Active substanceAminosalicylic acidAminosalicylic acid
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  • Dosage form: & nbsplyophilizate for solution for infusion
    Composition:sodium aminosalicylate dihydrate - 3 g.
    Description:

    porous mass or powder of white or white with yellowish or white with pinkish or white with a grayish hue.

    Pharmacotherapeutic group:anti-tuberculosis drug
    ATX: & nbsp

    J.04.A.A.01   Aminosalicylic acid

    Pharmacodynamics:

    Aminosalicylic acid has a bacteriostatic effect against Mycobacterium tuberculosis, reduces the likelihood of bacterial resistance to streptomycin and isoniazid. The mechanism of action is associated with inhibition of the synthesis of folic acid and with the suppression of the formation of mycobacterium, a component of the mycobacterial wall, which leads to a decrease in the capture of iron M. tuberculosis. Aminosalicylic acid acts against actively multiplying Mycobacterium tuberculosis (the minimum inhibitory concentration (MIC) is 1-5 μg / ml). Virtually does not work on Mycobacterium tuberculosis in the stage of rest and located intracellularly. Does not affect other mycobacteria. It is used only in combination with other anti-tuberculosis drugs.

    Pharmacokinetics:

    The maximum concentration of aminosalicylic acid in the blood is determined immediately after administration. Binding to plasma proteins - 50-60%. It is well distributed in tissues and body fluids, kidneys, lungs, liver. Achieves high concentrations in pleural efflorescence and caseous tissue. In the cerebrospinal fluid penetrates moderately (only with inflammation of the meninges). Penetrates into breast milk.Metabolised in the liver (more than 50% acetylated to inactive metabolites) and partially in the stomach. The half-life (T1 / 2) with normal renal function is 30-60 min, with impaired -. To 23 hours, 80% of excreted by the kidneys by glomerular filtration (50% as a acetylated derivative). The total clearance depends on both the metabolic rate and the excretion of the kidneys.

    Indications:

    Tuberculosis of various forms and localizations (in combination with other anti-TB drugs), including multidrug-resistant tuberculosis to other anti-tuberculosis drugs.

    Contraindications:

    - Hypersensitivity to aminosalicylic acid and other salicylates;

    - Severe renal and / or hepatic insufficiency;

    - Stomach ulcer and duodenal ulcer, inflammatory bowel disease in the acute stage;

    - Decompensated hypothyroidism;

    - Epilepsy;

    - Decompensated chronic heart failure, arterial hypertension;

    - Individual intolerance to salicylates (in history);

    - Deficiency of glucose-6-fosfatdegidrogenazy;

    - Hypocoagulation;

    - Thrombophlebitis;

    - Edema caused by hypernatremia;

    - Amyloidosis of internal organs;

    - Lactation period.

    Carefully:

    Diabetes mellitus, acute hepatitis, compensated hypothyroidism, chronic heart failure, gastrointestinal diseases (in the anamnesis), renal and / or hepatic insufficiency of mild and moderate severity, pregnancy.

    Pregnancy and lactation:

    In pregnancy, the drug is used only if the expected benefit for the mother exceeds the potential risk to the fetus and in the absence of alternative therapy. If it is necessary to use the drug during lactation, breastfeeding should be stopped.

    Dosing and Administration:

    Intravenously infuzionalno.

    The daily dose of the drug PASK sodium salt is administered once a day in the form of a single dose. The duration of the infusion is 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 potassium salt by oral administration or addition to the infusion solution.

    Adults and children over 14 years of age receive a dose of 10-15 g per day; for children 7-14 years of age - 200 mg / kg of body weight per day; for children under 6 years (incl.preterm infants, infants) - 200-300 mg / kg body weight per day (the maximum daily dose for children is 10 g); a malnourished adult (with a body weight of less than 50 kg), the maximum daily dose is 6 g / day.

    The duration of therapy on average is 1-2 months. If necessary, the course can be extended (the total duration of treatment is determined individually, depending on the severity of the disease). The drug can be used in the intermittent mode, alternating intravenous administration and reception of aminosalicylic acid inside.

    If it is necessary to use the drug for a long 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 results of a preliminary assessment of the potassium concentration in the blood plasma.

    Rules for the preparation and administration of an infusion solution

    For the preparation of the infusion solution, the contents of 1 bottle / vial (3 g preparation) is dissolved in 100 ml of water for injection. The prepared solution contains 3 g of PASK sodium salt in 100 ml of water (3% solution).

    It is necessary to achieve complete dissolution of the contents of the bottle / bottle. Apply freshly prepared solutions. In the case of turbidity when diluted - application of the solution is prohibited. A solution prepared for intravenous administration should be stored at room temperature for a maximum of 12 hours, including the time of infusion. The preparation can be administered by means of an injection pump with adjustable feed. Intravenous infusion is administered. Begin the injection with 30 drops of solution per minute and, in the absence of local and general reactions, after 15 minutes the infusion rate is increased to 40-60 drops per minute. At the first application, not more than 200 ml of the solution (6 g of the drug) are injected, and in the absence of side effects - 400 ml of the solution.

    Side effects:

    From the digestive system: loss of appetite, nausea, vomiting, flatulence, increased salivation, abdominal pain, diarrhea or constipation, colic pain in the abdomen (with a high infusion rate), peptic ulcer with bleeding, drug-induced hepatitis (including fatal), increased activity of "hepatic" transaminases, jaundice, hyperbilirubinemia, hepatic insufficiency, heartburn.

