Aminocaproic acid

INSTRUCTION FOR MEDICAL USE OF THE MEDICINAL PRODUCT AMINOCAPROIC ACID

Composition:

Active substance: aminocaproic acid;

1 tablet contains 500 mg of aminocaproic acid;

Excipients: colloidal anhydrous silicon dioxide, povidone (polyvinylpyrrolidone), sodium croscarmellose, magnesium stearate.

Pharmaceutical form. Tablets.

Main physicochemical properties: white, flat cylindrical tablets with beveled edges and a score line. Marbling on the surface of the tablets is permissible.

Pharmacotherapeutic group.

Antihemorrhagic agents. Inhibitors of fibrinolysis. ATC code B02A A01.

Pharmacological Properties

Pharmacodynamics

Aminocaproic acid inhibits fibrinolysis in blood and tissues. By blocking plasminogen activators and partially suppressing the action of plasmin, it exerts a specific hemostatic effect in bleeding associated with increased fibrinolysis. In addition, aminocaproic acid inhibits the action of streptokinase, urokinase, and tissue kinases, which promote fibrinolysis activation; neutralizes the effects of kallikrein, trypsin, hyaluronidase, reduces capillary permeability, and suppresses antibody formation. Due to inhibition of fibrinolysis, it demonstrates a broad spectrum of pharmacological activity, including immunosuppressive, anti-inflammatory, and antiallergic effects, providing high therapeutic efficacy in various diseases accompanied by fibrinolysis activation.

Aminocaproic acid inhibits pathological proteolytic activity caused by the influenza virus, and suppresses viral replication by acting at the early stages of virus interaction with susceptible cells. It improves certain cellular and humoral parameters of specific and non-specific defense in respiratory viral infections. The drug is low-toxic.

Pharmacokinetics

Aminocaproic acid is well absorbed after oral administration. Its concentration in blood reaches maximum levels within 1–2 hours. It is actively excreted unchanged by the kidneys—approximately 40–60% of aminocaproic acid is eliminated within 4 hours.

Clinical characteristics.

Indications. Prevention and treatment of parenchymal hemorrhages, hemorrhages from mucous membranes, menorrhagia, bleeding from erosions and gastric or intestinal ulcers. Prevention of bleeding during surgery on the liver, lungs, and pancreas. Various forms of hyperfibrinolysis, including that associated with the use of thrombolytic agents and massive transfusion of stored blood. As a symptomatic agent—bleeding caused by thrombocytopenia and qualitative platelet insufficiency (dysfunctional thrombocytopenia).

Contraindications. Hypersensitivity to the drug, predisposition to thrombosis and thromboembolic disorders, disseminated intravascular coagulation syndrome, macrohematuria, kidney diseases with impaired renal function, renal failure, hematuria, severe form of ischemic heart disease, cerebrovascular disorders.

Interaction with other medicinal products and other types of interactions.

Aminocaproic acid tablets may be used concomitantly with infusions of glucose solutions, hydrolysates, and anti-shock solutions.

When taken orally, it combines well with thrombin. The effect of the drug is diminished by antiplatelet agents and both direct and indirect-acting anticoagulants. Concurrent use with estrogen-containing contraceptives and clotting factor IX increases the risk of thromboembolism.

Use with caution in patients taking retinoids.

Special precautions for use.

Use with caution in patients with heart disease, and in cases of hepatic and/or renal insufficiency.

During treatment with the drug, monitoring of blood fibrinolytic activity and fibrinogen levels is recommended.

The use of the drug is not recommended in cases of hematuria (due to the risk of developing acute renal failure).

For menorrhagia, administration from the first to the last day of menstruation is effective.

Fatty foods should be avoided during treatment with the drug.

Use during pregnancy or breastfeeding. The drug is contraindicated during pregnancy. Its use in women for prevention of excessive blood loss during childbirth is not advisable due to the possible development of thromboembolic complications.

If it is necessary to use the drug, breastfeeding should be discontinued.

