AMINOCAPROIC ACID IN PLASTIC CONTAINER
Clinical safety rating: caution
Comprehensive clinical and safety monograph for AMINOCAPROIC ACID IN PLASTIC CONTAINER (AMINOCAPROIC ACID IN PLASTIC CONTAINER).
Aminocaproic acid is a lysine analog that binds to plasminogen and prevents its conversion to plasmin, thereby inhibiting fibrinolysis and stabilizing clots. It also inhibits plasmin directly at high doses.
| Metabolism | Primarily excreted unchanged in urine (up to 80-90%). Minor hepatic metabolism via conjugation; inactive metabolites. |
| Excretion | Primarily renal (approximately 80-90% excreted unchanged in urine via glomerular filtration). |
| Half-life | Terminal elimination half-life is approximately 2-3 hours in patients with normal renal function. In end-stage renal disease, half-life may be prolonged to 7-10 hours. |
| Protein binding | Low, approximately 2-4% bound to plasma proteins (mainly albumin). |
| Volume of Distribution | Approximately 0.3-0.4 L/kg, indicating distribution primarily in extracellular fluid. |
| Bioavailability | Oral bioavailability is approximately 70-80% (immediate-release tablets). Intravenous administration yields 100% bioavailability. |
| Onset of Action | Intravenous: Onset within minutes when given as a loading dose of 4-5 g infused over 1 hour, with antifibrinolytic effect detected within 1-2 hours. |
| Duration of Action | Duration of action is 3-6 hours after a single intravenous dose, corresponding to the drug's half-life. Continuous infusion may be required for sustained effect in ongoing bleeding. |
4-5 g IV over 1 hour followed by 1 g/h IV for 8 hours or until bleeding is controlled; max 30 g/24h.
| Dosage form | INJECTABLE |
| Renal impairment | CrCl 50-80 mL/min: reduce dose by 25%; CrCl 15-49 mL/min: reduce dose by 50%; CrCl <15 mL/min: reduce dose by 75%. |
| Liver impairment | No dose adjustment required based on Child-Pugh class. |
| Pediatric use | Loading dose: 100 mg/kg IV (max 5 g); maintenance: 33.3 mg/kg/h IV (max 1 g/h); max total dose 18 g/m²/24h. |
| Geriatric use | Start at lower end of dosing range; monitor renal function as elderly patients may have reduced CrCl; adjust dose according to renal function. |
| 1st trimester | Consult provider |
| 2nd trimester | Consult provider |
| 3rd trimester | Consult provider |
Clinical note
Comprehensive clinical and safety monograph for AMINOCAPROIC ACID IN PLASTIC CONTAINER (AMINOCAPROIC ACID IN PLASTIC CONTAINER).
| Breastfeeding | It is not known whether aminocaproic acid is excreted in human milk. Caution should be exercised when administered to a nursing woman. M/P ratio: Unknown. |
| Teratogenic Risk | Animal studies have not shown teratogenic effects. There are no adequate and well-controlled studies in pregnant women. Use during pregnancy only if clearly needed. First trimester: No known teratogenic risk. Second trimester: No known risk. Third trimester: No known risk; however, risk of thrombosis may be increased. |
■ FDA Black Box Warning
NONE
| Serious Effects |
["Active intravascular clotting or DIC (unless receiving heparin).","Known hypersensitivity to aminocaproic acid.","Severe renal impairment (CrCl < 50 mL/min) is a relative contraindication due to risk of accumulation."]
| Precautions | ["Risk of thrombotic events (e.g., myocardial infarction, stroke, pulmonary embolism) especially in patients with disseminated intravascular coagulation (DIC) or thrombophilia.","Do not use in patients with active intravascular clotting or DIC without concurrent heparin.","May cause hypotension, bradycardia, or arrhythmias with rapid intravenous administration.","Use caution in patients with renal impairment due to risk of accumulation.","May cause skeletal muscle weakness or rhabdomyolysis with prolonged high doses.","Avoid in patients with upper urinary tract bleeding due to risk of clot formation and obstruction."] |
| Food/Dietary | No significant food interactions. Maintain adequate hydration unless fluid restriction is indicated. |
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| Fetal Monitoring |
| Monitor fibrinogen levels, coagulation parameters, vital signs, and signs of thrombosis. In pregnancy, monitor for uterine bleeding and fetal heart rate. |
| Fertility Effects | No known effects on fertility. Animal reproduction studies have not been conducted. |
| Clinical Pearls | Monitor for thrombotic events, especially with concurrent use of oral contraceptives or factor IX complex concentrates. Rapid intravenous administration may cause hypotension. Do not administer if urine output is low or if DIC is suspected. Use with caution in patients with cardiac, hepatic, or renal disease. |
| Patient Advice | Report any signs of blood clots such as leg pain, swelling, chest pain, or sudden shortness of breath. · Inform your doctor if you are using oral contraceptives or estrogen therapy. · Avoid activities that increase bleeding risk until your condition stabilizes. · This medication helps stop bleeding by preventing clot breakdown. · Seek immediate medical help for severe headache, vision changes, or unexplained pain. |