Generic Name: Aminocaproic Acid
Class: Hemostatics
VA Class: BL300
CAS Number: 60-32-2

Introduction

A synthetic monoamino carboxylic acid that is an inhibitor of fibrinolysis.b

Uses for Amicar

Bleeding Due to Elevated Fibrinolytic Activity

Treatment of excessive bleeding resulting from systemic hyperfibrinolysis and urinary fibrinolysis.b In life-threatening situations, fresh whole blood, fibrinogen infusions, and other emergency measures also may be required.b

Used in systemic hyperfibrinolysis associated with surgical complications following heart surgery (with or without cardiac bypass procedures) and portacaval shunt; in carcinoma of the lung, prostate, cervix, or stomach; in abruptio placentae; and in hematologic disorders such as amegakaryocytic thrombocytopenia accompanying aplastic anemia (reduces the need for platelet transfusions).108 b

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Used in urinary fibrinolysis associated with complications of severe trauma, anoxia, and shock,a and as manifested by surgical hematuria especially following prostatectomy and nephrectomy,b or in nonsurgical hematuria accompanying polycystic or neoplastic disease of the GU tract.b

Used in conjunction with heparin therapy in patients with acute promyelocytic leukemia; initiate therapy when plasma α2-antiplasmin (α2-plasmin inhibitor) levels have decreased to <40% of normal levels.107

Ocular Hemorrhage

Has been used effectively for the prevention of secondary ocular hemorrhage in patients with nonperforating traumatic hyphema.100 101 102 103 104 105 106 Designated an orphan drug by FDA for topical treatment of traumatic hyphema.119

Hereditary Hemorrhagic Telangiectasia

Has been used orally for the management of hereditary hemorrhagic telangiectasia.112

Amicar Dosage and Administration

Administration

Administer orally or by IV infusion.b

Oral Administration

Administer orally if the patient is able to take oral medication.b

IV Administration

For solution and drug compatibility information, see Compatibility under Stability.

Administer by IV infusion.b

Avoid rapid IV administration; hypotension, bradycardia, and/or arrhythmia may result.b

Dilution

For the initial infusion (loading dose), add 4–5 g of aminocaproic acid (16–20 mL of the injection) to 250 mL of diluent.b

For maintenance infusions, add 1 g of aminocaproic acid (4 mL of the injection) to 50 mL of diluent to provide a final concentration of approximately 20 mg/mL.b

Rate of Administration

Initial infusion (loading dose): Infuse 4–5 g over 1 hour in adults.b

Maintenance infusion: Infuse 1 g per hour in adults.b

Dosage

Pediatric Patients

Bleeding Due to Elevated Fibrinolytic Activity
Oral

100 mg/kg or 3 g/m2 during the first hour, then 33.3 mg/kg per hour or 1 g/m2 per hour (maximum 18 g/m2 in 24 hours) has been used.a Manufacturer states that safety and efficacy not established in pediatric patients.b

IV

Initial infusion (loading dose): 100 mg/kg or 3 g/m2 over 1 hour has been used.a Manufacturer states that safety and efficacy not established in pediatric patients.b

Maintenance infusion

Maintenance infusion: 33.3 mg/kg per hour or 1 g/m2 per hour (maximum 18 g/m2 in 24 hours) has been used.a Manufacturer states that safety and efficacy not established in pediatric patients.b

Adults

Bleeding Due to Elevated Fibrinolytic Activity
Oral

5 g during the first hour, then 1–1.25 g per hour for about 8 hours or until bleeding has been controlled.a b

IV

Initial infusion (loading dose): 4–5 g over 1 hour.b

Maintenance infusion: 1 g per hour for about 8 hours or until bleeding has been controlled.b

Ocular Hemorrhage
Oral

100 mg/kg (up to 5 g) every 4 hours, up to a maximum daily dosage of 30 g, for 5 days has been used;100 101 102 103 lower daily dosages also may be effective.102

Hereditary Hemorrhagic Telangiectasia
Oral

1 or 1.5 g twice daily for 1–2 months, followed by 1–2 g daily.112

Prescribing Limits

Pediatric Patients

Bleeding Due to Elevated Fibrinolytic Activity
Oral or IV

Maximum 18 g/m2 in 24 hours.a

Adults

Ocular Hemorrhage
Oral

Maximum 30 g daily.100 101 102 103

Cautions for Amicar

Contraindications

  • Active intravascular clotting process.b

  • When it is not clear whether hemorrhage is secondary to primary fibrinolysis or disseminated intravascular coagulation (DIC), the distinction must be made before aminocaproic acid is administered.b Do not use without concomitant heparin therapy in patients with evidence of DIC.b

