Aminocaproic acid (injection)

Aminocaproic acid (injection)
Adult Indications & Dosage
Pediatric Indications & Dosage
Contraindications
Warnings & Precautions
Adverse Reactions
Drug Interactions
Use in Specific Populations
Administration & Monitoring
Overdosage
Pharmacology
Clinical Studies
How Supplied
Images
Patient Counseling Information
Precautions with Alcohol
Brand Names
Look-Alike Names

Editor-In-Chief: C. Michael Gibson, M.S., M.D. [1]; Associate Editor(s)-in-Chief: Alonso Alvarado, M.D. [2]

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Overview

Aminocaproic acid (injection) is a hemostatic that is FDA approved for the treatment of acute bleeding syndromes due to elevated fibrinolytic activity. Common adverse reactions include abdominal pain, nausea, vomiting, diarrhea, headache dizziness, confusion, hallucinations, blurred vision, tinnitus.

Adult Indications and Dosage

FDA-Labeled Indications and Dosage (Adult)

Acute Bleeding Syndromes due to Elevated Fibrinolytic Activity

Dosing Information

Oral administration

• An identical dosage regimen may be followed by administering aminocaproic acid tablets or aminocaproic acid oral solution as follows:

• For the treatment of acute bleeding syndromes due to elevated fibrinolytic activity, it is suggested that 5 aminocaproic acid 1000 mg tablets or 10 aminocaproic acid 500 mg tablets (5 g) or 20 milliliter of aminocaproic acid oral Solution (5 g) be administered during the first hour of treatment, followed by a continuing rate of 1 aminocaproic acid 1000 mg tablet or 2 aminocaproic acid 500 mg tablets (1 g) or 5 milliliter of aminocaproic acid oral solution (1.25 g) per hour. This method of treatment would ordinarily be continued for about 8 hours or until the bleeding situation has been controlled.

IV administration

• Aminocaproic acid injection is administered by infusion, utilizing the usual compatible intravenous vehicles (e.g., Sterile Water for Injection, Sodium Chloride Injection 0.9%, Dextrose Injection 5% or Ringer’s Injection). Although Sterile Water for Injection is compatible for intravenous injection, the resultant solution is hypo-osmolar. Rapid injection of aminocaproic acid injection undiluted into a vein is not recommended.
• For the treatment of acute bleeding syndromes due to elevated fibrinolytic activity, it is suggested that 16 to 20 mL (4 to 5 g) of aminocaproic acid injection in 250 mL of diluent be administered by infusion during the first hour of treatment, followed by a continuing infusion at the rate of 4 mL (1 g) per hour in 50 mL of diluent. This method of treatment would ordinarily be continued for about 8 hours or until the bleeding situation has been controlled. * Parenteral drug products should be inspected visually for particulate matter and discoloration prior to administration, whenever solution and container permit.

Off-Label Use and Dosage (Adult)

Guideline-Supported Use

Condition 1

• Developed by: (Organisation)

• Class of Recommendation: (Class) (Link)

• Strength of Evidence: (Category A/B/C) (Link)

• Dosing Information/Recommendation

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Condition 2

• Developed by: (Organisation)

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Non–Guideline-Supported Use

Intraocular Hemorrhage

• Dosing Information

• 100 mg/kg PO q4h.

Postoperative Hemorrhage Prophylaxis

• Dosing Information

• Administer 3 boluses (10 gram each) of epsilon-aminocaproic acid (EACA) diluted in saline solution 0.9% (total volume 40mL) after anesthesia induction, administration of protamine and administration of heparin in the pump.

Dental Procedure Hemorrhage Prophylaxis and Treatment in Hemophilic Patients

• Dosing information

• 100 mg/kg 4 to 6 hours after surgery PO to a maximum dose of 6 g q6h.

Pediatric Indications and Dosage

FDA-Labeled Indications and Dosage (Pediatric)

There is limited information regarding Aminocaproic acid (injection) FDA-Labeled Indications and Dosage (Pediatric) in the drug label.

Off-Label Use and Dosage (Pediatric)

Guideline-Supported Use

There is limited information regarding Off-Label Guideline-Supported Use of Aminocaproic acid in pediatric patients.

Non–Guideline-Supported Use

Post-Surgery Intraocular Hemorrhage

• Dosing Information

• 5 g 60 minutes before surgery, then 5 g q6h.

Contraindications

Aminocaproic acid should not be used when there is evidence of an active intravascular clotting process.

When there is uncertainty as to whether the cause of bleeding is primary fibrinolysis or disseminated intravascular coagulation (DIC), this distinction must be made before administering aminocaproic acid.

