tirofiban (Aggrastat)
Classes: Antiplatelet Agents, Cardiovascular; Glycoprotein IIb/IIIa Inhibitors
Dosing and uses of Aggrastat (tirofiban)
Adult dosage forms and strengths
premixed IV infusion solution
- 5mg/100mL (50mcg/mL)
- 12.5mg/250mL (50mcg/mL)
IV solution vials
- 5mg/100mL vial (50mcg/mL)
- 3.75mg/15mL bolus vial (250mcg/mL)
Non-ST Elevated Acute Coronary Syndrome
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)
Loading dose: 25 mcg/kg IV infused within 5 min, THEn
Post loading dose infusion: 0.15 mcg/kg/min IV for up to 18 hr
Refer to prescribing information for dosing chart by weight and CrCL
Renal Impairment
CrCl ≤60 mL/min: Decrease post loading dose infusion by 50% to 0.075 mcg/kg/min IV
Pediatric dosage forms and strengths
Safety and efficacy not established
Aggrastat (tirofiban) adverse (side) effects
>10%
Bleeding, minor (11%)
1-10%
Pelvic pain (6%)
Coronary artery dissection (5%)
Bradycardia (4%)
Dizziness (3%)
Lower extremity pain (3%)
Edema (2%)
Sweating (2%)
Bleeding, major (1-2%)
Thrombocytopenia (1.5%)
Warnings
Contraindications
Hypersensitivity, history of thrombocytopenia with tirofiban
Active/history of internal bleeding (within last 30 days), intracranial hemorrhage or neoplasm
History of stroke within last 30 days or any history of hemorrhagic stroke
AV malformation or aneurysm, aortic dissection, severe HTN, acute pericarditis
Current use of another parenteral glycoprotein IIb/IIIa inhibitor
Cautions
Platelets <150,000/cu.mm, hemorrhagic retinopathy, chronic Hd
Rates of major bleeds with the recommended high-dose bolus (ie, 25 mcg/kg/min loading dose) were consistent with the rates observed in the PRISM-PLUS regimen (original dosage regimen); there was a trend toward greater bleeding in ST segment elevation myocardial infarction (STEMI) patients treated with fibrinolytics prior to administration tirofiban using the high-dose bolus during rescue PCI
Pregnancy and lactation
Pregnancy category: B
Lactation: not known if excreted in breast milk, nursing not a priority in ACS pts
Pregnancy categories
A: Generally acceptable. Controlled studies in pregnant women show no evidence of fetal risk.
B: May be acceptable. Either animal studies show no risk but human studies not available or animal studies showed minor risks and human studies done and showed no risk.
C: Use with caution if benefits outweigh risks. Animal studies show risk and human studies not available or neither animal nor human studies done.
D: Use in LIFE-THREATENING emergencies when no safer drug available. Positive evidence of human fetal risk.
X: Do not use in pregnancy. Risks involved outweigh potential benefits. Safer alternatives exist.
NA: Information not available.
Pharmacology of Aggrastat (tirofiban)
Mechanism of action
Blocks binding of fibrinogen and von Willebrand factor to glycoprotein IIb/IIIa receptor on platelet surface; inhibits platelet aggregation
Pharmacokinetics
Half-life: 2 hr
Duration: 4 hr
Protein bound: 65%
Vd: 22-42 L
Clearance: 213-314 mL/min
Excretion: Urine (65%); feces (25%)
Dialyzable: Yes
Administration
IV Incompatibilities
Y-site: diazepam
IV Compatibilities
Solution: D5W, D5/½NS, Ns
Y-site: amiodarone, atropine, bivalirudin, dobutamine, dopamine, epinephrine, famotidine, furosemide, heparin, lidocaine, midazolam, morphine, nitroglycerin, KCl, propranoloL
IV Preparation
Available only as premixed 50 mcg/mL solution for injection (100 mL or 250 mL bags)
IV Administration
See adult dosing for infusion rate
Storage
Store at 25°C (77°F) with excursions permitted between 15-30°C (59-86°F)
Do not freeze
Protect from light during storageIV IncompatibilitiesY-site: diazepamIV CompatibilitiesSolution: D5W, D5/½NS, NSY-site: amiodarone, atropine, bivalirudin, dobutamine, dopamine, epinephrine, famotidine, furosemide, heparin, lidocaine, midazolam, morphine, nitroglycerin, KCl, propranololIV PreparationAvailable only as premixed 50 mcg/mL solution for injection (100 mL or 250 mL bags)IV AdministrationSee adult dosing for infusion rateStorageStore at 25°C (77°F) with excursions permitted between 15-30°C (59-86°F)Do not freezeProtect from light during storage
