Version October 2024
Acute bleeding: Oral, IV: Loading dose: 4 to 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 is controlled; maximum daily dose: 30 g.
Extracorporeal membrane oxygenation, refractory bleeding (off-label use): IV: Loading dose of 4 to 5 g; followed by an infusion of 1 to 1.25 g/hour until bleeding is controlled (Ref).
Intracranial hemorrhage associated with thrombolytic treatment (alternative therapy) (off-label use):
Note: Consider for use in addition to cryoprecipitate or when cryoprecipitate is contraindicated in patients who have a symptomatic intracranial hemorrhage after receiving thrombolytic within the past 24 hours (Ref).
IV: Loading dose: 4 to 5 g, followed by 1 g/hour for 8 hours until bleeding is controlled (Ref).
Mouth and mucosal bleeding in patients with hemostatic defects (eg, hemophilia, von Willebrand disease, other factor deficiencies associated with bleeding) (adjunctive therapy):
Note: Generally, use in conjunction with (and not as a substitute for) replacement of the appropriate clotting factor, especially in individuals with hemophilia. Do not give simultaneously with an activated prothrombin complex concentrate, as this can increase the risk of thromboembolism; if used concurrently, they should be separated by ≥12 hours (Ref). Consultation with a hemophilia treatment center is advised.
Oral: 50 to 100 mg/kg every 6 hours until wound has healed (Ref).
Perioperative prevention of blood loss and transfusion (eg, cardiac surgery, other surgeries with significant blood loss) (off-label use):
Note: Dosing and timing of administration varies widely; use is procedure and institution specific. Recommendations provided below are usual dosage ranges from a variety of surgeries; refer to institutional protocols for details on specific surgeries.
Usual dose and range: IV: Loading dose of 5 to 10 g (or 75 to 150 mg/kg), followed by 1 g/hour (or 10 to 15 mg/kg/hour) until the end of the procedure or up to 8 hours after the procedure (Ref).
Subarachnoid hemorrhage, prevention of early aneurysmal rebleeding (off-label use):
Note: Routine use prior to aneurysm repair is not recommended (Ref). Optimal regimen has not been established; refer to institutional protocol.
IV: Loading dose: 4 to 5 g immediately after diagnosis, followed by 1 g/hour infusion for up to 72 hours (Ref).
Thrombocytopenia (severe), bleeding (off-label use):
Loading dose: IV: 100 mg/kg (maximum dose: 5 g) over 30 to 60 minutes, followed by 1 g/hour; maximum daily dose: 24 g (Ref). When bleeding has ceased, may consider transitioning to maintenance dose.
Maintenance: Oral, IV: 1 to 4 g every 4 to 12 hours; maximum daily dose: 24 g; duration of therapy varies depending on etiology and patient factors, but may continue maintenance dose until platelet count is stable without the need for transfusions and the risk of bleeding is minimized (Ref).
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 (Ref).
No dosage adjustment provided in the manufacturer's labeling.
Refer to adult dosing.
(For additional information see "Aminocaproic acid: Pediatric drug information")
Hematuria (gross; upper tract), refractory: Limited data available: Children ≥11 years and Adolescents: Oral: 100 mg/kg/dose every 6 hours; continue for 2 days beyond resolution of hematuria; dosing based on case series (n=4) which showed hematuria resolution within 2 to 7 days; risks and benefits must be weighed prior to use (Ref).
Hemorrhage (oral, epistaxis, menorrhagia) in patients with hemostatic disorders, adjunct treatment: Limited data available: Infants, Children, and Adolescents: Oral: 50 to 100 mg/kg/dose every 6 hours; maximum daily dose: 24 g/day (Ref).
Mucosal bleeding in thrombocytopenia/platelet dysfunction, treatment: Limited data available: Infants, Children, and Adolescents: Oral, IV: 50 to 100 mg/kg/dose every 6 hours; maximum daily dose: 24 g/day (Ref).
