Active substanceAminocaproic acidAminocaproic acid
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  • Dosage form: & nbspsolution for infusions
    Composition:

    Active substance: aminocaproic acid 50.0 g; Excipients: sodium chloride - 9.0 g; water for injection - up to 1.0 liter.

    Theoretical osmolarity - 690 mOsmol / l
    Description:

    Colorless transparent solution.

    Pharmacotherapeutic group:Hemostatic agent, inhibitor of fibrinolysis
    ATX: & nbsp

    B.02.A.A.01   Aminocaproic acid

    Pharmacodynamics:Amino-caproic acid refers to 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-kinin (inhibits the activating action of streptokinase, urokinase, tissue kinases for fibrinolysis), neutralizes the effects of kallikrein, trypsin and hyaluronidase, reduces the permeability of capillaries. Amino-caproic acid has anti-allergic activity, enhances detoxifying function of the liver, inhibits antibody formation.
    Pharmacokinetics:

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

    Indications:

    - Bleeding (hyperfibrinolysis, hypo- and afibrinogenemia)

    - bleeding during surgical interventions on organs rich in fibrinolysis activators (brain and spinal cord, lungs, heart, vessels, thyroid and pancreas, prostate gland);

    - diseases of internal organs with hemorrhagic syndrome;

    - premature placental abruption, prolonged delay in the smear cavity of a dead fetus, complicated abortion;

    - for the prevention of secondary hypophybrinogenemia in the case of mass transfusions of canned blood.

    Contraindications:

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

    Carefully:

    Arterial hypotension, bleeding from the upper urinary tract (due to the risk of intra-venous 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, perhaps only if the expected benefit exceeds the potential risk), subarachnoid hemorrhage, hepatic insufficiency ,violation of kidney function, valvular heart disease, children under 1 year.

    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 are no data on excretion of aminocaproic acid in breast milk, and therefore, the period of treatment should abandon breastfeeding.

    Dosing and Administration:

    Intravenously drip. The daily dose for adults is 5.0 - 30.0 g. If it is necessary to achieve a quick effect (acute hyperfibrinogenemia), inject intravenously drip to 100 ml of sterile 50 mg / ml solution on isotonic sodium chloride solution at a rate of 50-60 drops per minute. During the first hour, a dose of 4.0 - 5.0 g is administered, in the case of continuing bleeding - until it stops completely - 1.0 g every hour for not more than 8 hours. If necessary, administer 50 mg / ml acid solution of aminocaproic repeat.

    Children - at the rate of 100.0 mg / kg body weight in the first hour, then 33.0 mg / kg / h, the maximum daily dose - 18.0 g / m2 surface of the body. The daily dose for adults is 5.0 - 30.0 g. The daily dose for children under 1 year is 3.0 g; 2 - 6 years - 3.0 - 6.0 g; 7 - 10 years - 6.0 - 9.0 g; from 10 years - both for adults. With 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 g. The duration of therapy is 3 - 14 days.

    Side effects:

    The undesirable reactions observed in patients are listed below. The frequency of adverse reactions was classified as follows: very frequent (10%), frequent (from 1% to 10%), infrequent (from 0.1% to 1%), rare (from 0.01% to 0.1%), very rare (<0.01%) and unidentified frequencies .

    From the cardiovascular system: often - lowering blood pressure, orthostatic arterial hypotension; infrequently bradycardia; rarely - ischemia of peripheral tissues; unknown frequency - subendocardial hemorrhage, thrombosis;

    From the hemopoietic system and lymphatic system: infrequently - agranulocytosis, coagulation disorder; frequency unknown - leukopenia, thrombocytopenia;

    From the immune system: infrequently - allergic and anaphylactic reactions; frequency unknown - maculopapular rashes;

    With moans of the senses: often - nasal congestion; rarely - reduced visual acuity, lacrimation.

    From the musculoskeletal system: infrequently - muscle weakness, myalgia; rarely - increased activity of CK, myositis; frequency unknown - acute myopathy, myoglobinuria, rhabdomyolysis;

    From the central nervous system: often - dizziness, noise in the ears, headache; very rarely - confusion, convulsions, delirium, hallucinations, increased intracranial pressure, impaired cerebral circulation, fainting; From the gastrointestinal tract: often - abdominal pain, diarrhea, nausea, vomiting;

    From the urinary system: frequency unknown - acute renal failure, increased blood urea nitrogen, renal colic, impaired renal function;

    From the upper respiratory tract: infrequently - shortness of breath; rarely - pulmonary embolism; frequency unknown - inflammation of the upper respiratory tract;

    Local reactions: infrequently - skin rash, itching;

    On the part of the body as a whole: often - general weakness, pain and necrosis at the injection site; infrequently - swelling.

    Overdose:

    Symptoms: lowering of blood pressure, convulsions, acute renal failure.

    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, a solution of glucose (dextrose), 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.

    Simultaneous use of aminocaproic acid with concentrates of prothrombin complex, preparations of coagulation factor IX and estrogens can increase the risk of thrombosis.

    Aminocaproic acid inhibits the action of plasminogen activators and, to a lesser extent, plasmin activity.

    In addition, no drugs should be added to the aminocaproic acid solution.

    Special instructions:

    When prescribing a drug, it is required to establish a source of bleeding and monitor the fibrinolytic activity of the blood and the concentration of fibrinogen in the blood.It is necessary to control the coagulogram, especially in ischemic heart disease, after myocardial infarction, in pathological processes in the liver.

    It is not recommended to use aminocaproic acid in women to prevent increased bleeding in childbirth due to an increased risk of thrombosis in the postpartum period.

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

    In rare cases, after long-term use, the lesion of the skeletal musculature and necrosis of the muscle fibers is described. Clinical manifestations can range from mild to moderate muscle weakness to severe proximal myopathy with rhabdomyolysis, myoglobinuria, and acute renal failure. It is necessary to monitor CK in patients who have undergone long-term treatment. The use of aminocaproic acid should be discontinued if there is an increase in CK. When there is myopathy, it is necessary to consider the possibility of myocardial damage.

    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:

    100 ml and 250 ml in plastic bottles with sealed neck of low density polyethylene, produced by Borealis AG, Austria, Bassel Sales and Marketing Company BV Netherlands, "Ipeos Sales of Belgeam II.V." Belgium, or the relevant European Pharmacopoeia or the European Standard ISO (Ph. Eur, ISO), with protective cap of polyethylene or polypropylene, having a thermoplastic elastomer liner and aluminum protective foil, manufactured by West Pharmaceutical Services Deutschland GmbH & Co. KG Germany, and a ring holder at the bottom of the bottle or without it.

    1 bottle is placed in an individual cardboard pack together with instructions for use.

    For 15, 24, 28 or 36 bottles are placed in boxes of corrugated cardboard with an equal number of instructions for use (for hospitals).
    Storage conditions:

    In the dark place at a temperature of no higher than 25 ° C.

    Keep out of the reach of children.

    Shelf life:

    3 years.Do not use after the expiration date printed on the package.

    Terms of leave from pharmacies:On prescription
    Registration number:LP-002869
    Date of registration:24.02.2015
    Expiration Date:24.02.2020
    The owner of the registration certificate:ALIUM PFK, LLC ALIUM PFK, LLC Russia
    Manufacturer: & nbsp
    Information update date: & nbsp07.08.2017
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