Tirofiban Hydrochloride (2 brand names, 2 dosage forms, 2 routes)
Available dosage forms: SOLUTION, INJECTABLE.
Routes of administration: INJECTION, INTRAVENOUS.
Brand Names
- AGGRASTAT
- TIROFIBAN HYDROCHLORIDE
Indications and Usage
Tirofiban Hydrochloride Injection is indicated to reduce the rate of thrombotic cardiovascular events (combined endpoint of death, myocardial infarction, or refractory ischemia/repeat cardiac procedure) in patients with non-ST elevation acute coronary syndrome (NSTE-ACS).
Contraindications
Tirofiban Hydrochloride Injection is contraindicated in patients with: Severe hypersensitivity reaction to Tirofiban Hydrochloride Injection (i.e., anaphylactic reactions) [see Adverse Reactions ( 6.2)] . A history of thrombocytopenia following prior exposure to Tirofiban Hydrochloride Injection [see Adverse Reactions ( 6.1)] . Active internal bleeding or a history of bleeding diathesis, major surgical procedure or severe physical trauma within the previous month [see Adverse Reactions ( 6.1)] .
Drug Interactions
Concomitant use of fibrinolytics, anticoagulants and antiplatelet drugs increases the risk of bleeding.
Mechanism of Action
Tirofiban Hydrochloride is a reversible antagonist of fibrinogen binding to the GP IIb/IIIa receptor, the major platelet surface receptor involved in platelet aggregation. When administered intravenously, Tirofiban Hydrochloride inhibits ex vivoplatelet aggregation in a dose- and concentration-dependent manner. When given according to the PRISM-PLUS regimen of 0.4 mcg/kg/min over 30 minutes followed by a 0.1 mcg/kg/min maintenance infusion, > 90% inhibition of platelet aggregation is attained by the end of the 30-minute infusion. When given according to the recommended regimen of 25 mcg/kg followed by a 0.15 mcg/kg/min maintenance infusion, > 90% inhibition of platelet aggregation is attained within 10 minutes. Platelet aggregation inhibition is reversible following cessation of the infusion of Tirofiban Hydrochloride.
Overdosage
In clinical trials, inadvertent overdosage with Tirofiban Hydrochloride Injection occurred in doses up to 2 times the recommended dose for initial infusion doses. Inadvertent overdosage occurred in doses up to 9.8 times the 0.15 mcg/kg/min maintenance infusion rate. The most frequently reported manifestation of overdosage was bleeding, primarily minor mucocutaneous bleeding events and minor bleeding at the sites of cardiac catheterization [see Warnings and Precautions ( 5.1)]. Overdosage of Tirofiban Hydrochloride Injection should be treated by assessment of the patient’s clinical condition and cessation or adjustment of the drug infusion as appropriate. Tirofiban Hydrochloride can be removed by hemodialysis.