Prevention of bleeding associated with dental procedures in hemophilic patients: Limited data available: Infants, Children, and Adolescents: Oral: 50 to 100 mg/kg/dose every 6 hours; maximum daily dose: 24 g/day; used in conjunction with DDAVP or factor replacement therapy; continue for up to 7 days or until mucosal healing is complete (Ref).
Prevention of bleeding associated with extracorporeal membrane oxygenation (ECMO), high-bleeding risk patients: Limited data available: Infants, Children, and Adolescents: IV: 100 mg/kg prior to or immediately after cannulation, followed by a continuous IV infusion of 25 to 30 mg/kg/hour for up to 72 hours; target activated clotting time (ACT) range during therapy of 180 to 200 seconds has been used (Ref); variable results; patients requiring surgery just prior to or while on ECMO seem to benefit most.
Prevention of perioperative bleeding: Limited data available:
Cardiac surgery with cardiopulmonary bypass:
Infants and Children <2 years: Dosing regimens variable: IV: In the largest trial (n=120, all patients <20 kg), a dose of 75 mg/kg was administered at the beginning and end of cardiopulmonary bypass (CPB), and 75 mg/100 mL was added to the CPB priming fluid (Ref). Another study group in 2 separate trials (n=110, age range: 2 months to 14 years) used a 100 mg/kg dose after induction, during CPB pump priming, and when weaning CPB (over 3 hours) for a total of 3 doses (Ref).
Children ≥2 years and Adolescents: IV: 100 mg/kg after induction, during CPB pump priming, and when weaning CPB (over 3 hours) for a total of 3 doses; regimen used in 2 separate trials (n=110, age range: 2 months to 14 years) (Ref).
Craniofacial reconstruction surgery:
Infants ≥6 months to Children ≤2 years: IV: 100 mg/kg administered over 10 minutes, followed by a continuous IV infusion of 40 mg/kg/hour until the end of surgery (ie, completion of skin closure). Dosing based on an open-label, non-randomized, dose escalation, population pharmacokinetic trial (n=18, median age: 39 weeks) (Ref).
Spinal surgery (eg, idiopathic scoliosis) :
Children ≥11 years and Adolescents: IV: 100 mg/kg (maximum dose: 5 g) administered over 15 to 30 minutes after induction, followed by a continuous IV infusion of 10 mg/kg/hour for the remainder of the surgery; discontinued at time of wound closure (Ref).
Traumatic hyphema: Limited data available: Infants, Children, and Adolescents: Oral: 50 to 100 mg/kg/dose every 4 hours for 5 days; maximum daily dose: 30 g/day (Ref).
There are no dosage adjustments are provided in the manufacturer's labeling; aminocaproic acid may accumulate in patients with decreased renal function; use with caution.
There are no dosage adjustments are provided in the manufacturer's labeling.
The following adverse drug reactions and incidences are derived from product labeling unless otherwise specified. 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
Disseminated intravascular coagulation (without heparin); evidence of an active intravascular clotting process.
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 disseminated intravascular coagulation.
• IV administration: Avoid rapid IV administration; may induce hypotension, bradycardia, or arrhythmia; rapid injection of undiluted solution is not recommended.
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 [DSC]) [contains edetate (edta) disodium, methylparaben, propylparaben, saccharin sodium; raspberry flavor]
Generic: 25% (236.5 mL)
Tablet, Oral:
Amicar: 500 mg [DSC], 1000 mg [DSC] [scored]
Generic: 500 mg, 1000 mg
Yes
Solution (Aminocaproic Acid Intravenous)
250 mg/mL (per mL): $0.33 - $0.56
Solution (Aminocaproic Acid Oral)
0.25 g/mL (per mL): $13.47
Tablets (Aminocaproic Acid Oral)
500 mg (per each): $7.16 - $31.84
1000 mg (per each): $13.55 - $43.98
Disclaimer: A representative AWP (Average Wholesale Price) price or price range is provided as reference price only. A range is provided when more than one manufacturer's AWP price is available and uses the low and high price reported by the manufacturers to determine the range. The pricing data should be used for benchmarking purposes only, and as such should not be used alone to set or adjudicate any prices for reimbursement or purchasing functions or considered to be an exact price for a single product and/or manufacturer. Medi-Span expressly disclaims all warranties of any kind or nature, whether express or implied, and assumes no liability with respect to accuracy of price or price range data published in its solutions. In no event shall Medi-Span be liable for special, indirect, incidental, or consequential damages arising from use of price or price range data. Pricing data is updated monthly.
