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Amicar
Classes
Synthetic Antifibrinolytics
Administration
Oral solution: Administer using a calibrated measuring device.
Visually inspect parenteral products for particulate matter and discoloration prior to administration whenever solution and container permit.
Use of an infusion pump is recommended to ensure accurate dosing.
Rapid injection of undiluted drug is NOT recommended. Rapid administration may result in hypotension, bradycardia, and/or arrhythmia.[50659]
Intermittent IV Infusion
Dilute the initial dose (4 to 5 g of aminocaproic acid) in 250 mL of 0.9% Sodium Chloride Injection, 5% Dextrose Injection, or Lactated Ringer's Injection. Although Sterile Water for Injection is compatible, the resultant solution is hypoosmolar.
Administer IV over 1 hour.[50659]
Continuous IV Infusion
After the initial dose, infuse at a rate of 1 g/hour in 50 mL of diluent. This method of treatment is usually continued for 8 hours or until bleeding is controlled.[50659]
NOTE: Aminocaproic acid is not FDA-approved for topical administration.
Pressure packs: Use gauze pressure packs containing aminocaproic acid, or a small piece of oxidized cellulose soaked in approximately 2 molar aminocaproic acid (prepared from the 250 mg/mL parenteral product).
Oral rinse: Rinse with hydrogen peroxide, followed by saline, then rinse with 1.25 g aminocaproic acid oral solution for 30 seconds.
Cotton swabs: For use in unconscious patients or children, apply oral solution with a cotton swab.
Intravesical Administration
NOTE: Aminocaproic Acid is not FDA-approved for intravesical administration.
Administer via a 22F or 24F three-way Foley catheter inserted into the bladder.
Irrigate the bladder with 0.9% Sodium Chloride to remove all clots.
Irrigate bladder continuously with a solution containing 200 mg of aminocaproic acid added to each liter of 0.9% Sodium Chloride, starting in the recovery room at a rate adjusted according to the severity of bleeding. Adjust the rate of irrigation as urine clears, and continue for 24 hours after urine becomes clear.
Adverse Reactions
bradycardia / Rapid / Incidence not known
arrhythmia exacerbation / Early / Incidence not known
increased intracranial pressure / Early / Incidence not known
stroke / Early / Incidence not known
seizures / Delayed / Incidence not known
renal failure (unspecified) / Delayed / Incidence not known
thrombosis / Delayed / Incidence not known
pulmonary embolism / Delayed / Incidence not known
agranulocytosis / Delayed / Incidence not known
rhabdomyolysis / Delayed / Incidence not known
myoglobinuria / Delayed / Incidence not known
visual impairment / Early / Incidence not known
skin necrosis / Early / Incidence not known
anaphylactoid reactions / Rapid / Incidence not known
hypotension / Rapid / Incidence not known
hallucinations / Early / Incidence not known
delirium / Early / Incidence not known
confusion / Early / Incidence not known
ejaculation dysfunction / Delayed / Incidence not known
leukopenia / Delayed / Incidence not known
thrombocytopenia / Delayed / Incidence not known
myopathy / Delayed / Incidence not known
dyspnea / Early / Incidence not known
edema / Delayed / Incidence not known
phlebitis / Rapid / Incidence not known
syncope / Early / Incidence not known
dizziness / Early / Incidence not known
headache / Early / Incidence not known
fatigue / Early / Incidence not known
weakness / Early / Incidence not known
myalgia / Early / Incidence not known
diarrhea / Early / Incidence not known
nausea / Early / Incidence not known
abdominal pain / Early / Incidence not known
vomiting / Early / Incidence not known
nasal congestion / Early / Incidence not known
malaise / Early / Incidence not known
tinnitus / Delayed / Incidence not known
injection site reaction / Rapid / Incidence not known
rash / Early / Incidence not known
pruritus / Rapid / Incidence not known
Common Brand Names
Amicar
Dea Class
Rx
Description
Oral and parenteral inhibitor of fibrinolysis
Used for enhancing hemostasis when fibrinolysis contributes to bleeding
Associated with potential risk for clotting or thrombosis.
Dosage And Indications
5 g PO the first hour, followed by 1 to 1.25 g/hour PO for 8 hours or until bleeding is controlled. Max: 30 g/day.
50 to 100 mg/kg/dose PO every 6 hours. Max: 24 g/day.
4 to 5 g IV over 1 hour, followed by 1 g/hour continuous IV infusion for 8 hours or until bleeding is controlled. Max: 30 g/day.[50659]
100 to 200 mg/kg IV, followed by 100 mg/kg IV every 6 hours. Max: 30 g/day. Alternatively, 100 mg/kg or 3 g/m2 IV, followed by 33.3 mg/kg/hour or 1 g/m2/hour continuous IV infusion, not to exceed 18 g/m2/day.
100 mg/kg/dose PO every 4 to 6 hours until mucosal healing is complete (10 to 14 days). Max: 2 g/dose and 24 g/day.
50 to 100 mg/kg/dose PO every 6 hours until mucosal healing is complete (10 to 14 days). Max: 24 g/day.
100 mg/kg/dose IV every 4 to 6 hours until mucosal healing is complete (10 to 14 days). Max: 4 g/dose and 24 g/day.
Soak small piece of oxidized cellulose in approximately 2 molar solution and pack tooth socket.[24534]
1.25 g PO as oral rinse for 30 seconds after initial rinses with hydrogen peroxide followed by saline. Repeat every 4 hours until bleeding is controlled.[24535]
4 or 5 g IV followed by 1 g/hour continuous IV infusion for up to 72 hours with treatment discontinued 4 to 6 hours before angiography when possible.[58114] [58115] [58116] Guidelines recommend short-term (less than 72 hours) therapy to reduce the risk of early aneurysm rebleeding for patients with unavoidable delay in obliteration of aneurysm, a significant risk of rebleeding, and no compelling medical contraindications.[58117]
20 mg/100 mL continuous bladder irrigation until 24 hours after the urine becomes clear.[24536]
NOTE: Topical aminocaproic acid has been designated an orphan drug by the FDA for this indication.
100 mg/kg/dose PO (Max: 5 g/dose) every 4 hours for 5 days. Max: 30 g/day.[24959]
100 mg/kg/dose PO every 4 hours for 5 days. Max: 30 g/day.[24960] Relative efficacy compared with placebo has not been studied in a high-risk pediatric population.
16 g/day PO in divided doses every 4 or 6 hours for up to a month then 2 to 12 g/day PO in 2 to 4 divided doses. Usual dose: 2 g PO 3 times daily (range, 1 g PO twice daily to 4 g PO 3 times daily).
5 to 10 g IV, followed by 1 to 2 g/hour continuous IV infusion. Alternatively, 100 mg/kg IV, followed by 10 mg/kg/hour continuous IV infusion. When given in combination with DDAVP, 5 g IV once preoperatively. Guidelines recommend aminocaproic acid to reduce blood loss and blood transfusion during cardiac procedures.
4 to 5 g IV over 1 hour, followed by 1 g/hour continuous IV infusion until bleeding is controlled. There is potential for benefit in all patients, but particularly when blood products are contraindicated or declined by patient/family or if cryoprecipitate is not available in a timely manner.
†Indicates off-label use
Dosing Considerations
Specific guidelines for dosage adjustments in hepatic impairment are not available; it appears that no dosage adjustments are needed.
Specific guidelines for dosage adjustments in renal impairment are not available; dosage should be modified depending on clinical response and degree of renal impairment.
Drug Interactions
Anti-inhibitor Coagulant Complex: (Major) Use of aminocaproic acid within approximately 6 to 12 hours after the administration of anti-inhibitor coagulant complex (human) is not recommended, due to the increased risk of thrombosis.
Factor IX: (Major) In general, aminocaproic acid should not be administered simultaneously with factor IX complex, factor IX concentrates, factor IX Fc fusion protein, recombinant, and factor IX albumin fusion protein, recombinant due to the increased risk of thrombosis. Some hematologists recommend separating administration of aminocaproic acid from these clotting factor complexes by 8 hours. Aminocaproic acid has been used concurrently with human factor IX complexes or anti-inhibitor coagulant complex perioperatively in hemophiliac patients. The risk of developing thrombosis, however, is increased. In rare instances, thrombosis leading to acute myocardial infarction or gangrene has been reported in patients with hemophilia receiving combination therapy with factor IX concentrate and aminocaproic acid. Concomitant administration of aminocaproic acid with purer formulations of factor IX may also result in an increased risk of thrombosis.
