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Pronunciation
(a mee noe ka PROE ik AS id)
Generic Available (U.S.)
Yes
Index Terms
U.S. Brand Names
Pharmacologic Category
Pharmacologic Category Synonyms
Use: Labeled Indications
To enhance hemostasis when fibrinolysis contributes to bleeding (causes may include cardiac surgery, hematologic disorders, neoplastic disorders, abruption placentae, hepatic cirrhosis, and urinary fibrinolysis)
Use: Unlabeled/Investigational
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
Pregnancy Risk Factor
C
Pregnancy Considerations
Animal reproductive studies have not been conducted.
Lactation
Excretion in breast milk unknown/use caution
Contraindications
Disseminated intravascular coagulation (without heparin); evidence of an active intravascular clotting process
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: Injection contains benzyl alcohol which has been associated with "gasping syndrome" in neonates.
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.
• I.V. administration: Avoid rapid I.V. administration; may induce hypotension, bradycardia, or arrhythmia; rapid injection of undiluted solution is not recommended.
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, injectionsite 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, myocardial lesion
Drug Interactions
Anti-inhibitor Coagulant Complex: Antifibrinolytic Agents may enhance the thrombogenic effect of Anti-inhibitor Coagulant Complex. Risk X: Avoid combination
Factor IX: Aminocaproic Acid may enhance the adverse/toxic effect of Factor IX. Specifically, use of this combination may increase the risk of thrombosis. Risk X: Avoid combination
Factor IX Complex (Human): Aminocaproic Acid may enhance the adverse/toxic effect of Factor IX Complex (Human). Specifically, use of this combination may increase the risk of thrombosis. Risk X: 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. Risk C: Monitor therapy
Tretinoin (Systemic): May enhance the thrombogenic effect of Antifibrinolytic Agents. Risk C: Monitor therapy
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 I.V. 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).
Reconstitution
Dilute I.V. solution in D5W, 0.9% sodium chloride, or Ringer's injection.
Compatibility
Stable in D5W, NS, Ringer's injection
Mechanism of Action
Binds competitively to plasminogen; blocking the binding of plasminogen to fibrin and the subsequent conversion to plasmin, resulting in inhibition of fibrin degradation (fibrinolysis).
Pharmacodynamics/Kinetics
Onset of action: ~1-72 hours
Distribution: Widely through intravascular and extravascular compartments
Vd: Oral: 23 L, I.V.: 30 L
Metabolism: Minimally hepatic
Half-life elimination: ~2 hours
Time to peak: Oral: Within 2 hours
Excretion: Urine (65% as unchanged drug, 11% as metabolite)
Dosage
Acute bleeding syndrome:
Children (unlabeled use): Oral, I.V.: Loading dose: 100-200 mg/kg during the first hour, followed by continuous infusion at 33.3 mg/kg/hour (I.V.) or 100 mg/kg (oral or I.V.) every 6 hours
Adults: Oral, I.V.: Loading dose: 4-5 g during the first hour, followed by 1 g/hour (or 1.25 g/hour using oral solution) for 8 hours or until bleeding controlled (maximum daily dose: 30 g)
Control of bleeding in thrombocytopenia (unlabeled use): Adults:
Initial: I.V.: 100 mg/kg over 30-60 minutes
Maintenance: Oral: 1-3 g every 6 hours
Control of oral bleeding in congenital and acquired coagulation disorder (unlabeled use): Adults: Oral: 50-60 mg/kg every 4 hours
Prevention of dental procedure bleeding in patients on oral anticoagulant therapy (unlabeled 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 (unlabeled use): I.V.:
Children: 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 protamine reversal of heparin
Adults: 10 g over 20-30 minutes prior to skin incision, followed by 1-2.5 g/hour (usual dose 2 g/hour) until the end of operation (may continue infusion for 4 hours after protamine reversal of heparin). May add 10 g to cardiopulmonary bypass circuit priming solution.
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 prior to protamine reversal of heparin
Traumatic hyphema (unlabeled use): Children and Adults: Oral: 100 mg/kg/dose every 4 hours (maximum daily dose: 30 g)
Dosing adjustment in renal impairment: May accumulate in patients with decreased renal function.
Administration: I.V.
Rapid I.V. injection (IVP) of undiluted solution is not recommended due to possible hypotension, bradycardia, and arrhythmia.
