Aminocaproic acid works as an antifibrinolytic. It is a derivative of the amino acid lysine. It binds reversibly to the kringle domain of plasminogen and blocks the binding of plasminogen to fibrin and its activation to plasmin.

Clinical use

Aminocaproic acid is used to treat excessive postoperative bleeding. It can be given orally or intravenously. One scenario where it may be useful is to treat bleeding after dental extractions in patients with hemophilia, because the oral mucosa is rich in plasminogen activators. A meta-analysis found that lysine analogs like aminocaproic acid significantly reduced blood loss in patients undergoing coronary artery bypass grafting.

Side effects

Its side effects are mainly related to the gastrointestinal tract and include nausea, vomiting, abdominal pain, and diarrhea. The main risk associated with aminocaproic acid is the increased risk for thrombosis because of the inhibition of fibrinolysis.

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How to Reduce Blood Loss During Cardiac Surgery
From American Family Physician, 3/1/00 by Anne D. Walling

Excessive bleeding is a major cause of morbidity and mortality associated with cardiac surgery. Many strategies have been suggested to minimize perioperative bleeding. Levi and colleagues studied all available data on the three most common pharmacologic interventions designed to reduce bleeding associated with cardiac surgery.

Their search for studies of aprotinin, lysine analogs (such as aminocaproic acid and tranexamic acid) and desmopressin in adult cardiac surgery identified 128 randomized controlled clinical trials. Trials were selected for the study if they were of good design, included information on patient selection and follow-up, and included at least one clinically relevant outcome, such as mortality, rethoracotomy, transfusion use and perioperative myocardial infarction. After analysis, 72 trials met criteria for inclusion in the study.

The trials using aprotinin and lysine analogs showed a significant decrease in mortality. In complicated surgery, mortality was reduced by one half. In complicated and uncomplicated surgery, mortality in patients treated with desmopressin did not differ from that in patients given placebo. Overall, treatment with aprotinin and lysine analogs decreased the rate of surgical re-exploration, but the chance of rethoracotomy varied with the dosage of the drug used and the degree of complexity of the surgery. The rate of rethoracotomy was reduced, but not significantly, by the use of desmopressin. Aprotinin and lysine analogs reduced the proportion of patients receiving blood transfusion by about 20 percent. The rate of blood transfusion was also reduced with desmopressin treatment but to a lesser extent. The risk of perioperative myocardial infarction was not increased by use of aprotinin and lysine analogs but was significantly increased in patients receiving desmopressin.

Although the data are based on different dosages of the study drugs and involve patients undergoing surgeries of varying complexity, the authors conclude that aprotinin and lysine analogs decrease perioperative blood loss, mortality and the need for rethoracotomy and blood transfusion.

Anne D. Walling, M.D.

Levi M, et al. Pharmacological strategies to decrease excessive blood loss in cardiac surgery: a meta-analysis of clinically relevant endpoints. Lancet December 4, 1999;354:1940-7.

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