Aminocaproic Acid Tablets USP 500 mg, 1000 mg and Oral Solution 0.25 g/mL

Rx only

Aminocaproic acid is 6-aminohexanoic acid, which acts as an inhibitor of fibrinolysis.

Its chemical structure is:

Aminocaproic acid is soluble in water, acid, and alkaline solutions; it is sparingly soluble in methanol and practically insoluble in chloroform.

Aminocaproic acid oral solution for oral administration contains 0.25 g/mL of aminocaproic acid and the following inactive ingredients: citric acid (anhydrous), methylparaben, propylene glycol, propylparaben, purified water, saccharin sodium, sorbitol solution and natural and artificial flavor.

Each aminocaproic acid tablet for oral administration contains either 500 mg or 1000 mg of aminocaproic acid and the following inactive ingredients: magnesium stearate, povidone and stearic acid. The 1000 mg tablet also contains crospovidone.

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.

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). Mean ± SD peak plasma concentrations (164 ± 28 mcg/mL) were reached within 1.2 ± 0.45 hours.

After oral administration, the apparent volume of distribution was estimated to be 23.1 ± 6.6 L (mean ± SD). Correspondingly, the volume of distribution after intravenous administration has been reported to be 30.0 ± 8.2 L. After prolonged administration, aminocaproic acid has been found to distribute throughout extravascular and intravascular compartments of the body, penetrating human red blood cells as well as other tissue cells.

Renal excretion is the primary route of elimination. 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. Renal clearance (116 mL/min) approximates endogenous creatinine clearance. The total body clearance is 169 mL/min. The terminal elimination half-life for aminocaproic acid is approximately 2 hours.

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).

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.

In patients with upper urinary tract bleeding, aminocaproic acid administration has been known to cause intrarenal obstruction in the form of glomerular capillary thrombosis or clots in the renal pelvis and ureters. For this reason, aminocaproic acid should not be used in hematuria of upper urinary tract origin, unless the possible benefits outweigh the risk.

Subendocardial hemorrhages have been observed in dogs given intravenous infusions of 0.2 times the maximum human therapeutic dose of aminocaproic acid and in monkeys given 8 times the maximum human therapeutic dose of aminocaproic acid.

Fatty degeneration of the myocardium has been reported in dogs given intravenous doses of aminocaproic acid at 0.8 to 3.3 times the maximum human therapeutic dose and in monkeys given intravenous doses of aminocaproic acid at 6 times the maximum human therapeutic dose.

Rarely, skeletal muscle weakness with necrosis of muscle fibers has been reported following prolonged administration. Clinical presentation may range from mild myalgias with weakness and fatigue to a severe proximal myopathy with rhabdomyolysis, myoglobinuria, and acute renal failure. Muscle enzymes, especially creatine phosphokinase (CPK) are elevated. CPK levels should be monitored in patients on long-term therapy. Aminocaproic acid administration should be stopped if a rise in CPK is noted. Resolution follows discontinuation of aminocaproic acid; however, the syndrome may recur if aminocaproic acid is restarted.

The possibility of cardiac muscle damage should also be considered when skeletal myopathy occurs. One case of cardiac and hepatic lesions observed in man has been reported. The patient received 2 g of aminocaproic acid every 6 hours for a total dose of 26 g. Death was due to continued cerebrovascular hemorrhage. Necrotic changes in the heart and liver were noted at autopsy.

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.

An identical dosage regimen may be followed by administering aminocaproic acid tablets or aminocaproic acid oral solution as follows:

For the treatment of acute bleeding syndromes due to elevated fibrinolytic activity, it is suggested that 5 aminocaproic acid 1000 mg tablets or 10 aminocaproic acid 500 mg tablets (5 g) or 20 milliliters of aminocaproic acid oral solution (5 g) be administered during the first hour of treatment, followed by a continuing rate of 1 aminocaproic acid 1000 mg tablet or 2 aminocaproic acid 500 mg tablets (1 g) or 5 milliliters 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 has been controlled.

Aminocaproic Acid Oral Solution USP, 0.25 g/mL

Each mL of raspberry-flavored oral solution contains 0.25 g/ mL of aminocaproic acid and is supplied in bottles of 8 fl. oz. (237 mL), NDC 61748-044-08 and 16 fl. oz. (473 mL), NDC 61748-044-16.

Aminocaproic Acid Tablets USP, 500 mg

Each round, white tablet, debossed “VP” score “045”on one side contains 500 mg of aminocaproic acid and is supplied in bottles of 100 tablets, NDC 61748-045-01, and hospital unit-dose cartons of 100 tablets (10 blister cards of 10 tablets per blister card), NDC 61748-045-11.

Aminocaproic Acid Tablets USP, 1000 mg

Each oblong, white tablet, engraved with “XP” on one side and scored on the other with “A” to the left of the score and “20” on the right contains 1000 mg of aminocaproic acid in bottles of 100 tablets, NDC 61748-046-01.

Store at 20° to 25°C (68° to 77°F)[see USP Controlled RoomTemperature].

Dispense in a tight container with a child-resistant closure.

R_x only

Manufactured by:
MIKART, INC.
Atlanta, GA 30318

Marketed by:
VersaPharm, Inc. – An Akorn Company

Lake Forest, IL 60045

¹Stefanini M, Dameshek W: The Hemorrhagic Disorders, Ed. 2, New York, Grune and Stratton, 1962; pp. 510-514.

Code 658A00

Rev. 03/17    

Bottle Label – 16 fl oz (473 mL)

NDC 61748-044-16  

AMINOCAPROIC ACID  

ORAL SOLUTION USP

0.25 grams/mL

CONTENTS: 16 fl oz (473 mL) 

     Bottle Label - 16 fl oz (473 mL)

Bottle Label – 500 mg Tablet

NDC 61748-045-01

Aminocaproic Acid

Tablets USP 500 mg

Each tablet contains:

Aminocaproic Acid.......... 500 mg

Rx Only

Contents: 100 Tablets

Bottle Label – 1000 mg Tablet   

NDC 61748-046-01

Aminocaproic Acid

Tablets USP 1000 mg

Each tablet contains:

Aminocaproic Acid.......... 1000 mg

Rx Only

Contents: 100 Tablets