MI Flashcards
Clopidogrel
prodrug
selective irreversible inhibitor of ADP induced platelet aggregation
inhibits P2Y12 receptor
Has no effect on TXA or 5HT
Use: MI or stroke occured previously
active metabolite via CYP 2C19/minor role 3A4 which gives a free thiol metabolites which then forms a disulfide linkage with a free SH present on the receptor and thereby inactivates it
inactive metabolites via esterases
ADR: rash, intracranial hemorrhage, neutropenia, inc bleed time, thrombotic thrombocytopenic purpura
DDI: CYP inducers/inhibitors, atorvastatin dec effectiveness, PPI
Ticlopidine
Prodrug
inhibits P2Y12 receptor
activated by CYP2C19/3A4 resulting in formation of a disulfide linkage with ADP receptor
It is an inhibitor of CYP 3A4 and 2C19
Use: prevent stroke and MI in pt undergoing coronary stent surgery
ADR: N/V, diarrhea, neutropenia (occurs more than clopidogrel), thrombotic thrombocytopenic purpura
DDI: aspirin, warfarin, antacid may dec absorption, CYP
Prasugrel
irreversible inhibition of platelet aggregation
more potent as antiplatelet
effective in reducing moretality in nonfatal MI and stroke (same as clopidogrel)
superior when used for pt undergoing PCI
Use: pt with ACS who are managed by PCI (unstable angina, STEMI, non STEMI MI)
Has dec reliance on CYP for activation. Can use esterases now.
ADR: higher inc risk of bleed, thrombotic thrombocytopenic purpura
Ticagrelor
Antiplatelet drug
Binds reversibly to allosteric site rather than the ADP binding site
NO hepatic activation, NOT a prodrug, active as parent drug and as metabolite
approved for use in STEMI, pt with thrombotic event (stroke, MI)
superior to clopidogrel in recducing mortality
first pass effect due to metabolism by CYP 3A4
ADR: higher inc risk of bleed, SOB, dizzy, HA
DDI: CYP
Dipyridamole
MOA: inhibits adenosine uptake by RBC, PDE inhibition in platelelts, and inhibition of TXA synthesis
Use: prevent MI recurrence and prophylactically as an adjunct to warfarin in heart valave replacement
metabolized in liver via glucuronidation
substrate for p-gp
high PPB
ADR: chest pain, exacerbation of angina, altered ECG, HA, dizzy
DDI: antiplatelet agents, PDE inhibitors
eptifibatide
cyclic peptide
found in venom of pygmy rattlesnakes
admin: infusion
doesn’t bind vitronectin receptors
inhibits Gp IIb IIIa receptor
metab: deamination which requires renal elimination (renal dx pt should use abciximab)
ADR: bleed, thrombocytopenia, hypotension
Tirofiban
Use: non Q wave MI, unstable angina
similar to eptifibatide
ADR: bleed
admin: infusion
