Aminocaproic acid

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

Composition:

Active substance: aminocaproic acid;

1 ml of solution contains 50 mg of aminocaproic acid;

Excipients: sodium chloride, water for injections.

Pharmaceutical form. Infusion solution.

Main physicochemical properties: clear, colorless solution.

Theoretical osmolarity 689 mosmol/L.

Pharmacotherapeutic group. Antihemorrhagic agents. Fibrinolysis inhibitors.
ATC code B02A A01.

Pharmacological properties.

Pharmacodynamics.

Aminocaproic acid solution exerts hemostatic and antifibrinolytic effects in bleeding caused by increased fibrinolysis. Its action is associated with blockade of plasminogen activators and partial inhibition of plasmic activity. The drug also inhibits biogenic polypeptides – kinins. It promotes stabilization of fibrin and its deposition within the vascular bed, and induces aggregation of platelets and erythrocytes.

Aminocaproic acid exerts anti-allergic and antiviral effects, and enhances the liver's detoxification function. It inhibits proteolytic activity associated with the influenza virus. Aminocaproic acid exerts an inhibitory effect on the early stages of virus interaction with susceptible cells and also suppresses the proteolytic activity of hemagglutinin. As a result, functionally active influenza virus protein responsible for its infectious activity is not formed, and the amount of progeny infectious virus is reduced. Aminocaproic acid not only demonstrates antiviral activity but also improves certain cellular and humoral parameters of specific and non-specific body defense during respiratory viral infections.

Pharmacokinetics.

After intravenous administration, the effect of aminocaproic acid appears within 15–20 minutes. It is rapidly excreted by the kidneys; 40–60% of the administered dose is eliminated in urine within 4 hours. In case of impaired renal excretory function, blood concentration of aminocaproic acid increases significantly.

Clinical characteristics.

Indications.

Bleeding after surgical operations and various pathological conditions associated with
increased fibrinolytic activity of blood and tissues.

Used to prevent the development of secondary hypofibrinogenemia during massive transfusions of preserved blood.

For treatment and prevention of influenza and acute respiratory viral infections in children and adults.

Contraindications.

Hypersensitivity to the drug. Predisposition to thrombosis and thromboembolic disorders; thromboembolism; coagulopathies due to disseminated intravascular coagulation; kidney diseases with impaired renal function; renal failure; hematuria; pregnancy, childbirth, and breastfeeding period; severe form of ischemic heart disease. Cerebrovascular disorders.

Interaction with other medicinal products and other types of interactions.

The effect of the drug is weakened by anticoagulants and direct-acting and indirect-acting antiplatelet agents. Concurrent use with estrogen-containing contraceptives and blood coagulation factor IX increases the risk of thromboembolism. Use with caution in patients taking retinoids (including tretinoin).

Special precautions for use.

Coagulogram monitoring is required during intravenous administration, especially in patients with ischemic heart disease, after myocardial infarction, or with pathological liver conditions. The drug is contraindicated in cases of hematuria due to the risk of developing acute renal failure (see section "Contraindications"). It is recommended to avoid fatty foods during treatment with this drug.

Use with caution in patients with heart diseases. If it is necessary to administer the drug to patients with cardiac conditions, monitoring of plasma creatine phosphokinase levels is recommended. Do not use any remaining medication. This medicinal product contains 15.4 mmol (or 354.05 mg)/100 ml dose of sodium. Caution is advised when administering to patients on a sodium-controlled diet.

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 use is necessary, breastfeeding should be discontinued.

Ability to influence the 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 affecting the central nervous system.

Method of Administration and Dosage

Aminocaproic acid solution is intended for oral or intravenous use.

For oral administration in adults, administer 5 g (100 mL) of the drug initially, followed by 1 g (20 mL) every hour for 8 hours, until complete cessation of bleeding.

If rapid effect is required (e.g., acute hypofibrinogenemia), administer up to 100 mL of solution (5 g) intravenously by drip infusion at a rate of 50–60 drops per minute over 15–30 minutes. During the first hour, administer 4–5 g; in cases of prolonged bleeding—until complete cessation—administer 1 g every hour, but not for more than 8 hours.

