli eziphathwe nge-ARB kubonise ukwanda kwe-serum creatinine ngo-50% izenzakalo, kanye nezenzakalo ezimbi ezihlobene nomsebenzi we-renal zaziphakeme kakhulu eqenjini le-ticagrelor kuneqembu le-clopidogrel.Ngakho-ke, i-clopidogrel + i-aspirin kufanele ibe yisinqumo sokuqala ezigulini ezinokuhluleka kwezinso.

8, Ukwelashwa kwe-Antiplatelet ezigulini ezine-gout/hyperuricemia

Ukusetshenziswa isikhathi eside kwe-ticagrelor kuye kwaboniswa ukwandisa ingozi ye-gout.I-Gout iyindlela evamile yokwelapha engavamile yokwelashwa kwe-ticagrelor, okungenzeka ihlotshaniswe nomphumela we-metabolites esebenzayo ye-ticagrelor ku-uric acid metabolism.Ngakho-ke i-clopidogrel iyindlela yokwelapha ye-antiplatelet engcono kakhulu ye-gout. /iziguli ze-hyperuricemia.

9, Ukwelashwa kwe-Antiplatelet ngaphambi kwe-CABG (i-coronary artery bypass grafting)

Iziguli ezihlelelwe i-CABG ezithatha i-aspirin yedosi ephansi (75 kuya ku-100 mg) akudingeki ziyeke ngaphambi kokuhlinzwa;Iziguli ezithola i-P2Y12 inhibitor kufanele zicabangele ukuyeka i-ticagrelor okungenani izinsuku ezingu-3 kanye ne-clopidogrel okungenani izinsuku ezingu-5 ngaphambi kokuhlinzwa.

10, Ukusebenza okuphansi kwe-clopidogrel

Ukusebenza okuphansi kwamaplatelet ku-clopidogrel kungaholela esikhathini se-ischemia.Ukuze unqobe i-reactivity ephansi ye-clopidogrel, ukwandisa umthamo we-clopidogrel noma ukuyifaka esikhundleni se-ticagrelor kuyisinqumo esivamile.

Ekuphetheni, i-ticagrelor yenza ngokushesha futhi ine-plate ye-inhibitory effect eqinile.Ekwelapheni i-acute coronary syndrome, i-ticagrelor inomphumela ongcono we-antithrombotic, ongaqhubeka nokunciphisa ukufa, kodwa unengozi enkulu yokopha, futhi unemiphumela emibi kakhulu efana ne-dyspnea, contusion, bradycardia, gout njalonjalo kune-clopidogrel.