I.V.: Acute bleeding syndrome: Administer loading dose over 1 hour, followed by a continuous infusion
I.V.: Prevention of perioperative bleeding associated with cardiac surgery (unlabeled use): Administer loading dose over 20-30 minutes prior to skin incision, followed by a continuous infusion until the end of operation or as 2 additional bolus doses (over 20-30 minutes) given after heparin administration and at discontinuation of cardiopulmonary bypass prior to protamine reversal of heparin.
Administration: I.V. Detail
pH: 6.8 (adjusted); range: 6-7.6
Monitoring Parameters
Fibrinogen, fibrin split products, creatine phosphokinase (with long-term therapy), BUN, creatinine
Patient Education
This medication may cause muscle weakness and fatigue.
Dental Health: Effects on Dental Treatment
No significant effects or complications reported (see Effects on Bleeding)
Dental Health: Vasoconstrictor/Local Anesthetic Precautions
No information available to require special precautions
Mental Health: Effects on Mental Status
May cause drowsiness
Mental Health: Effects on Psychiatric Treatment
May cause hypotension which may be exacerbated by psychotropics; rarely may cause seizures; use caution with clozapine and bupropion
Nursing: Physical Assessment/Monitoring
Monitor and report signs of bleeding, thromboembolism, hypotension, or CNS changes.
Dosage Forms
Excipient information presented when available (limited, particularly for generics); consult specific product labeling.
Injection, solution: 250 mg/mL (20 mL)
Solution, oral: 1.25 g/5 mL (237 mL, 473 mL)
Syrup, oral:
Amicar®: 1.25 g/5 mL (473 mL) [raspberry flavor]
Tablet, oral: 500 mg
Amicar®: 500 mg, 1000 mg [scored]
Pricing: U.S. (www.drugstore.com)
Tablets (Amicar)
500 mg (30): $103.39
Tablets (Aminocaproic Acid)
500 mg (100): $186.47
References
Bartholomew JR, Salgia R, and Bell WR, “Control of Bleeding in Patients With Immune and Nonimmune Thrombocytopenia With Aminocaproic Acid,” Arch Intern Med, 1989, 149(9):1959-61.
Casati V, Guzzon D, Oppizzi M, et al, “Hemostatic Effects of Aprotinin, Tranexamic Acid and Epsilon-Aminocaproic Acid in Primary Cardiac Surgery,” Ann Thorac Surg, 1999, 68(6):2252-57.
Chauhan S, Das SN, Bisoi A, et al, “Comparison of Epsilon Aminocaproic Acid and Tranexamic Acid in Pediatric Cardiac Surgery,” J Cardiothorac Vasc Anesth, 2004, 18(2):141-43.
Crouch ER Jr, Williams PB, Gray MK, et al, “Topical Aminocaproic Acid in the Treatment of Traumatic Hyphema,” Arch Ophthalmol, 1997, 115(9):1106-12.
Daily PO, Lamphere JA, Dembitsky WP, et al, “Effect of Prophylactic Epsilon-Aminocaproic Acid on Blood Loss and Transfusion Requirements in Patients Undergoing First-time Coronary Artery Bypass Grafting: A Randomized, Pprospective, Double-Blind Study,” J Thorac Cardiovasc Surg, 1994, 108(1):99-108.
de Peppo A, Pierri MD, Scafuri A, et al, “Intraoperative Antifibrinolysis and Blood-Saving Techniques in Cardiac Surgery: Prospective Trial of 3 Antifibrinolytic Drugs,” Tex Heart Inst J, 1995, 22(3):231-6.
Douketis JD, Berger PB, Dunn AS, et al, “The Perioperative Management of Antithrombotic Therapy: American College of Chest Physicians Evidence-Based Clinical Practice Guidelines (8th Edition),” Chest, 2008, 133(6 Suppl):299-339.
Eagle KA, Guyton RA, Davidoff R, et al, “ACC/AHA 2004 Guideline Update for Coronary Artery Bypass Graft Surgery: A Report of the American College of Cardiology/American Heart Association Task Force on Practice Guidelines (Committee to Update the 1999 Guidelines for Coronary Artery Bypass Graft Surgery),” Circulation, 2004, 110(14):e340-437.
Eaton MP, “Antifibrinolytic Therapy in Surgery for Congenital Heart Disease,” Anest Analg, 2008, 106(4):1087-100.
