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22 Cards in this Set
- Front
- Back
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Aspirin MOA
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Irreversibly acetylates serine of COX, stearically inhibiting arachidonate binding, inhibiting thromboxane production
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What is the major eicosanoid produced by platelets?
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Thromboxane
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What drug should you not take with aspirin and why?
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Ibuprofen, b/c it has a greater affinity for the serine residue
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Describe the absorption of aspirin.
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Regular - rapidly absorbed in stomach and upper small intestines. Reaches platelet inhibition in 60 minutes. enteric-coated aspirin has delayed absorption that is sometimes incomplete and subject to first pass metabolism to salicylate.
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What is the major COX product of endothelial cells?
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PGI2
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Describe the affects of aspirin with dosing levels.
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30-75 (antiplatelet), 300 (analgesic, antipyretic, vascular, GI), >2000 (antiinflammatory)
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What are the adverse effects of aspirin?
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GI (dyspepsia, bleeding), tinnitus, anaphylaxis, hemorrhagic stroke, aggravation of gout
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MOA of dipyridamole
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Inhibits platelet phosphodiesterase (increased cAMP, inhibits platelet aggregation), increases plasma adenosine
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Describe the preparation and absorption of dipyridamole.
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Sustained release preparation, absorption requires a low pH
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Dipyridamole side effects
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Headaches (improve with time, GI, dizziness, flushing, hypotension, syncope
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What are the drug interactions of dipyridamole?
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Causes accumulation of adenosine, hypotension with IV adenosine given for supraventricular tachycardia
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What are the thienopyridines?
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Clopidogrel, ticlopidine
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Thienopyridine MOA
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Primary (inhibition of ADP induced platelet activation - probably covalently modifies cysteine thiol of the Gi linked ADP receptor), minor (inhibits the GP IIb/IIIa receptor, interferes with vWF function)
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Describe ticlopidine absorption.
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80% absorbed rapidly, increased by food, decreased by antacids
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Thienopyridines: pharmacokinetics
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Prodrugs, hepatic bioactivation, delay of onset requires loading, long half life
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What is the other name for clopidogrel?
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Plavix
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What is the main toxicity for clopidogrel?
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GI bleeding
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What is plasugrel?
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Novel thienopyridine with high IPA in clopidogrel hyporesponders
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What is the main glycoprotein IIb/IIIa inhibitor?
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Abciximab
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GIIb/IIIa: found where? function?
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Platelets and megakaryocytes, allows fibrinogen to crosslink platelets
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What is the primary indication for GP IIb/IIIa inhibitors?
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Percutaneous coronary interventions
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What is the main toxicity for GP IIb/IIIa inhibitors?
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GI bleeding
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