General Articles

Aminocaproic acid

MEDICATION SAFETY ISSUES
Sound-alike/look-alike issues:
Amicar® may be confused with amikacin, Amikin®, Omacor®

U.S. BRAND NAMES — Amicar®

PHARMACOLOGIC CATEGORY
Antifibrinolytic Agent
Antihemophilic Agent
Hemostatic Agent
Lysine Analog

DOSING: ADULTS
Acute bleeding syndrome: Oral, I.V.: Loading dose: 4-5 g during the first hour, followed by 1 g/hour for 8 hours (or 1.25 g/hour using oral solution) or until bleeding controlled (maximum daily dose: 30 g)

Control of bleeding in thrombocytopenia (unlabeled use):
Initial: I.V.: 100 mg/kg over 30-60 minutes
Maintenance: Oral: 1-3 g every 6 hours

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

Prevention of dental procedure bleeding in patients on oral anticoagulant therapy (unlabeled use): Oral rinse: Hold 4 g/10 mL in mouth for 2 minutes then spit out. Repeat every 6 hours for 2 days after procedure (Souto, 1996). Concentration and frequency may vary by institution and product availability.

Prevention of perioperative bleeding associated with cardiac surgery (unlabeled use): I.V.: 10 g over 20-30 minutes prior to skin incision, followed by 1-2.5 g/hour (usual dose 2 g/hour) until the end of operation (may continue infusion for 4 hours after protamine reversal of heparin). May add 10 g to cardiopulmonary bypass circuit priming solution.
or
10 g over 20-30 minutes prior to skin incision, followed by 10 g after heparin administration then 10 g at discontinuation of cardiopulmonary bypass prior to protamine reversal of heparin

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.: Loading dose: 100-200 mg/kg during the first hour, followed by continuous infusion at 33.3 mg/kg/hour (I.V.) or 100 mg/kg (oral or I.V.) every 6 hours

Prevention of perioperative bleeding associated with cardiac surgery (unlabeled use): I.V.: 100 mg/kg given over 20-30 minutes after induction and prior to incision, 100 mg/kg during cardiopulmonary bypass, and 100 mg/kg after protamine reversal of heparin

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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)

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
Amicar®: 500 mg, 1000 mg

DOSAGE FORMS: CONCISE
Injection, solution: 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
Amicar®: 500 mg, 1000 mg

GENERIC EQUIVALENT AVAILABLE — Yes

ADMINISTRATION — Rapid I.V. injection (IVP) of undiluted solution is not recommended due to possible hypotension, bradycardia, and arrhythmia.

I.V.: Acute bleeding syndrome: Administer loading dose over 1 hour, followed by a continuous infusion

I.V.: Prevention of perioperative bleeding associated with cardiac surgery (unlabeled use): Administer loading dose over 20-30 minutes prior to skin incision, followed by a continuous infusion until the end of operation or as 2 additional bolus doses (over 20-30 minutes) given after heparin administration and at discontinuation of cardiopulmonary bypass prior to protamine reversal of heparin.

COMPATIBILITY — Stable in D5W, NS, Ringer’s injection

USE — To enhance hemostasis when fibrinolysis contributes to bleeding (causes may include cardiac surgery, hematologic disorders, neoplastic disorders, abruption placentae, hepatic cirrhosis, and urinary fibrinolysis)

USE – UNLABELED / INVESTIGATIONAL — Treatment of traumatic hyphema; control bleeding in thrombocytopenia; control oral bleeding in congenital and acquired coagulation disorders; topical treatment (mouth rinse) of bleeding associated with dental procedures in patients on oral anticoagulant therapy; prevention of perioperative bleeding associated with cardiac surgery

ADVERSE REACTIONS SIGNIFICANT — Frequency not defined.