In case of recurrent bleeding, repeat administration of the 5% solution.

Children.

For moderate increase in fibrinolytic activity, administer aminocaproic acid once daily to children at a dose of 0.05 g/kg body weight per day. The dose depending on the child's age is as follows:

• under 1 year: single dose – up to 2.5 mL, daily dose – 15 mL;
• 2 to 6 years: single dose – 2.5–5 mL, daily dose – 15–30 mL;
• 7 to 10 years: single dose – 5–7 mL, daily dose – 30–45 mL;
• 11 to 18 years: single dose – 7–14 mL, daily dose – 45–90 mL.

Doses for children in acute bleeding are as follows:

• under 1 year: single dose – 5 mL, daily dose – 30 mL;
• 2 to 4 years: single dose – 5–7.5 mL, daily dose – 30–45 mL;
• 5 to 8 years: single dose – 7.5–10 mL, daily dose – 45–60 mL;
• 9 to 10 years: single dose – 15 mL, daily dose – 90 mL;
• 11 to 14 years: single dose – 20 mL, daily dose – 120 mL;
• 15 to 18 years: single dose – 28 mL, daily dose – 160 mL.

Duration of treatment is 3 to 14 days.

For prevention and treatment of influenza and acute respiratory viral infections (ARVI), the drug should be used
orally and locally (0.5−1.0 mL into the nose 3−4 times daily).

Oral administration in children:

• children under 2 years – 1–2 g (20–40 mL of 5% solution per day), i.e., 1–2 teaspoons 4 times daily (0.02–0.04 g/kg as a single dose); may be added to food or drinks;
• children aged 2 to 6 years – 2–4 g (40–80 mL of 5% solution per day) – 2–4 teaspoons 4 times daily;
• children aged 7 years and older and adults – 4–5 g (80–100 mL of 5% solution per day), divided into 4 doses per day.

For more accurate dosing, it is advisable to use a needle-free medical syringe with a volume of 10 or 20 mL.

Local application of aminocaproic acid is also justified. It is recommended to insert cotton swabs moistened with 5% aminocaproic acid solution into the nasal passages every 3–4 hours for 5–10 minutes, or to instill (administer by drops) 3–5 drops of the solution into each nostril at the same intervals.

Aminocaproic acid, if necessary, may be used in combination with other antiviral agents, interferon, and its inducers.

Intranasal instillations of aminocaproic acid (3–4 times daily) should be performed during the epidemic period for prophylaxis, supplemented by enteral (as in treatment) use of the drug in infection foci upon contact with an infected person.

Duration of oral administration of aminocaproic acid in 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 dose and prescribe a repeated course of treatment.

Children.

There are no data regarding restrictions on the use of the drug in children.

Overdose.

Symptoms: Sudden decrease in blood fibrinolytic activity. Pronounced adverse effects: dizziness, nausea, diarrhea, skin rash, orthostatic hypotension, seizures, headache, nasal congestion, acute renal failure, rhabdomyolysis, myoglobinuria. Increased adverse reactions, thrombus formation, embolism. Hemorrhages may occur with prolonged use (more than 6 days) of high doses (in adults – more than 24 g per day).

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

Adverse Reactions.

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

Gastrointestinal system: nausea, diarrhea, vomiting.

Hematological system: coagulation disorders; with prolonged use (more than 6 days) of high doses (in adults – more than 24 g per day) – hemorrhages.

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

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

Immune system: hypersensitivity reactions, including allergic reactions, rash.

General disorders: injection site reactions.

Urinary system: myoglobinuria, acute renal failure.

Other: rhabdomyolysis. If the infusion rate is exceeded, bradycardia, extrasystoles, chills, and fever may occur.

Shelf life. 3 years.

Storage conditions.

Store at a temperature not exceeding 25 °C. Keep in the original packaging. Store out of reach of children. Store bottles in an upright position.

Packaging.

100 ml in glass bottles.

Prescription status.

Prescription only.

Manufacturer.

Yuria-Pharm LLC.

Manufacturer's address and place of business.

108, Kobzarska Street, Cherkasy, Cherkasy region, 18030, Ukraine.

Tel.: (044) 281-01-01.