eptifibatide
Summary
Eptifibatide is a synthetic cyclic peptide that reversibly inhibits platelet glycoprotein IIb/IIIa receptors, preventing platelet aggregation. It's used as an antiplatelet agent in acute coronary syndromes and percutaneous coronary interventions to reduce thrombotic complications.
Detail
Eptifibatide is a cyclic heptapeptide derived from rattlesnake venom that acts as a competitive, reversible antagonist of the glycoprotein IIb/IIIa receptor on platelets. This receptor is the final common pathway for platelet aggregation, binding fibrinogen and von Willebrand factor to cross-link activated platelets. By blocking this receptor, eptifibatide prevents platelet aggregation regardless of the initial stimulus (ADP, thrombin, collagen, etc.). It has a short half-life (2.5 hours) and is eliminated primarily by the kidneys. Clinical uses include non-ST elevation acute coronary syndromes (NSTEMI/unstable angina) and as adjunctive therapy during percutaneous coronary intervention (PCI). Major adverse effects include bleeding complications, particularly when combined with other anticoagulants. Contraindications include active bleeding, severe hypertension, recent surgery, and thrombocytopenia. Unlike irreversible antiplatelet agents like clopidogrel, its effects can be reversed relatively quickly by discontinuation due to its reversible binding and short half-life.
Sources
- First Aid for the USMLE Step 1
- Katzung's Basic and Clinical Pharmacology
- Braunwald's Heart Disease: A Textbook of Cardiovascular Medicine
- UpToDate
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