Aminocaproic Acid (Monograph)

Brand name: Amicar
Drug class: Hemostatics
VA class: BL300
CAS number: 60-32-2

Medically reviewed by Drugs.com on Jul 24, 2023. Written by ASHP.

Introduction

A synthetic monoamino carboxylic acid that is an inhibitor of fibrinolysis.

Uses for Aminocaproic Acid

Bleeding Due to Elevated Fibrinolytic Activity

Treatment of excessive bleeding resulting from systemic hyperfibrinolysis and urinary fibrinolysis. In life-threatening situations, fresh whole blood, fibrinogen infusions, and other emergency measures also may be required.

Used in systemic hyperfibrinolysis associated with surgical complications following heart surgery (with or without cardiac bypass procedures) and portacaval shunt; in carcinoma of the lung, prostate, cervix, or stomach; in abruptio placentae; and in hematologic disorders such as amegakaryocytic thrombocytopenia accompanying aplastic anemia (reduces the need for platelet transfusions).

Used in urinary fibrinolysis associated with complications of severe trauma, anoxia, and shock, and as manifested by surgical hematuria especially following prostatectomy and nephrectomy, or in nonsurgical hematuria accompanying polycystic or neoplastic disease of the GU tract.

Used in conjunction with heparin therapy in patients with acute promyelocytic leukemia^{† [off-label]}; initiate therapy when plasma α₂-antiplasmin (α₂-plasmin inhibitor) levels have decreased to <40% of normal levels.

Ocular Hemorrhage

Has been used effectively for the prevention of secondary ocular hemorrhage in patients with nonperforating traumatic hyphema^{† [off-label]}. Designated an orphan drug by FDA for topical treatment of traumatic hyphema.

Hereditary Hemorrhagic Telangiectasia

Has been used orally for the management of hereditary hemorrhagic telangiectasia^{† [off-label]}.

Aminocaproic Acid Dosage and Administration

Administration

Administer orally or by IV infusion.

Oral Administration

Administer orally if the patient is able to take oral medication.

IV Administration

For solution and drug compatibility information, see Compatibility under Stability.

Administer by IV infusion.

Avoid rapid IV administration; hypotension, bradycardia, and/or arrhythmia may result.

Dilution

For the initial infusion (loading dose), add 4–5 g of aminocaproic acid (16–20 mL of the injection) to 250 mL of diluent.

For maintenance infusions, add 1 g of aminocaproic acid (4 mL of the injection) to 50 mL of diluent to provide a final concentration of approximately 20 mg/mL.

Rate of Administration

Initial infusion (loading dose): Infuse 4–5 g over 1 hour in adults.

Maintenance infusion: Infuse 1 g per hour in adults.

Dosage

Pediatric Patients

Bleeding Due to Elevated Fibrinolytic Activity† [off-label]

Oral

100 mg/kg or 3 g/m² during the first hour, then 33.3 mg/kg per hour or 1 g/m² per hour (maximum 18 g/m² in 24 hours) has been used. Manufacturer states that safety and efficacy not established in pediatric patients.

IV

Initial infusion (loading dose): 100 mg/kg or 3 g/m² over 1 hour has been used. Manufacturer states that safety and efficacy not established in pediatric patients.

Maintenance infusion

Maintenance infusion: 33.3 mg/kg per hour or 1 g/m² per hour (maximum 18 g/m² in 24 hours) has been used. Manufacturer states that safety and efficacy not established in pediatric patients.

Adults

Bleeding Due to Elevated Fibrinolytic Activity

Oral

5 g during the first hour, then 1–1.25 g per hour for about 8 hours or until bleeding has been controlled.

IV

Initial infusion (loading dose): 4–5 g over 1 hour.

Maintenance infusion: 1 g per hour for about 8 hours or until bleeding has been controlled.

Ocular Hemorrhage† [off-label]

Oral

100 mg/kg (up to 5 g) every 4 hours, up to a maximum daily dosage of 30 g, for 5 days has been used; lower daily dosages also may be effective.

Hereditary Hemorrhagic Telangiectasia†

Oral

1 or 1.5 g twice daily for 1–2 months, followed by 1–2 g daily.

Prescribing Limits

Pediatric Patients

Bleeding Due to Elevated Fibrinolytic Activity†

Oral or IV

Maximum 18 g/m² in 24 hours.

Adults

Ocular Hemorrhage

Oral

Maximum 30 g daily.

