AGGRASTAT
Clinical safety rating: caution
Comprehensive clinical and safety monograph for AGGRASTAT (AGGRASTAT).
Tirofiban is a reversible antagonist of glycoprotein IIb/IIIa receptor, inhibiting platelet aggregation by blocking fibrinogen binding.
| Metabolism | Tirofiban is metabolized primarily via hepatic CYP3A4, with less involvement of CYP2C9; also undergoes conjugation. |
| Excretion | Renal: 65% unchanged drug; biliary/fecal: minimal (<5%) |
| Half-life | Terminal half-life: ~2 hours; clinical context: requires continuous IV infusion for sustained antiplatelet effect |
| Protein binding | 65% bound to plasma proteins (primarily albumin) |
| Volume of Distribution | Vd: 0.5 L/kg; indicates distribution largely in extracellular fluid |
| Bioavailability | Not applicable (administered only intravenously); oral bioavailability: 0% |
| Onset of Action | Intravenous: within minutes; peak effect at 30 minutes |
| Duration of Action | Platelet function recovers within 4-8 hours after discontinuation (due to short half-life) |
A loading dose of 25 mcg/kg administered intravenously over 3 minutes, followed by a maintenance infusion of 0.15 mcg/kg/min for up to 18 hours. For patients with severe renal impairment (GFR <30 mL/min), the maintenance infusion rate is reduced to 0.075 mcg/kg/min.
| Dosage form | SOLUTION |
| Renal impairment | For GFR <30 mL/min (or serum creatinine >2.0 mg/dL): loading dose unchanged (25 mcg/kg IV), maintenance infusion reduced to 0.075 mcg/kg/min. No adjustment for GFR ≥30 mL/min. |
| Liver impairment | No specific dose adjustments are recommended for hepatic impairment based on Child-Pugh classification; use with caution in severe hepatic impairment due to increased bleeding risk. |
| Pediatric use | Safety and efficacy in pediatric patients have not been established. No recommended dosing. |
| Geriatric use | No specific dose adjustment is recommended based on age alone; however, elderly patients (≥65 years) may have a higher incidence of bleeding. Monitor renal function and adjust dose if GFR <30 mL/min as per renal adjustment. |
| 1st trimester | Consult provider |
| 2nd trimester | Consult provider |
| 3rd trimester | Consult provider |
Clinical note
Comprehensive clinical and safety monograph for AGGRASTAT (AGGRASTAT).
| Breastfeeding | Unknown if excreted in human milk. Caution advised. M/P ratio not determined. |
| Teratogenic Risk | Pregnancy Category B. Animal studies show no fetal harm. No adequate human studies; use only if clearly needed. Risk of hemorrhage in mother and fetus, especially during labor and delivery. |
| Fetal Monitoring | Monitor platelets, hemoglobin, activated clotting time (ACT), and signs of bleeding. Fetal heart rate monitoring during labor. |
■ FDA Black Box Warning
WARNING: Serious bleeding risk. Use with caution in patients at increased bleeding risk. Discontinue promptly if active bleeding or thrombocytopenia occurs.
| Serious Effects |
["Active internal bleeding or history of bleeding diathesis","Severe hypertension (systolic >180 mmHg or diastolic >110 mmHg)","Major surgery or serious trauma within 30 days","History of intracranial hemorrhage, neoplasm, arteriovenous malformation, or aneurysm","History of thrombocytopenia with prior GP IIb/IIIa receptor antagonists","Hemodialysis dependence"]
| Precautions | ["Bleeding events (major/minor hemorrhage); avoid concomitant use with other antithrombotics unless necessary","Thrombocytopenia (monitor platelet count within 6 hours of infusion and daily)","Increased risk with renal impairment (dose adjustment required for creatinine clearance <30 mL/min)","Hypersensitivity reactions (rare)"] |
| Food/Dietary | No known food interactions with AGGRASTAT. No dietary restrictions required during therapy. |
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| Fertility Effects | No data on human fertility effects. Animal studies show no impairment. |
| Clinical Pearls | AGGRASTAT (tirofiban) is a glycoprotein IIb/IIIa receptor antagonist used intravenously in acute coronary syndrome (ACS) management, particularly in patients undergoing percutaneous coronary intervention (PCI). Key pearls: 1) Monitor platelet count within 6 hours of infusion start and daily to detect thrombocytopenia; 2) Concomitant use with heparin increases bleeding risk; require close monitoring of aPTT/ACT; 3) Contraindicated in patients with history of intracranial hemorrhage, recent major surgery/trauma, or severe hypertension; 4) Half-life is ~2 hours; effects reversible within 4-6 hours of discontinuation; 5) Dose adjustment required for renal impairment (CrCl <30 mL/min). |
| Patient Advice | This medication helps prevent blood clots during heart procedures. · You may bleed more easily; avoid activities that could cause injury. · Report any unusual bruising, bleeding, or blood in urine/stool immediately. · Avoid taking aspirin, ibuprofen, or other NSAIDs unless prescribed by a doctor. · Inform all healthcare providers, including dentists, that you are on AGGRASTAT. |