Aminocaproic acid

U.S. BRAND NAMES — Amicar®

PHARMACOLOGIC CATEGORY
Hemostatic Agent

DOSING: ADULTS
Acute bleeding syndrome: Oral, I.V.: 4-5 g during the first hour, followed by 1 g/hour for 8 hours or until bleeding controlled (maximum daily dose: 30 g)

Control bleeding in thrombocytopenia (unlabeled use):
Initial: I.V.: 0.1 g/kg over 30-60 minutes
Maintenance: Oral: 1-3 g every 6 hours

Control oral bleeding in congenital and acquired coagulation disorder (unlabeled use): Oral: 50-60 mg/kg every 4 hours

Traumatic hyphema (unlabeled use): Oral: 100 mg/kg/dose every 4 hours (maximum daily dose: 30 g)

DOSING: PEDIATRIC

(For additional information see "Aminocaproic acid: Pediatric drug information")
Acute bleeding syndrome (unlabeled use): Oral, I.V.: 100-200 mg/kg during the first hour, followed by continuous infusion at 33.3 mg/kg/hour or 100 mg/kg (oral or I.V.) every 6 hours

Traumatic hyphema (unlabeled use): Oral: Refer to adult dosing.

DOSING: ELDERLY — Refer to adult dosing.

DOSING: RENAL IMPAIRMENT — May accumulate in patients with decreased renal function.

DOSAGE FORMS — Excipient information presented when available (limited, particularly for generics); consult specific product labeling.

Injection, solution: 250 mg/mL (20 mL)
Amicar®: 250 mg/mL (20 mL) [contains benzyl alcohol]

Solution, oral: 1.25 g/5 mL (240 mL, 480 mL)

Syrup:
Amicar®: 1.25 g/5 mL (480 mL) [raspberry flavor]

Tablet [scored]: 500 mg, 1000 mg
Amicar®: 500 mg, 1000 mg

DOSAGE FORMS: CONCISE
Injection, solution: 250 mg/mL (20 mL)
Amicar®: 250 mg/mL (20 mL)

Solution, oral: 1.25 g/5 mL (480 mL)

Syrup:
Amicar®: 1.25 g/5 mL

Tablet [scored]: 500 mg, 1000 mg
Amicar®: 500 mg, 1000 mg

GENERIC EQUIVALENT AVAILABLE — Yes

ADMINISTRATION — I.V.: May be administered over 30-60 minutes or by continuous infusion; rapid I.V. injection (IVP) should be avoided due to possible hypotension, bradycardia, and arrhythmia.

COMPATIBILITY — Stable in D5W, NS.

Compatibility when admixed: Compatible: Netilmicin.

USE — Treatment of excessive bleeding from fibrinolysis

USE - UNLABELED / INVESTIGATIONAL — Treatment of traumatic hyphema; control bleeding in thrombocytopenia; control oral bleeding in congenital and acquired coagulation disorders

ADVERSE REACTIONS SIGNIFICANT — Frequency not defined.

Cardiovascular: Arrhythmia, bradycardia, hypotension, peripheral ischemia, syncope, thrombosis

Central nervous system: Confusion, delirium, dizziness, fatigue, hallucinations, headache, intracranial hypertension, malaise, seizure, stroke

Dermatologic: Rash, pruritus

Gastrointestinal: Abdominal pain, anorexia, cramps, diarrhea, GI irritation, nausea

Genitourinary: Dry ejaculation

Hematologic: Agranulocytosis, bleeding time increased, leukopenia, thrombocytopenia

Neuromuscular & skeletal: CPK increased, myalgia, myositis, myopathy, rhabdomyolysis (rare), weakness

Ophthalmic: Watery eyes, vision decreased

Otic: Tinnitus

Renal: Failure (rare), myoglobinuria (rare)

Respiratory: Dyspnea, nasal congestion, pulmonary embolism

CONTRAINDICATIONS — Hypersensitivity to aminocaproic acid or any component of the formulation; disseminated intravascular coagulation (without heparin); evidence of an intravascular clotting process

WARNINGS / PRECAUTIONS — Avoid rapid I.V. administration; may induce hypotension, bradycardia, or arrhythmia. Aminocaproic acid may accumulate in patients with decreased renal function. Intrarenal obstruction may occur secondary to glomerular capillary thrombosis or clots in the renal pelvis and ureters. 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. Inhibition of fibrinolysis may promote clotting or thrombosis; more likely due to the presence of DIC. Subsequently, use with great caution in patients with, or at risk for, veno-occlusive disease of the liver. Benzyl alcohol is used as a preservative in the injection, therefore, these products should not be used in the neonate. Do not administer with factor IX complex concentrates or anti-inhibitor coagulant complexes.

DRUG INTERACTIONS — Increased toxic effect with oral contraceptives, estrogens.

PREGNANCY RISK FACTOR — C (show table)

PREGNANCY IMPLICATIONS — Reproductive studies have not been conducted.

LACTATION — Excretion in breast milk unknown/use caution

PRICING — (data from drugstore.com)
Tablets (Amicar)
500 mg (30): $78.37

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

REFERENCE RANGE — Therapeutic concentration: >130 mcg/mL (concentration necessary for inhibition of fibrinolysis)

TOXICOLOGY / OVERDOSE COMPREHENSIVE — Symptoms include acute renal failure, delirium, diarrhea, hepatic necrosis, nausea, seizures, transient hypotension, and thromboembolism. Aminocaproic acid may be removed by hemodialysis.

INTERNATIONAL BRAND NAMES — Acidum e-aminocapronicum (PL); Amicar (AE, BH, CY, EG, IQ, IR, JO, KW, LB, LY, OM, QA, SA, SY, YE, ZA); Caproamin (VE); Caprolisin (IT); Hamostat (IN); Ipsilon (AR, BR, JP, PY, UY); Resplamin (JP); Syrop acidi e-aminocapronici (PL)

MECHANISM OF ACTION — Competitively inhibits activation of plasminogen to plasmin, also, a lesser antiplasmin effect

PHARMACODYNAMICS / KINETICS
Onset of action: ~1-72 hours

Distribution: Widely through intravascular and extravascular compartments
Vd: Oral: 23 L, I.V.: 30 L

Metabolism: Minimally hepatic

Half-life elimination: 2 hours

Time to peak: Oral: Within 2 hours

Excretion: Urine (65% as unchanged drug, 11% as metabolite)

PATIENT INFORMATION — Report any signs of bleeding; change positions slowly to minimize dizziness