Cautions for Aminocaproic Acid

Contraindications

• Active intravascular clotting process.

• When it is not clear whether hemorrhage is secondary to primary fibrinolysis or disseminated intravascular coagulation (DIC), the distinction must be made before aminocaproic acid is administered. Do not use without concomitant heparin therapy in patients with evidence of DIC.

Warnings/Precautions

Warnings

Urinary Tract Bleeding

Intrarenal obstruction via glomerular capillary thrombosis or clots in the renal pelvis and ureters reported in patients with upper urinary tract bleeding. The drug should not be used in patients with hematuria of upper urinary tract origin unless the potential benefits outweigh risks.

Musculoskeletal Effects

Skeletal muscle weakness with necrosis of muscle fiber reported with prolonged administration. Presentation may range from mild myalgias with weakness and fatigue to severe proximal myopathy with rhabdomyolysis, myoglobinuria, and renal failure; CK levels are elevated. Manifestations resolve with drug discontinuance but may recur if therapy is reinstated.

Monitor CK concentrations with long-term therapy. Discontinue drug if an increase in CK occurs.

If skeletal myopathy occurs, consider possibility of cardiac muscle damage.

Benzyl Alcohol in Neonates

Aminocaproic acid injection contains as a preservative benzyl alcohol, which has been associated with toxicity (fatalities) in neonates. (See Pediatric Precautions.)

General Precautions

Should be used only in acute, life-threatening situations involving hemorrhage resulting from hyperfibrinolysis that has been confirmed by laboratory studies.

Clot Formation

If aminocaproic acid is present, clots formed in vivo may not undergo spontaneous lysis as do normal clots because aminocaproic acid in the clot may inhibit spontaneous fibrinolysis. No clear-cut evidence for in vivo drug-induced thrombosis; however, the hazard of this theoretical complication remains a possibility.

CNS Effects

Neurological deficits (hydrocephalus, cerebral ischemia, cerebral vasospasm) associated with use of antifibrinolytic agents in the management of subarachnoid hemorrhage. Causal relationship to the drugs not established.

Specific Populations

Pregnancy

Category C.

Lactation

Not known if aminocaproic acid is distributed into milk; caution if used in nursing women.

Pediatric Use

Safety and efficacy not established.

Large amounts of benzyl alcohol (i.e., 100–400 mg/kg daily) have been associated with toxicity (fatal “gasping syndrome”) in neonates (see Warnings); each mL of aminocaproic acid injection in multiple-dose vials contains 9 mg of benzyl alcohol.

Common Adverse Effects

Nausea, vomiting, cramping, abdominal pain, diarrhea, dizziness, malaise, fever, conjunctival suffusion, dyspnea, nasal congestion, headache, edema, pruritus, rash.

Specific Drugs

Aminocaproic Acid Pharmacokinetics

Absorption

Bioavailability

Rapidly and completely absorbed from the GI tract; peak plasma concentrations are attained within about 1 hour following a 5-g dose.

Special Populations

Plasma concentrations may be higher in patients with severe renal impairment.

Distribution

Extent

Distributed through extravascular as well as intravascular compartments; penetrates human red blood cells and other body cells.

Not known if aminocaproic acid is distributed into milk.

Plasma Protein Binding

Not bound.

Elimination

Metabolism

The major portion of aminocaproic acid is not metabolized.

Elimination Route

Eliminated principally in urine as unchanged drug (65%) and the adipic acid metabolite (11%).

Half-life

2 hours.

Special Populations

Removed by hemodialysis; may be removed by peritoneal dialysis.

Stability

Storage

Oral

Tablets

15–30°C; tight containers.

Syrup

15–30°C; tight containers. Do not freeze.

Parenteral

Injection

15–30°C. Do not freeze.

Compatibility

Parenteral

Solution CompatibilityHID

Y-Site CompatibilityHID

Actions

• Aminocaproic acid inhibits the activation of plasminogen; also inhibits the action of fibrinolysin (plasmin).

Advice to Patients

• Importance of informing clinician of existing or contemplated concomitant therapy, including prescription and OTC drugs and dietary or herbal products.

• Importance of women informing clinicians if they are or plan to become pregnant or plan to breast-feed.

• Importance of advising patients of other important precautionary information. (See Cautions.)

Preparations

Excipients in commercially available drug preparations may have clinically important effects in some individuals; consult specific product labeling for details.

Please refer to the ASHP Drug Shortages Resource Center for information on shortages of one or more of these preparations.

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