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Aminocaproic Acid

Pronunciation

(a mee noe ka PROE ik AS id)

Index Terms

  • EACA
  • Epsilon Aminocaproic Acid

Dosage Forms

Excipient information presented when available (limited, particularly for generics); consult specific product labeling. [DSC] = Discontinued product

Solution, Intravenous:

Generic: 250 mg/mL (20 mL)

Solution, Oral:

Amicar: 25% (236.5 mL) [contains edetate disodium, methylparaben, propylparaben, saccharin sodium; raspberry flavor]

Syrup, Oral:

Amicar: 25% (473 mL [DSC]) [raspberry flavor]

Generic: 25% (237 mL [DSC], 473 mL [DSC])

Tablet, Oral:

Amicar: 500 mg, 1000 mg [scored]

Generic: 500 mg [DSC], 1000 mg [DSC]

Brand Names: U.S.

  • Amicar

Pharmacologic Category

  • Antifibrinolytic Agent
  • Antihemophilic Agent
  • Hemostatic Agent
  • Lysine Analog

Pharmacology

Binds competitively to plasminogen; blocking the binding of plasminogen to fibrin and the subsequent conversion to plasmin, resulting in inhibition of fibrin degradation (fibrinolysis).

Distribution

Widely through intravascular and extravascular compartments; Vd: Oral: 23 L, IV: 30 L

Metabolism

Minimally hepatic

Excretion

Urine (65% as unchanged drug, 11% as metabolite)

Onset of Action

~1 to 72 hours

Time to Peak

Oral: 1.2 ± 0.45 hours

Half-Life Elimination

1 to 2 hours

Use: Labeled Indications

To enhance hemostasis when fibrinolysis contributes to bleeding (causes may include cardiac surgery, hematologic disorders, neoplastic disorders, abruptio placentae, hepatic cirrhosis, and urinary fibrinolysis)

Use: Unlabeled

Treatment of traumatic hyphema; control bleeding in thrombocytopenia; control oral bleeding in congenital and acquired coagulation disorders; topical treatment (mouth rinse) of bleeding associated with dental procedures in patients on oral anticoagulant therapy; prevention of perioperative bleeding associated with cardiac surgery; prevention of bleeding associated with extracorporeal membrane oxygenation (ECMO); prevention of perioperative bleeding associated with spinal surgery (eg, idiopathic scoliosis)

Contraindications

Disseminated intravascular coagulation (without heparin); evidence of an active intravascular clotting process

Dosing: Adult

Acute bleeding: Oral, IV: Loading dose: 4-5 g during the first hour, followed by 1 g/hour for 8 hours (or 1.25 g/hour using oral solution) or until bleeding controlled (maximum daily dose: 30 g)

Control of bleeding with severe thrombocytopenia (off-label use) (Bartholomew, 1989; Gardner, 1980):

Initial: IV: 100 mg/kg (maximum dose: 5 g) over 30-60 minutes

Maintenance: Oral, IV: 1-4 g every 4-8 hours or 1 g/hour (maximum daily dose: 24 g)

Control of oral bleeding in congenital and acquired coagulation disorder (off-label use): Oral: 50-60 mg/kg every 4 hours (Mannucci, 1998)

Prevention of dental procedure bleeding in patients on oral anticoagulant therapy (off-label use): Oral rinse: Hold 4 g/10 mL in mouth for 2 minutes then spit out. Repeat every 6 hours for 2 days after procedure (Souto, 1996). Concentration and frequency may vary by institution and product availability.

Prevention of perioperative bleeding associated with cardiac surgery (off-label use): IV: Loading dose of 75-150 mg/kg (typically 5-10 g), followed by 10-15 mg/kg/hour (typically 1 g/hour); may add 2-2.5 g/L of cardiopulmonary bypass circuit priming solution (Gravlee, 2008)

or

Loading dose of 10 g followed by 2 g/hour during surgery; no medication added to the bypass circuit (Fergusson, 2008)

or

10 g over 20-30 minutes prior to skin incision, followed by 10 g after heparin administration then 10 g at discontinuation of cardiopulmonary bypass (Vander Salm, 1996)

Traumatic hyphema (off-label use): Oral: 50 mg/kg/dose every 4 hours (maximum daily dose: 30 g) for 5 days (Brandt, 2001; Crouch, 1999)

Dosing: Geriatric

Refer to adult dosing.