Warnings/Precautions

Warnings

Urinary Tract Bleeding

Intrarenal obstruction via glomerular capillary thrombosis or clots in the renal pelvis and ureters reported in patients with upper urinary tract bleeding.b The drug should not be used in patients with hematuria of upper urinary tract origin unless the potential benefits outweigh risks.b

Musculoskeletal Effects

Skeletal muscle weakness with necrosis of muscle fiber reported with prolonged administration.b Presentation may range from mild myalgias with weakness and fatigue to severe proximal myopathy with rhabdomyolysis, myoglobinuria, and renal failure; CK levels are elevated.b Manifestations resolve with drug discontinuance but may recur if therapy is reinstated.b

Monitor CK concentrations with long-term therapy.b Discontinue drug if an increase in CK occurs.b

If skeletal myopathy occurs, consider possibility of cardiac muscle damage.b

Benzyl Alcohol in Neonates

Aminocaproic acid injection contains as a preservative benzyl alcohol, which has been associated with toxicity (fatalities) in neonates.b (See Pediatric Precautions.)

General Precautions

Should be used only in acute, life-threatening situationsa involving hemorrhage resulting from hyperfibrinolysis that has been confirmed by laboratory studies.b

Clot Formation

If aminocaproic acid is present, clots formed in vivo may not undergo spontaneous lysis as do normal clots because aminocaproic acid in the clot may inhibit spontaneous fibrinolysis.b No clear-cut evidence for in vivo drug-induced thrombosis; however, the hazard of this theoretical complication remains a possibility.b

CNS Effects

Neurological deficits (hydrocephalus, cerebral ischemia, cerebral vasospasm) associated with use of antifibrinolytic agents in the management of subarachnoid hemorrhage.b Causal relationship to the drugs not established.b

Specific Populations

Pregnancy

Category C.b

Lactation

Not known if aminocaproic acid is distributed into milk; caution if used in nursing women.b

Pediatric Use

Safety and efficacy not established.b 111

Large amounts of benzyl alcohol (i.e., 100–400 mg/kg daily) have been associated with toxicity (fatal “gasping syndrome”) in neonates (see Warnings); each mL of aminocaproic acid injection in multiple-dose vials contains 9 mg of benzyl alcohol.b

Common Adverse Effects

Nausea,b vomiting,b cramping,a abdominal pain,b diarrhea,b dizziness,b malaise,b fever,a conjunctival suffusion,a dyspnea,b nasal congestion,b headache,b edema,b pruritus,b rash.b

Interactions for Amicar

Specific Drugs

Drug

Interaction

Anti-inhibitor coagulant complex

Increased risk of thrombosisb

Factor IX complex

Increased risk of thrombosisb

Amicar Pharmacokinetics

Absorption

Bioavailability

Rapidly and completely absorbed from the GI tract; peak plasma concentrations are attained within about 1 hour following a 5-g dose.b 111

Special Populations

Plasma concentrations may be higher in patients with severe renal impairment.b

Distribution

Extent

Distributed through extravascular as well as intravascular compartments; penetrates human red blood cells and other body cells.b

Not known if aminocaproic acid is distributed into milk.b

Plasma Protein Binding

Not bound.a

Elimination

Metabolism

The major portion of aminocaproic acid is not metabolized.b 111

Elimination Route

Eliminated principally in urine as unchanged drug (65%) and the adipic acid metabolite (11%).b 111

Half-life

2 hours.b

Special Populations

Removed by hemodialysis; may be removed by peritoneal dialysis.b 111 121

Stability

Storage

Oral

Tablets

15–30°C; tight containers.b

Syrup

15–30°C; tight containers.b Do not freeze.b

Parenteral

Injection

15–30°C.b Do not freeze.b

Compatibility

For information on systemic interactions resulting from concomitant use, see Interactions.

