Aminocaproic acid binds reversibly to the kringle domain of plasminogen and blocks the binding of plasminogen to fibrin and its activation to plasmin. With NO activation of plasmin, there is a reduction in fibrinolysis. This consequently will reduce the amount of bleeding post surgery. Elevated plasma levels of lipoprotein(a) have been shown to increase the risk of vascular disease. Lipoprotein 9a)a has two components, apolipoprotein B-100, linked to apolipoprotein (a). Aminocaproic acid may change the conformation of apoliprotein (a), changing its binding properties and potentially preventing the formation of lipoprotein (a).
Aminocaproic acid (Amicar) is FDA-approved for use in the treatment of acute bleeding due to elevated fibrinolytic activity. It also carries an Orphan Drug designation from the FDA for the prevention of recurrent hemorrhage in patients with traumatic hyphema. In clinical practice, aminocaproic acid is frequently used off-label for control of bleeding in patients with severe thrombocytopenia, control of oral bleeding in patients with congenital and acquired coagulation disorders, control of perioperative bleeding associated with cardiac surgery, prevention of excessive bleeding in patients on anticoagulation therapy undergoing invasive dental procedures, and reduction of the risk of catastrophic hemorrhage in patients with acute promyelocytic leukemia.
AMICAR (aminocaproic acid) is generally well tolerated. The following adverse experiences have been reported:
Edema, headache, malaise.
Allergic and anaphylactoid reactions, anaphylaxis.
Bradycardia, hypotension, peripheral ischemia, thrombosis.
Abdominal pain, diarrhea, nausea, vomiting.
Agranulocytosis, coragulation disorder, leukopenia, thrombocytopenia.
CPK increased, muscle weakness, myalgia, myopathy, myositis, rhabdomyolysis.
Confusion, convulsions, delirium, dizziness, hallucinations, intracranial hypertension, stroke, syncope.
Dyspnea, nasal congestion, pulmonary embolism.
Tinnitus, vision decreased, watery eyes.
BUN increased, renal failure. There have been some reports of dry ejaculation during the period of AMICAR (aminocaproic acid) treatment. These have been reported to date only in hemophilia 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.
An identical dosage regimen may be followed by administering AMICAR (aminocaproic acid) Tablets or AMICAR (aminocaproic acid) Oral Solution as follows:
For the treatment of acute bleeding syndromes due to elevated fibrinolytic activity, it is suggested that 5 AMICAR (aminocaproic acid) 1000 mg Tablets or 10 AMICAR (aminocaproic acid) 500 mg Tablets (5 g) or 20 milliliter of AMICAR (aminocaproic acid) Oral Solution (5 g) be administered during the first hour of treatment, followed by a continuing rate of 1 AMICAR (aminocaproic acid) 1000 mg Tablet or 2 AMICAR (aminocaproic acid) 500 mg Tablets (1 g) or 5 milliliter of AMICAR (aminocaproic acid) Oral Solution (1.25 g) per hour. This method of treatment would ordinarily be continued for about 8 hours or until the bleeding situation has been controlled.
Prolongation of the template bleeding time has been reported during continuous intravenous infusion of AMICAR (aminocaproic acid) at dosages exceeding 24 g/day. Platelet function studies in these patients have not demonstrated any significant platelet dysfunction. However, in vitro studies have shown that at high concentrations (7.4 mMol/L or 0.97 mg/mL and greater) aminocaproic acid inhibits ADP and collagen-induced platelet aggregation, the release of ATP and serotonin, and the binding of fibrinogen to the platelets in a concentration-response manner. Following a 10 g bolus of AMICAR (aminocaproic acid) , transient peak plasma concentrations of 4.6 mMol/L or 0.60 mg/mL have been obtained. The concentration of AMICAR (aminocaproic acid) necessary to maintain inhibition of fibrinolysis is 0.99 mMol/L or 0.13 mg/mL. Administration of a 5 g bolus followed by 1 to 1.25 g/hr should achieve and sustain plasma levels of 0.13 mg/mL. Thus, concentrations which have been obtained 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. However, higher plasma concentrations of AMICAR (aminocaproic acid) may occur in patients with severe renal failure.
You should not flush aminocaproic acid down the toilet or pour them into a drain unless instructed to do so. It is important to properly discard this product when it is expired or no longer needed. Consult your pharmacist for more details about how to safely discard your product.
Before using this drug, tell your doctor if:
Tell all of your health care providers that you take this medicine. This includes your doctors, nurses, pharmacists, and dentists.
Have blood work checked as you have been told by the doctor. Talk with the doctor.
This medicine may affect certain lab tests. Tell all of your health care providers and lab workers that you take this medicine (aminocaproic acid tablets).
Is it safe during pregnancy or breastfeeding?
There are no adequate studies in women for determining risk when using aminocaproic acid during pregnancy or while breastfeeding. Please always consult with your doctor to weigh the potential benefits and risks before taking aminocaproic acid. Aminocaproic acid is pregnancy risk category C, according to the US Food and Drug Administration (FDA).
FDA pregnancy risk category reference below: