Active substanceAminosalicylic acidAminosalicylic acid
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  • Dosage form: & nbspsolution for infusions
    Composition:

    100 ml of solution contains:

    active substance: sodium aminosalicylate dihydrate 3.0 g;

    Excipients: disodium edetate 0.05 g, sodium sulfite 0.5 g, water for injection up to 100 ml.

    Description:

    Transparent, colorless or yellowish liquid.

    Pharmacotherapeutic group:anti-tuberculosis drug
    ATX: & nbsp

    J.04.A.A.01   Aminosalicylic acid

    Pharmacodynamics:

    Anti-tuberculosis drug. Provides bacteriostatic action. The basis of tuberculostatic action is competition with para-amino benzoic acid (PABA) for the active center of dihydropteroate synthetase, an enzyme that converts PABA into dihydrofolic acid, and inhibits the synthesis of folic acid in a microbial cell and / or the synthesis of the components of the cell wall of microbacteria, reducing the capture of iron by the latter. On tuberculostatic activity inferior to isoniazid and streptomycin. Is active only in relation to Mycobacterium tuberculosis (minimal inhibitory concentration in vitro 1-5 μg / ml). It acts on mycobacteria, which are in a state of active reproduction and practically does not affect the mycobacteria at rest. Slightly affects the pathogen, located intracellularly. Does not affect other mycobacteria. Primary resistance is rare, secondary development is slow. It is used only in combination with other anti-tuberculosis drugs, which slows the development of resistance to them.

    Pharmacokinetics:

    The maximum concentrations of the drug in the blood are determined immediately after administration. Metabolised in the liver. 80% of aminosalicylic acid is excreted in urine, and more than 50% is excreted in acetylated form. The process of acetylation is not genetically determined, as is the case with isoniazid. Sodium para-aminosalicylate is excreted by glomerular filtration.

    In the cerebrospinal fluid the drug penetrates only with inflammation of the meninges.

    About 50-60% of aminosalicylic acid binds to proteins.

    Within a day, 90-100% of the body is excreted % the accepted dose.

    Indications:

    Different forms and localization of tuberculosis in combination with other anti-TB drugs. Most often, aminosalicylic acid is prescribed for patients with multiple drug resistance to other anti-tuberculosis drugs.

    Contraindications:

    - Hypersensitivity to aminosalicylic acid;

    - hypersensitivity to other salicylates;

    - impaired renal and hepatic function;

    - heart failure in the stage of decompensation;

    - peptic ulcer of the stomach and duodenum;

    - epilepsy;

    - enterocolitis in the exacerbation phase;

    - Myxedema in the phase of exacerbation.

    Carefully:Deficiency of glucose-6-phosphate dehydrogenase, compensated hypothyroidism.
    Pregnancy and lactation:

    It is possible to use aminosalicylic acid in pregnancy if the expected benefit to the mother exceeds the potential risk to the fetus. If it is necessary to use aminosalicylic acid during lactation, breastfeeding should be stopped.

    Dosing and Administration:

    Intravenously.

    The infusion process by intravenous administration should take 2-4 hours. If the administration is to be carried out for a longer period of time, it is recommended to maintain the electrolyte balance with the help of potassium salt by its oral administration or by adding a certain amount of the appropriate potassium preparation for infusion, based on the preliminary assessment of the potassium content in the blood plasma.

    The daily dose for adults and children over 14 years is 10-15 g.

    The daily dose for children aged 6 to 14 years is 200 mg / kg body weight. The maximum daily dose is 12 g (400 ml of solution).

    For preterm infants, newborns, infants and children up to six years of age, the daily dose is usually 200 mg / kg of body weight.The duration of the course of therapy on average is 1 -2 months. If necessary, the course can be extended.

    Interval of drug administration: it is recommended to administer a daily dose of the drug 1 time per day. If necessary, the daily dose of the drug can be divided into 2 injections. The drug can be used in the intermittent mode, alternating intravenous administration and oral administration.

    Compatible solutions: it is not recommended to mix with other solutions.
    Side effects:

    Allergic reactions: fever, hives, purpura, enanthema, bronchospasm, joint pain, medical hepatitis. Allergic reactions may appear in a few days, although they mostly occur between the 2nd and 7th week of treatment (most often at 4-5 weeks). Quincke's edema, swelling of the joints, fever caused by the administration of drugs, lupus-like reactions, reactions accompanied by spleen, liver, kidney, digestive tract, bone marrow and nervous system (eg, radicular pain, meningism, polymorphic exudative erythema in the form of syndrome Stevens-Johnson syndrome or Lyell's syndrome).In the lungs, a temporary (including allergic) infiltrate can be formed (Leffler's syndrome).

    From the gastrointestinal tract: excessive salivation, nausea, vomiting, worsening or loss of appetite, abdominal pain, diarrhea, flatulence, constipation.

    From the cardiovascular system: pericarditis, vasculitis.

    From the nervous system: optic neuritis, encephalopathy.