The following tests can be applied to differentiate the two conditions:

• Platelet count is usually decreased in DIC but normal in primary fibrinolysis.
• Protamine paracoagulation test is positive in DIC; a precipitate forms when protamine sulfate is dropped into citrated plasma. The test is negative in the presence of primary fibrinolysis.
• The euglobulin clot Iysis test is abnormal in primary fibrinolysis but normal in DIC.

AMICAR must not be used in the presence of DIC without concomitant heparin.

Warnings

In patients with upper urinary tract bleeding, aminocaproic acid administration has been known to cause intrarenal obstruction in the form of glomerular capillary thrombosis or clots in the renal pelvis and ureters. For this reason, aminocaproic acid should not be used in hematuria of upper urinary tract origin, unless the possible benefits outweigh the risk.

Subendocardial hemorrhages have been observed in dogs given intravenous infusions of 0.2 times the maximum human therapeutic dose of aminocaproic acid and in monkeys given 8 times the maximum human therapeutic dose of aminocaproic acid.

Fatty degeneration of the myocardium has been reported in dogs given intravenous doses of aminocaproic acid at 0.8 to 3.3 times the maximum human therapeutic dose and in monkeys given intravenous doses of aminocaproic acid at 6 times the maximum human therapeutic dose.

Rarely, skeletal muscle weakness with necrosis of muscle fibers has been reported following prolonged administration. Clinical presentation may range from mild myalgias with weakness and fatigue to a severe proximal myopathy with rhabdomyolysis, myoglobinuria, and acute renal failure. Muscle enzymes, especially creatine phosphokinase (CPK) are elevated. CPK levels should be monitored in patients on long-term therapy. Aminocaproic acid administration should be stopped if a rise in CPK is noted. Resolution follows discontinuation of aminocaproic acid; however, the syndrome may recur if aminocaproic acid is restarted.

The possibility of cardiac muscle damage should also be considered when skeletal myopathy occurs. One case of cardiac and hepatic lesions observed in man has been reported. The patient received 2 g of aminocaproic acid every 6 hours for a total dose of 26 g. Death was due to continued cerebrovascular hemorrhage. Necrotic changes in the heart and liver were noted at autopsy.

Precautions

General

Aminocaproic acid inhibits both the action of plasminogen activators and to a lesser degree, plasmin activity. The drug should not be administered without a definite diagnosis and/or laboratory finding indicative of hyperfibrinolysis (hyperplasminemia). Inhibition of fibrinolysis by aminocaproic acid may theoretically result in clotting or thrombosis. However, there is no definite evidence that administration of aminocaproic acid has been responsible for the few reported cases of intravascular clotting which followed this treatment. Rather, it appears that such intravascular clotting was most likely due to the patient's preexisting clinical condition, e.g., the presence of DIC. It has been postulated that extravascular clots formed in vivo may not undergo spontaneous Iysis as do normal clots.

Reports have appeared in the literature of an increased incidence of certain neurological deficits such as hydrocephalus, cerebral ischemia, or cerebral vasospasm associated with the use of antifibrinolytic agents in the treatment of subarachnoid hemorrhage (SAH). All of these events have also been described as part of the natural course of SAH, or as a consequence of diagnostic procedures such as angiography. Drug relatedness remains unclear.

Aminocaproic acid should not be administered with Factor IX Complex concentrates or Anti-Inhibitor Coagulant concentrates, as the risk of thrombosis may be increased.

Laboratory Tests

The use of aminocaproic acid should be accompanied by tests designed to determine the amount of fibrinolysis present. There are presently available: (a) general tests such as those for the determination of the Iysis of a clot of blood or plasma; and (b) more specific tests for the study of various phases of the fibrinolytic mechanisms. These latter tests include both semiquantitative and quantitative techniques for the determination of profibrinolysin, fibrinolysin, and antifibrinolysin.

Laboratory Test Interactions

• Prolongation of the template bleeding time has been reported during continuous intravenous infusion of aminocaproic acid at dosages exceeding 24 g/day.
• Platelet function studies in these patients have not demonstrated any significant platelet dysfunction. However, in vitro studies have shown that at high concentrations (7.4 mMol/L or 0.97 mg/mL and greater) aminocaproic acid inhibits ADP and collagen-induced platelet aggregation, the release of ATP and serotonin, and the binding of fibrinogen to the platelets in a concentration-response manner.
• Following a 10 g bolus of aminocaproic acid, transient peak plasma concentrations of 4.6 mMol/L or 0.60 mg/mL have been obtained. The concentration of aminocaproic acid necessary to maintain inhibition of fibrinolysis is 0.99 mMol/L or 0.13 mg/mL. Administration of a 5 g bolus followed by 1 to 1.25 g/hr should achieve and sustain plasma levels of 0.13 mg/mL.
• Concentrations which have been obtained in vivo clinically in patients with normal renal function are considerably lower than the in vitro concentrations found to induce abnormalities in platelet function tests.