Dosing: Pediatric

Prevention of perioperative bleeding associated with cardiac surgery (off-label use): IV: 100 mg/kg given over 20-30 minutes after induction and prior to incision, 100 mg/kg during cardiopulmonary bypass, and 100 mg/kg after heparin reversal over 3 hours (Chauhan, 2004)

Prevention of bleeding associated with extracorporeal membrane oxygenation (ECMO) (off-label use): IV: 100 mg/kg prior to or immediately after cannulation, followed by 25-30 mg/kg/hour for up to 72 hours (Downard, 2003; Horwitz, 1998; Wilson, 1993)

Prevention of perioperative bleeding associated with spinal surgery (eg, idiopathic scoliosis) (off-label use): Children and Adolescents: IV: 100 mg/kg given over 15-20 minutes after induction, followed by 10 mg/kg/hour for the remainder of the surgery; discontinue at time of wound closure (Florentino-Pineda, 2001; Florentino-Pineda, 2004)

Traumatic hyphema (off-label use): Oral: Refer to adult dosing.

Dosing: Renal Impairment

May accumulate in patients with decreased renal function. When used during cardiopulmonary bypass in anephric patients, a normal or slightly reduced loading dose and a continuous infusion rate of 5 mg/kg/hour has been recommended (Gravlee, 2008).

Dosing: Hepatic Impairment

No dosage adjustment provided in the manufacturer’s labeling.

Reconstitution

Dilute IV solution in D5W, 0.9% sodium chloride, or Ringer's injection.

Administration

Rapid IV injection (IVP) of undiluted solution is not recommended due to possible hypotension, bradycardia, and arrhythmia.

IV: May administer loading dose over 15-60 minutes depending on indication; a continuous infusion may be necessary.

Compatibility

Stable in D5W, NS, Ringer’s injection

Storage

Store intact vials, tablets, and syrup at 15°C to 30°C (59°F to 86°F). Do not freeze injection or syrup. Solutions diluted for IV use in D5W or NS to concentrations of 10-100 mg/mL are stable at 4°C (39°F) and 23°C (73°F) for 7 days (Zhang, 1997).

Drug Interactions

Anti-inhibitor Coagulant Complex (Human): Antifibrinolytic Agents may enhance the thrombogenic effect of Anti-inhibitor Coagulant Complex (Human). Avoid combination

Factor IX Complex (Human) [(Factors II, IX, X)]: Aminocaproic Acid may enhance the adverse/toxic effect of Factor IX Complex (Human) [(Factors II, IX, X)]. Specifically, use of this combination may increase the risk of thrombosis. Avoid combination

Fibrinogen Concentrate (Human): Antifibrinolytic Agents may enhance the adverse/toxic effect of Fibrinogen Concentrate (Human). Specifically, the risk for thrombosis may be increased. Fibrinogen Concentrate (Human) may enhance the adverse/toxic effect of Antifibrinolytic Agents. Specifically, the risk for thrombosis may be increased. Monitor therapy

Tretinoin (Systemic): May enhance the thrombogenic effect of Antifibrinolytic Agents. Monitor therapy

Adverse Reactions

Frequency not defined.

Cardiovascular: Arrhythmia, bradycardia, edema, hypotension, intracranial hypertension, peripheral ischemia, syncope, thrombosis

Central nervous system: Confusion, delirium, dizziness, fatigue, hallucinations, headache, malaise, seizure, stroke

Dermatologic: Rash, pruritus

Gastrointestinal: Abdominal pain, anorexia, cramps, diarrhea, GI irritation, nausea, vomiting

Genitourinary: Dry ejaculation

Hematologic: Agranulocytosis, bleeding time increased, leukopenia, thrombocytopenia

Local: Injection site necrosis, injection site pain, injection site reactions

Neuromuscular & skeletal: CPK increased, myalgia, myositis, myopathy, rhabdomyolysis (rare), weakness

