Aggrastat

Aggrastat is the brand name for tirofiban, a nonpeptide antagonist of the glycoprotein IIb/IIIa receptor. Tirofiban reversibly inhibits the final common pathway of platelet aggregation by preventing fibrinogen and von Willebrand factor from binding to activated platelets, thereby reducing platelet aggregation and thrombus formation in acute coronary syndromes.

Indications for Aggrastat include the management of acute coronary syndromes, such as unstable angina and non–ST-segment elevation myocardial infarction (NSTEMI), and as an adjunct to percutaneous coronary intervention to reduce ischemic complications when used with standard therapies like aspirin and heparin.

Administration and pharmacokinetics are intravenous. Aggrastat is given as an initial loading or bolus dose followed by a continuous maintenance infusion. Onset of antiplatelet effect is rapid, and effects diminish after the infusion is stopped due to the drug’s short duration of action. Renal function can influence clearance, and dose adjustments may be considered in renal impairment.

Contraindications include active major bleeding, a history of intracranial hemorrhage, recent major surgery or trauma, severe uncontrolled hypertension, known bleeding diatheses, and other conditions with high bleeding risk. Caution is advised in patients with moderate renal impairment and in those receiving concomitant anticoagulants or other antiplatelet agents.

Adverse effects are primarily related to bleeding, including major and minor bleeding. Thrombocytopenia, hypersensitivity reactions, hypotension, and rarely renal dysfunction can occur. When used with other anticoagulants, the risk of bleeding is increased, so careful monitoring of bleeding and platelet counts is recommended.