Medically reviewed on Sep 10, 2018
(a mee noe ka PROE ik AS id)
- Epsilon Aminocaproic Acid
Excipient information presented when available (limited, particularly for generics); consult specific product labeling. [DSC] = Discontinued product
Generic: 250 mg/mL (20 mL)
Amicar: 25% (236.5 mL) [contains edetate disodium, methylparaben, propylparaben, saccharin sodium; raspberry flavor]
Generic: 25% (237 mL [DSC], 473 mL [DSC])
Amicar: 500 mg, 1000 mg [scored]
Generic: 500 mg [DSC], 1000 mg [DSC]
Brand Names: U.S.
- Antifibrinolytic Agent
- Antihemophilic Agent
- Hemostatic Agent
- Lysine Analog
Binds competitively to plasminogen; blocking the binding of plasminogen to fibrin and the subsequent conversion to plasmin, resulting in inhibition of fibrin degradation (fibrinolysis).
Widely through intravascular and extravascular compartments; Vd: Oral: 23 L, IV: 30 L
Urine (65% as unchanged drug, 11% as metabolite)
Onset of Action
~1 to 72 hours
Time to Peak
Oral: 1.2 ± 0.45 hours
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)
Off Label Uses
Bleeding associated with dental procedures in patients on oral anticoagulant therapy (mouth rinse)
Data from a limited number of patients studied suggest that aminocaproic acid may be beneficial for the prevention of bleeding associated with dental procedures in patients on oral anticoagulant therapy (mouth rinse) [Souto 1996]. Additional data may be necessary to further define the role of aminocaproic acid in this condition.
Bleeding (control) in severe thrombocytopenia
Data from a limited number of patients studied (case series) in patients with amegakaryocytic thrombocytopenia and immune thrombocytopenia who were refractory to usual therapies suggests that aminocaproic acid may be beneficial for the control of bleeding associated with severe thrombocytopenia [Bartholomew 1989], [Gardner 1980]. Additional data may be necessary to further define the role of aminocaproic acid in this condition.
Bleeding (prevention) associated with extracorporeal membrane oxygenation (infants/children/adolescents)
Data from an unblinded, retrospective study evaluating the use of aminocaproic acid in patients (1 day to 19 years of age) who were treated with extracorporeal membrane oxygenation (ECMO) over a 10 year period suggests that aminocaproic acid may be beneficial in the prevention of bleeding, mostly surgical site, associated with ECMO. Of note, most patients included in this evaluation were neonates [Downard 2003]. In a prior study, neonates who were to be treated with ECMO at high risk of bleeding were administered aminocaproic acid and compared to a low-risk population who were not treated with aminocaproic acid [Wilson 1993]. Additionally, data from a multi-institutional, randomized, placebo-controlled trial in neonates (with varying degrees of bleeding risk) treated with ECMO also suggested that the use of aminocaproic acid is safe; however, the overall incidence of bleeding complications may not be reduced [Horwitz 1998]. Additional trials may be necessary to further define the role of aminocaproic acid in this condition.
Control of refractory bleeding associated with extracorporeal membrane oxygenation
Data from a limited number of patients studied (cases series) suggests that the use of aminocaproic acid may be beneficial for the control of refractory bleeding in patients on extracorporeal membrane oxygenation (ECMO) [Buckley 2016]. Additional data may be necessary to further define the role of aminocaproic acid to control bleeding associated with ECMO.
Intracranial hemorrhage associated with thrombolytics (plasminogen-activator) (eg, alteplase, reteplase, or tenecteplase)
Based on the Neurocritical Care Society and the Society of Critical Care Medicine guideline for reversal of antithrombotics in intracranial hemorrhage, aminocaproic acid is suggested as a reversal agent for use in intracranial hemorrhage due to thrombolytics (plasminogen-activator) (eg, alteplase, reteplase, tenecteplase) in cases where cryoprecipitate (preferred therapy) is contraindicated or not available in a timely manner.
Oral bleeding (control) in congenital and acquired coagulation disorders
Data from a limited number of clinical trials suggest that aminocaproic acid may be beneficial for the control of oral bleeding in congenital and acquire coagulation disorders [Lucas 1981]. Clinical experience also suggests the utility of aminocaproic acid in managing the treatment of oral bleeding in congenital and acquired coagulation disorders [Mannucci 1998]. Additional data may be necessary to further define the role of aminocaproic acid in this condition.
Perioperative bleeding (prevention) associated with cardiac surgery
Data from three randomized, prospective, placebo-controlled studies supports the use of aminocaproic acid in the prevention of perioperative bleeding associated with cardiac surgery [Fergusson 2008], [Penta de Peppo 1995], [Vander Salm 1996]. Additionally, data from a prospective randomized controlled trial in children undergoing cardiac surgery for cyanotic heart disease supports the use of aminocaproic acid to reduce postoperative blood loss and packed red blood cell and platelet transfusions [Chauhan 2004].