Cardiovascular: Arrhythmia, bradycardia, edema, hypotension, intracranial hypertension, peripheral ischemia, syncope, thrombosis

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

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Dermatologic: Rash, pruritus

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

Genitourinary: Dry ejaculation

Hematologic: Agranulocytosis, bleeding time increased, leukopenia, thrombocytopenia

Local: Injection site necrosis, injection site pain, injectionsite reactions

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

Ophthalmic: Vision decreased, watery eyes

Otic: Tinnitus

Renal: BUN increased, intrarenal obstruction (glomerular capillary thrombosis), myoglobinuria (rare), renal failure (rare)

Respiratory: Dyspnea, nasal congestion, pulmonary embolism

Miscellaneous: Allergic reaction, anaphylactoid reaction, anaphylaxis

Postmarketing and/or case reports: Hepatic lesion, myocardial lesion

CONTRAINDICATIONS — Disseminated intravascular coagulation (without heparin); evidence of an active intravascular clotting process

WARNINGS / PRECAUTIONS
Concerns related to adverse effects: 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. Skeletal muscle weakness: Ranging from mild myalgias and fatigue to severe myopathy with rhabdomyolysis and acute renal failure has been reported with prolonged use. Monitor CPK; discontinue treatment with a rise in CPK.

Disease-related concerns: Renal impairment: Use with caution in patients with renal impairment; may accumulate.

Concurrent drug therapy issues: Blood products: Do not administer with factor IX complex concentrates or anti-inhibitor coagulant complexes; may increase risk for thrombosis.

Dosage form specific issues: Benzyl alcohol: Injection contains benzyl alcohol which has been associated with “gasping syndrome” in neonates.

Other warnings/precautions: Appropriate use: 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. I.V. administration: Avoid rapid I.V. administration; may induce hypotension, bradycardia, or arrhythmia; rapid injection of undiluted solution is not recommended.

DRUG INTERACTIONS
Anti-inhibitor Coagulant Complex: Antifibrinolytic Agents may enhance the thrombogenic effect of Anti-inhibitor Coagulant Complex. Risk X: Avoid combination

Factor IX: Aminocaproic Acid may enhance the adverse/toxic effect of Factor IX. Specifically, use of this combination may increase the risk of thrombosis. Risk X: Avoid combination

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Factor IX Complex (Human): Aminocaproic Acid may enhance the adverse/toxic effect of Factor IX Complex (Human). Specifically, use of this combination may increase the risk of thrombosis. Risk X: Avoid combination

Fibrinogen Concentrate (Human): Antifibrinoly

tic Agents may enhance the adverse/toxic effect of Fibrinogen Concentrate (Human). Specifically, the risk for thrombosis may be increased. Fibrinogen Concentrate (Human) may enhance the adverse/toxic effect of Antifibrinolytic Agents. Specifically, the risk for thrombosis may be increased. Risk C: Monitor therapy

Tretinoin (Oral): May enhance the thrombogenic effect of Antifibrinolytic Agents. Risk C: Monitor therapy

PREGNANCY RISK FACTOR — C (show table)

PREGNANCY IMPLICATIONS — Animal reproductive studies have not been conducted.

LACTATION — Excretion in breast milk unknown/use caution

PRICING — (data from drugstore.com)
Tablets (Amicar)
500 mg (30): $103.40

Tablets (Aminocaproic Acid)
500 mg (100): $177.59

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

INTERNATIONAL BRAND NAMES — Acepramin (HU); Acidum e-aminocapronicum (PL); Amicar (AE, AU, BH, CY, EG, IL, IQ, IR, JO, KW, LB, LY, OM, QA, SA, SY, YE, ZA); Caproamin (ES, VE); Caproamin Fides (ES); Caprolest (NL); Caprolisin (IT); EAC (DE); Epsamon (CH); Epsicaprom (PT); Epsilon (FI); Hamostat (IN); Hemocaprol (ES); Hexalense (FR); Ipron (TW); Ipsilon (AR, BR, JP, PY, UY); Resplamin (JP); Syrop acidi e-aminocapronici (PL)

MECHANISM OF ACTION — Binds competitively to plasminogen; blocking the binding of plasminogen to fibrin and the subsequent conversion to plasmin, resulting in inhibition of fibrin degradation (fibrinolysis).

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


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