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15 Cards in this Set
- Front
- Back
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Antiplatelet Drugs
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Acetylsalicyclic Acid
P2Y12 Antags PDE Inhibitors GPIIb/IIIa Antags |
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Aspirin MOA
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Inhibit TXA2 formation
Inhibit plt activation and agg |
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Aspirin Characteristics
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Lack of response may be due to aspirin resistance
Extrinsic mech: INC platelet function due to exogenous substances (smoking), other NSAIDS, INC plt turnover, inadeq dosing Intrinsic Mech: inducible COX2 activity, genetic polymorphism, production of TXA precursor, polymorphism GPIIb/IIIa Rc making plt less dep on TXA for activation |
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Aspirin PK
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Rapid abs in stomach and upper stomach
Peak conc in 15-20 mins Peak INHIBITORY eff: 1 hr post admin IRREV INHIB of Cox... for the rest of the plt lifespan... 7 days |
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Aspirin Use
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Secondary Prevention of TIA, ischemic stroke, and MI
Prevention of ischemic events in pts with angina Prevention of CABG occlusion |
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Aspirin ADR/Limitations
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Risk of GI events: ulceration and bleeding
Allergic rxn Irreversible plt inhib not very eff antithrombotic drug but widely used due to ease of use |
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ADP Receptor Antag
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P2Y12
Clopidogrel Ticlopidine Prasugrel Cangrelor Ticagrelor |
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Clopidogrel MOA
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Block ADP binding at ADP receps
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Clopidogrel Characteristics
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Combined with aspirin
Std prevention of MI in ACS and for thrombosis prevention after coronary stent and angioplasty Resistance: Great inter-individual variation in response to abs and metab |
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Clopidogrel PK
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Rapid abs after oral admin (>50%)
Parent drug and metabolites bind well to plasma prot (90%) Prodrug: must be metab-ed in liver |
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Clopidogrel Use
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Secondary prevention of ischemic complications after MI, ischemic stroke, and estab-ed peripheral arterial disease
Secondary prevention of ischemic complications in pts with ACS without ST segment elevation |
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Clopidogrel ADR/Limitations
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Only slightly more eff than aspirin
More expensive As with aspirin it binds irreversibly to plts |
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Ticlopidine MOA
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Block ADP binding at ADP recep
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Ticlopidine PK
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similar to clopidogrel
food inc abs |
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Ticlopidine ADR/Limitations
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Rare fatal ADRs
neutropenia and bone marrow aplasia Less favorable adr profile than clopidogrel |
