Aminocaproic acid (oral)

Aminocaproic acid (oral)
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: Ammu Susheela, M.D. [2]

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Overview

Aminocaproic acid (oral) is a hemostatic agent that is FDA approved for the treatment of surgical complications following heart surgery (with or without cardiac bypass procedures) and portacaval shunt; hematological disorders such as amegakaryocytic thrombocytopenia (accompanying aplastic anemia); acute and life-threatening abruptio placentae; hepatic cirrhosis; and neoplastic disease such as carcinoma of the prostate, lung, stomach, and cervix. 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)

Indication

AMICAR is useful in enhancing hemostasis when fibrinolysis contributes to bleeding. In life-threatening situations, transfusion of appropriate blood products and other emergency measures may be required.

Fibrinolytic bleeding may frequently be associated with surgical complications following heart surgery (with or without cardiac bypass procedures) and portacaval shunt; hematological disorders such as amegakaryocytic thrombocytopenia (accompanying aplastic anemia); acute and life-threatening abruptio placentae; hepatic cirrhosis; and neoplastic disease such as carcinoma of the prostate, lung, stomach, and cervix.

Urinary fibrinolysis, usualIy a normal physiological phenomenon, may contribute to excessive urinary tract fibrinolytic bleeding associated with surgical hematuria (following prostatectomy and nephrectomy) or nonsurgical hematuria (accompanying polycystic or neoplastic diseases of the genitourinary system)

Dosage

An identical dosage regimen may be followed by administering AMICAR Tablets or AMICAR Oral Solution as follows:

For the treatment of acute bleeding syndromes due to elevated fibrinolytic activity, it is suggested that 5 AMICAR 1000 mg Tablets or 10 AMICAR 500 mg Tablets (5 g) or 20 milliliter of AMICAR Oral Solution (5 g) be administered during the first hour of treatment, followed by a continuing rate of 1 AMICAR 1000 mg Tablet or 2 AMICAR 500 mg Tablets (1 g) or 5 milliliter of AMICAR 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.

Off-Label Use and Dosage (Adult)

Guideline-Supported Use

There is limited information regarding Off-Label Guideline-Supported Use of Aminocaproic acid (oral) in adult patients.

Non–Guideline-Supported Use

There is limited information regarding Off-Label Non–Guideline-Supported Use of Aminocaproic acid (oral) in adult patients.

Pediatric Indications and Dosage

FDA-Labeled Indications and Dosage (Pediatric)

There is limited information regarding FDA-Labeled Use of Aminocaproic acid (oral) in pediatric patients.

Off-Label Use and Dosage (Pediatric)

Guideline-Supported Use

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

Non–Guideline-Supported Use

There is limited information regarding Off-Label Non–Guideline-Supported Use of Aminocaproic acid (oral) in pediatric patients.

Contraindications

• AMICAR 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 AMICAR.

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, AMICAR 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, AMICAR 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 AMICAR and in monkeys given 8 times the maximum human therapeutic dose of AMICAR.

Fatty degeneration of the myocardium has been reported in dogs given intravenous doses of AMICAR at 0.8 to 3.3 times the maximum human therapeutic dose and in monkeys given intravenous doses of AMICAR 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. AMICAR administration should be stopped if a rise in CPK is noted. Resolution follows discontinuation of AMICAR; however, the syndrome may recur if AMICAR 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.

Adverse Reactions

Clinical Trials Experience

There is limited information regarding Clinical Trial Experience of Aminocaproic acid (oral) in the drug label.

Postmarketing Experience

AMICAR 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.

Drug Interactions

• Drug

• Description

Use in Specific Populations

Pregnancy

Pregnancy Category (FDA): C

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

Pregnancy Category (AUS):

• Australian Drug Evaluation Committee (ADEC) Pregnancy Category

There is no Australian Drug Evaluation Committee (ADEC) guidance on usage of Aminocaproic acid (oral) in women who are pregnant.

Labor and Delivery

There is no FDA guidance on use of Aminocaproic acid (oral) 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

There is no FDA guidance on the use of Aminocaproic acid (oral) with respect to pediatric patients.

Geriatic Use

There is no FDA guidance on the use of Aminocaproic acid (oral) with respect to geriatric patients.

Gender

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

Race

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

Renal Impairment

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

Hepatic Impairment

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

Females of Reproductive Potential and Males

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

Immunocompromised Patients

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

Administration and Monitoring

Administration

• Oral

Monitoring

Muscle enzymes, especially creatine phosphokinase (CPK) are elevated. CPK levels should be monitored in patients on long-term therapy

IV Compatibility

There is limited information regarding IV Compatibility of Aminocaproic acid (oral) in the drug label.

Overdosage

• A few cases of acute overdosage with AMICAR administered intravenously have been reported. The effects have ranged from no reaction to transient hypotension to severe acute renal failure leading to death. One patient with a history of brain tumor and seizures experienced seizures after receiving an 8 gram bolus injection of AMICAR. The single dose of AMICAR causing symptoms of overdosage or considered to be life-threatening is unknown. Patients have tolerated doses as high as 100 grams while acute renal failure has been reported following a dose of 12 grams.