Parenteral

Solution CompatibilityHID

Compatible

Dextrose 5% in water

Sodium chloride 0.9%

Y-Site CompatibilityHID

Compatible

Fenoldopam mesylate

Actions

  • Aminocaproic acid inhibits the activation of plasminogen; also inhibits the action of fibrinolysin (plasmin).b

Advice to Patients

  • Importance of informing clinician of existing or contemplated concomitant therapy, including prescription and OTC drugs and dietary or herbal products.b

  • Importance of women informing clinicians if they are or plan to become pregnant or plan to breast-feed.b

  • Importance of advising patients of other important precautionary information.b (See Cautions.)

Preparations

Excipients in commercially available drug preparations may have clinically important effects in some individuals; consult specific product labeling for details.

Aminocaproic Acid

Routes

Dosage Forms

Strengths

Brand Names

Manufacturer

Oral

Solution

1.25 g/5 mL

Amicar Syrup (with parabens)

Xanodyne

Aminocaproic Acid Syrup

VersaPharm

Tablets

500 mg

Amicar (with povidone; scored)

Xanodyne

Aminocaproic Acid Tablets

VersaPharm

1 g

Amicar (with povidone; scored)

Xanodyne

Parenteral

For injection concentrate, for IV infusion

250 mg/mL (5 g)

Amicar Intravenous (with benzyl alcohol 0.9%)

Xanodyne

Aminocaproic Acid Injection (with benzyl alcohol 0.9%)

American Regent, Hospira

Comparative Pricing

This pricing information is subject to change at the sole discretion of DS Pharmacy. This pricing information was updated 02/2014. Actual costs to patients will vary depending on the use of specific retail or mail-order locations and health insurance copays.

Amicar 500MG Tablets (XANODYNE PHARMACEUTICALS): 30/$103.39 or 90/$285.98

Aminocaproic Acid 500MG Tablets (VERSAPHARM): 100/$195.79 or 300/$566.19

AHFS DI Essentials. © Copyright, 2004-2014, Selected Revisions August 1, 2007. American Society of Health-System Pharmacists, Inc., 7272 Wisconsin Avenue, Bethesda, Maryland 20814.

† Use is not currently included in the labeling approved by the US Food and Drug Administration.

References

Only references cited for selected revisions after 1984 are available electronically.

100. Crouch ER Jr, Frenkel M. Aminocaproic acid in the treatment of traumatic hyphema. Am J Ophthalmol. 1976; 81:355-60. [IDIS 70329] [PubMed 769560]

101. McGetrick JJ, Jampol LM, Goldberg MF et al. Aminocaproic acid decreases secondary hemorrhage after traumatic hyphema. Arch Ophthalmol. 1983; 101:1031-3. [IDIS 172818] [PubMed 6870623]

102. Palmer DJ, Goldberg MF, Frenkel M et al. A comparison of two dose regimens of epsilon aminocaproic acid in the prevention and management of secondary traumatic hyphemas. Ophthalmology. 1986; 93:102-8. [PubMed 3951807]

103. Kutner B, Fourman S, Brein K et al. Aminocaproic acid reduces the risk of secondary hemorrhage in patients with traumatic hyphema. Arch Ophthalmol. 1987; 105:206-8. [IDIS 225461] [PubMed 3813951]

104. Goldfarb MS, Bulas KE, Rosenberg S et al. Aminocaproic acid treatment of recurrent postoperative hyphemas. Ann Ophthalmol. 1984; 16:690,692-3,696-7. [PubMed 6476703]

105. Goldberg MF. Antifibrinolytic agents in the management of traumatic hyphema. Arch Ophthalmol. 1983; 101:1029-30. [PubMed 6347147]

106. Love DC. Treatment of traumatic hyphema. JAMA. 1985; 253:345-6. [IDIS 194852] [PubMed 3965787]

107. Schwartz BS, Williams EC, Conlan MG et al. Epsilon-aminocaproic acid in the treatment of patients with acute promyelocytic leukemia and acquired alpha-2-plasmin inhibitor deficiency. Ann Intern Med. 1986; 105:873-7. [IDIS 223520] [PubMed 3465267]

108. Gardner FH, Helmer RE III. Aminocaproic acid: use in control of hemorrhage in patients with amegakaryocytic thrombocytopenia. JAMA. 1980; 243:35-7. [IDIS 107007] [PubMed 6965311]

109. Kang Y, Lewis JH, Navalgund A et al. Epsilon-aminocaproic acid for the treatment of fibrinolysis during liver transplantation. Anesthesiology. 1987 66:766-73. (IDIS 230629)

110. Immunex Corporation. Amicar (aminocaproic acid) syrup, tablets, and injection prescribing information. Seattle, WA; 1998 Apr 13.

