AMINOCAPROIC ACID

INSTRUCTIONS FOR MEDICAL USE OF THE MEDICINAL PRODUCT AMINOCAPROIC ACID (ACIDUM AMINOCAPROICUM)

Composition:

Active substance: aminocaproic acid;

1 sachet contains 1 g of aminocaproic acid.

Pharmaceutical form.

Powder for oral administration.

Main physicochemical properties: white or almost white crystalline powder or colorless crystals.

Pharmacotherapeutic group.

Antihemorrhagic agents. Fibrinolysis inhibitors. ATC code B02AA01.

Pharmacological properties.

Pharmacodynamics.

A specific hemostatic agent used for bleeding caused by increased fibrinolysis.

The mechanism of specific action is due to competitive inhibition of plasminogen activators and partial inhibition of plasmin activity (at high doses), as well as inhibition of biogenic polypeptides—kinins.

It suppresses the activating effect of streptokinase, urokinase, and tissue kallikreins on fibrinolytic processes, neutralizes the effects of kallikrein, trypsin, and hyaluronidase, and reduces capillary permeability.

By inhibiting fibrinolysis, aminocaproic acid exhibits a broad spectrum of pharmacological activity, including immunosuppressive, anti-inflammatory, and antiallergic effects, providing high therapeutic efficacy in various diseases accompanied by activation of fibrinolysis.

Aminocaproic acid inhibits pathological proteolytic activity induced by the influenza virus, suppresses viral replication by acting at early stages of virus-cell interaction. It improves certain cellular and humoral parameters of specific and non-specific defense in respiratory viral infections.

Pharmacokinetics.

After oral administration, it is rapidly absorbed in the upper gastrointestinal tract. Maximum blood concentration in adults and adolescents is reached within 2–3 hours. It practically does not bind to plasma proteins. Partially (10–15%) undergoes biotransformation in the liver; the remainder is excreted by the kidneys predominantly unchanged. Within one day, approximately 60% of the administered dose is eliminated from the body (with normal kidney function).

In case of impaired renal excretory function, drug accumulation may occur.

Clinical characteristics.

Indications.

Prevention and treatment of parenchymal hemorrhages, hemorrhages from mucous membranes, menorrhagia, bleeding from gastric and intestinal erosions and 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 in bleeding caused by thrombocytopenia and qualitative platelet defects (dysfunctional thrombocytopenia).

Contraindications.

Increased individual sensitivity to aminocaproic acid, predisposition to thrombosis and thromboembolic disorders, thromboembolism, disseminated intravascular coagulation syndrome, macrohematuria, kidney diseases with impaired renal function, renal failure, hematuria, severe form of ischemic heart disease, cerebrovascular disorders, pregnancy, labor, breastfeeding.

Interaction with other medicinal products and other types of interactions.

When taken orally, combines well with thrombin. The effect of the drug is reduced by antiplatelet agents and direct and indirect-acting anticoagulants. Concomitant use with estrogen-containing contraceptives and coagulation 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 diseases and in cases of hepatic and/or renal insufficiency.

If administration of the drug is necessary for patients with heart diseases, monitoring of creatine phosphokinase levels in blood plasma is recommended.

The use of the drug is contraindicated in hematuria (due to the risk of developing acute renal failure).

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

During treatment with the drug, blood fibrinolytic activity and fibrinogen levels should be monitored.

It is recommended to avoid fatty foods during treatment with the drug.

Use during pregnancy or breastfeeding.

The drug is contraindicated during pregnancy. Its use in women for prophylaxis 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 influence reaction rate when driving or operating machinery.

During treatment, patients should refrain from driving vehicles and engaging in potentially hazardous activities due to the possibility of adverse reactions such as dizziness.

Dosage and Administration

Take orally during or after meals, dissolving the powder in sweetened water or drinking it with sweetened water. Divide the daily dose into 3–6 doses for adults and into 3–5 doses for children.

Mild increase in fibrinolytic activity.
Adults are usually prescribed a daily dose of 5–24 g (5–24 sachets).

For children under 1 year of age, the single dose is 0.05 g/kg of body weight (but not more than 1 g). The daily dose for children under 1 year is 3 g (3 sachets), for children aged 2–6 years — 3–6 g (3–6 sachets), for children aged 7–10 years — 6–9 g (6–9 sachets). For adolescents, the maximum daily dose is 10–15 g (10–15 sachets).

Acute bleeding (including gastrointestinal).
Administer 5 g (5 sachets) initially, followed by 1 g (1 sachet) every hour (for no more than 8 hours) until bleeding stops. The daily dose for acute bleeding in children under 1 year is 6 g (6 sachets), for children aged 2–4 years — 6–9 g (6–9 sachets), for children aged 5–8 years — 9–12 g (9–12 sachets), for children aged 9–10 years — 18 g (18 sachets).

Subarachnoid hemorrhage.
Administer a daily dose of 6–9 g (6–9 sachets) to adults.

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

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

Prevention and control of bleeding during dental procedures.
Administer 2–3 g (2–3 sachets) 3–5 times daily to adults.

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

The duration of treatment depends on the severity of the condition and is determined individually by the physician. The physician may also adjust the dose and prescribe a repeated course of treatment.

Children. The medicinal product can be used in pediatric practice.

Overdose.

Symptoms: intensification of adverse effects, thrombus formation, embolism. With prolonged use (more than 6 days) of high doses (over 24 g/day for adults) — hemorrhages.

Treatment: discontinue the drug, symptomatic therapy.

Adverse reactions.

The medicinal product is generally well tolerated, but the following adverse reactions may occur.

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

Gastrointestinal tract: nausea, vomiting, diarrhea.

Blood and lymphatic system: impaired blood coagulation; with prolonged use (more than 6 days) of high doses (in adults — more than 24 g per day) — hemorrhages.

Nervous system: headache, dizziness, tinnitus, seizures.

Immune system: possible hypersensitivity reactions, including skin rashes.

Respiratory system, thoracic organs and mediastinum: nasal congestion, catarrhal symptoms of upper respiratory tract.

Skeletal muscle system: myoglobinuria, rhabdomyolysis.

Urinary system: acute renal failure.

Adverse effects are rare and dose-dependent; they usually disappear when the dose is reduced.

Reporting of suspected adverse reactions

Reporting suspected adverse reactions after marketing authorization is of great importance. It allows continuous monitoring of the benefit-risk balance of the medicinal product. Healthcare professionals and patients or their legal representatives are encouraged to report all suspected adverse reactions and lack of efficacy via the Automated Pharmacovigilance Information System at the following link: https://aisf.dec.gov.ua/.

Shelf life. 5 years.

Storage conditions.

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

Keep out of reach of children.

The prepared solution should be stored in a refrigerator at 2–8 °C for no more than 36 hours.

Packaging.

1 g of powder in a sachet № 1.

1 g of powder in a sachet, 10 sachets in a cardboard box.

Availability category. Over-the-counter.

Manufacturer.

LLC "Istok-Plus".

Manufacturer's address and location of business activity.

4 Makarenka Street, Zaporizhzhia, 69032, Ukraine.