Adverse Reactions

Clinical Trials Experience

Aminocaproic acid is generally well tolerated. The following adverse experiences have been reported:

• General: Edema, headache, malaise.
• Hypersensitivity Reactions: Allergic and anaphylactoid reactions, anaphylaxis.
• Cardiovascular: Bradycardia, hypotension, peripheral ischemia, thrombosis.
• Gastrointestinal: Abdominal pain, diarrhea, nausea, vomiting.
• Hematologic: Agranulocytosis, coagulation disorder,leukopenia, thrombocytopenia.
• Musculoskeletal: CPK increased, muscle weakness, myalgia, myopathy (see WARNINGS), myositis, rhabdomyolysis.
• Neurologic: Confusion, convulsions, delirium, dizziness, hallucinations,intracranial hypertension, stroke, syncope.
• Respiratory: Dyspnea, nasal congestion, pulmonary embolism.
• Skin: Pruritis, rash.
• Special Senses: Tinnitus, vision decreased, watery eyes.
• Urogenital: BUN increased, renal failure. There have been some reports of dry ejaculation during the period of AMICAR treatment. These have been reported to date only in hemophilia patients who received the drug after undergoing dental surgical procedures. However, this symptom resolved in all patients within 24 to 48 hours of completion of therapy.

Postmarketing Experience

There is limited information regarding Aminocaproic acid (injection) Postmarketing Experience in the drug label.

Drug Interactions

There is limited information regarding Aminocaproic acid (injection) Drug Interactions in the drug label.

Use in Specific Populations

Pregnancy

Pregnancy Category (FDA): C Animal reproduction studies have not been conducted with aminocaproic acid. It is also not known whether aminocaproic acid can cause fetal harm when administered to a pregnant woman or can affect reproduction capacity. Aminocaproic acid should be given to a pregnant woman only if clearly needed.
Pregnancy Category (AUS): There is no Australian Drug Evaluation Committee (ADEC) guidance on usage of Aminocaproic acid (injection) in women who are pregnant.

Labor and Delivery

There is no FDA guidance on use of Aminocaproic acid (injection) during labor and delivery.

Nursing Mothers

It is not known whether this drug is excreted in human milk. Because many drugs are excreted in human milk, caution should be exercised when AMICAR is administered to a nursing woman.

Pediatric Use

Safety and effectiveness in pediatric patients have not been established.

Geriatic Use

There is no FDA guidance on the use of Aminocaproic acid (injection) in geriatric settings.

Gender

There is no FDA guidance on the use of Aminocaproic acid (injection) with respect to specific gender populations.

Race

There is no FDA guidance on the use of Aminocaproic acid (injection) with respect to specific racial populations.

Renal Impairment

Higher plasma concentrations of aminocaproic acid may occur in patients with severe renal failure.

Hepatic Impairment

There is no FDA guidance on the use of Aminocaproic acid (injection) in patients with hepatic impairment.

Females of Reproductive Potential and Males

There is no FDA guidance on the use of Aminocaproic acid (injection) in women of reproductive potentials and males.

Immunocompromised Patients

There is no FDA guidance one the use of Aminocaproic acid (injection) in patients who are immunocompromised.

Administration and Monitoring

Administration

(Oral/Intravenous/etc)

Monitoring

Condition 1

(Description regarding monitoring, from Warnings section)

Condition 2

(Description regarding monitoring, from Warnings section)

Condition 3

(Description regarding monitoring, from Warnings section)

IV Compatibility

Solution

Compatible

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Not Tested

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Variable

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Incompatible

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Y-Site

Compatible

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Not Tested

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Variable

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Incompatible

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Admixture

Compatible

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Not Tested

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Variable

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Incompatible

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Syringe

Compatible

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Not Tested

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Variable

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Incompatible

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TPN/TNA

Compatible

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Not Tested

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Variable

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Incompatible

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Overdosage

Acute Overdose

Signs and Symptoms

(Description)

Management

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Chronic Overdose

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Pharmacology

Aminocaproic acid (injection)
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Mechanism of Action

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Clinical Studies

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How Supplied

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Storage

There is limited information regarding Aminocaproic acid (injection) Storage in the drug label.

Images

Drug Images

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Patient Counseling Information

(Patient Counseling Information)

Precautions with Alcohol

Alcohol-Aminocaproic acid interaction has not been established. Talk to your doctor about the effects of taking alcohol with this medication.

Brand Names

There is limited information regarding Aminocaproic acid (injection) Brand Names in the drug label.

Look-Alike Drug Names

• (Paired Confused Name 1a) — (Paired Confused Name 1b)
• (Paired Confused Name 2a) — (Paired Confused Name 2b)
• (Paired Confused Name 3a) — (Paired Confused Name 3b)

Drug Shortage Status

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References

The contents of this FDA label are provided by the National Library of Medicine.