Aminocaproic Acid (Monograph)

Drug class: Hemostatics

Medically reviewed by Drugs.com on Dec 10, 2024. Written by ASHP.

Introduction

Antifibrinolytic agent; synthetic lysine analog.

Uses for Aminocaproic Acid

Treatment of Bleeding Due to Elevated Fibrinolytic Activity

Used for management of acute bleeding disorders due to elevated fibrinolytic activity. In life-threatening situations, transfusion of appropriate blood products and other emergency measures may be required.

Manufacturers state that aminocaproic acid should be used only after hyperfibrinolysis has been confirmed with a definite diagnosis and/or laboratory studies.

Situations associated with fibrinolytic bleeding in which aminocaproic acid may be used include bleeding associated with heart surgery (with or without cardiac bypass procedures) and portacaval shunt; carcinoma of the lung, prostate, cervix, or stomach; abruptio placentae; hepatic cirrhosis; and hematologic disorders such as amegakaryocytic thrombocytopenia accompanying aplastic anemia (reduces the need for platelet transfusions).

Patients with hepatic cirrhosis may experience bleeding from hyperfibrinolytic activity. American Gastroenterology Association (AGA) states that antifibrinolytic therapy such as aminocaproic acid may be considered in those with persistent bleeding from mucosal oozing or puncture wound bleeding consistent with impaired clot integrity.

Also has been used in situations where urinary fibrinolysis contributes to excessive urinary tract fibrinolytic bleeding associated with surgical hematuria such as that following prostatectomy and nephrectomy, or nonsurgical hematuria accompanying polycystic or neoplastic disease of the genitourinary tract.

Hyphema

Has been used orally or topically (applied directly to the eye) for the prevention of secondary ocular hemorrhage in patients with nonperforating traumatic hyphema^{† [off-label]}. Designated an orphan drug by FDA for topical treatment of traumatic hyphema.

A 2023 Cochrane review found no good evidence to support use of antifibrinolytic agents in traumatic hyphema other than possibly to reduce the rate of secondary hemorrhage.

Prevention of Perioperative Bleeding

Has been used for prophylaxis of postoperative bleeding^{† [off-label]}.

Antifibrinolytics (aminocaproic acid and tranexamic acid) are commonly used as a blood conservation approach during cardiac surgery and have been shown to reduce bleeding and transfusion rates.

Antifibrinolytics also have been used to inhibit fibrinolysis during liver transplantation; however, there is much less evidence with aminocaproic acid than tranexamic acid in this setting.

Prevention of Bleeding During Dental Procedures

Antifibrinolytic agents such as aminocaproic acid are commonly used to prevent excessive bleeding following minor oral surgery and dental extractions in patients with inherited bleeding disorders (e.g., hemophilia, von Willebrand disease)^{† [off-label]}.

The Medical and Scientific Advisory Council (MASAC) of the National Hemophilia Foundation recommends the use of antifibrinolytic agents (e.g., aminocaproic acid, tranexamic acid) as adjunctive treatment of mouth or other mucosal bleeding in patients with hemophilia or von Willebrand disease.

Hereditary Angioedema

Antifibrinolytics such as aminocaproic acid have been used for long-term prophylaxis in patients with hereditary angioedema (HAE)^{† [off-label]} due to a deficiency of complement 1 (C1)-esterase inhibitor. Considered second-line therapy for this use.

Hereditary Hemorrhagic Telangiectasia

Has been used orally for the management of hereditary hemorrhagic telangiectasia^{† [off-label]}. However, oral tranexamic acid is recommended in current expert guidelines for the management of epistaxis in patients with hereditary hemorrhagic telangiectasia.

Aminocaproic Acid Dosage and Administration

General

Pretreatment Screening

• Perform appropriate testing to determine the amount of fibrinolysis present.

Patient Monitoring

• Monitor creatine kinase (CK, creatine phosphokinase, CPK) levels in patients on long-term therapy.

Administration

Administer orally or by IV infusion.

Oral Administration

Administer orally (as tablets or oral solution) if the patient is able to take oral medication.

IV Administration

Administer by IV infusion after dilution.

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

Dilution

For the initial infusion to be administered during the first hour of treatment, manufacturer suggests that 4–5 g of aminocaproic acid (16–20 mL of the injection concentrate) be added to 250 mL of diluent.

For maintenance infusions, add 1 g of aminocaproic acid (4 mL of the injection concentrate) to 50 mL of diluent.

Compatible with the following solutions: sterile water for injection, 0.9% sodium chloride injection, 5% dextrose injection, and Ringer's injection. Although the injection is compatible with sterile water for injection, resultant solutions are hypo-osmolar.

Standardize for Safety

Standardized concentrations for IV aminocaproic acid have been established through Standardize 4 Safety (S4S), a national patient safety initiative to reduce medication errors, especially during transitions of care. Because recommendations from the S4S panels may differ from the manufacturer’s prescribing information, caution is advised when using concentrations that differ from labeling, particularly when using rate information from the label. For additional information on S4S, see [Web].

Dosage

Pediatric Patients

Bleeding Due to Elevated Fibrinolytic Activity

Oral or IV

Although safety and efficacy in children not established, the drug has been used as a hemostatic agent in pediatric patients^† at an IV or oral loading dose of 100–200 mg/kg, followed by a maintenance dosage of 100 mg/kg per dose every 4 to 6 hours (maximum dose of 30 g/24 hour). .