Ability to affect reaction speed when driving or operating machinery. During treatment, patients should refrain from driving vehicles or engaging in potentially hazardous activities due to possible adverse reactions affecting the central nervous system.

Administration and Dosage

Aminocaproic acid tablets are intended for oral administration. The daily dose for adults should be divided into 3–6 doses, and for children into 3–5 doses.

Mildly expressed increase in fibrinolytic activity of blood. Adults are usually prescribed a daily dose of 5–24 g (10–48 tablets).

The daily dose for children aged 3–6 years is 3–6 g (6–12 tablets), for children aged 7–10 years – 6–9 g (12–18 tablets). For adolescents, the maximum daily dose is 10–15 g (20–30 tablets).

Acute bleeding (associated with increased fibrinolytic activity, including gastrointestinal bleeding). The initial dose for adults is 5 g (10 tablets) within the first hour of treatment, followed by 1–2 g (2–4 tablets) every hour for 8 hours, or until bleeding stops. The daily dose for children with acute hemorrhage: aged 3–4 years – 6–9 g (12–18 tablets), 5–8 years – 9–12 g (18–24 tablets), 9–10 years – 18 g (36 tablets).

Traumatic hyphema. Administer at a dose of 0.1 g/kg body weight every 4 hours (but not exceeding 24 g/day) for 5 days.

Menometrorrhagia associated with intrauterine contraceptive devices. Administer 3 g (6 tablets) every 6 hours.

Prevention and control of bleeding during dental procedures. Adults should be prescribed 2–3 g (4–6 tablets) 3–5 times daily.

For adults, the average daily dose is 10–18 g (20–36 tablets), and the maximum daily dose is 24 g (48 tablets). The treatment course lasts 3–14 days.

Children under 3 years of age should be administered the drug in another pharmaceutical form.

In conditions associated with various types of hyperfibrinolysis, the duration of oral administration of aminocaproic acid depends on the clinical picture and severity of the disease and is determined individually by the physician. The dose upon repeated administration depends on the condition of the blood coagulation system. The physician may adjust the dose and prescribe a repeated course of treatment.

Children. The drug may be administered to children aged 3 years and older according to the dosage recommendations specified in the section "Administration and Dosage."

Overdose.

Symptoms: Increased incidence of adverse reactions, thrombus formation, embolism. With prolonged use (more than 6 days) of high doses (in adults – more than 24 g per day) – hemorrhages.

Treatment. In case of overdose, discontinue the drug and provide appropriate symptomatic therapy.

Adverse Reactions.

The drug is generally well tolerated; however, the following adverse reactions may occur.

Allergic reactions: hypersensitivity reactions are possible, including skin rashes, nasal congestion, and catarrhal symptoms of the upper respiratory tract.

Cardiovascular system: orthostatic hypotension, subendocardial hemorrhage, bradycardia, arrhythmias.

Gastrointestinal tract: nausea, diarrhea, vomiting.

Blood system: impaired blood coagulation, hemorrhages.

Central nervous system: headache, dizziness, tinnitus, seizures.

Urinary system: acute renal failure, myoglobinuria.

Musculoskeletal system: rhabdomyolysis.

Adverse effects are rare and dose-dependent; they usually resolve upon dose reduction.

Shelf life. 4 years.

Storage conditions. Store in the original packaging at a temperature not exceeding 25 °C.

Keep out of reach of children.

Packaging. 10 tablets in a blister pack, 2 blisters per carton, or 20 tablets in a container.

Prescription status. Prescription only.

Manufacturer. JSC "FITOFARM".

Manufacturer's address and place of business.

2 Sybirtseva Street, Bakhmut, Donetsk region, 84500, Ukraine.

Marketing Authorization Holder. JSC "FITOFARM".

Address of the Marketing Authorization Holder.

7, Verkhovnoyi Rady Avenue, Kyiv, 02100, Ukraine, floor 3, room 18.