Yes: Injection

Hemostatic Agent

Treatment of excessive bleeding from fibrinolysis

C

Disseminated intravascular coagulation, hematuria of upper urinary tract, use of Factor IX concentrate or Anti-inhibitor coagulant concentrate

Rapid I.V. administration of the undiluted drug is not recommended; aminocaproic acid may accumulate in patients with decreased renal function; do not use in hematuria of upper urinary tract origin unless possible benefits outweigh risks; use with caution in patients with cardiac, renal or hepatic disease; do not administer without a definite diagnosis of laboratory findings indicative of hyperfibrinolysis; use in breast-feeding women is not recommended

1% to 10%:

Cardiovascular: Hypotension, bradycardia, arrhythmia

Central nervous system: Dizziness, headache, malaise, fatigue

Dermatologic: Rash

Gastrointestinal: GI irritation, nausea, cramps, diarrhea

Hematologic: Decreased platelet function, elevated serum enzymes

Neuromuscular & skeletal: Myopathy, weakness

Otic: Tinnitus

Respiratory: Nasal congestion

<1%: Convulsions, ejaculation problems, rhabdomyolysis, renal failure

Symptoms of overdose include nausea, diarrhea, delirium, hepatic necrosis, thromboembolism

Increased toxic effect with oral contraceptives, estrogens

Competitively inhibits activation of plasminogen to plasmin, also, a lesser antiplasmin effect

Oral: Peak effect: Within 2 hours; Therapeutic effect: Within 1-72 hours after dose

Distribution: Widely distributes through intravascular and extravascular compartments

Metabolism: Minimal hepatic

Half-life: 1-2 hours

Elimination: 68% to 86% excreted as unchanged drug in urine within 12 hours

In the management of acute bleeding syndromes, oral dosage regimens are the same as the I.V. dosage regimens in adults and children

Acute bleeding syndrome:

Children: Oral, I.V.: 100 mg/kg or 3 g/m² during the first hour, followed by continuous infusion at the rate of 33.3 mg/kg/hour or 1 g/m²/hour; total dosage should not exceed 18 g/m²/24 hours

Traumatic hyphema: Oral: 100 mg/kg/dose every 6-8 hours

Adults:

Oral: For elevated fibrinolytic activity, administer 5 g during first hour, followed by 1-1.25 g/hour for approximately 8 hours or until bleeding stops

I.V.: 4-5 g in 250 mL of diluent during first hour followed by continuous infusion at the rate of 1-1.25 g/hour in 50 mL of diluent, continue for 8 hours or until bleeding stops

Maximum daily dose: Oral, I.V.: 30 g

Dosing adjustment in renal impairment: Oliguria or ESRD: Reduce dose by 15% to 25%

Fibrinogen, fibrin split products, creatine phosphokinase (with long-term therapy)

Therapeutic concentration: >130 mg/mL (concentration necessary for inhibition of fibrinolysis)

potassium, creatine phosphokinase [CPK] (S)

May cause drowsiness

May cause hypotension which may be exacerbated by psychotropics; rarely may cause seizures; use caution with clozapine and bupropion

No information available to require special precautions

No effects or complications reported

Take oral medication exactly as directed. This medication may cause dizziness and fatigue (use caution when driving or engaging in tasks that require alertness until response to drug is known); hypotension (use caution when rising from a lying or sitting position or climbing stairs); menstrual irregularities, increased body hair, or sexual dysfunction (should reverse when treatment is completed); or nausea or vomiting (small frequent meals, frequent mouth care, sucking lozenges, or chewing gum may help). Report immediately chest pain; dyspnea; swelling; nosebleed; warmth, swelling, pain, or redness in calves; skin rash; muscle pain or weakness; ringing in ears; or acute abdominal cramping. Pregnancy/breast-feeding precautions: Inform prescriber if you are or intend to be pregnant. Consult prescriber if breast-feeding.

Administration by infusion using appropriate I.V. solution (dextrose 5% or sodium chloride 0.9%); rapid I.V. injection (IVP) should be avoided since hypotension, bradycardia, and arrhythmia may result. Aminocaproic acid may accumulate in patients with decreased renal function.

Injection: 250 mg/mL (20 mL, 96 mL, 100 mL)

Syrup: 1.25 g/5 mL (480 mL)

Tablet: 500 mg

Korzenik JR, Topazian MD, and White R, "Treatment of Bleeding in Hereditary Hemorrhagic Telangiectasia With Aminocaproic Acid," N Engl J Med, 1994, 331(18):1236.

McGetrick JJ, Jampol LM, Goldberg MP, et al, "Aminocaproic Acid Decreases Secondary Hemorrhage After Traumatic Hyphema," Arch Ophthalmol, 1983, 101(7):1031-3.