The intravenous and oral LD50 of AMICAR were 3.0 and 12.0 g/kg, respectively, in the mouse and 3.2 and 16.4 g/kg, respectively, in the rat. An intravenous infusion dose of 2.3 g/kg was lethal in the dog. On intravenous administration, tonic-clonic convulsions were observed in dogs and mice.

No treatment for overdosage is known, although evidence exists that AMICAR is removed by hemodialysis and may be removed by peritoneal dialysis. Pharmacokinetic studies have shown that total body clearance of AMICAR is markedly decreased in patients with severe renal failure.

Pharmacology

There is limited information regarding Aminocaproic acid (oral) Pharmacology in the drug label.

Mechanism of Action

Structure

File:Aminocaproic acid (oral)01.png

This image is provided by the National Library of Medicine.

AMICAR is soluble in water, acid, and alkaline solutions; it is sparingly soluble in methanol and practically insoluble in chloroform.

AMICAR (aminocaproic acid) Oral Solution for oral administration, contains 0.25 g/mL of aminocaproic acid with methylparaben 0.20%, propylparaben 0.05%, edetate disodium 0.30% as preservatives and the following inactive ingredients: sodium saccharin, sorbitol solution, citric acid anhydrous, natural and artificial raspberry flavor and an artificial bitterness modifier.

Each AMICAR (aminocaproic acid) Tablet, for oral administration contains 500 mg or 1000 mg of aminocaproic acid and the following inactive ingredients: povidone, crospovidone, stearic acid, and magnesium stearate.

Pharmacodynamics

There is limited information regarding Pharmacodynamics of Aminocaproic acid (oral) in the drug label.

Pharmacokinetics

The fibrinolysis-inhibitory effects of AMICAR appear to be exerted principally via inhibition of plasminogen activators and to a lesser degree through antiplasmin activity.

In adults, oral absorption appears to be a zero-order process with an absorption rate of 5.2 g/hr. The mean lag time in absorption is 10 minutes. After a single oral dose of 5 g, absorption was complete (F=1). Mean ± SD peak plasma concentrations (164 ± 28 mcg/mL) were reached within 1.2 ± 0.45 hours.

After oral administration, the apparent volume of distribution was estimated to be 23.1 ± 6.6 L (mean ± SD). Correspondingly, the volume of distribution after intravenous administration has been reported to be 30.0 ± 8.2 L. After prolonged administration, AMICAR has been found to distribute throughout extravascular and intravascular compartments of the body, penetrating human red blood cells as well as other tissue cells.

Renal excretion is the primary route of elimination. Sixty-five percent of the dose is recovered in the urine as unchanged drug and 11% of the dose appears as the metabolite adipic acid. Renal clearance (116 mL/min) approximates endogenous creatinine clearance. The total body clearance is 169 mL/min. The terminal elimination half-life for AMICAR is approximately 2 hours.

Nonclinical Toxicology

There is limited information regarding Nonclinical Toxicology of Aminocaproic acid (oral) in the drug label.

Clinical Studies

There is limited information regarding Clinical Studies of Aminocaproic acid (oral) in the drug label.

How Supplied

• AMICAR®

(aminocaproic acid)

AMICAR Oral Solution, 0.25 g/mL

Each mL of raspberry-flavored oral solution contains 0.25 g/mL of aminocaproic acid.

16 Fl. Oz. (473 mL) Bottle – NDC 49411-052-16

Store at 20°-25°C (68°-77°F)[see USP Controlled Room Temperature];Dispense in Tight Containers; Do Not Freeze.

AMICAR 500 mg Tablets

Each round, white tablet, engraved with XP on one side and scored on the other with A to the left of the score and 10 on the right, contains 500 mg of aminocaproic acid.

Bottle of 100 – NDC 49411-050-01

Store at 20°-25°C (68°-77°F)[see USP Controlled Room Temperature];Dispense in Tight Containers; Do Not Freeze.

AMICAR 1000 mg Tablets

Each oblong, white tablet, engraved with XP on one side and scored on the other with A to the left of the score and 20 on the right, contains 1000 mg of aminocaproic acid.

Bottle of 100 – NDC 49411-051-01

Storage

• Store at 20°-25°C (68°-77°F)[see USP Controlled Room Temperature];Dispense in Tight Containers; Do Not Freeze.

Images

Drug Images

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Package and Label Display Panel

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Patient Counseling Information

There is limited information regarding Patient Counseling Information of Aminocaproic acid (oral) in the drug label.

Precautions with Alcohol

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

Brand Names

• AMICAR®

Look-Alike Drug Names

There is limited information regarding Aminocaproic acid (oral) Look-Alike Drug Names in the drug label.

Drug Shortage Status

Price

References

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

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