AMINOCAPROIC
Clinical safety rating: caution
Comprehensive clinical and safety monograph for AMINOCAPROIC (AMINOCAPROIC).
Competitive inhibition of plasminogen activation and, to a lesser extent, noncompetitive inhibition of plasmin, thereby preventing fibrinolysis and promoting clot stability.
| Metabolism | Primarily renal elimination; minimal hepatic metabolism (<1%) via unidentified pathways. |
| Excretion | Primarily renal (>95%) as unchanged drug via glomerular filtration and tubular secretion. Less than 1% biliary/fecal. |
| Half-life | Terminal elimination half-life: 2 hours (normal renal function); prolonged to 4–10 hours in renal impairment. Clinically, dosing interval must be adjusted in renal dysfunction to avoid accumulation. |
| Protein binding | Approximately 0–5% (negligible). Primarily free in plasma; no significant protein binding to albumin or other proteins. |
| Volume of Distribution | 0.3–0.4 L/kg. Distributes mainly into extracellular fluid; limited penetration into cells or CSF unless meninges inflamed. |
| Bioavailability | Oral: ~100% (well-absorbed, no significant first-pass metabolism). |
| Onset of Action | IV: immediate (within minutes) due to direct antifibrinolytic effect; oral: 1–2 hours. |
| Duration of Action | IV: 3–4 hours (single dose); oral: 4–6 hours. Duration correlates with plasma levels maintained above 130 mcg/mL required for antifibrinolytic effect; repeat dosing necessary for sustained effect. |
4-5 g orally or intravenously as a loading dose, followed by 1 g/hour continuous infusion or 1 g every 4-6 hours orally. Maximum dose 30 g/day.
| Dosage form | TABLET |
| Renal impairment | CrCl 50-80 mL/min: 75% of usual dose; CrCl 15-50 mL/min: 50% of usual dose every 12 hours; CrCl <15 mL/min: 25% of usual dose every 24 hours. |
| Liver impairment | No dosage adjustment required for hepatic impairment; however, use with caution in severe liver disease. |
| Pediatric use | Loading dose: 100-200 mg/kg intravenously or orally, followed by 100 mg/kg/dose every 6 hours (maximum 5 g/dose) or continuous infusion of 33 mg/kg/hour (maximum 1 g/hour). |
| Geriatric use | Start at lower end of dosing range due to potential age-related renal impairment; adjust based on creatinine clearance. |
| 1st trimester | Consult provider |
| 2nd trimester | Consult provider |
| 3rd trimester | Consult provider |
Clinical note
Comprehensive clinical and safety monograph for AMINOCAPROIC (AMINOCAPROIC).
| Breastfeeding | Unknown if excreted in human breast milk. Low molecular weight suggests potential for excretion. No M/P ratio available. Caution is advised; consider the drug's mechanism (fibrinolysis inhibition) and theoretical risk to infant hemostasis. Avoid use in breastfeeding women unless essential. |
| Teratogenic Risk | Aminocaproic acid is an antifibrinolytic agent. Limited human data; animal studies show no teratogenicity. Trimester-specific risks: First trimester: insufficient data to determine risk, avoid unless clearly needed. Second trimester: no known specific risks, but use only if benefit outweighs potential risk. Third trimester: theoretical risk of placental hemorrhage due to fibrinolytic inhibition, but no controlled studies. FDA pregnancy category C. |
■ FDA Black Box Warning
None.
| Serious Effects |
["Active thromboembolic disease (e.g., deep vein thrombosis, pulmonary embolism)","History of thromboembolic events","Disseminated intravascular coagulation (DIC) without heparin anticoagulation","Hypersensitivity to aminocaproic acid"]
| Precautions | ["Thrombotic events (e.g., pulmonary embolism, cerebral thrombosis) – avoid in patients with active thromboembolic disease or history of thrombosis","Risk of seizures, especially with high doses or in patients with renal impairment","Renal dysfunction – dose adjustment required","Myopathy and rhabdomyolysis, particularly with prolonged use or combination with statins","Not indicated for disseminated intravascular coagulation (DIC) without concomitant heparin"] |
| Food/Dietary | No specific food interactions. Maintain normal diet unless directed otherwise. |
Loading safety data…
| Fetal Monitoring | Monitor maternal blood pressure, signs of thrombosis (e.g., chest pain, dyspnea, leg swelling), and bleeding. Fetal monitoring: consider fetal heart rate monitoring if used in third trimester given potential placental effects. Also monitor maternal renal function as drug is renally excreted. |
| Fertility Effects | No known impairment of fertility in animal studies. Human data insufficient to assess effects on female or male fertility. Theoretical concerns about ovulation inhibition due to antifibrinolytic effects on ovarian function have not been confirmed. |
| Clinical Pearls | Aminocaproic acid is a lysine analog that inhibits fibrinolysis by competitively binding to plasminogen and plasmin. It is used for acute bleeding due to hyperfibrinolysis, such as in cardiac surgery, liver transplantation, or prostatectomy. Avoid in disseminated intravascular coagulation (DIC) unless hyperfibrinolysis is predominant. Rapid IV administration may cause hypotension, bradycardia, or arrhythmia. Monitor for thrombosis, especially in patients with thrombotic risk factors. |
| Patient Advice | Take this medication exactly as prescribed to control bleeding. · Report any signs of blood clots: sudden chest pain, shortness of breath, leg pain/swelling, or vision changes. · Do not take with oral contraceptives or hormone therapy unless approved by your doctor; may increase clotting risk. · Avoid strenuous activity or heavy lifting that may cause bleeding. · Inform all healthcare providers that you take this medication before any surgery or dental work. |