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.
Oral: May administer without regard to food.
Parenteral: Do not administer undiluted; rapid IV injection (IVP) of undiluted solution is not recommended due to possible hypotension, bradycardia, and arrhythmia.
Intermittent IV infusion: After further dilution, administer over 10 to 60 minutes (rate dependent upon use) (Ref).
Continuous IV infusion: Must further dilute prior to administration.
IV infusion: 5000 mg in 250 mL (concentration: 20 mg/mL) of D5W, NS, or Ringer's injection
Active bleeding: To enhance hemostasis when fibrinolysis contributes to bleeding (causes may include cardiac surgery, hematologic disorders, neoplastic disorders, abruptio placentae, hepatic cirrhosis, and urinary fibrinolysis).
Extracorporeal membrane oxygenation, refractory bleeding; Intracranial hemorrhage associated with thrombolytic treatment (alternative therapy); Mouth and mucosal bleeding in patients with hemostatic defects (eg, hemophilia, von Willebrand disease, other factor deficiencies associated with bleeding) (adjunctive therapy); Perioperative prevention of blood loss and transfusion (eg, cardiac surgery, other surgeries with significant blood loss); Subarachnoid hemorrhage, prevention of early aneurysmal rebleeding; Thrombocytopenia (severe), bleeding
Amicar may be confused with amikacin, Amikin
Amicar [US] may be confused with Omacor brand name for Omega-3-Acid Ethyl Esters [multiple international markets]
None known.
Note: Interacting drugs may not be individually listed below if they are part of a group interaction (eg, individual drugs within “CYP3A4 Inducers [Strong]” are NOT listed). For a complete list of drug interactions by individual drug name and detailed management recommendations, use the drug interactions program by clicking on the “Launch drug interactions program” link above.
Anti-inhibitor Coagulant Complex (Human): Antifibrinolytic Agents may enhance the thrombogenic effect of Anti-inhibitor Coagulant Complex (Human). Risk X: Avoid combination
Factor IX Complex (Human) [(Factors II, IX, X)]: Antifibrinolytic Agents may enhance the adverse/toxic effect of Factor IX Complex (Human) [(Factors II, IX, X)]. Specifically, the risk for thrombosis may be increased. Risk X: Avoid combination
Prothrombin Complex Concentrate (Human) [(Factors II, VII, IX, X), Protein C, and Protein S]: Antifibrinolytic Agents may enhance the adverse/toxic effect of Prothrombin Complex Concentrate (Human) [(Factors II, VII, IX, X), Protein C, and Protein S]. Specifically, the risk for thrombosis may be increased. Risk X: Avoid combination
Tretinoin (Systemic): May enhance the thrombogenic effect of Antifibrinolytic Agents. Management: Concomitant use of antifibrinolytics and tretinoin is not recommended. If combined, monitor patients closely for any signs of thrombotic complications. Risk D: Consider therapy modification
Animal reproduction studies have not been conducted.
It is not known if aminocaproic acid is excreted in breast milk. The manufacturer recommends that caution be exercised when administering aminocaproic acid to nursing women
Fibrinogen, fibrin split products, creatine phosphokinase (with long-term therapy), BUN, creatinine
Binds competitively to plasminogen; blocking the binding of plasminogen to fibrin and the subsequent conversion to plasmin, resulting in inhibition of fibrin degradation (fibrinolysis).
Onset of action: ~1 to 72 hours
Distribution: Widely through intravascular and extravascular compartments; Vd: Oral: 23 L; IV: 30 L
Metabolism: Minimally hepatic
Bioavailability: Oral: 100%
Half-life elimination: 1 to 2 hours
Time to peak: Oral: 1.2 ± 0.45 hours
Excretion: Urine (65% as unchanged drug, 11% as metabolite)
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