Perioperative bleeding (prevention) associated with spinal surgery (eg, idiopathic scoliosis)
Data from a limited number of patients studied suggest that aminocaproic acid may be beneficial for the prevention of perioperative bleeding associated with spinal surgery (eg, idiopathic scoliosis) [Florentino-Pineda 2001]. Subsequently, data from a prospective, randomized, double-blind study in children (11 to 18 years of age) undergoing a posterior spinal fusion for idiopathic scoliosis [Florentino-Pineda 2004]. Additional data may be necessary to further define the role of aminocaproic acid in this condition.
Current evidence suggests aminocaproic acid may be an effective option for prevention of rebleeding in patients with SAH, provided therapy does not continue past 72 hours after the event and there are no thromboembolic risk factors. Incidents of early rebleeding are often fatal and are a primary concern in SAH; however, thrombotic events also remain a serious concern because of a lack of data from adequately powered studies demonstrating the risk of adverse events. Other guideline recommendations to avoid rebleeding include tranexamic acid (another antifibrinolytic), a titratable agent to control hypertension (SBP less than 160 mm Hg), and surgical interventions, such as clipping or endovascular coiling.
Data from one prospective, randomized, placebo-controlled, double-blind, multicenter study and one randomized, placebo-controlled study support the use of aminocaproic acid in the treatment of secondary hemorrhage after traumatic hyphema [Crouch 1997], [McGetrick 1983]. Clinical experience also suggests the utility of aminocaproic acid in managing this condition [Brandt 2001], [Crouch 1999]. Additional trials may be necessary to further define the role of aminocaproic acid in this condition.
Disseminated intravascular coagulation (without heparin); evidence of an active intravascular clotting process
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 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 to 60 minutes
Maintenance: Oral, IV: 1 to 4 g every 4 to 8 hours or 1 g/hour (maximum daily dose: 24 g). Additional data may be necessary to further define the role of aminocaproic acid in the treatment of this condition.
Control of oral bleeding in congenital and acquired coagulation disorder (off-label use): Oral: 50 to 60 mg/kg every 4 hours (Mannucci 1998). Additional data may be necessary to further define the role of aminocaproic acid in the treatment of this condition.
Control of refractory bleeding associated with extracorporeal membrane oxygenation (off-label use): IV: 4 to 5 g loading dose; follow with an infusion of 1 to 1.25 g/hour until bleeding controlled (Buckley 2016). Additional data may be necessary to further define the role of aminocaproic acid in the treatment of this condition.
Intracranial hemorrhage associated with thrombolytics (plasminogen-activator) (eg, alteplase, reteplase, tenecteplase) (off-label use): IV: 4 to 5 g (as an alternative to cryoprecipitate); check fibrinogen levels after administration, if fibrinogen <150 mg/dL, cryoprecipitate is recommended (NCS/SCCM [Frontera 2016]).
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. Additional data may be necessary to further define the role of aminocaproic acid in the treatment of this condition.
Prevention of perioperative bleeding associated with cardiac surgery (off-label use): IV: Loading dose of 75 to 150 mg/kg (typically 5 to 10 g), followed by 10 to 15 mg/kg/hour (typically 1 g/hour); may add 2 to 2.5 g/L of cardiopulmonary bypass circuit priming solution (Gravlee 2008)
Loading dose of 10 g followed by 2 g/hour during surgery; no medication added to the bypass circuit (Fergusson 2008)
10 g over 20 to 30 minutes prior to skin incision, followed by 10 g after heparin administration then 10 g at discontinuation of cardiopulmonary bypass (Vander Salm1996)
Subarachnoid hemorrhage (off-label use): IV: Loading dose of 4 g followed by 1 g/hour infusion for up to 72 hours after SAH onset. Note: Discontinue infusion 4 hours prior to angiography or 2 hours prior to endovascular ablation of aneurysm (Diringer 2011; Starke 2008). Additional data may be necessary to further define the role of aminocaproic acid in the treatment of this condition.
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)
Refer to adult dosing.
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.
Dilute IV solution in D5W, 0.9% sodium chloride, or Ringer's injection.
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.
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).
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
Tretinoin (Systemic): May enhance the thrombogenic effect of Antifibrinolytic Agents. Monitor therapy
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
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
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.
• 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.
• 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.
Fibrinogen, fibrin split products, creatine phosphokinase (with long-term therapy), BUN, creatinine
Pregnancy Risk Factor
Animal reproduction studies have not been conducted.
• 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, difficulty speaking or thinking, change in balance, or vision changes), signs of DVT (edema, warmth, numbness, change in color, or pain in the extremities), abnormal heartbeat, 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.
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- Drug class: miscellaneous coagulation modifiers
Other brands: Amicar