Hereditary Angioedema

Oral

In pediatric patients requiring long-term prophylaxis for hereditary angioedema^†, aminocaproic acid has been administered at a dosage of 0.05 g/kg orally twice a day (with dosage ranging from 0.025 g/kg twice a day to 0.1 g/kg twice a day).

Adults

Bleeding Due to Elevated Fibrinolytic Activity

Oral

5 g (as tablets or oral solution) during the first hour, then 1 g (as oral tablets) or 1.25 g (as oral solution) per hour for about 8 hours or until bleeding has been controlled.

IV

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

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

Hyphema†

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; lower daily dosages also may be effective.

Prevention of Perioperative Bleeding

IV

For prevention of bleeding during cardiac surgery^†, aminocaproic acid has been administered IV as a loading dose of 1–15 g at induction of anesthesia, followed by a maintenance dosage of 1–2 g/hour during surgery. In another study in patients undergoing cardiac surgery, aminocaproic acid was administered as a bolus loading dose of 150 mg/kg followed by a maintenance infusion of 15 mg/kg/hour. The drug was administered following anesthetic induction.

Prevention of Bleeding During Dental Procedures

Oral or IV

For the treatment of mouth or other mucosal bleeds in individuals with hemophilia or von Willebrand disease^†, an oral aminocaproic acid dose of 50 to 100 mg/kg has been administered. A dose of factor concentrate must be administered first to form the clot, followed by aminocaproic acid given every 6 hours to preserve the clot until healing occurs in about 10 to 14 days. Aminocaproic acid also may be administered IV following dental (e.g., wisdom tooth extraction) or ENT (e.g., tonsillectomy) surgery.

Hereditary Angioedema

Oral

For long-term prophylaxis in adults with hereditary angioedema^†, aminocaproic acid has been administered at a dosage of 2 g orally 3 times a day (with dosage ranging from 1 g twice a day to 4 g 3 times a day).

Hereditary Hemorrhagic Telangiectasia†

Oral

1 or 1.5 g twice daily for 1–2 months, followed by 1–2 g daily has been used.

Cautions for Aminocaproic Acid

Contraindications

• Active intravascular clotting process.

• 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. Do not use without concomitant heparin therapy in patients with evidence of DIC.

Warnings/Precautions

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 who received aminocaproic acid. Do not use in patients with hematuria of upper urinary tract origin unless the potential benefits outweigh risks.

Musculoskeletal Effects

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

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

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

Benzyl Alcohol in Neonates

Aminocaproic acid injection contains benzyl alcohol, which has been associated with toxicity (fatalities) in neonates. (See Pediatric Use under Cautions.)

Hyperfibrinolysis

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

Clot Formation

Inhibition of fibrinolysis by aminocaproic acid may theoretically result in clotting or thrombosis; however, there is no definite evidence that the drug is responsible for cases of intravascular clotting that have occurred following administration.

CNS Effects

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

Specific Populations

Pregnancy

Animal reproduction studies have not been conducted with aminocaproic acid. It is not known whether aminocaproic acid can cause fetal harm when administered to a pregnant woman or can affect reproductive capacity. Aminocaproic acid should be given to a pregnant woman only if clearly needed.

Lactation

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

Pediatric Use

Safety and efficacy not established.

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

American Academy of Pediatrics (AAP) states that the presence of small amounts of the preservative in a commercially available injection should not proscribe its use when indicated in neonates.

Common Adverse Effects

Adverse effects have included nausea, vomiting, cramping, abdominal pain, diarrhea, dizziness, malaise, dyspnea, nasal congestion, headache, edema, pruritus.

Drug Interactions

Specific Drugs

Aminocaproic Acid Pharmacokinetics

Absorption

Bioavailability

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

Special Populations

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

Distribution

Extent

After prolonged administration, distributed through extravascular as well as intravascular compartments; penetrates human red blood cells and other body cells.

Not known if aminocaproic acid is distributed into human milk.

Elimination

Metabolism

The major portion of aminocaproic acid is not metabolized.

Elimination Route

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

Half-life

Approximately 2 hours.

Special Populations

Removed by hemodialysis; may be removed by peritoneal dialysis.

Stability

Storage

Oral

Tablets

20–25°C; tight, child-resistant containers. Do not freeze.

Oral Solution

20–25°C; tight, child-resistant containers. Do not freeze.

Parenteral

Injection

20–25°C (excursions permitted to 15–30°C).

Actions

• Synthetic lysine derivative; inhibitor of fibrinolysis.

• Inhibits the activation of plasminogen; also inhibits the action of plasmin. Inhibits binding of plasmin to fibrin by occupying lysine-binding sites of plasminogen.

Advice to Patients

• Advise patients to inform their clinician of existing or contemplated concomitant therapy, including prescription and OTC drugs and dietary or herbal products.

• Advise patients to inform their clinicians if they are or plan to become pregnant or plan to breast-feed.

• Inform patients of other important precautionary information.

Additional Information

The American Society of Health-System Pharmacists, Inc. represents that the information provided in the accompanying monograph was formulated with a reasonable standard of care, and in conformity with professional standards in the field. Readers are advised that decisions regarding use of drugs are complex medical decisions requiring the independent, informed decision of an appropriate health care professional, and that the information contained in the monograph is provided for informational purposes only. The manufacturer’s labeling should be consulted for more detailed information. The American Society of Health-System Pharmacists, Inc. does not endorse or recommend the use of any drug. The information contained in the monograph is not a substitute for medical care.

Preparations

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

Please refer to the ASHP Drug Shortages Resource Center for information on shortages of one or more of these preparations.

* available from one or more manufacturer, distributor, and/or repackager by generic (nonproprietary) name

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