Aminocaproic acid

INSTRUCTION FOR MEDICAL USE OF THE MEDICINAL PRODUCT AMINOCAPRONIC ACID (AMINOCAPRONIC ACID)

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 odourless powder.

Pharmacotherapeutic group. Antihemorrhagic agents. Fibrinolysis inhibitors.

ATC code B02A A01.

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 kinases on fibrinolytic processes, neutralizes the effects of kallikrein, trypsin, and hyaluronidase, and reduces capillary permeability.

Aminocaproic acid exerts antiallergic and antiviral effects and enhances the liver's detoxifying function. It inhibits proteolytic activity associated with the influenza virus. Aminocaproic acid exerts an inhibitory effect on various stages of virus interaction with susceptible cells and also suppresses proteolytic processing of hemagglutinin. As a result, a functionally active viral protein responsible for the infectivity of the influenza virus is not formed, and the yield of progeny infectious virus is reduced.

Aminocaproic acid not only demonstrates antiviral activity but also improves certain cellular and humoral parameters of specific immune defense during 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 is practically not bound to plasma proteins. Partially (10–15%) undergoes biotransformation in the liver; the remainder is primarily excreted by the kidneys in unchanged form. Approximately 60% of the administered dose is eliminated from the body within 24 hours (with normal renal function).

Accumulation of the drug may occur in case of impaired urinary excretion function.

Clinical characteristics.

Indications.

Prevention and treatment of parenchymal hemorrhages, mucosal hemorrhages, 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 thrombolytic agents and massive transfusion of stored blood. Symptomatic treatment of bleeding caused by thrombocytopenia and qualitative platelet insufficiency (dysfunctional thrombocytopenia).

Treatment and prevention of influenza and acute respiratory viral infections (ARVI) in children and adults.

Contraindications.

Hypersensitivity to aminocaproic acid, predisposition to thrombosis and thromboembolic disorders, thromboembolism, coagulopathy due to disseminated intravascular coagulation (DIC), kidney diseases with impaired renal function, renal failure, hematuria, pregnancy, labor, breastfeeding, severe form of ischemic heart disease, cerebrovascular disorders.

Interaction with other medicinal products and other forms of interaction.

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

Use with caution in patients taking retinoids.

Special precautions.

Use with caution in patients with heart diseases and hepatic insufficiency.

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

For menorrhagia, the drug is effective when taken from the first to the last day of menstruation.

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

It is recommended to avoid fatty foods during treatment with this 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 risk of thromboembolic complications.

If it is necessary to use the medicinal product, 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 possible adverse reactions (e.g., dizziness).

Method of Administration and Dosage

Administer orally, during or after meals, dissolving the powder in sweetened water or taking it with sweetened water.

The daily dose for adults should be divided into 3–6 doses; for children — into 3–5 doses.

Mildly increased fibrinolytic activity.
Adults are usually prescribed a daily dose of 5–24 g (5–24 packets).

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

Acute bleeding (including gastrointestinal).
For adults: administer 5 g (5 packets), then 1 g (1 packet) every hour (for no more than 8 hours) until bleeding stops completely. The daily dose for children with acute blood loss: under 1 year — 6 g (6 packets), 2–4 years — 6–9 g (6–9 packets), 5–8 years — 9–12 g (9–12 packets), 9–10 years — 18 g (18 packets).

Subarachnoid hemorrhage.
For adults: administer a daily dose of 6–9 g (6–9 packets).

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.

Metrorrhagia associated with intrauterine contraceptive devices.
Administer 3 g (3 packets) every 6 hours.

Prevention and control of bleeding during dental procedures.
For adults: administer 2–3 g (2–3 packets) 3–5 times daily.

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

Influenza, acute respiratory viral infections in children and adults.

The medicinal product should be used orally and locally. For oral administration, dissolve the preparation at a rate of 1 g (1 packet) of aminocaproic acid in two tablespoons of sweetened boiled water to obtain a 5% solution.

Oral dosage:

• Children under 2 years of age — 1–2 g (1–2 packets) per day (20–40 ml of 5% solution) — 1–2 teaspoons 4 times daily (0.02–0.04 g/kg — single dose); may be added to food or drinks;
• Children aged 2–6 years — 2–4 g (2–4 packets) per day (40–80 ml of 5% solution) — 1–2 tablespoons 4 times daily;
• Children aged 7–10 years — 4–5 g (4–5 packets) per day, taken with water, or with food or drinks;
• Adolescents and adults — 5–8 g (5–8 packets) per day — 1–2 packets 4–5 times daily, taken with water, or with food or drinks.

To prepare and measure the solution more accurately, it is advisable to use a 10 or 20 ml medical syringe without a needle.

Simultaneously, local use of aminocaproic acid is recommended. Every 3 hours, insert cotton swabs thoroughly moistened with a 5% solution of aminocaproic acid prepared in unsweetened water into each nostril for 5–10 minutes, or instill (drop) 3–5 drops of this solution into each nostril at the specified intervals. The solution may also be used for inhalations.

In severe hyper-toxic forms of influenza or ARVI, the dosage may be increased to the maximum levels recommended for children with mildly increased fibrinolytic activity.

For treatment of influenza and ARVI in adults, aminocaproic acid may be used at the same dosages as for adolescents. Aminocaproic acid may be used in combination with other antiviral agents, interferon, and its inducers, if necessary.

Intranasal instillations of aminocaproic acid solution (3–4 times daily) are advisable during the epidemic period for prophylaxis, which may be supplemented by oral administration (as in treatment) in infection foci upon contact with an infected person.

The duration of oral administration of aminocaproic acid for influenza and ARVI is 3–7 days.

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

Children.
The medicinal product may be used in children from the first year of life.

Overdose.

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

Treatment: discontinue the drug, symptomatic therapy.

Adverse reactions.

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

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

Gastrointestinal system: nausea, vomiting, diarrhea.

Blood clotting 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.

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

Immune system: possible hypersensitivity reactions, skin rash.

Urinary system: acute renal failure, myoglobinuria.

Musculoskeletal system: rhabdomyolysis.

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

Shelf life. 2 years.

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

Keep out of reach of children.

Packaging. Oral powder, 1 g per sachet, 10 sachets in a pack (1×10) or 10 double-packed sachets (2×5) in a box.

Availability. Over-the-counter.

Manufacturer. LIMITED LIABILITY COMPANY "CORPORATION "ZDOROVIYA".

Manufacturer's address and place of business.

Ukraine, 61013, Kharkiv region, city of Kharkiv, Shevchenko Street, building 22.