Eberle B, Mayer E, Hafner G, et al, “High-Dose Epsilon-Aminocaproic Acid Versus Aprotinin: Antifibrinolytic Efficacy in First-Time Coronary Operations,” Ann Thorac Surg, 1998, 65(3):667-73.
Fergusson DA, Hebert PC, Mazer CD, et al, “A Comparison of Aprotinin and Lysine Analogues in High-Risk Cardiac Surgery,” N Engl J Med, 2008, 358(22):2319-31.
Gardner FH and Helmer RE 3rd, “Aminocaproic Acid. Use in Control of Hemorrhage in Patients With Amegakaryocytic Thrombocytopenia,” JAMA, 1980, 243(1):35-7.
Haut MT, Mauro VF, and Davis HH, “Effect of Renal Failure and Hemodialysis on Aminocaproic Acid Plasma Concentrations,” DICP, 1989, 23(11):922-3.
Hirsh J, Guyatt G, Albers GW, et al, “Executive Summary: American College of Chest Physicians Evidence-Based Clinical Practice Guidelines (8th Edition),” Chest, 2008, 133(6 Suppl):71-109.
Kikura M, Levy JH, Tanaka KA, et al, “A Double-Blind, Placebo-Controlled Trial of Epsilon-Aminocaproic Acid for Reducing Blood Loss in Coronary Artery Bypass Grafting Surgery,” J Am Coll Surg, 2006, 202(2):216-22.
Lucas ON and Albert TW, “Epsilon Aminocaproic Acid in Hemophiliacs Undergoing Dental Extractions: A Concise Review,” Oral Surg Oral Med Oral Pathol, 1981, 51(2):115-20.
Mannucci P, “Hemostatic Drugs,” N Engl J Med, 1998, 339(4):245-53.
McGetrick JJ, Jampol LM, Goldberg MP, et al, “Aminocaproic Acid Decreases Secondary Hemorrhage After Traumatic Hyphema,” Arch Ophthalmol, 1983, 101(7):1031-3.
Patatanian E and Fugate SE,, “Hemostatic Mouthwashes in Anticoagulated Patients Undergoing Dental Extraction,” Ann Pharmacother, 2006, 40(12):2205-10.
Pieramici DJ, Goldberg MF, Melia M, et al, “A Phase III, Multicenter, Randomized, Placebo-Controlled Clinical Trial of Topical Aminocaproic Acid (Caprogel) in the Management of Traumatic Hyphema,” Ophthalmology, 2003, 110(11):2106-12.
Pinosky ML, Kennedy DJ, Fishman RL, et al, “Tranexamic Acid Reduces Bleeding After Cardiopulmonary Bypass When Compared to Epsilon Aminocaproic Acid and Placebo,” J Card Surg, 1997, 12(5):330-8.
Sane DC, Califf RM, Topol EJ, et al, " Bleeding During Thrombolytic Therapy for Acute Myocardial Infarction: Mechanisms and Management," Ann Intern Med, 1989, 111(12):1010-22.
Souto JC, Olover A, Zuazu-Jausoro I, et al, “Oral Surgery in Anticoagulated Patients Without Reducing the Dose of Oral Anticoagulant: A Prospective Randomized Study,” J Oral Maxillofac Surg, 1996, 54(1):27-32.
Teboul BK, Jacob JL, Barsoum-Homsy M, et al, “Clinical Evaluation of Aminocaproic Acid for Managing Traumatic Hyphema in Children,” Ophthalmology, 1995, 102(11):1646-53.
Vander Salm TJ, Kaur S, Lancey RA, et al, “Reduction of Bleeding After Heart Operations Through the Prophylactic Use of Epsilon-Aminocaproic Acid,” J Thorac Cardiovasc Surg, 1996, 112(4):1098-107
Walton W, Von Hagen S, Grigorian R, et al, “Management of Traumatic Hyphema,” Surv Ophthalmol, 2002, 47(4):297-334.
Zhang YP and Trissel LA, “Stability of Aminocaproic Acid Injection Admixtures in 5% Dextrose Injection and 0.9% Sodium Chloride Injection,” Int J Pharm Compound, 1997, 1(2):132-4.
International Brand Names
Lexi-Comp.com
Last full review/revision March 2011
Content last modified March 2011
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