Adult: For enhancing haemostasis when fibrinolysis contributes to bleeding (may be associated with surgical complications after heart surgery and portacaval shunts, abruptio placentae, hepatic cirrhosis, haematologic disorders, neoplastic diseases and in urinary fibrinolysis): 4-5 g loading dose via infusion over 1 hour, followed by continuous infusion at a rate of 1 g/hour for up to 8 hours or until the bleeding has been controlled. Max: 30 g daily.
Oral Haemorrhage
Adult: For enhancing haemostasis when fibrinolysis contributes to bleeding (may be associated with surgical complications after heart surgery and portacaval shunts, abruptio placentae, hepatic cirrhosis, haematologic disorders, neoplastic diseases and in urinary fibrinolysis): 5 g loading dose during the 1st hour (tab/oral solution), followed by 1 g hourly (tab) or 1.25 g hourly (oral solution) for up to 8 hours or until the bleeding has been controlled. Max: 30 g daily.
Renal Impairment
Dose reduction may be needed.
Administration
May be taken with or without food. May be taken w/ meals to prevent GI upset.
Reconstitution
IV infusion: Dilute in NaCl 0.9% solution, dextrose 5% in water, or Ringer's solution.
Contraindications
Active intravascular clotting process, disseminated intravascular coagulation (without concomitant heparin). Concomitant use with factor IX complex and anti-inhibitor coagulant complex.
Special Precautions
Patient with cardiac disease or haematuria of upper urinary tract origin. Aminocaproic acid must not be administered without a definite diagnosis and/or laboratory findings of hyperfibrinolysis. Avoid rapid IV administration. Renal and hepatic impairment. Pregnancy and lactation.
Adverse Reactions
Significant: Skeletal muscle weakness including myalgia with weakness and fatigue, increased creatine phosphokinase (CPK) levels, severe myopathy with rhabdomyolysis, myoglobinuria, and acute renal failure (particularly with prolonged use); intrarenal obstruction in the form of glomerular capillary thrombosis or clots in the renal pelvis and ureter. Blood and lymphatic system disorders: Agranulocytosis, leucopenia, thrombocytopenia, coagulation disorder. Cardiac disorders: Arrhythmia, bradycardia, myocardial lesion. Ear and labyrinth disorders: Tinnitus. Eye disorders: Decreased vision, watery eyes. Gastrointestinal disorders: Nausea, vomiting, diarrhoea, abdominal pain. General disorders and administration site conditions: Oedema, malaise, fever; inj site reactions (e.g. pain, necrosis). Hepatobiliary disorders: Hepatic lesion. Immune system disorders: Allergic and anaphylactoid reactions. Investigations: Increased BUN. Metabolism and nutrition disorders: Anorexia, hyperkalaemia. Musculoskeletal and connective tissue disorders: Myositis. Nervous system disorders: Headache, dizziness, seizures, stroke. Psychiatric disorders: Delirium, confusion, hallucinations. Respiratory, thoracic and mediastinal disorders: Dyspnoea, nasal congestion, pulmonary embolism. Skin and subcutaneous tissue disorders: Pruritus, rash. Vascular disorders: Thrombosis, hypotension, syncope, peripheral ischaemia.
If uncertain, perform tests to differentiate whether the cause of bleeding is primary fibrinolysis or disseminated intravascular coagulation (e.g. platelet count, protamine paracoagulation test, euglobulin clot lysis test) before treatment. Monitor levels of fibrinogen, fibrin split products, BUN, and serum creatinine. Obtain CPK levels for patients on long-term therapy. Assess for signs and symptoms of bleeding.
Overdosage
Symptoms: IV: Transient hypotension, severe acute renal failure, seizures. Management: Haemodialysis or peritoneal dialysis may be considered.
Drug Interactions
Enhanced thrombogenic effect with oral tretinoin. Potentially Fatal: Increased risk of thrombosis with factor IX complex and anti-inhibitor coagulant complex.
Lab Interference
IV: May cause prolongation of template bleeding time during continuous infusion at doses >24 g daily.
Action
Description: Mechanism of Action: Aminocaproic acid, a synthetic monoamino carboxylic acid, is an antifibrinolytic agent used similarly to tranexamic acid. It competitively binds to plasminogen, sequentially blocking plasminogen binding to fibrin and subsequent conversion to plasmin, leading to the inhibition of fibrin degradation. Onset: Approx 1-72 hours. Pharmacokinetics: Absorption: Rapidly and completely absorbed from the gastrointestinal tract. Bioavailability: 100% (oral). Time to peak plasma concentration: 1.2 ± 0.45 hours (oral). Distribution: Widely distributed through intravascular and extravascular compartments; readily penetrates human RBCs and other tissue cells. Volume of distribution: 23 L (oral); 30 L (IV). Metabolism: Minimally metabolised in the liver. Excretion: Via urine (65% as unchanged drug, 11% as adipic acid metabolite). Elimination half-life: 1-2 hours.
Chemical Structure
Aminocaproic acid Source: National Center for Biotechnology Information. PubChem Compound Summary for CID 564, Aminocaproic acid. https://pubchem.ncbi.nlm.nih.gov/compound/Aminocaproic-acid. Accessed Oct. 26, 2023.
B02AA01 - aminocaproic acid ; Belongs to the class of amino acid antifibrinolytics. Used in the treatment of hemorrhage.
References
Amicar Injection, Syrup, Tablet (Xanodyne Pharmaceuticals, Inc.). U.S. FDA. https://www.fda.gov. Accessed 11/09/2023.Amicar Solution and Tablet (Akorn Operating Company LLC). DailyMed. Source: U.S. National Library of Medicine. https://dailymed.nlm.nih.gov/dailymed. Accessed 11/09/2023.Aminocaproic Acid Injection, Solution (Hospira, Inc.). DailyMed. Source: U.S. National Library of Medicine. https://dailymed.nlm.nih.gov/dailymed. Accessed 11/09/2023.Aminocaproic Acid. Gold Standard Drug Database in ClinicalKey [online]. Elsevier Inc. https://www.clinicalkey.com. Accessed 17/10/2023.Anon. Aminocaproic Acid. AHFS Clinical Drug Information [online]. Bethesda, MD. American Society of Health-System Pharmacists, Inc. https://www.ahfscdi.com. Accessed 11/09/2023.Anon. Aminocaproic Acid. Lexicomp Online. Hudson, Ohio. Wolters Kluwer Clinical Drug Information, Inc. https://online.lexi.com. Accessed 11/09/2023.Buckingham R (ed). Aminocaproic Acid. Martindale: The Complete Drug Reference [online]. London. Pharmaceutical Press. https://www.medicinescomplete.com. Accessed 11/09/2023.
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