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Oral and parenteral inhibitor of fibrinolysisUsed for enhancing hemostasis when fibrinolysis contributes to bleedingAssociated with potential risk for clotting or thrombosis.
Amicar/Aminocaproic Acid Intravenous Inj Sol: 1mL, 250mgAmicar/Aminocaproic Acid Oral Sol: 0.25g, 1mLAmicar/Aminocaproic Acid Oral Tab: 500mg, 1000mg
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.
100 to 200 mg/kg/dose PO once, followed by 100 mg/kg/dose PO every 6 hours. Max: 30 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.
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.
6 g PO immediately after surgery, then 6 g PO every 6 hours for 9 to 10 days. Max: 30 g/day.
Soak small piece of oxidized cellulose in approximately 2 molar solution and pack tooth socket.
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.
May apply with a cotton swab.
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.   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.
20 mg/100 mL continuous bladder irrigation until 24 hours after the urine becomes clear.
100 mg/kg/dose PO (Max: 5 g/dose) every 4 hours for 5 days. Max: 30 g/day.
100 mg/kg/dose PO every 4 hours for 5 days. Max: 30 g/day. 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 g IV before skin incision, followed by 1 g/hr continuous IV infusion for 6 to 8 hours. In combination with DDAVP, 5 g IV once preoperatively.
†Indicates off-label use
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.
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.
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.Intermittent IV InfusionDilute 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.Continuous IV InfusionAfter 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.
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 AdministrationNOTE: 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.
Amicar:- Store at controlled room temperature (between 68 and 77 degrees F)
Aminocaproic acid is contraindicated in patients with an active intravascular clotting process or disseminated intravascular coagulation (DIC) without concomitant heparin. Distinguish whether bleeding is a result of primary fibrinolysis or DIC before aminocaproic acid initiation. In DIC, the platelet count is usually decreased, protamine paracoagulation test is positive, and the euglobulin clot lysis test is normal. Do not administer aminocaproic acid without a definitive diagnosis and/or laboratory finding indicative of hyperfibrinolysis (hyperplasminemia). Inhibition of fibrinolysis by aminocaproic acid may theoretically result in clotting or thrombosis. However, there is no direct evidence that aminocaproic acid use has been responsible for the few reported cases of intravascular clotting after treatment. Rather, it appears that such intravascular clotting was most likely attributable to the patient's preexisting clinical condition (e.g., DIC). 
Do not use aminocaproic acid in hematuria of upper urinary tract origin, unless the potential benefits outweigh the risk. Aminocaproic acid use in patients with upper urinary tract bleeding has been known to cause intrarenal obstruction in the form of glomerular capillary thrombosis or clots in the renal pelvis and ureters. 
Aminocaproic acid use may cause laboratory test interference. Prolongation of the template bleeding time has been reported during aminocaproic acid continuous intravenous infusion at dosages exceeding 24 g/day. Platelet function studies in these patients have not demonstrated any platelet dysfunction. However, in vitro studies have shown that at high concentrations (7.4 mMol/L or 0.97 mg/mL or more), aminocaproic acid inhibits ADP and collagen-induced platelet aggregation, serotonin and ATP release, and the binding of fibrinogen to the platelets in a concentration-response manner. Concentrations achieved in vivo clinically in patients with normal renal function are considerably lower than the in vitro concentrations found to induce abnormalities in platelet function tests. 
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. 
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. 
bradycardia / Rapid / Incidence not knownarrhythmia exacerbation / Early / Incidence not knownincreased intracranial pressure / Early / Incidence not knownstroke / Early / Incidence not knownseizures / Delayed / Incidence not knownrenal failure (unspecified) / Delayed / Incidence not knownthrombosis / Delayed / Incidence not knownpulmonary embolism / Delayed / Incidence not knownagranulocytosis / Delayed / Incidence not knownrhabdomyolysis / Delayed / Incidence not knownmyoglobinuria / Delayed / Incidence not knownvisual impairment / Early / Incidence not knownskin necrosis / Early / Incidence not knownanaphylactoid reactions / Rapid / Incidence not known
hypotension / Rapid / Incidence not knownhallucinations / Early / Incidence not knowndelirium / Early / Incidence not knownconfusion / Early / Incidence not knownejaculation dysfunction / Delayed / Incidence not knownleukopenia / Delayed / Incidence not knownthrombocytopenia / Delayed / Incidence not knownmyopathy / Delayed / Incidence not knowndyspnea / Early / Incidence not knownedema / Delayed / Incidence not knownphlebitis / Rapid / Incidence not known
syncope / Early / Incidence not knowndizziness / Early / Incidence not knownheadache / Early / Incidence not knownfatigue / Early / Incidence not knownweakness / Early / Incidence not knownmyalgia / Early / Incidence not knowndiarrhea / Early / Incidence not knownnausea / Early / Incidence not knownabdominal pain / Early / Incidence not knownvomiting / Early / Incidence not knownnasal congestion / Early / Incidence not knownmalaise / Early / Incidence not knowntinnitus / Delayed / Incidence not knowninjection site reaction / Rapid / Incidence not knownrash / Early / Incidence not knownpruritus / Rapid / Incidence not known
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: (Severe) 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.
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.
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.  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.