Aminocaproic acid-SOLOfarm - instructions for use, dose, side effects, contraindications

Aminocaproic acid refers to the synthetic analogues of lysine. It inhibits fibrinolysis, competitively saturating the lysine-binding receptors, through which plasminogen (plasmin) binds to fibrinogen (fibrin). The drug also inhibits biogenic polypeptides-kinins (inhibits the activating action of streptokinase, urokinase, tissue kinases for fibrinolysis), neutralizes the effects of kallikrein, trypsin, and hyaluronidase, and reduces the permeability of capillaries. Aminocaproic acid has anti-allergic activity, enhances the detoxifying function of the liver, inhibits antibody formation.

Pharmacokinetics:With intravenous administration, the effect is manifested after 15-20 minutes. The drug is quickly excreted by the kidneys - 40-60% of the administered amount after 4 hours is excreted in the urine unchanged.If the excretory function of the kidneys is disturbed, the concentration of aminocaproic acid in the blood increases significantly.

Indications:

- Bleeding (hyperfibrinolysis, hypo- and afibrinogenemia).

- Bleeding during surgical interventions and pathological conditions accompanied by increased fibrinolytic activity of blood (for neurosurgical, intracavitary, thoracic, gynecological and urological operations, including prostate, lung, pancreas, tonsillectomy, after dental interventions, in operations with using the device of artificial circulation, in operations on the vessels in the region of the ear, throat, nose).

- Diseases of internal organs with hemorrhagic syndrome.

- Premature detachment of the placenta, prolonged retention in the uterine cavity of the dead fetus, complicated abortion.

- Prevention of secondary hypophybrinogenemia in massive transfusions of canned blood.

Contraindications:

Hypersensitivity to the drug, a tendency to thrombosis and thromboembolic diseases, hypercoagulation (thrombosis, thromboembolism), coagulopathy due to diffuse intravascular coagulation,disorders of cerebral circulation, pregnancy, the period of breastfeeding.

Carefully:Arterial hypotension, bleeding from the upper urinary tract (due to the risk of intracranial obstruction due to thrombosis of the glomerular capillaries or the formation of clots in the lumen of the pelvis and ureters, the use in this case is possible only if the expected benefit exceeds the potential risk), subarachnoid hemorrhage, hepatic insufficiency, renal dysfunction, children under 1 year of age, valvular heart disease (due to lack of clinical data on safety and efficacy).

Pregnancy and lactation:

The use of the drug during pregnancy is contraindicated. Data on the use of aminocaproic acid in pregnant women are limited. In animal studies, fertility disorders and a teratogenic effect were detected with aminocaproic acid.

There is no data on the excretion of aminocaproic acid in breast milk, and therefore, during the period of treatment, breastfeeding should be abandoned.

Dosing and Administration:

Intravenously drip.If it is necessary to achieve a rapid effect (acute fibrinogenemia), inject up to 100 ml of 50 mg / ml solution at a rate of 50-60 drops per minute for 15-30 minutes. During the first hour, 4.0-5.0 g (80-100 ml) is administered and then, if necessary, 1.0 g (20 ml) every hour for about 8 hours or until the bleeding is completely stopped. In the case of continuing or repeated bleeding, infusions are repeated every 4 hours.

The daily intake for adults is 5.0-30.0 g.

Children, at the rate of 100 mg / kg - in 1 hour, then 33 mg / kg / h; the maximum daily dose is 18 g / m²surface of the body. The daily dose for children under 1 year is 3.0 g; 2-6 years old - 3,0-6,0 g; 7-10 years - 6.0-9.0 g; from 10 years - both for adults. In acute blood loss: children under 1 year - 6.0 g, 2-4 years - 6.0-9.0 g, 5-8 years - 9.0-12.0 g, 9-10 years - 18.0 d. The duration of treatment is -3-14 days.

Side effects:

The undesirable reactions observed in patients are listed below. The incidence of adverse reactions was classified as follows: very frequent (≥ 10%), frequent (1-10%), infrequent (0.1-1%), rare (0.01-0.1%), very rare (<0 , 01%) and an unknown frequency.

General disorders and disorders at the site of administration: often - general weakness, pain and necrosis at the injection site; infrequently - edema, skin rash, itchy skin.

Immune system disorders: infrequently - allergic and anaphylactoid reactions; unknown frequency - maculopapular rashes.

Heart Disease: infrequently bradycardia.

Vascular disorders: often - arterial hypotension, orthostatic hypotension: rarely - peripheral ischemia; unknown frequency - subendocardial hemorrhage, thrombosis.

Disorders from the gastrointestinal tract: often - abdominal pain, diarrhea, nausea, vomiting.

Violations from the blood and lymphatic system: infrequently - agranulocytosis, a violation of coagulation; unknown frequency - leukopenia, thrombocytopenia.

Disorders from the musculoskeletal system and connective tissue: infrequently - muscle weakness, myalgia; rarely - increased activity of creatine phosphokinase (CK), myositis; unknown frequency - myopathy, myoglobinuria, rhabdomyolysis.

Impaired nervous system: often - dizziness, headache; very rarely - confusion, convulsions, delirium, hallucinations, intracranial hypertension, stroke, fainting.