    From the urinary system: proteinuria, hematuria, crystalluria, albuminuria, cylindruria, increased urea concentration in blood plasma, glucosuria.

    From the hematopoietic system: leukopenia (up to agranulocytosis), thrombocytopenia, a decrease in prothrombin, an increase in prothrombin time, accompanied by bleeding and hemorrhagic purpura, neutropenia, lymphocytosis, B 12-deficiency megaloblastic anemia, hemolytic anemia with a positive breakdown of Coombs.

    Allergic reactions: rash (hives, purpura, enanthema, exfoliative dermatitis, erythema, a syndrome resembling infectious mononucleosis or lymphoma), eosinophilia, bronchospasm, arthralgia, fever, Quincke's edema, Stevens-Johnson syndrome, Lyell syndrome, anaphylactic shock.

    Other: hypothyroidism, goiter, myxedema, hypokalemia, acidosis, hypoglycemia, hyperglycemia, Leffler's syndrome (eosinophilic pneumonia, migratory pulmonary infiltrate), swelling of the joints, psychosis, paralysis, seizures, superinfection, reactions similar to lupus erythematosus, accompanied by lesions of the spleen, liver, kidneys, digestive tract, bone marrow and nervous system (for example,pain of radicular nature, meningism), pericarditis, optic neuritis, vasculitis, encephalopathy, itching.

    Reactions at the site of administration: possibly the appearance of hematomas and phlebitis.

    Overdose:

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

    Treatment: withdrawal of the drug, symptomatic therapy is indicated.

    Interaction:

    Increases the concentration of isoniazid in the blood due to competition for common metabolic pathways. Simultaneous use with isoniazid increases the risk of hemolytic anemia.

    It interferes with the assimilation of cyanocobalamin (vitamin B12), which can lead to the development of 12-deficiency anemia.

    Increases the concentration of phenytoin in the blood plasma.

    Reduces the concentration of digoxin in the blood.

    Strengthens the effect of indirect anticoagulants (coumarin derivatives, indanedione) - correction of the dose of indirect anticoagulants is required.

    Aminosalicylic acid inhibits the absorption of folic acid, as a result of which the toxicity of methotrexate (a folic acid antagonist) may increase.

    When using thyroid hormones, their analogs, antagonists (including antithyroid drugs), it should be borne in mind that aminosalicylic acid is used to change the concentration of thyroxine and thyroid-stimulating hormone.

    Simultaneous use with ethionamide increases the risk of hepatotoxicity. Diphenhydramine reduces the effectiveness of aminosalicylic acid.

    Probenecid reduces the excretion of aminosalicylic acid, increasing its concentration in the blood plasma.

    Ammonium chloride increases the risk of developing crystalluria.

    Simultaneous use with salicylates, phenylbutazone or other non-steroidal anti-inflammatory drugs increases the concentration of aminosalicylic acid in the blood plasma.


    The drug is pharmaceutically incompatible with solutions of rifampicin and protionamide.

    Special instructions:

    During the treatment it is necessary to regularly perform urine and blood tests, monitor the functional state of the liver. In the presence of symptoms of liver dysfunction, such as increased activity of "liver" transaminases, jaundice, fever, therapy with the drug should be discontinued and a study of the functional state of the liver.

    Used in combination with other anti-tuberculosis drugs.

    Decreased kidney function against tuberculous intoxication or specific tuberculosis lesions is not a contraindication to the use.

    The solution of the drug is administered intravenously infusion with careful monitoring of the doctor. To prevent the development of hematomas and phlebitis at the injection site, thin needles should be used, alternating veins to introduce a solution.

    The development of proteinuria and hematuria require a temporary discontinuation of the drug.

    At the first sign indicating an allergic reaction, the drug should be discontinued and desensitizing therapy administered.

    To prevent crystalluria, it is necessary to "alkalinize" urine, especially having an acid reaction.

    In patients with diabetes it is necessary to monitor the concentration of glucose in the blood plasma.

    Non-enzymatic determination of glucose and urobilinogen in the urine can give false positive results.

    The medicinal preparation contains from 308 to 352 mg of sodium ions.

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

    There is no data on the study of the effect of aminosalicylic acid on the ability to drive vehicles and perform other actions that require concentration of attention and speed of psychomotor reactions. Care should be taken when management of vehicles and mechanisms, taking into account the potential for paralysis, seizures,neuritis of the optic nerve, which may occur when using this drug. When these undesirable phenomena appear, one should refrain from performing these activities.

    Form release / dosage:

    Lyophilizate for solution for infusions 3 g.

    Packaging:

    For 3 g in bottles / bottles with a capacity of 100 ml. Each bottle / bottle together with the instruction for use is placed in a pack of cardboard.

    Packaging for hospitals: 56 packs with an equal number of instructions for use in a group container.
    Storage conditions:

    Store in a dry, dark place at a temperature of no higher than 25 ° C.

    Keep out of the reach of children.

    Shelf life:

    2 years.

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

    Terms of leave from pharmacies:On prescription
    Registration number:LP-002801
    Date of registration:29.12.2014
    The owner of the registration certificate:BELMEDPREPARATY, RUP BELMEDPREPARATY, RUP Republic of Belarus
    Manufacturer: & nbsp
    BELMEDPREPARATY, RUP Republic of Belarus
    Information update date: & nbsp29.12.2014
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