Overview
11 DESCRIPTION Tirofiban hydrochloride injection contains tirofiban hydrochloride, a non-peptide antagonist of the platelet GP IIb/IIIa receptor, which inhibits platelet aggregation. Tirofiban hydrochloride monohydrate is chemically described as N- (butylsulfonyl)- O -[4-(4-piperidinyl)butyl]-L-tyrosine monohydrochloride monohydrate.
Mechanism of Action
12 CLINICAL PHARMACOLOGY 12.1 Mechanism of Action Tirofiban hydrochloride injection 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 injection inhibits ex vivo platelet 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.
Indications
- 1 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). Tirofiban hydrochloride injection is a platelet aggregation inhibitor 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...
Common Doses
- 25 mcg
- 0.15 mcg
- 60 mL
- 0.075 mcg
Dosage
2 DOSAGE AND ADMINISTRATION Administer intravenously 25 mcg/kg within 5 minutes and then 0.15 mcg/kg/min for up to 18 hours. In patients with creatinine clearance ≤ 60 mL/min, give 25 mcg/kg within 5 minutes and then 0.075 mcg/kg/min. ( 2 ) 2.1 Recommended Dosage The recommended dosage is 25 mcg/kg administered intravenously within 5 minutes and then 0.15 mcg/kg/min for up to 18 hours. 2.2 Administration For intravenous use only. Parenteral drug products should be inspected visually for particulate matter and discoloration prior to administration whenever solution and container permit.
Contraindications
- 4 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 )] .
Side Effects
- 6 ADVERSE REACTIONS Bleeding is the most commonly reported adverse reaction. ( 6.1 ) To report SUSPECTED ADVERSE REACTIONS, contact Sagent Pharmaceuticals at 1-866-625-1618 or FDA at 1-800-FDA-1088 or www.fda.gov/medwatch . 6.1 Clinical Trial Experience Because clinical trials are conducted under widely varying conditions, adverse reaction rates observed in the clinical trials of a drug cannot be directly compared to rates in the clinical trials of another drug and may not reflect the rates observed in clinical practice.
Interactions
- 7 DRUG INTERACTIONS Concomitant use of fibrinolytics, anticoagulants and antiplatelet drugs increases the risk of bleeding. Coadministration of fibrinolytics, anticoagulants and antiplatelet agents, increases the risk of bleeding. ( 7 )