Active substanceAminosalicylic acidAminosalicylic acid
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  • Dosage form: & nbsplyophilizate for solution for infusion
    Composition:

    Each infusion bottle contains:

    Active substance - aminosalicylic acid 13.49 g.
    Description:Powder of white or light gray color.
    Pharmacotherapeutic group:anti-tuberculosis drug
    ATX: & nbsp

    J.04.A.A.01   Aminosalicylic acid

    Pharmacodynamics:

    Aminosalicylic acid (PASK) has bacteriostatic action against Mycobacterium tuberculosis. It reduces the likelihood of bacterial resistance to streptomycin and isoniazid, the mechanism of action is associated with the 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 on the mycobacteria that are in the active state propagation, and virtually no effect on Mycobacterium in the resting stage. Slightly affects the pathogen, located intracellularly.

    Aminosalicylic acid is active only in relation to M. tuberculosis. Does not affect other non-tuberculosis mycobacteria.

    Pharmacokinetics:

    Features of clinical pharmacology aminosalicylic acid - is the rapid formation in the acidic environment of a toxic inactive metabolite and a short half-life in the serum, which for an unbound drug is one hour. Metabolised in the liver and partially in the stomach. 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. Aminosalicylic acid is derived 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.

    Indications:

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

    Contraindications:

    Individual intolerance to the drug;

    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.

    Pregnancy and lactation:

    Possible use of the drug PASK in pregnancy in the event that the expected benefit for the mother exceeds the potential risk to the fetus. If you need to use the drug PASK during lactation should stop breastfeeding.

    Dosing and Administration:

    Intravenously.

    As a solvent, 500 ml of water for injection should be used.

    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 potassium salt by oral administration or addition to the infusion solution.

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

    For preterm infants, infants and children up to six years of age, the daily dose is usually 200-300 mg / kg body weight.

    If it is necessary to use the preparation 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 the relevant potassium preparation for infusion, based on the results of a preliminary assessment of the potassium content in the blood plasma.

    Side effects:

    The most common side effect of the gastrointestinal tract is excessive salivation, nausea, vomiting, deterioration or a loss appetite, pain in the abdomen, diarrhea, flatulence, constipation.

    Allergic reactions: fever, dermatitis such as urticaria or purpura, enanthema,asthmatic phenomena, pain in the joints, eosinophilia, rarely agranulocytosis, leukopenia, thrombocytopenia, drug-induced hepatitis. Allergic reactions may appear in a few days, although they mostly arise in period between the 2nd and the 7th week of treatment (most often at 4-5 weeks). Occasionally, side effects such as severe allergic reactions (eg, Quincke's edema), swelling of the joints, fever caused by the administration of drugs, reactions similar to lupus erythematosus, accompanied by lesions of the spleen, liver, kidneys, digestive tract, bone marrow and nervous system eg, radicular pain, meningism, polymorphic exudative erythema in the form of Stevens-Johnson syndrome or syndrome Laella).

    With a long course of treatment with PASC, in rare cases, there may be an increase in prothrombin time, accompanied by bleeding, and in exceptional cases - accompanied by hemorrhagic rash.

    With a varying frequency (from rare to very frequent cases), a mild transient microhematuria, albuminuria and cylindruria can occur.

    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 a presence of uremic reaction, especially in patients with impaired renal function and acidosis.

    There are rare reports of a moderate transient increase in transaminase activity, sometimes accompanied by jaundice. Approximately 25% of patients who have an allergic reaction to PASC have liver damage, and in 10% cases it may lead to the onset of liver failure and death.

    Often, especially when using high doses, there is a worsening of the thyroid function, accompanied by the appearance of goitre.

    Rare side effects are abrupt violations of electrolyte balance, mainly in the form of hypokalemia with high doses of the drug, especially in elderly patients with edema and hypertension, as well as patients suffering from meningitis. With the introduction of large doses of the drug, the loss of cations can cause acidosis; most often it occurs in children.

    Occasionally, normoglycemic or hyperglycemic glucosuria.

    In some cases, a temporary (including allergic) infiltrate can be formed in the lungs (Löffler syndrome).

    In some cases, there may be symptoms of paralysis, clonic-tonic convulsions, and psychosis.

    With prolonged use in higher doses - hypothyroidism, goitre, superinfection.
    Overdose:

    In case of acute allergic reactions, such as anaphylactic shock, the drug should be stopped immediately and appropriate measures taken (administration of antihistamines, corticosteroids and sympathomimetics, artificial respiration).

    In case of poisoning, the drug should be discontinued, if necessary - hemodialysis.

    Interaction:

    PASC disrupts the absorption of rifampicin, erythromycin and lincomycin.

    PASK disrupts the absorption of vitamin B12, resulting in the development of anemia. The use of PAS together with isoniazid or phenytoin leads to an increase in the duration of isoniazid or phenytoin in the blood plasma. Use of PASC along with salicylates, phenylbutazone or other Anti-inflammatory drugs with increased ability to bind proteins,leads to an increase in the concentration and an increase in the duration of PAS in the blood plasma.

    The use of PASC together with diphenylhydramine leads to a decrease concentration of PAS in the blood plasma.

    PASK inhibits folate absorption and can enhance the toxicity of folate antagonists, such as, for example, methotrexate.

    Special instructions:

    During treatment, it is necessary to regularly perform blood and urine tests, to monitor liver function.

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

    Dosage of PAS should be carefully checked, and the patient should be examined regularly if he / she has severe liver or kidney dysfunction, suffers from diabetes or has a gastrointestinal ulcer.

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

    Incompatibility with other substances

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

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

    So far, there has been no evidence that the PASC has any adverse effect on the ability to drive a vehicle or work on any machines.

    Form release / dosage:Lyophilizate for solution for infusion.
    Packaging:

    Lyophilizate for the preparation of a solution for infusions containing 13.49 g of sodium 4-aminosalicylate (equivalent to 11.72 g of free acid 4-aminosalicylic and 1.77 g of sodium ions).

    For 13.49 g of the drug in a transparent glass bottle with a capacity of 500 ml (type 1, hydrolytic class 1) with a plug of bromobutyl rubber and an aluminum cap with a plastic disc. The bottle is placed in wrapping light-protective paper. For 10 bottles and 10 transfloors, along with the instructions for use are placed in a cardboard box (for hospitals).

    Storage conditions:

    List B.

    Store at a temperature not exceeding + 25 ° ะก.

    Protect from light.

    Keep out of the reach of children.

    Ready-to-use solution should be used immediately after its preparation.
    Shelf life:

    4 years.

    Do not use after the time specified on the package.

    Terms of leave from pharmacies:On prescription
    Registration number:LS-000157
    Date of registration:25.02.2010
    The owner of the registration certificate:Rimzer Artsynaimitel, AGRimzer Artsynaimitel, AG Germany
    Manufacturer: & nbsp
    Representation: & nbspSVYCH LLC SVYCH LLC Russia
    Information update date: & nbsp23.04.2012
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