Disturbances from the respiratory system, organs of the thorax and mediastinum: often - nasal congestion; infrequently - shortness of breath: rarely - thromboembolism of the pulmonary artery; an unknown frequency - inflammation of the upper respiratory tract.

Disorders from the side of the organ of vision: rarely - decreased vision, lacrimation.

Hearing disorders and labyrinthine disturbances: often - noise in the ears.

Disorders from the kidneys and urinary tract: unknown frequency - an increase in urea in the blood serum, acute renal failure, renal colic, impaired renal function.

Violations of the genitals and breast: an unknown frequency - dry ejaculation.

Overdose:

Symptoms: arterial hypotension, cardiac and acute renal failure, convulsions, in some rare cases, possible hypercoagulable with a risk of thrombosis and embolism.

To correct the increased clotting of blood, streptokinase, urokinase, fibrinolysin and heparin are recommended.

Treatment: discontinuation of the drug, symptomatic therapy.

Aminocaproic acid is excreted in hemodialysis and peritoneal dialysis.

Interaction:

You can combine with the introduction of hydrolysates, solutions of dextrose (glucose), anti-shock solutions. In acute fibrinolysis, additionally, fibrinogen should be administered at an average daily dose of 2.0-4.0 g (maximum dose of 8.0 g).

Do not mix aminocaproic acid solution with solutions containing levulose, penicillin, and blood products.

Decrease in efficacy with simultaneous reception of anticoagulants of direct and indirect action, antiplatelet agents.

The simultaneous use of aminocaproic acid with preparations of coagulation factors II, VII, IX and X in combination [prothrombin complex] may be accompanied by an increased risk of thrombosis.

Do not add any medications to the aminocaproic acid solution.

Special instructions:

Aminocaproic acid inhibits the action of plasminogen activators and, to a lesser extent, plasmin activity. The drug should not be prescribed without a specific diagnosis and / or laboratory confirmation of hyperfibrinolysis.

When prescribing the drug, it is necessary to establish a source of bleeding and to control the fibrinolytic activity of the blood and the concentration of fibrinogen in the blood.

With intravenous administration, coagulogram monitoring is necessary, especially in coronary heart disease, after myocardial infarction, in pathological processes in the liver.

The use of aminocaproic acid in women is not recommended for the purpose of preventing increased blood loss during childbirth due to the possibility of thromboembolic complications in the postpartum period.

In rare cases, after prolonged use, lesions of skeletal muscles with necrosis of muscle fibers were recorded. Clinical manifestations can range from mild myalgia with weakness and fatigue to severe proximal myopathy with rhabdomyolysis, myoglobinuria, and acute renal failure. In this case, there is an increase in the activity of muscle enzymes in the blood serum, primarily CFC. Therefore, it is necessary to monitor the activity of CK in patients during prolonged therapy. In case of an increase in the activity of CKK, treatment with the drug should be discontinued. When myopathy occurs, the possibility of myocardial damage must be considered.

With rapid administration, it is possible to develop arterial hypotension, bradycardia, and cardiac rhythm disturbances.

The use of aminocaproic acid may alter the results of studies of platelet function.

Effect on the ability to drive transp. cf. and fur:

Data are not available due to the exclusive use of the drug in a hospital setting.

Form release / dosage:

Solution for infusions 50 mg / ml.

Packaging:

For 100 or 250 ml in polypropylene bottles (does not contain PVC), from polypropylene for infusion and injection preparations in accordance with the requirements of the European Pharmacopoeia of the current edition.

Vials are of 2 types.

Type 1 (Polyflac) - bottles with a self-falling body, with a scale and hinge holder, sealed with welded polypropylene caps. Caps can be with 2 separate sterile ports, closed protective polypropylene stoppers, or have 2 sterile ports covered with protective aluminum foil. In the case of 2 separate sterile ports, the sterility of the other port is preserved when one port is opened.

Type 2 (Polyflak EH) - bottles with a self-falling body, with a scale and a loop-holder, and a head intended for connection of a standard infusion system. Each bottle is closed with a lid.It is allowed to wrap each vial with film.

For 100 or 250 ml in bottles glass or glass bottles, sealed with rubber stoppers, crimped with aluminum or combined caps.

One bottle or bottle is glass, or a polypropylene type 1 bottle together with instructions for use in a pack of cardboard.

For hospitals

From 1 to 40 bottles or bottles together with instructions for use in an amount equal to the number of bottles (bottles) in a corrugated box of cardboard.

Storage conditions:

Store at a temperature not exceeding 25 ° C.

Keep out of the reach of children.

Shelf life:

3 years.

Do not use after the expiration date!

Terms of leave from pharmacies:On prescription

Registration number:LP-004476

Date of registration:28.09.2017

Expiration Date:28.09.2022

The owner of the registration certificate:GROTEKS, LLC GROTEKS, LLC Russia

Manufacturer: & nbsp

GROTEKS, LLC Russia

Information update date: & nbsp18.10.2017

Illustrated instructions

Instructions

Aminocaproic acid-SOLOfarm (Aminocaproic acid-SOLOpharm)