AMICAR
Clinical safety rating: caution
Comprehensive clinical and safety monograph for AMICAR (AMICAR).
Competitive inhibition of plasminogen activation, reducing fibrinolysis by blocking the binding of plasminogen to fibrin.
| Metabolism | Primarily renal excretion; minimal hepatic metabolism. |
| Excretion | Renal: >99% of absorbed dose excreted unchanged in urine. Biliary/fecal: negligible (<1%). |
| Half-life | Terminal elimination half-life: 2 hours (range 1-3.5 hours). After high doses or renal impairment, half-life may prolong (up to 5-10 hours). |
| Protein binding | Approximately 80% bound to albumin, with minimal binding to alpha-1-acid glycoprotein. |
| Volume of Distribution | Vd: 0.03–0.07 L/kg (approximate plasma volume). Low distribution reflects minimal extravascular penetration; primarily remains in intravascular space. |
| Bioavailability | Oral: approximately 50% (range 30-60%) due to incomplete absorption; IV: 100%. |
| Onset of Action | IV administration: within 5-10 minutes (fibrinolytic inhibition begins). Oral: 1-2 hours to reach therapeutic plasma concentrations. |
| Duration of Action | IV: ~3 hours after single dose; sustained effect with continuous infusion. Oral: ~3-5 hours. Clinical effect persists as long as plasma levels >0.01 mM. |
4-5 g IV loading dose over 1 hour, followed by 1 g/hour IV continuous infusion for 8 hours or until bleeding controlled; oral: 5 g PO initially, then 1-1.25 g PO every hour as needed.
| Dosage form | TABLET |
| Renal impairment | GFR >80 mL/min: no adjustment; GFR 50-80 mL/min: reduce dose by 25%; GFR 10-50 mL/min: reduce dose by 50%; GFR <10 mL/min: reduce dose by 75%. |
| Liver impairment | No specific adjustment recommended; use with caution in severe hepatic impairment due to limited data. |
| Pediatric use | 100 mg/kg IV loading dose (max 5 g) over 1 hour, followed by 33.3 mg/kg/hour IV continuous infusion (max 1 g/hour); adjust for bleeding response. |
| Geriatric use | Consider dose reduction based on renal function; usual adult dosing may be used if GFR >80 mL/min; monitor for hypotension and thrombotic events. |
| 1st trimester | Consult provider |
| 2nd trimester | Consult provider |
| 3rd trimester | Consult provider |
Clinical note
Comprehensive clinical and safety monograph for AMICAR (AMICAR).
| Breastfeeding | Not known if excreted in breast milk. M/P ratio not available. Caution advised; consider risk of infant thrombosis. |
| Teratogenic Risk | FDA Pregnancy Category B. Animal studies have not demonstrated fetal risk, but no adequate human studies in pregnant women. Use only if clearly needed. First trimester: no known teratogenic effects. Second and third trimesters: theoretical risk of thrombosis; consider benefit vs. risk. |
| Fetal Monitoring |
■ FDA Black Box Warning
Not approved for use in patients with subarachnoid hemorrhage due to risk of cerebral edema and cerebral infarction.
| Serious Effects |
Active intravascular clotting process (e.g., disseminated intravascular coagulation), known hypersensitivity to aminocaproic acid, patients with subarachnoid hemorrhage.
| Precautions | Risk of thromboembolic events, including venous thrombosis and pulmonary embolism; avoid in patients with active intravascular clotting; renal impairment requires dose adjustment; ocular muscle myotoxicity with long-term use; potential for seizures. |
| Food/Dietary | No significant food interactions. Grapefruit juice does not affect aminocaproic acid metabolism. |
Loading safety data…
| Monitor for thrombosis, visual disturbances, headache, nausea, myopathy, and hypotension. Fetal monitoring as clinically indicated. |
| Fertility Effects | No known effects on fertility in animal studies. Human data lacking. |
| Clinical Pearls | Amicar (aminocaproic acid) is an antifibrinolytic used to reduce bleeding in conditions with excessive fibrinolysis. It can cause hypotension with rapid IV infusion. Monitor for thrombotic events, especially in patients with DIC. Contraindicated in active intravascular clotting. Use with caution in renal impairment; dose adjustment required if CrCl < 80 mL/min. |
| Patient Advice | Take this medication exactly as prescribed to prevent bleeding complications. · Report any signs of blood clots such as chest pain, shortness of breath, or leg swelling immediately. · Avoid aspirin or NSAIDs unless directed by your doctor, as they may increase bleeding risk. · If you miss a dose, take it as soon as possible, but skip it if it's almost time for the next dose. Do not double up. · Store at room temperature away from light and moisture. |