DrugindexOnline^{2nd edition}

Pronouncation: (uh-mee-no-kuh-PRO-ik acid)
Class: Hemostatic

Trade Names:
Amicar
- Tablets 500 mg
- Syrup 250 mg/mL

Trade Names:
Aminocaproic Acid
- Injection 250 mg/mL

Mechanism of Action

Pharmacology

Inhibits fibrinolysis to stop bleeding.

Pharmacokinetics

Absorption

Oral

Zero order process; absorption rate of 5.2 g/h. C _max is about 164 mcg/mL; T _max is about 1.2 h.

Distribution

Oral

Vd is about 23.1 L.

IV

Vd is about 30 L.

Metabolism

Metabolite is adipic acid.

Elimination

Renally eliminated. 65% is recovered in the urine as unchanged drug and 11% as the metabolite adipic acid. Renal clearance is 116 mL/min and total body clearance is 169 mL/min. T _1/2 is about 2 h.

Duration

3 h for single IV dose.

Indications and Usage

Treatment of excessive bleeding from systemic hyperfibrinolysis and urinary fibrinolysis.

Unlabeled Uses

Prevention of recurrence of subarachnoid hemorrhage; management of amegakaryocytic thrombocytopenia; abortion; or prevention of attacks of hereditary angioneurotic edema.

Contraindications

Active intravascular clotting; DIC; administration to newborns.

Dosage and Administration

Adults

IV/PO 4 to 5 g in first hour; then 1 to 1.25 g/h for 8 h or until bleeding is controlled. Dosage over 30 g/24 h is not recommended.

General Advice

IV infusion

• Dilute as 1 g/50 mL diluent. Compatible diluents include Sterile Water for Injection, normal saline, D5W, and Ringer's solution.
• Infuse dose over 30 min to 1 h.

Storage/Stability

Store in tightly closed container at room temperature.

Drug Interactions

Oral contraceptives or estrogens

May lead to increase in clotting factors, producing state of hypercoagulation.

Laboratory Test Interactions

Serum potassium levels

Serum potassium level may be elevated, especially in impaired renal function.

Adverse Reactions

Cardiovascular

Bradycardia; hypotension; peripheral ischemia; thrombosis.

CNS

Dizziness; headache; delirium; hallucinations; confusion; intracranial hypertension; stroke; syncope.

Dermatologic

Rash; pruritus.

EENT

Tinnitus; decreased vision; watery eyes.

GI

Nausea; diarrhea; abdominal pain; vomiting.

Genitourinary

Increased BUN; renal failure.

Hematologic

Agranulocytosis; coagulation disorder; leukopenia; thrombocytopenia.

Respiratory

Dyspnea; nasal congestion; pulmonary embolism.

Miscellaneous

Injection site reaction; pain and necrosis; myalgia; myositis; myopathy (characterized by muscle weakness, fatigue, elevated creatinine phosphokinase, rhabdomyolysis associated with myoglobinuria and renal failure); edema; allergic and anaphylactic reactions; anaphylaxis; malaise.

Precautions

Pregnancy

Category C .

Lactation

Undetermined.

Children

Safety and efficacy not established.

Upper urinary tract bleeding

Not used in treatment of hematuria of upper UT origin unless possible benefits outweigh risks.

Overdosage

Symptoms

Hypotension, severe acute renal failure.

Patient Information

• Caution patient to avoid sudden position changes to prevent orthostatic hypotension.
• Advise patient to use soft toothbrush or sponge for dental care.
• Instruct patient to report the following symptoms to health care provider: gingival bleeding, epistaxis, hematuria, skin changes (eg, ecchymosis, petechiae), difficulty in urination, reddish-brown urine, chest or leg pain, or difficulty breathing.