tirofiban (Aggrastat): Dosing and Uses

Dosing and uses of Aggrastat (tirofiban)

• Adult
• Pediatric

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