AMINOCAPROIC ACID

Aminocaproic acid, USP is 6-aminohexanoic acid, which acts as an inhibitor of fibrinolysis. Its chemical structure is: Aminocaproic acid, USP is soluble in water, acid, and alkaline solutions; it is sparingly soluble in methanol and practically insoluble in chloroform. Aminocaproic acid Oral Solution, USP for oral administration, contains 0.25 g/mL of aminocaproic acid, USP with methylparaben 0.20%, propylparaben 0.05%, edetate disodium 0.30% as preservatives and the following inactive ingredients: sodium saccharin, sorbitol solution, citric acid anhydrous, natural and artificial raspberry flavor and an artificial bitterness modifier. chemstructure

Aminocaproic acid is useful in enhancing hemostasis when fibrinolysis contributes to bleeding. In life- threatening situations, transfusion of appropriate blood products and other emergency measures may be required. Fibrinolytic bleeding may frequently be associated with surgical complications following heart surgery (with or without cardiac bypass procedures) and portacaval shunt; hematological disorders such as amegakaryocytic thrombocytopenia (accompanying aplastic anemia); acute and life-threatening abruptio placentae; hepatic cirrhosis; and neoplastic disease such as carcinoma of the prostate, lung, stomach, and cervix. Urinary fibrinolysis, usually a normal physiological phenomenon, may contribute to excessive urinary tract fibrinolytic bleeding associated with surgical hematuria (following prostatectomy and nephrectomy) or nonsurgical hematuria (accompanying polycystic or neoplastic diseases of the genitourinary system). (See WARNINGS . )

A dosage regimen may be followed by administering Aminocaproic acid Oral Solution as follows: For the treatment of acute bleeding syndromes due to elevated fibrinolytic activity, it is suggested that 20 milliliter of Aminocaproic acid Oral Solution (5 g) be administered during the first hour of treatment, followed by a continuing rate of 5 milliliter of Aminocaproic acid Oral Solution (1.25 g) per hour. This method of treatment would ordinarily be continued for about 8 hours or until the bleeding situation has been controlled.

Aminocaproic acid should not be used when there is evidence of an active intravascular clotting process. When there is uncertainty as to whether the cause of bleeding is primary fibrinolysis or disseminated intravascular coagulation (DIC), this distinction must be made before administering aminocaproic acid. The following tests can be applied to differentiate the two conditions: Platelet count is usually decreased in DIC but normal in primary fibrinolysis. Protamine paracoagulation test is positive in DIC; a precipitate forms when protamine sulfate is dropped into citrated plasma. The test is negative in the presence of primary fibrinolysis. The euglobulin clot lysis test is abnormal in primary fibrinolysis but normal in DIC. Aminocaproic acid must not be used in the presence of DIC without concomitant heparin.

Aminocaproic acid is generally well tolerated. The following adverse experiences have been reported: General: Edema, headache, malaise. Hypersensitivity Reactions: Allergic and anaphylactoid reactions, anaphylaxis. Cardiovascular: Bradycardia, hypotension, peripheral ischemia, thrombosis. Gastrointestinal: Abdominal pain, diarrhea, nausea, vomiting. Hematologic: Agranulocytosis, coagulation disorder, leukopenia, thrombocytopenia. Musculoskeletal: CPK increased, muscle weakness, myalgia, myopathy (see WARNINGS ), myositis, rhabdomyolysis. Neurologic: Confusion, convulsions, delirium, dizziness, hallucinations, intracranial hypertension, stroke, syncope. Respiratory: Dyspnea, nasal congestion, pulmonary embolism. Skin: Pruritis, rash. Special Senses: Tinnitus, vision decreased, watery eyes. Urogenital: BUN increased, renal failure. There have been some reports of dry ejaculation during the period of aminocaproic acid treatment. These have been reported to date only in hemophilia patients who received the drug after undergoing dental surgical procedures. However, this symptom resolved in all patients within 24 to 48 hours of completion of therapy. To report SUSPECTED ADVERSE REACTIONS, contact Biocon Pharma Inc., at 1-866-924-6266 or FDA at 1-800-FDA-1088 or www.fda.gov/medwatch.