Prothrombin Complex Concentrate, Human: (Major) In general, aminocaproic acid should not be administered simultaneously with factor IX complex, factor IX concentrates, factor IX Fc fusion protein, recombinant, and factor IX albumin fusion protein, recombinant due to the increased risk of thrombosis. Some hematologists recommend separating administration of aminocaproic acid from these clotting factor complexes by 8 hours. Aminocaproic acid has been used concurrently with human factor IX complexes or anti-inhibitor coagulant complex perioperatively in hemophiliac patients. The risk of developing thrombosis, however, is increased. In rare instances, thrombosis leading to acute myocardial infarction or gangrene has been reported in patients with hemophilia receiving combination therapy with factor IX concentrate and aminocaproic acid. Concomitant administration of aminocaproic acid with purer formulations of factor IX may also result in an increased risk of thrombosis.
Thrombolytic Agents: (Contraindicated) The actions of aminocaproic acid can antagonize the actions of thrombolytic agents. Although antifibrinolytic agents can be beneficial in the treatment of thrombolytic-induced hemorrhage, the safety of concomitant administration of these agents has not been confirmed.
Tretinoin, ATRA: (Major) Rare cases of fatal thrombotic complications have been reported in patients treated with systemic tretinoin, and antifibrinolytic agents. This is thought to be due to the persistent procoagulant tendency often associated with systemic tretinoin, ATRA therapy. Monitor patients closely and avoid if possible.
How Supplied
Amicar/Aminocaproic Acid Intravenous Inj Sol: 1mL, 250mg
Amicar/Aminocaproic Acid Oral Sol: 0.25g, 1mL
Amicar/Aminocaproic Acid Oral Tab: 500mg, 1000mg
Maximum Dosage
30 g/day IV or PO; 36 g/day IV or PO has been used off-label in subarachnoid hemorrhage.
30 g/day IV or PO; 36 g/day IV or PO has been used off-label in subarachnoid hemorrhage.
Safety and efficacy have not been established.
Safety and efficacy have not been established.
Mechanism Of Action
Aminocaproic acid inhibits both the activity of plasminogen activators and to a lesser degree, plasmin activity by binding to lysine-binding sites within the plasminogen/plasmin molecule, which interferes with the ability of plasmin to lyse fibrin clots. Low concentrations of epsilon-aminocaproic acid (EACA) inhibit in vitro profibrinolysin activation by streptokinase and urokinase. Aminocaproic acid may suppress chymotrypsin proteolytic enzymes and antigen-antibody reactions. Aminocaproic acid does not alter the concentrations of clotting factors. EACA diminishes the tuberculin reaction in patients sensitive to tuberculin. The antihistaminic action of this agent is not clinically significant.
Pharmacokinetics
Aminocaproic acid is administered orally and intravenously. Apparent Vd is estimated to be 23.1 L after oral administration and 30 L after intravenous administration. With prolonged administration, aminocaproic acid distributes throughout extravascular and intravascular compartments, penetrating red blood cells and other tissue cells. Renal excretion is the primary route of elimination; 65% of the dose is recovered in the urine unchanged, and 11% appears as the metabolite adipic acid. Renal clearance (116 mL/minute) approximated endogenous creatinine clearance. Total body clearance is 169 mL/minute. Terminal elimination half-life is approximately 2 hours.[28471] [50659]
Affected cytochrome P450 isoenzymes and drug transporters: none
Oral absorption appears to be a zero-order process with an absorption rate of 5.2 g/hour. Mean lag time in absorption is 10 minutes. After a single oral dose of 5 g, absorption was complete. Mean peak plasma concentrations (164 mcg/mL) were attained 1.2 hours.[28471]
Pregnancy And Lactation
Use aminocaproic acid during pregnancy only if clearly needed. It is not known whether aminocaproic acid can cause fetal harm when administered during human pregnancy or if it affects reproduction capacity. Animal reproduction studies with aminocaproic acid have not been conducted.[28471] [50659]
It is not known if aminocaproic acid is excreted into breast milk. Because many drugs are excreted into breast milk, use aminocaproic acid with caution in a breast-feeding woman.[28471] [50659]