Ophthalmic: Vision decreased, watery eyes

Otic: Tinnitus

Renal: BUN increased, intrarenal obstruction (glomerular capillary thrombosis), myoglobinuria (rare), renal failure (rare)

Respiratory: Dyspnea, nasal congestion, pulmonary embolism

Miscellaneous: Allergic reaction, anaphylactoid reaction, anaphylaxis

Postmarketing and/or case reports: Hepatic lesion, hyperkalemia, myocardial lesion

Warnings/Precautions

Concerns related to adverse effects:

• Intrarenal obstruction: May occur secondary to glomerular capillary thrombosis or clots in the renal pelvis and ureters; do not use in hematuria of upper urinary tract origin unless possible benefits outweigh risks.

• Skeletal muscle weakness: Ranging from mild myalgias and fatigue to severe myopathy with rhabdomyolysis and acute renal failure has been reported with prolonged use. Monitor CPK; discontinue treatment with a rise in CPK.

Disease-related concerns:

• Renal impairment: Use with caution in patients with renal impairment; may accumulate.

Concurrent drug therapy issues:

• Blood products: Do not administer with factor IX complex concentrates or anti-inhibitor coagulant complexes; may increase risk for thrombosis.

Dosage form specific issues:

• Benzyl alcohol and derivatives: Some dosage forms may contain benzyl alcohol; large amounts of benzyl alcohol (≥99 mg/kg/day) have been associated with a potentially fatal toxicity (“gasping syndrome”) in neonates; the “gasping syndrome” consists of metabolic acidosis, respiratory distress, gasping respirations, CNS dysfunction (including convulsions, intracranial hemorrhage), hypotension and cardiovascular collapse (AAP ["Inactive" 1997]; CDC, 1982); some data suggests that benzoate displaces bilirubin from protein binding sites (Ahlfors, 2001); avoid or use dosage forms containing benzyl alcohol with caution in neonates. See manufacturer’s labeling.

Other warnings/precautions:

• Appropriate use: Do not administer without a definite diagnosis of laboratory findings indicative of hyperfibrinolysis. Inhibition of fibrinolysis may promote clotting or thrombosis; more likely due to the presence of DIC.

• IV administration: Avoid rapid IV administration; may induce hypotension, bradycardia, or arrhythmia; rapid injection of undiluted solution is not recommended.

Monitoring Parameters

Fibrinogen, fibrin split products, creatine phosphokinase (with long-term therapy), BUN, creatinine

Pregnancy Risk Factor

C

Pregnancy Considerations

Animal reproduction studies have not been conducted.

Patient Education

• Discuss specific use of drug and side effects with patient as it relates to treatment. (HCAHPS: During this hospital stay, were you given any medicine that you had not taken before? Before giving you any new medicine, how often did hospital staff tell you what the medicine was for? How often did hospital staff describe possible side effects in a way you could understand?)

• Patient may experience nausea, vomiting, abdominal pain, diarrhea, loss of strength and energy, or rhinitis. Have patient report immediately to prescriber signs of severe cerebrovascular disease (change in strength on one side is greater than the other, trouble speaking or thinking, change in balance, or change in eyesight), signs of DVT (edema, warmth, numbness, change in color, or pain in the extremities), arrhythmia, bradycardia, bruising, bleeding, urinary retention, change in amount of urine passed, muscle pain, muscle weakness, edema, seizures, passing out, severe dizziness, hallucinations, confusion, angina, coughing up blood, shortness of breath, chills, pharyngitis, severe headache, vision changes, tinnitus, or severe injection site pain or irritation (HCAHPS).

• Educate patient about signs of a significant reaction (eg, wheezing; chest tightness; fever; itching; bad cough; blue skin color; seizures; or swelling of face, lips, tongue, or throat). Note: This is not a comprehensive list of all side effects. Patient should consult prescriber for additional questions.

Intended Use and Disclaimer: Should not be printed and given to patients. This information is intended to serve as a concise initial reference for health care professionals to use when discussing medications with a patient. You must ultimately rely on your own discretion, experience and judgment in diagnosing, treating, and advising patients.

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