Aminocaproic acid

Aminocaproic acid (also known as ε-aminocaproic acid) is a synthetic amino acid compound that is used in medical practice as a hemostatic agent. It shows its properties as an antifibrinolytic agent, i.e. It prevents the breakdown of blood clots and prevents their dissolution.

Aminocaproic acid is commonly used to control bleeding in a variety of situations including surgery, trauma, prescription for disseminated intravascular coagulation (DIC), and to reduce menstrual bleeding in women with hyperfibrinolysis.

This medicine is available in various forms for use, including solution for injection and topical application as lubricants or mouthwash solutions. The dosage and route of administration may vary depending on the specific situation and doctor's advice.

Indications Aminocaproic acid

1. Surgery: In surgery, especially on organs at high risk of bleeding, such as the heart, liver or prostate. Aminocaproic acid helps control bleeding and reduce the amount of blood lost.
2. Injuries: For severe injuries and wounds to prevent or reduce bleeding.
3. Hyperfibrinolysis: Aminocaproic acid may be used to control increased breakdown of blood clots in patients with hyperfibrinolysis, such as in complications associated with surgery and in hemorrhagic conditions such as fibrinolytic anemia.
4. Bleeding due to disseminated intravascular coagulation (DIC): Aminocaproic acid may be used to reduce the risk of bleeding in this condition.
5. Menstrual bleeding: For the control of heavy and prolonged menstrual bleeding in women.

Release form

Solution for infusion

This is the most common form of release of aminocaproic acid. The solution is usually available in a concentration of 5% and is intended for intravenous administration.

• Concentrations and packaging:
  • 100 ml, 200 ml or 250 ml vials or plastic containers.
  • The solution can be used to control active bleeding or to prevent bleeding during surgical procedures.

Pharmacodynamics

1. Antifibrinolytic action: The main mechanism of action of aminocaproic acid is its ability to inhibit the activity of the plasminogen-plasmin system, which is responsible for the destruction of fibrin. Plasmin, the active form of plasminogen, breaks down fibrin, the main component of blood clots, which leads to their dissolution. Aminocaproic acid blocks the conversion of plasminogen to plasmin, thereby reducing the activity of the fibrinolytic system.
2. Prevention of bleeding: Aminocaproic acid is often used to prevent or stop bleeding associated with various conditions such as surgery, disseminated intravascular coagulation, hemorrhagic diathesis, and others.
3. Topical use: In addition to intravenous administration, aminocaproic acid can be used topically, for example, as a solution for gargling, instillation or impregnation, to reduce bleeding in dental surgeries, in gynecology and others.
4. Additional effects: In some cases, aminocaproic acid may have some anti-inflammatory and anti-allergic effects.

Pharmacokinetics

1. Absorption: Aminocaproic acid is well absorbed from the gastrointestinal tract after oral administration. Peak plasma concentrations are usually reached 2-3 hours after administration.
2. Distribution: It is well distributed throughout the body, including plasma, tissues and organs. Binding to blood plasma proteins is low.
3. Metabolism: Aminocaproic acid is practically not metabolized in the liver and is excreted from the body in unchanged form.
4. Excretion: Most of aminocaproic acid is excreted unchanged by the kidneys.
5. Excretionhalf-life: The half-life of aminocaproic acid from the body is about 2 hours.

Dosing and administration

Method of Application:

• Intravenously slowly (to prevent the risk of thrombosis and other adverse reactions).

Dosage:

• Adults: The initial dose is 4-5 g (80-100 ml of 5% solution) administered during the first hour, then 1 g (20 ml of 5% solution) every hour for the first 8 hours or until bleeding stops. The maximum daily dose should not exceed 30 g.
• Children: The dosage for children is 100 mg per kg of body weight in the first hour, then 33 mg per kg every hour thereafter for 8 hours or until bleeding stops.