111. Abbott Laboratories. Aminocaproic acid injection prescribing information. Chicago, IL; 1992 May.

112. Saba HI, Morelli GA, Logrono LA. Brief report: treatment of bleeding in hereditary hemorrhagic telangiectasia with aminocaproic acid. N Engl J Med. 1994; 330:1789-90. [IDIS 331546] [PubMed 8190155]

113. Phillips MD. Stopping bleeding in hereditary telangiectasia. N Engl J Med. 1994; 330:1822-3. [IDIS 331549] [PubMed 8190162]

114. American Academy of Pediatrics Committee on Fetus and Newborn and Committee on Drugs. Benzyl alcohol: toxic agent in neonatal units. Pediatrics. 1983; 72:356-8. [IDIS 175725] [PubMed 6889041]

115. Anon. Benzyl alcohol may be toxic to newborns. FDA Drug Bull. 1982; 12(2):10-1. [PubMed 7188569]

116. Gershanik J, Boecler B, Ensley H et al. The gasping syndrome and benzyl alcohol poisoning. N Engl J Med. 1982; 307:1384-8. [IDIS 160823] [PubMed 7133084]

117. Menon PA, Thach BT, Smith CH et al. Benzyl alcohol toxicity in a neonatal intensive care unit: incidence, symptomatology, and mortality. Am J Perinatol. 1984; 1:288-92. [PubMed 6440575]

118. Anderson CW, Ng KJ, Andresen B et al. Benzyl alcohol poisoning in a premature newborn infant. Am J Obstet Gynecol. 1984; 148:344-6. [IDIS 181207] [PubMed 6695984]

119. Food and Drug Administration. Orphan designations pursuant to section 526 of the Federal Food and Cosmetic Act as amended by the Orphan Drug Act (P.L. 97-414) to June 28, 1996. Rockville, MD; 1996 Jul.

120. Food and Drug Administration. Amicar (aminocaproic acid) syrup [September 14, 1999: Immunex]. MedWatch drug labeling changes. Rockville, MD; September 1999. From FDA website ().

121. Food and Drug Administration. Amicar (aminocaproic acid) tablets, injection, syrup [April 16, 1997: Immunex]. MedWatch drug labeling changes. Rockville, MD; April 1997. From FDA website ().

122. Mangano DT, for the Multicenter Study of Perioperative Ischemia Research Group. Aspirin and mortality from coronary bypass surgery. N Engl J Med. 2002; 347:1309-17. [IDIS 488783] [PubMed 12397188]

HID. Trissel LA. Handbook on injectable drugs. 14th ed. Bethesda, MD: American Society of Health-System Pharmacists; 2007:98.

a. AHFS drug information 2006. McEvoy GK, ed. Aminocaproic Acid. Bethesda, MD: American Society of Health-System Pharmacists; 2006:1544-46.

b. Xanodyne Pharmaceuticals. Amicar (aminocaproic acid) injection, syrup, and tablets prescribing information. Florence, KY; 2004 Sep.

c. American Academy of Pediatrics Committee on Fetus and Newborn and Committee on Drugs. Benzyl alcohol: toxic agent in neonatal units. Pediatrics. 1983; 72:356 8. [IDIS 175725] [PubMed 6889041]

d. Anon. Benzyl alcohol may be toxic to newborns. FDA Drug Bull. 1982; 12(2):10 11.

e. Centers for Disease Control. Neonatal deaths associated with use of benzyl alcohol. MMWR. 1982; 31:290 1. [IDIS 150868] [PubMed 6810084]

f. Gershanik J, Boecler B, Ensley H et al. The gasping syndrome and benzyl alcohol poisoning. N Engl J Med. 1982; 307:1384 8. [IDIS 160823] [PubMed 7133084]

g. Menon PA, Thach BT, Smith CH et al. Benzyl alcohol toxicity in a neonatal intensive care unit: incidence, symptomatology, and mortality. Am J Perinatol. 1984; 1:288 92. [PubMed 6440575]

h. Anderson CW, Ng KJ, Andresen B et al. Benzyl alcohol poisoning in a premature newborn infant. Am J Obstet Gynecol. 1984; 148:344 6. [IDIS 181207] [PubMed 6695984]

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