Aminocaproic acid-darnitsa
Ukraine
Table of Contents
INSTRUCTIONS FOR MEDICAL USE OF THE MEDICINAL PRODUCT AMINOCAPROIC ACID-DARNITSA (Acidum aminocapronicum-DARNITSA)
Composition:
Active substance: aminocaproic acid;
100 ml of solution contains 5 g of aminocaproic acid;
Excipients: sodium chloride, water for injections.
Pharmaceutical form. Infusion solution.
Main physicochemical properties: clear, colorless liquid.
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, promotes stabilization of fibrin and its deposition within the vascular bed, and induces aggregation of platelets and erythrocytes.
Aminocaproic acid exhibits antiallergic and antiviral effects and enhances hepatic detoxification function. The drug inhibits proteolytic activity associated with the influenza virus. Aminocaproic acid suppresses early stages of virus interaction with susceptible cells and also inhibits proteolytic processing of hemagglutinin. As a result, functionally active viral protein responsible for influenza virus infectivity 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 and non-specific body defense in respiratory viral infections.
Pharmacokinetics.
After intravenous administration, the effect manifests within 15–20 minutes. The drug is rapidly excreted by the kidneys: 40–60% of the administered dose is excreted in urine within 4 hours. In case of impaired renal excretory function, the concentration of aminocaproic acid in blood increases significantly.
Clinical characteristics.
Indications.
Surgical operations and pathological processes accompanied by increased fibrinolytic activity of blood and tissues.
For prevention of secondary hypofibrinogenemia during massive transfusions of preserved blood.
Contraindications.
Thromboembolism, coagulopathies due to disseminated intravascular coagulation, renal failure, childbirth, cerebral circulation disorders, predisposition to thrombosis, hematuria, severe form of ischemic heart disease, hypersensitivity to components of the drug, predisposition to thromboembolic diseases, kidney diseases with impaired function.
Interaction with other medicinal products and other types of interactions.
The effect of the drug is reduced by anticoagulants and direct-acting and indirect-acting antiplatelet agents.
Concomitant 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.
Use with caution in patients with heart diseases. If it is necessary to administer the drug to patients with cardiac disorders, monitoring of plasma creatine phosphokinase levels is recommended. Administration of the drug requires control of coagulogram, especially in ischemic heart disease, after myocardial infarction, and in pathological processes in the liver. The drug is contraindicated in hematuria due to the risk of developing acute renal failure.
Fatty foods should be excluded during treatment with this medication.
Do not use any remaining drug.
This medicinal product contains sodium. If the patient is on a sodium-controlled diet, caution should be exercised when using this medicinal product.
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 drug, breastfeeding should be discontinued.
Ability to affect reaction speed when driving or operating machinery.
Data regarding the effect of the drug on reaction speed when driving or operating machinery are lacking, as the drug is administered under hospital conditions.
Method of Administration and Dosage
The medicinal product is administered intravenously.
Dosage
In cases requiring rapid effect (acute hypofibrinogenemia), administer up to 100 mL of the 5% solution by drip 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 – up to complete cessation of bleeding – administer 1 g hourly, but not more than 8 g in total. In cases of recurrent bleeding, repeat administration of the medicinal product with 4-hour intervals, but not more frequently than every 8 hours.
Children
In cases of moderate increase in fibrinolytic activity, the medicinal product "Aminocaproic Acid-Darnitsia" should be administered once daily at a dose of 0.05 g/kg body weight per day. The dosage depending on age is as follows:
- Children under 1 year: single dose – up to 2.5 mL, daily dose – 15 mL;
- Children aged 2 to 6 years: single dose – 2.5–5 mL, daily dose – 15–30 mL;
- Children aged 7 to 10 years: single dose – 5–7 mL, daily dose – 30–45 mL;
- Children aged 11 to 18 years: single dose – 7–14 mL, daily dose – 45–90 mL.
In cases of acute bleeding, dosages are as follows:
- Children under 1 year: single dose – 5 mL, daily dose – 30 mL;
- Children aged 2 to 4 years: single dose – 5–7.5 mL, daily dose – 30–45 mL;
- Children aged 5 to 8 years: single dose – 7.5–10 mL, daily dose – 45–60 mL;
- Children aged 9 to 10 years: single dose – 15 mL, daily dose – 90 mL;
- Children aged 11 to 14 years: single dose – 20 mL, daily dose – 120 mL;
- Children aged 15 to 18 years: single dose – 28 mL, daily dose – 160 mL.
Duration of treatment: 3 to 14 days.
Method of Administration
Do not insert needle(s) into areas of the polymer flask not intended for this purpose; use only sterile ports!
For infusion therapy, follow this procedure:
- Remove the protective plastic cap with tamper-evident seal (if present).
- Tear off protective valve(s) № 1 as shown in Fig. 1 and Fig. 2 (the manufacturer may use different types and materials for protective valves).
- Remove the cap from the needle and insert it into any of the special ports № 2 of the infusion medicinal product flask (see Fig. 1 and Fig. 2).
- The other sterile port may be used to introduce other medicinal products into the infusion flask (№ 4, see Fig. 3), or, if necessary, to insert a venting needle to improve flow rate (№ 4, see Fig. 3).
- Hang the flask using the special ring № 3 located at the bottom of the flask (see Fig. 3).
Children
The medicinal product may be used in pediatric practice.
Overdose
Symptoms: Exacerbation of adverse reactions such as dizziness, nausea, diarrhea, skin rash, orthostatic hypotension, seizures, headache, nasal congestion, acute renal failure, rhabdomyolysis, myoglobinuria, hypercoagulability, enhanced thrombosis, embolism. Sudden decrease in blood fibrinolytic activity. 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 administration of the medicinal product and provide appropriate symptomatic therapy. To prevent increased thrombosis, administer Reosorbilact, 0.9% sodium chloride solution, or Ringer's solution. If indicated, additional administration of dipyridamole or other anticoagulant medicinal products may be considered.
Adverse reactions.
Respiratory, thoracic and mediastinal disorders: nasal congestion, catarrhal symptoms of the upper respiratory tract.
Gastrointestinal disorders: nausea, diarrhea, vomiting.
Renal and urinary disorders: myoglobinuria, acute renal failure.
Nervous system disorders: headache, dizziness, tinnitus, seizures.
Cardiovascular disorders: orthostatic hypotension, subendocardial hemorrhage, bradycardia, arrhythmia.
Blood and lymphatic system disorders: coagulation disorders; with prolonged use (more than 6 days) of high doses (in adults – more than 24 g per day) – hemorrhage.
Immune system disorders: hypersensitivity reactions, including allergic reactions.
Skin and subcutaneous tissue disorders: skin rash.
Musculoskeletal and connective tissue disorders: rhabdomyolysis.
If the infusion rate is exceeded, bradycardia, extrasystoles, chills, and increased body temperature may occur.
Reporting of suspected adverse reactions.
Reporting of suspected adverse reactions after medicinal product authorization is an important procedure. It allows continuous monitoring of the benefit-risk ratio of the medicinal product. Healthcare professionals should report any suspected adverse reactions through the national reporting system.
Shelf life. 3 years.
Storage conditions.
Store in the original packaging at a temperature not exceeding 25 °C. Do not freeze.
Keep out of reach and sight of children.
Packaging.
100 ml in bottles; 100 ml in a bottle, 1 bottle in a pack.
Prescription status. Prescription only.
Manufacturer. JSC "Pharmaceutical Company "Darnytsia".
Manufacturer's name and address of the place of business.
13, Borispilska Street, Kyiv, 02093, Ukraine.