| Item |
Information |
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Drug Groups
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approved; investigational |
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Description
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An antifibrinolytic agent that acts by inhibiting plasminogen activators which have fibrinolytic properties. [PubChem] |
| Indication |
For use in the treatment of excessive postoperative bleeding. |
| Pharmacology |
Aminocaproic acid works as an antifibrinolytic. It is a derivative of the amino acid lysine. The fibrinolysis-inhibitory effects of aminocaproic acid appear to be exerted principally via inhibition of plasminogen activators and to a lesser degree through antiplasmin activity. Aminocaproic acid may be a possible prophylactic for vascular disease, as it may prevent formation of lipoprotein (a), a risk factor for vascular disease. |
| Toxicity |
A few cases of acute overdosage with intravenous administration have been reported. The effects have ranged from no reaction to transient hypotension to severe acute renal failure leading to death. The intravenous and oral LD50 were 3.0 and 12.0 g/kg respectively in the mouse and 3.2 and 16.4 g/kg respectively in the rat. An intravenous infusion dose of 2.3 g/kg was lethal in the dog. |
| Affected Organisms |
| • |
Humans and other mammals |
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| Biotransformation |
Sixty-five percent of the dose is recovered in the urine as unchanged drug and 11% of the dose appears as the metabolite adipic acid. |
| Absorption |
Absorbed rapidly following oral administration. In adults, oral absorption appears to be a zero-order process with an absorption rate of 5.2 g/hr. The mean lag time in absorption is 10 minutes. After a single oral dose of 5 g, absorption was complete (F=1). |
| Half Life |
The terminal elimination half-life is approximately 2 hours. |
| Elimination |
Renal excretion is the primary route of elimination, whether aminocaproic acid is administered orally or intravenously. |
| Distribution |
* 23.1 ± 6.6 L |
| Clearance |
* 169 mL/min |
| External Links |
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