aminocaproic acid

Action and Spectrum

Actions and Spectrum: 

aminocaproic acid is a medication that works by inhibiting the breakdown of fibrin in the blood. Fibrin is a protein that forms blood clots necessary for wound healing and also for preventing excessive bleeding. aminocaproic acid prevents the breakdown of fibrin by blocking the action of plasmin, an enzyme that breaks down fibrin. 

The primary action of aminocaproic acid is to promote clotting and prevent bleeding. It is commonly used to treat conditions that involve excessive bleeding or the risk of bleeding, such as in surgeries, dental procedures, or patients with certain medical conditions. 

Regarding its spectrum, aminocaproic acid is effective against systemic and localized fibrinolysis. This means that it can be used to treat both general bleeding disorders and bleeding specific to certain body parts, such as the lungs, urinary tract, or reproductive system. 

Drug Interaction

Adverse Reaction

Frequency not defined 

Coagulation disorder 

Intracranial hypertension 

Myopathy 

Dyspnea 

Abdominal pain 

Pruritus 

Vision decrease 

Confusion 

Peripheral ischemia 

Renal failure 

Bradycardia 

Injection site reactions (pain/necrosis) 

Congestion 

Nausea 

Dizziness 

Edema 

Thrombosis 

Agranulocytosis 

Stroke 

Rash 

Convulsions 

Dry ejaculation 

Syncope 

Pulmonary embolism 

Malaise 

Headache 

Tinnitus 

Vomiting 

Leukopenia 

Anaphylaxis 

Muscle weakness 

Diarrhea 

Black Box Warning

Black Box Warning: 

aminocaproic acid has a black box warning regarding the risk of thrombosis (blood clots) and cardiac arrest. The warning states that aminocaproic acid should be generally used with caution in patients with a history of thrombosis or hypercoagulable conditions and in patients with active intravascular clotting. 

The warning also states that aminocaproic acid should be administered slowly and with close monitoring in patients with cardiac disease, as it may increase the risk of cardiac arrest.

Patients receiving aminocaproic acid should also be monitored for signs and symptoms of thrombosis, such as shortness of breath (SOB), chest pain, or swelling in the extremities. 

Contraindication / Caution

Contraindication/Caution: 

Contraindication 

aminocaproic acid is contraindicated in patients with a history of hypersensitivity or allergy to the medication or its components. It is contraindicated in patients with active intravascular clotting, disseminated intravascular coagulation (DIC), or severe renal impairment. 

Additionally, aminocaproic acid should be used cautiously in patients with a history of thrombosis or hypercoagulable conditions, as it may increase the risk of thrombosis and clot formation. Patients with cardiac disease or congestive heart failure should also be monitored closely, as aminocaproic acid may increase the risk of cardiac arrest or other cardiovascular events. 

It is important to note that aminocaproic acid should only be used under a physician’s close supervision and that the medication’s risks and benefits should be carefully considered for each patient. Patients and healthcare providers should discuss any concerns or questions regarding the use of aminocaproic acid and its potential risks and contraindications. 

Caution 

There are several cautions that healthcare providers should be aware of when prescribing aminocaproic acid: 

• Renal impairment: aminocaproic acid is primarily excreted by the kidneys, so patients with renal impairment may be at increased risk of adverse effects. Dosage adjustments may be necessary for these patients. 
• Thromboembolic events: aminocaproic acid can increase the risk of thromboembolic events, such as DVT (deep vein thrombosis) or pulmonary embolism (PE).  
• Cardiac disease: aminocaproic acid may increase the risk of cardiac arrest or other cardiovascular events, especially in preexisting or congestive heart failure patients. These patients should be monitored closely while receiving aminocaproic acid. 
• Pregnancy and breastfeeding: The safety of aminocaproic acid during pregnancy and breastfeeding is not well established. These populations should only use it if the potential benefits outweigh the risks. 
• Drug interactions: aminocaproic acid may interact with other medications, such as anticoagulants or thrombolytics, which may increase the risk of bleeding or thromboembolic events. Healthcare providers should review a patient’s medication list before prescribing aminocaproic acid to avoid potential drug interactions. 

Pregnancy / Lactation

Pregnancy consideration:  

US FDA pregnancy category: C 

Lactation:   

Excreted into human milk is Not known. 

