tirofiban (Rx)

>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%)

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

While published data cannot definitively establish the absence of risk, available published case reports have not established an association with therapy during pregnancy and major birth defects, miscarriage, or adverse maternal or fetal outcomes

Untreated myocardial infarction can be fatal to the pregnant woman and fetus; myocardial infarction is a medical emergency in pregnancy which can be fatal to pregnant woman and fetus if left untreated

Animal data

• Studies with intravenous doses up to 5 mg/kg/day (about 5 and 13 times maximum recommended daily human dose for rat and rabbit, respectively, compared on a body surface area basis) have revealed no harm to fetus

Lactation

There is no data on presence of drug in human milk, effects on breastfed infant, or on human milk production; however, the drug is present in rat milk; the developmental and health benefits of breastfeeding should be considered along with the mother’s clinical need for therapy and any potential adverse effects on breastfed child from therapy or from underlying maternal condition

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.

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

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