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.^b

Uses for Aminocaproic Acid

Bleeding Due to Elevated Fibrinolytic Activity

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

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).^{108 b}

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

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.¹⁰⁷

Ocular Hemorrhage

Has been used effectively for the prevention of secondary ocular hemorrhage in patients with nonperforating traumatic hyphema^{† [off-label]}.^{100 101 102 103 104 105 106} Designated an orphan drug by FDA for topical treatment of traumatic hyphema.¹¹⁹

Hereditary Hemorrhagic Telangiectasia

Has been used orally for the management of hereditary hemorrhagic telangiectasia^{† [off-label]}.¹¹²

Aminocaproic Acid Dosage and Administration

Administration

Administer orally or by IV infusion.^b

Oral Administration

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

IV Administration

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

Administer by IV infusion.^b

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

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.^b

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.^b

Rate of Administration

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

Maintenance infusion: Infuse 1 g per hour in adults.^b

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.^a Manufacturer states that safety and efficacy not established in pediatric patients.^b

IV

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

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.^a Manufacturer states that safety and efficacy not established in pediatric patients.^b

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.^{a b}

IV

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

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

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;^{100 101 102 103} lower daily dosages also may be effective.¹⁰²

Hereditary Hemorrhagic Telangiectasia†

Oral

1 or 1.5 g twice daily for 1–2 months, followed by 1–2 g daily.¹¹²

Prescribing Limits

Pediatric Patients

Bleeding Due to Elevated Fibrinolytic Activity†

Oral or IV

Maximum 18 g/m² in 24 hours.^a

Adults

Ocular Hemorrhage

Oral

Maximum 30 g daily.^{100 101 102 103}

Cautions for Aminocaproic Acid

Contraindications

• Active intravascular clotting process.^b

• 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.^b Do not use without concomitant heparin therapy in patients with evidence of DIC.^b

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.^b The drug should not be used in patients with hematuria of upper urinary tract origin unless the potential benefits outweigh risks.^b

Musculoskeletal Effects

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

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

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

Benzyl Alcohol in Neonates

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

General Precautions

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

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.^b No clear-cut evidence for in vivo drug-induced thrombosis; however, the hazard of this theoretical complication remains a possibility.^b

CNS Effects

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

Specific Populations

Pregnancy

Category C.^b

Lactation

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

Pediatric Use

Safety and efficacy not established.^{b 111}

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.^b

Common Adverse Effects

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

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.^{b 111}

Special Populations

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

Distribution

Extent

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

Not known if aminocaproic acid is distributed into milk.^b

Plasma Protein Binding

Not bound.^a

Elimination

Metabolism

The major portion of aminocaproic acid is not metabolized.^{b 111}

Elimination Route

Eliminated principally in urine as unchanged drug (65%) and the adipic acid metabolite (11%).^{b 111}

Half-life

2 hours.^b

Special Populations

Removed by hemodialysis; may be removed by peritoneal dialysis.^{b 111 121}

Stability

Storage

Oral

Tablets

15–30°C; tight containers.^b

Syrup

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

Parenteral

Injection

15–30°C.^b Do not freeze.^b

Compatibility

Parenteral

Solution CompatibilityHID

Y-Site CompatibilityHID

Actions

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

Advice to Patients

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

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

• Importance of advising patients of other important precautionary information.^b (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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