Pregnancy category: 

• Category A: well-controlled and Satisfactory studies do not show risk to the fetus in the first/later trimester.        
• Category B: there was no evidence of risk to the fetus in animal studies, and there were not enough studies on pregnant women        
• Category C: there was evidence of risk of adverse effects in animal reproduction studies, and no adequate evidence in human studies must take care of potential risks in pregnant women.       
• Category D: adequate data with sufficient evidence of human fetal risk from various platforms, but despite the potential risk, and used only in emergency cases for potential benefits.        
• Category X: Drugs listed in this category outweigh the risks over benefits. Hence these categories of drugs need to be avoided by pregnant women.        
• Category N: There is no data available for the drug under this category 

Pharmacology

Pharmacology: 

aminocaproic acid is a synthetic derivative of the amino acid lysine. It acts by inhibiting plasminogen’s activation plasmin, a key enzyme involved in the breakdown of blood clots. aminocaproic acid competes with plasminogen for binding to fibrin, the protein that forms blood clots, thereby preventing the conversion of plasminogen to plasmin and the subsequent breakdown of blood clots. 

In addition to its antifibrinolytic effects, aminocaproic acid has been shown to have some vasodilatory effects. It has been suggested that aminocaproic acid may work by blocking the release of vasoconstrictive substances, such as histamine and serotonin, from platelets and other cells. 

Pharmacodynamics: 

Mechanism of action: The medication works by inhibiting fibrinolysis by inhibiting plasminogen binding to fibrin and subsequent conversion to plasmin. By inhibiting this process, it prevents the breakdown of fibrin and promotes clot stability. Additionally, the medication exhibits antiplasmin activity, which further helps to prevent fibrinolysis and promote clot stability. 

Pharmacokinetics: 

Absorption 

aminocaproic acid is rapidly absorbed after oral administration, with peak plasma concentrations occurring within 2-3 hours. The bioavailability of the oral formulation is approximately 50%, and the absorption is not affected by food. 

Distribution 

aminocaproic acid is widely distributed throughout the body, including the liver, kidneys, lungs, and spleen. It has a volume of distribution of approximately 1.5 L/kg, indicating that it is distributed mainly in the extracellular fluid. 

Metabolism 

aminocaproic acid is metabolized in the liver by oxidation to the inactive metabolite 6-aminohexanoic acid. The metabolism of aminocaproic acid is not affected by age, gender, or renal function. 

Elimination and Excretion 

aminocaproic acid and its metabolites are primarily excreted in the urine, with approximately 90% of a dose being eliminated within 24 hours. The elimination half-life of aminocaproic acid is approximately 2 hours but may be prolonged in patients with renal impairment. 

Adminstartion

Administration: 

Oral administration 

aminocaproic acid is available in several formulations, including oral tablets, oral solutions, and intravenous injections. The dosage and route of administration depend on the indication being treated, the severity of the condition, and other factors, such as the patient’s age, weight, and renal function. 

For the treatment of bleeding and excessive bleeding, the usual adult oral dose of aminocaproic acid is 4-5 grams every 4-6 hours. The usual adult intravenous dose is 4-5 grams over 30-60 minutes, followed by a continuous infusion of 1-2 grams per hour as needed. 

The usual adult oral dose of aminocaproic acid is 1-1.5 grams every 6 hours to manage hereditary angioedema. For the prevention of bleeding during cardiac surgery, the usual adult intravenous dose of aminocaproic acid is 5 grams given over 30 minutes before surgery, followed by a continuous infusion of 1 gram per hour during surgery. 

aminocaproic acid should be administered under the close supervision of a healthcare provider experienced in antifibrinolytic medications. The medication should be generally used cautiously in patients with renal impairment, and the dose should be adjusted depending on the patient’s renal function. Following the healthcare provider’s instructions regarding the dosage, administration route, and treatment duration is essential. 

Patient Information Leaflet

Patient information leaflet 

Generic Name: aminocaproic acid 

Pronounced: [ a-MEE-noe-ka-PROE-ik-AS-id ] 

Why do we use aminocaproic acid? 

aminocaproic acid is a medication that is used for several indications, including: 

• Control of bleeding: aminocaproic acid can control bleeding in various situations, including surgery, dental procedures, and trauma. 
• Treatment of excessive bleeding: aminocaproic acid is also used to treat conditions associated with excessive bleeding, such as hemophilia and von Willebrand disease. 
• Management of hereditary angioedema: aminocaproic acid can be used to manage hereditary angioedema, a rare genetic condition that causes recurrent episodes of swelling in the face, limbs, and airways. 
• Preventing bleeding during cardiac surgery: aminocaproic acid is sometimes used to prevent excessive bleeding and reduce the need for blood transfusions. 
• Treatment of fibrinolysis: aminocaproic acid treats fibrinolysis, where blood clots break down too quickly, leading to excessive bleeding. 

aminocaproic acid is a medication used to control bleeding and manage conditions associated with excessive bleeding. It is typically administered under the close supervision of a healthcare provider and should only be used when the potential benefits outweigh the risks.