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Medication Safety Issues
Sound-alike/look-alike issues:
Amicar® may be confused with amikacin, Amikin®, Omacor®
Pronunciation
(a mee noe ka PROE ik AS id)
U.S. Brand Names
Index Terms
Generic Available
Yes
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 (Oral): 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
Take oral medication exactly as directed. This medication may cause dizziness and fatigue (use caution when driving or engaging in tasks that require alertness until response to drug is known); hypotension (use caution when rising from a lying or sitting position or climbing stairs); menstrual irregularities, increased body hair, or sexual dysfunction (should reverse when treatment is completed); or nausea or vomiting (small frequent meals, frequent mouth care, sucking lozenges, or chewing gum may help). Report immediately any chest pain; dyspnea; swelling; nosebleed; warmth, swelling, pain, or redness in calves; skin rash; muscle pain or weakness; ringing in ears; or acute abdominal cramping. Pregnancy/breast-feeding precautions: Inform prescriber if you are or intend to become pregnant. Consult prescriber if breast-feeding.
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 laboratory results on a regular basis during therapy. Monitor (teach patient to monitor and report) signs of adverse reactions (eg, bleeding, clotting, thromboembolism, hypotension, or CNS changes).
Oncology: Emetic Potential
Very low (<10%)
Oncology: Vesicant
No
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 (240 mL, 480 mL)
Syrup:
Amicar®: 1.25 g/5 mL (480 mL) [raspberry flavor]
Tablet [scored]: 500 mg
Amicar®: 500 mg, 1000 mg
Pricing: U.S. (www.drugstore.com)
Tablets (Amicar)
500 mg (30): $103.40
Tablets (Aminocaproic Acid)
500 mg (100): $177.59
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.
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.
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 September 2009
Content last modified September 2009
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