TIROFIBAN HYDROCHLORIDE
Clinical safety rating: safe
Animal studies have demonstrated safety
Reversible antagonist of the platelet glycoprotein IIb/IIIa receptor, inhibiting fibrinogen binding and platelet aggregation.
| Metabolism | Minimal hepatic metabolism; not a substrate of CYP450 enzymes. |
| Excretion | Renal excretion accounts for approximately 65% of the dose; 25% is eliminated in feces, and the remainder as metabolites. Biliary excretion is minor. |
| Half-life | Terminal elimination half-life is approximately 2 hours in healthy individuals, but may be prolonged to 4-6 hours in patients with severe renal impairment (CrCl <30 mL/min). |
| Protein binding | ~65% protein bound, primarily to albumin. |
| Volume of Distribution | Volume of distribution is approximately 0.25 L/kg, indicating distribution primarily in the extracellular fluid. |
| Bioavailability | Only available intravenously; bioavailability is 100% by IV administration. |
| Onset of Action | Intravenous bolus: onset of platelet aggregation inhibition occurs within 5 minutes. |
| Duration of Action | Platelet function returns to normal within 4-8 hours after discontinuation of infusion; bleeding time normalizes approximately 90 minutes after cessation. |
0.4 mcg/kg/min IV for 30 minutes, then 0.1 mcg/kg/min IV continuous infusion.
| Dosage form | SOLUTION |
| Renal impairment | CrCl < 30 mL/min or hemodialysis: reduce infusion rate to 0.05 mcg/kg/min. CrCl ≥ 30 mL/min: no adjustment. |
| Liver impairment | No specific dose adjustment recommended for hepatic impairment; use caution in severe hepatic dysfunction. |
| Pediatric use | Safety and efficacy in pediatric patients not established; no FDA-approved dosing. |
| Geriatric use | No specific adjustment; monitor renal function and bleeding risk in elderly patients with reduced creatinine clearance. |
| 1st trimester | Consult provider |
| 2nd trimester | Consult provider |
| 3rd trimester | Consult provider |
Clinical note
Other drugs that affect hemostasis increase bleeding risk Can cause severe bleeding and thrombocytopenia.
| Breastfeeding | No data available on excretion in human milk; M/P ratio unknown. Use with caution, considering importance of drug to mother and potential for serious adverse reactions in nursing infants (e.g., bleeding). |
| Teratogenic Risk | Pregnancy Category B. No evidence of risk in humans based on animal studies, but no adequate human studies in pregnant women. Use only if clearly needed. First trimester: No known fetal risk; second and third trimesters: Risk of maternal hemorrhage may affect fetal perfusion; avoid prolonged use near term due to risk of neonatal bleeding. |
■ FDA Black Box Warning
Bleeding: Tirofiban increases the risk of major bleeding, including intracranial and retroperitoneal hemorrhage. Use with caution in patients with increased bleeding risk.
| Common Effects | Bleeding |
| Serious Effects |
["Hypersensitivity to tirofiban or any component","Active internal bleeding or history of bleeding diathesis","History of intracranial hemorrhage, neoplasm, aneurysm, or stroke within 30 days","Major surgery or trauma within 6 weeks","Severe hypertension (systolic >180 mmHg or diastolic >110 mmHg)","Acute pericarditis","History of thrombocytopenia with GP IIb/IIIa inhibitors"]
| Precautions | ["Increased bleeding risk; monitor for bleeding signs","Avoid concomitant use with other antithrombotics unless necessary","Thrombocytopenia risk; monitor platelet counts","Elderly patients have increased bleeding risk","Renal impairment requires dose adjustment"] |
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| Fetal Monitoring | Monitor maternal platelet count, hemoglobin, hematocrit, signs of bleeding (e.g., epistaxis, gingival bleeding, hematuria). Fetal monitoring: assess for signs of hemorrhage or distress via ultrasound or fetal heart rate monitoring if concerns arise. |
| Fertility Effects | No known effect on human fertility based on available data. Animal studies did not show impaired fertility at clinically relevant doses. |