Use Aminocaproic acid during pregnancy

The use of aminocaproic acid during pregnancy can be justified only under strict medical indications and under medical supervision. There are no reliable data on the safety of this drug for pregnant women, so its use should be based on the assessment of potential risks and benefits for the mother and fetus.

If a pregnant woman has a medical indication for the use of aminocaproic acid, the physician should assess the risk of possible complications and decide on an appropriate treatment based on the individual clinical situation.

Contraindications

1. Hypersensitivity: People with known hypersensitivity to aminocaproic acid or any other components of the drug should avoid its use.
2. Thrombosis and thromboembolism: The drug should be used with caution in patients with clotting disorders and in those at increased risk of thrombosis or thromboembolism.
3. Cardiovascular Disease: In the presence of serious cardiovascular disease such as atrial fibrillation or myocardial infarction, the use of aminocaproic acid may be limited or require special caution.
4. Cerebrovascular disease: Patients with a history of cerebrovascular disease, such as stroke or transient ischemic attack, should use aminocaproic acid with caution.
5. Renal disorders: Due to the fact that aminocaproic acid is metabolized and excreted by the kidneys, its use may require dose adjustment in patients with impaired renal function.
6. Pregnancy and lactation: Information on the use of aminocaproic acid during pregnancy and lactation is limited. Therefore, use should be performed only when strictly indicated and under the supervision of a physician.
7. Pediatric Age: Instructions for use may contain age restrictions for children, so please read the directions and instructions carefully.

Side effects Aminocaproic acid

1. Systemic reactions: May include nausea, vomiting, diarrhea, abdominal pain, arterial hypotension, and dizziness.
2. Cardiovascular reactions: May include thromboembolic complications, including thrombosis and embolism.
3. Blood reactions: Blood coagulation disorders may occur, which may lead to thrombocytopenia or hypercoagulability.
4. Liver reactions: Increased activity of hepatic enzymes and jaundice of the skin may occur.
5. Allergic Reactions: May include skin rash, itching, urticaria, or angioedema.
6. Other rare reactions: May include headache, hypertension, insomnia or drowsiness, seizures, arrhythmias, and anemia.

Overdose

1. Thrombosis and thromboembolism: Overdose may lead to increased blood clotting and the development of thrombosis or thromboembolism, which can lead to serious complications such as myocardial infarction, stroke or pulmonary embolism.
2. Hypercoagulability: Increased blood clotting may lead to the development of hypercoagulability, which may be particularly dangerous in patients with thrombophilia or other clotting disorders.
3. Increase in blood pressure: High doses of aminocaproic acid may cause an increase in blood pressure, which can be especially dangerous for patients with hypertension or heart and vascular disease.
4. Increased likelihood of bleeding: Periodontal bleeding, nosebleeds and other bleeding may occur due to impaired hemostasis due to aminocaproic acid overdose.

Interactions with other drugs

1. Prothrombin drugs: Aminocaproic acid may increase the effect of anticoagulants such as heparin or warfarin. This may lead to increased bleeding time and risk of bleeding. Therefore, blood coagulation indices should be cautiously monitored during concomitant use.
2. Antifibrinolytic drugs: Combined use of aminocaproic acid with other antifibrinolytic drugs, such as tranexamic acid, may result in an increase in their action, which may increase the risk of thrombosis.
3. Aminoglycoside antibiotics: Aminocaproic acid may increase the nephrotoxic effects of aminoglycoside antibiotics such as gentamicin or amikacin, therefore their concomitant use may require cautious monitoring of renal function.
4. Anticonvulsants: The use of aminocaproic acid with anticonvulsants such as phenytoin or carbamazepine may reduce their effectiveness because aminocaproic acid may compete with them for binding sites on plasma proteins.
5. Drugs affecting renal function: Aminocaproic acid may have adverse effects on renal function, especially when administered in high doses or in patients with pre-existing renal dysfunction. Therefore, it should be used with caution in patients taking other drugs that may also affect renal function.