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Amicar (Epsilon Aminocaproic Acid)
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Pharmacology
Epsilon aminocaproic acid is a monoaminocarboxylic acid which acts as an effective inhibitor of fibrinolysis. The beneficial fibrinolysis-inhibitory effects of aminocaproic acid appear to be principally via inhibition of plasminogen activator substances and to a lesser degree, through antiplasmin activity. The drug is absorbed rapidly following oral administration. A major portion of the compound is recovered unmetabolized in the urine. The renal clearance of aminocaproic acid is high (about 75% of the creatinine clearance). Thus, the drug is excreted rapidly. After prolonged administration, aminocaproic acid distributes throughout both the extravascular and intravascular compartments of the body and readily penetrates human red blood and other tissue cells.
Epsilon aminocaproic acid is a monoaminocarboxylic acid which acts as an effective inhibitor of fibrinolysis. The beneficial fibrinolysis-inhibitory effects of aminocaproic acid appear to be principally via inhibition of plasminogen activator substances and to a lesser degree, through antiplasmin activity. The drug is absorbed rapidly following oral administration. A major portion of the compound is recovered unmetabolized in the urine. The renal clearance of aminocaproic acid is high (about 75% of the creatinine clearance). Thus, the drug is excreted rapidly. After prolonged administration, aminocaproic acid distributes throughout both the extravascular and intravascular compartments of the body and readily penetrates human red blood and other tissue cells.
Indications
Epsilon Aminocaproic Acid Is A Monoaminocarboxylic Acid Which Acts As An Effective Inhibitor Of Fibrinolysis. The Beneficial Fibrinolysis-inhibitory Effects Of Aminocaproic Acid Appear To Be Principally Via Inhibition Of Plasminogen Activator Substances And To A Lesser Degree, Through Antiplasmin Activity. The Drug Is Absorbed Rapidly Following Oral Administration. A Major Portion Of The Compound Is Recovered Unmetabolized In The Urine. The Renal Clearance Of Aminocaproic Acid Is High (about 75% Of The Creatinine Clearance). Thus, The Drug Is Excreted Rapidly. After Prolonged Administration, Aminocaproic Acid Distributes Throughout Both The Extravascular And Intravascular Compartments Of The Body And Readily Penetrates Human Red Blood And Other Tissue Cells.
Epsilon Aminocaproic Acid Is A Monoaminocarboxylic Acid Which Acts As An Effective Inhibitor Of Fibrinolysis. The Beneficial Fibrinolysis-inhibitory Effects Of Aminocaproic Acid Appear To Be Principally Via Inhibition Of Plasminogen Activator Substances And To A Lesser Degree, Through Antiplasmin Activity. The Drug Is Absorbed Rapidly Following Oral Administration. A Major Portion Of The Compound Is Recovered Unmetabolized In The Urine. The Renal Clearance Of Aminocaproic Acid Is High (about 75% Of The Creatinine Clearance). Thus, The Drug Is Excreted Rapidly. After Prolonged Administration, Aminocaproic Acid Distributes Throughout Both The Extravascular And Intravascular Compartments Of The Body And Readily Penetrates Human Red Blood And Other Tissue Cells.
Contraindications
Aminocaproic acid should not be used when there is evidence of an active intravascular clotting process.
When there is uncertainty as to whether the cause of bleeding is primary fibrinolysis or disseminated intravascular coagulation (DIC), this distinction must be made before administering aminocaproic acid. The following tests can be applied to differentiate the two conditions: Platelet count is usually decreased in DIC but normal in primary fibrinolysis.
Protamine Paracoagulation test is positive in DIC; a precipitate forms when protamine sulfate is dropped in citrated plasma. The test is negative in the presence of primary fibrinolysis.
The euglobin clot lysis test is abnormal in primary fibrinolysis, but normal in DIC.
Aminocaproic acid must not be used in the presence of DIC without concomitant heparin.
Pregnancy: The effect on the fetus and transplacental passage of this drug is unknown. Therefore, its use during the first and second trimesters should be confined to instances where need outweighs possible hazards.
Aminocaproic acid should not be used when there is evidence of an active intravascular clotting process.
When there is uncertainty as to whether the cause of bleeding is primary fibrinolysis or disseminated intravascular coagulation (DIC), this distinction must be made before administering aminocaproic acid. The following tests can be applied to differentiate the two conditions: Platelet count is usually decreased in DIC but normal in primary fibrinolysis.
Protamine Paracoagulation test is positive in DIC; a precipitate forms when protamine sulfate is dropped in citrated plasma. The test is negative in the presence of primary fibrinolysis.
