AMINOCAPROIC ACID
Clinical safety rating: caution
Comprehensive clinical and safety monograph for AMINOCAPROIC ACID (AMINOCAPROIC ACID).
Competitive inhibition of plasminogen activation, reducing fibrinolysis by binding to plasminogen and blocking its conversion to plasmin.
| Metabolism | Minimal hepatic metabolism; primarily excreted unchanged by the kidney (renal tubular secretion). |
| Excretion | Primarily renal (80-90% unchanged). A small fraction (<5%) is excreted as metabolites. No significant biliary/fecal elimination. |
| Half-life | Terminal elimination half-life is approximately 2 hours (range 1-3 hours) in patients with normal renal function. Prolonged in renal impairment (up to 20 hours in anuria). |
| Protein binding | Weakly bound to plasma proteins, primarily albumin. Reported as approximately 10-20% bound. |
| Volume of Distribution | Volume of distribution is approximately 0.5-0.6 L/kg, indicating distribution primarily in extracellular fluid and minimal tissue binding. |
| Bioavailability | Oral bioavailability is approximately 80-100% (well absorbed). |
| Onset of Action | Intravenous: immediate (within minutes). Oral: onset within 1-2 hours for hemostatic effect. |
| Duration of Action | Intravenous: approximately 3-4 hours. Oral: approximately 4-6 hours. Duration correlates with therapeutic plasma concentrations (≥130 μg/mL required for inhibition of fibrinolysis). |
Loading dose: 4-5 g intravenously (IV) over 1 hour, followed by continuous IV infusion of 1 g/hour for 8 hours or until bleeding controlled. Oral: 1 g every hour for 8 hours, then 1 g every 2 hours for 8 additional hours.
| Dosage form | SOLUTION |
| Renal impairment | CrCl 15-50 mL/min: reduce dose by 25-50%; CrCl <15 mL/min: reduce dose by 50-75% or use with caution; hemodialysis: supplement 1 g post-dialysis if needed. |
| Liver impairment | No specific Child-Pugh based adjustments recommended; use with caution in severe hepatic impairment due to potential coagulation factor abnormalities. |
| Pediatric use | Loading dose: 100-200 mg/kg IV over 1 hour, followed by continuous infusion of 33.3 mg/kg/hour; maximum 1 g/hour. Oral: 50-100 mg/kg every 6 hours; not to exceed 18 g/day. |
| Geriatric use | Renal function often decreased; adjust dose based on creatinine clearance. Start at lower end of dosing range and titrate to effect; monitor for thrombosis risk. |
| 1st trimester | Consult provider |
| 2nd trimester | Consult provider |
| 3rd trimester | Consult provider |
Clinical note
Comprehensive clinical and safety monograph for AMINOCAPROIC ACID (AMINOCAPROIC ACID).
| Breastfeeding | It is unknown if aminocaproic acid is excreted into human milk. No lactation studies exist; M/P ratio not established. Caution is advised, as the drug may affect hemostasis in the nursing infant. Consider alternative agents or discontinue breastfeeding during therapy. |
| Teratogenic Risk | Aminocaproic acid is an antifibrinolytic agent. There are no adequate and well-controlled studies in pregnant women. Animal studies have not reported teratogenic effects. In the first trimester, risk cannot be ruled out; use only if clearly needed. In second and third trimesters, potential risks include thrombosis and placental insufficiency due to its procoagulant effects. Fetal risks are theoretical and dose-dependent. |
■ FDA Black Box Warning
Not recommended for use in patients with upper urinary tract bleeding due to the risk of intrarenal obstruction in the form of clots.
| Serious Effects |
["Active intravascular clotting (e.g., DIC unless heparin is used)","Known hypersensitivity to aminocaproic acid"]
| Precautions | ["Increased risk of thrombosis; caution in patients with thrombotic events or DIC","Renal impairment requires dose adjustment","May cause hypotension, bradycardia, or arrhythmias with rapid IV administration","Seizures reported with high doses or prolonged use","Monitor for myopathy or rhabdomyolysis with long-term use"] |
| Food/Dietary | No known food interactions. |
Loading safety data…
| Fetal Monitoring | Monitor for signs of thrombosis (e.g., deep vein thrombosis, pulmonary embolism) in mother. Assess fetal heart rate and uterine activity if used during labor. Monitor coagulation parameters (e.g., PT, aPTT, fibrinogen) if prolonged therapy. Observe for maternal hypotension or bradycardia during intravenous administration. |
| Fertility Effects | No evidence of impaired fertility in animal studies. In humans, no adverse effects on fertility reported. However, systemic antifibrinolytic therapy may theoretically affect ovulation or implantation due to altered fibrinolysis; clinical significance unknown. |
| Clinical Pearls |
| Monitor for thrombotic events, especially in patients with DIC or history of thrombosis. Avoid in upper urinary tract bleeding due to risk of clot obstruction. Use with caution in hematuria of renal origin. Not effective for fibrinolytic bleeding outside the context of hyperfibrinolysis. |
| Patient Advice | Report any signs of blood clots like leg swelling, chest pain, or sudden shortness of breath. · Avoid use during pregnancy unless specifically prescribed. · Do not take additional over-the-counter medications without consulting your doctor. · Seek medical attention for new or unusual bleeding or bruising. · Inform all healthcare providers of your use of this medication. |