    From the hematopoiesis: eosinophilia, agranulocytosis, leukopenia, thrombocytopenia, B 12-deficiency anemia, hemolytic anemia with a positive Coombs breakdown. With a long course of treatment with aminosalicylic acid, in rare cases, an increase in prothrombin time may occur, accompanied by hemorrhagic rash or bleeding.

    From the urinary system: moderate transient microhematuria, albuminuria and cylindruria, normoglycemic or hyperglycemic glucosuria. Crystalluria can be prevented by maintaining a neutral or alkaline pH value of urine. It is possible to increase the level of urea in the blood, indicating the presence of uremic reaction, especially in patients with impaired renal function and acidosis.

    From the liver and bile ducts: a moderate transient increase in the activity of "liver" transaminases, sometimes accompanied by jaundice. Approximately 25% of patients with an allergic reaction to aminosalicylic acid have liver damage, and in 10% of cases it can lead to liver failure and death.

    From the endocrine system: when using high doses, there is a worsening of the thyroid function, accompanied by the appearance of goiter.

    Laboratory indicators: hyperbilirubinemia.

    Other: syndrome resembling infectious mononucleosis or lymphoma, hypokalemia with the introduction of high doses of the drug, especially in elderly patients with edema and hypertension, as well as in patients with meningitis. With the introduction of large doses of the drug, the loss of cations can cause acidosis, especially in children. Can be observed symptoms of paralysis, tonic-clonic seizures, as well as psychosis. With prolonged use in high doses - hypothyroidism, superinfection.

    Overdose:

    Symptoms: It is possible to increase dose-dependent side effects.

    Treatment: The drug should be discontinued, if necessary - hemodialysis.

    Interaction:

    Aminosalicylic acid disrupts the absorption of rifampicin, erythromycin and lincomycin.

    Aminosalicylic acid disrupts the absorption of vitamin B12, resulting in the development of anemia.

    The use of aminosalicylic acid together with isoniazid or phenytoin leads to an increase in the duration of isoniazid or phenytoin in the blood plasma.

    The use of aminosalicylic acid together with salicylates, phenylbutazone or other anti-inflammatory drugs with an increased ability to bind proteins leads to an increase in the concentration and an increase in the duration of the presence of aminosalicylic acid in the blood plasma.

    The use of aminosalicylic acid together with diphenhydramine leads to a decrease in the concentration of aminosalicylic acid in the blood plasma.

    Aminosalicylic acid inhibits the absorption of folic acid and can enhance the toxicity of folic acid antagonists, such as, for example, methotrexate.

    Aminosalicylic acid should not be administered simultaneously with solutions of rifampicin and protionamide in the total mixture; these substances should be administered separately.

    Aminosalicylic acid reduces the concentration of digoxin in the blood by 40%. Strengthens the effect of indirect anticoagulants - coumarin derivatives and indanedione (correction of the dose of anticoagulants is required). In applying iodinated thyroid hormones, their analogs and antagonists (including antithyroid drugs) should be taken into account that background aminobenzoic acid (PABA) changes the concentration of thyroxine (T4) and thyroid stimulating hormone (TSH) in the blood.

    Ammonium chloride increases the risk of developing crystalluria. Simultaneous use with ethionamide increases the risk of hepatotoxicity. Probenecid reduces the excretion of aminosalicylic acid, increasing its concentration in the plasma.

    Special instructions:

    During treatment, it is necessary to regularly perform blood and urine tests, monitor liver function (activity of "liver" transaminases).

    To prevent the formation of crystals, it is necessary to "alkalize" the urine, especially having an acid reaction.

    Sometimes a non-enzymatic determination of glucose and urobilinogen in the urine can give erroneous positive results.

    Used in combination with more active antituberculous drugs.Decreased kidney function against tuberculous intoxication or specific tuberculosis lesions is not a contraindication to the use. The development of proteinuria and hematuria requires a temporary discontinuation of the drug.

    At the first signs, indicating an allergic reaction, the drug should be stopped and desensitizing therapy should be given.

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

    There is no data on the study of adverse effects of aminosalicylic acid on the ability to drive a vehicle or work on any machines.

    Form release / dosage:

    Solution for infusions 30 mg / ml.

    Packaging:100 ml, 200 ml or 400 ml in glass bottles for blood, transfusion and infusion preparations, sealed with stoppers made of rubber compound and crimped with aluminum caps or caps with aluminum-plastic ones. Each bottle, together with instructions for use, is placed in a pack of cardboard.
    Storage conditions:

    In the dark place at a temperature of +8 ° C to +15 ° C.

    Keep out of the reach of children.

    Shelf life:

    1,5 years.

    Do not use after the expiration date.

    Terms of leave from pharmacies:On prescription
    Registration number:LS-002660
    Date of registration:01.09.2011
    The owner of the registration certificate:YURIYA-FARM, LLC YURIYA-FARM, LLC Ukraine
    Manufacturer: & nbsp
    Information update date: & nbsp01.09.2011
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