The euglobin clot lysis test is abnormal in primary fibrinolysis, but normal in DIC.
Aminocaproic acid must not be used in the presence of DIC without concomitant heparin.
Pregnancy: The effect on the fetus and transplacental passage of this drug is unknown. Therefore, its use during the first and second trimesters should be confined to instances where need outweighs possible hazards.
Safety Information / Warning
The drug is offered for use only in potentially acute life-threatening situations where hemorrhage results from an overactivity of the fibrinolytic system.
Antifertility effects, consistent with the drug's antifibrinolytic activity, have been suggested in some rodent studies.
In patients with upper urinary tract bleeding, administration of aminocaproic acid has been known to cause intrarenal obstruction in the form of glomerular capillary thrombosis, or clots in the renal pelvis and ureters. For this reason, aminocaproic acid should not be used in hematuria of upper urinary tract origin, unless the possible benefits outweigh the risk.
The drug is offered for use only in potentially acute life-threatening situations where hemorrhage results from an overactivity of the fibrinolytic system.
Antifertility effects, consistent with the drug's antifibrinolytic activity, have been suggested in some rodent studies.
In patients with upper urinary tract bleeding, administration of aminocaproic acid has been known to cause intrarenal obstruction in the form of glomerular capillary thrombosis, or clots in the renal pelvis and ureters. For this reason, aminocaproic acid should not be used in hematuria of upper urinary tract origin, unless the possible benefits outweigh the risk.
Precautions
The use of aminocaproic acid should be accompanied by tests designed to determine the amount of fibrinolysis present. There are presently available (a) general tests, such as those for the determination of the lysis of a clot of blood or plasma and (b) more specific tests for the study of various phases of fibrinolytic mechanisms. These latter tests include both semi-quantitative and quantitative techniques for the determination of profibrinolysin, fibrinolysin and anti-fibrinolysin.
Animal experiments indicate particular caution should be taken in administering aminocaproic acid to patients with cardiac, hepatic or renal diseases.
Demonstrable animal pathology in some cases has shown endocardial hemorrhages and myocardial fat degeneration. The use of this drug should thus be restricted to patients in whom the benefit expected would outweigh the hazard.
One case of cardiac and hepatic lesions observed in man has been reported. The patient received 2g of aminocaproic acid every 6 hours for a total dose of 26g. Death was due to continued cerebral vascular hemorrhage. Necrotic changes in the heart and liver were noted at autopsy.
Fibrinolysis is a normal process, potentially active at all times to ensure the fluidity of blood. Inhibition of fibrinolysis by aminocaproic acid may result in clotting or thrombosis. However, there is no definite evidence that administration of aminocaproic acid has been responsible for the few reported cases intravascular clotting which followed this treatment. Rather, it appears that such intravascular clotting was most likely due to the patient's pre-existing clinical condition, e.g., the presence of DIC.
It has been postulated that extravascular clots formed in vivo with incorporated aminocaproic acid may not undergo spontaneous lysis as do normal clots. However, it is the consensus of experts that the few reported cases of extravascular clotting could have occurred in the absence of aminocaproic acid treatment.
The use of aminocaproic acid should be accompanied by tests designed to determine the amount of fibrinolysis present. There are presently available (a) general tests, such as those for the determination of the lysis of a clot of blood or plasma and (b) more specific tests for the study of various phases of fibrinolytic mechanisms. These latter tests include both semi-quantitative and quantitative techniques for the determination of profibrinolysin, fibrinolysin and anti-fibrinolysin.
Animal experiments indicate particular caution should be taken in administering aminocaproic acid to patients with cardiac, hepatic or renal diseases.
Demonstrable animal pathology in some cases has shown endocardial hemorrhages and myocardial fat degeneration. The use of this drug should thus be restricted to patients in whom the benefit expected would outweigh the hazard.
One case of cardiac and hepatic lesions observed in man has been reported. The patient received 2g of aminocaproic acid every 6 hours for a total dose of 26g. Death was due to continued cerebral vascular hemorrhage. Necrotic changes in the heart and liver were noted at autopsy.
Fibrinolysis is a normal process, potentially active at all times to ensure the fluidity of blood. Inhibition of fibrinolysis by aminocaproic acid may result in clotting or thrombosis. However, there is no definite evidence that administration of aminocaproic acid has been responsible for the few reported cases intravascular clotting which followed this treatment. Rather, it appears that such intravascular clotting was most likely due to the patient's pre-existing clinical condition, e.g., the presence of DIC.
It has been postulated that extravascular clots formed in vivo with incorporated aminocaproic acid may not undergo spontaneous lysis as do normal clots. However, it is the consensus of experts that the few reported cases of extravascular clotting could have occurred in the absence of aminocaproic acid treatment.
Side Effects / Adverse Effects
Occasionally nausea, cramps, diarrhea, dizziness, tinnitus, malaise, conjunctival suffusion, nasal stuffiness, headache, myopathy and skin rash have been reported as results of the administration of aminocaproic acid. Only rarely has it been necessary to discontinue or reduce medication because of one or more of these effects.
There have also been some reports of dry ejaculation during the period of aminocaproic acid treatment. These have been reported to date only in hemophiliac patients who received the drug after undergoing dental surgical procedures. However, this symptom resolved in all patients within 24 to 48 hours of completion of therapy.
One case of a convulsion occurring, following i.v. administration of aminocaproic acid, has been reported. However, definite association between the seizure and the drug has not been established.
Occasionally nausea, cramps, diarrhea, dizziness, tinnitus, malaise, conjunctival suffusion, nasal stuffiness, headache, myopathy and skin rash have been reported as results of the administration of aminocaproic acid. Only rarely has it been necessary to discontinue or reduce medication because of one or more of these effects.
There have also been some reports of dry ejaculation during the period of aminocaproic acid treatment. These have been reported to date only in hemophiliac patients who received the drug after undergoing dental surgical procedures. However, this symptom resolved in all patients within 24 to 48 hours of completion of therapy.
One case of a convulsion occurring, following i.v. administration of aminocaproic acid, has been reported. However, definite association between the seizure and the drug has not been established.
Overdose
Information not available
Information not available
Recommended Dosage
Therapy is recommended as follows for all indications other than dental extractions in hemophiliacs: An initial priming dose of 5g of aminocaproic acid followed by 1 to 1.25g doses at hourly intervals thereafter should achieve and sustain plasma levels of 0.130mg/mL of the drug. This is the concentration apparently necessary for the inhibition of fibrinolysis. Administration of more than 30g in any 24-hour period is not recommended.
Oral Therapy: If the patient is able to take medication by mouth, an identical dosage regimen may be followed by administering the tablets as follows: For the treatment of acute bleeding syndromes due to elevated fibrinolytic activity, it is suggested that 10tablets (5g) of aminocaproic acid be administered during the first hour of treatment, followed by a continuing rate of 2tablets (1g)/hour. This method of treatment would ordinarily be continued for about 8hours or until the bleeding situation has been controlled.
Therapy for Hemophiliacs undergoing Dental Extractions: Following preoperative treatment with a loading dose of FactorVIII orIX to raise factor levels to at least 30to 50%, administer 6g orally as soon as possible postoperatively, followed by 6g orally every 6hours (total dose of 24g/24hours) for a 9-to 10-day period.
Therapy is recommended as follows for all indications other than dental extractions in hemophiliacs: An initial priming dose of 5g of aminocaproic acid followed by 1 to 1.25g doses at hourly intervals thereafter should achieve and sustain plasma levels of 0.130mg/mL of the drug. This is the concentration apparently necessary for the inhibition of fibrinolysis. Administration of more than 30g in any 24-hour period is not recommended.
Oral Therapy: If the patient is able to take medication by mouth, an identical dosage regimen may be followed by administering the tablets as follows: For the treatment of acute bleeding syndromes due to elevated fibrinolytic activity, it is suggested that 10tablets (5g) of aminocaproic acid be administered during the first hour of treatment, followed by a continuing rate of 2tablets (1g)/hour. This method of treatment would ordinarily be continued for about 8hours or until the bleeding situation has been controlled.
Therapy for Hemophiliacs undergoing Dental Extractions: Following preoperative treatment with a loading dose of FactorVIII orIX to raise factor levels to at least 30to 50%, administer 6g orally as soon as possible postoperatively, followed by 6g orally every 6hours (total dose of 24g/24hours) for a 9-to 10-day period.
Supplied / Packaging
Each round, scored, white tablet, engraved “LL” and “A10”, contains: epsilon aminocaproic acid 500mg. Energy: <4.2kJ (1kcal). Tartrazine-free. Bottles of100.
Each round, scored, white tablet, engraved “LL” and “A10”, contains: epsilon aminocaproic acid 500mg. Energy: <4.2kJ (1kcal). Tartrazine-free. Bottles of100.
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Brand Name
Amicar
Amicar
Generic Name
Epsilon Aminocaproic Acid
Epsilon Aminocaproic Acid
General Indications
Antifibrinolytic Agent
Antifibrinolytic Agent
