Active substancePyrazinamidePyrazinamide
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  • Dosage form: & nbspPills

    Composition:Active substance: pyrazinamide 500 mg
    Excipients: potato starch; povidone (medium molecular weight polyvinylpyrrolidone); magnesium stearate; talc.
    Description:Tablets are white or almost white in color, flat-cylindrical, with a facet and a risk. "Marble" is allowed.

    Pharmacotherapeutic group:Anti-tuberculosis drug.
    ATX: & nbsp

    J.04.A.K.01   Pyrazinamide

    Pharmacodynamics:Pyrazinamide is a synthetic antituberculous agent.Has a bacteriostatic or bactericidal effect depending on the concentration and sensitivity of the microorganism. More active on tuberculostatic activity than PASK, although inferior to isoniazid, streptomycin, rifampicin. It operates on mycobacteria, resistant to other anti-tuberculosis drugs of the II series. The drug penetrates well into the centers of tuberculous lesion. Its activity does not decrease in the acidic environment of caseous masses, and therefore it is often prescribed for caseous lymphadenitis, tuberculomas and caseous-pneumonic processes.

    Pharmacokinetics:Pyrazinamide well absorbed from the gastrointestinal tract. After ingesting an adult dose of 500 mg, a peak concentration of pyrazinamide in the blood plasma within 9-12 μg / ml is achieved within 2 hours, 7 μg / ml after 8 hours and 2 μg / ml after 24 hours.
    Pyrazinamide penetrates the tissues and body fluids, including the liver, lungs, cerebrospinal fluid. Approximately 50% binds to plasma proteins. The half-life is 9-10 hours in those patients whose liver and kidney function are not impaired. Within 24 hours, about 70% of the oral dose is excreted by the kidneys.About 4-14% of the dose is released unchanged. The residues are excreted as metabolites.

    Indications:It is used to treat tuberculosis.
    In combination with other anti-tuberculosis drugs are prescribed in the following cases:
    - pulmonary tuberculosis;
    - tuberculous meningitis;
    - tuberculosis of bones;
    urogenital tuberculosis.

    Contraindications:- individual intolerance;
    - liver disease;
    - gout;
    - Hyperuricemia;
    - Pregnancy, lactation;
    - Children's age up to 3 years.
    Dosing and Administration:The drug is used inside during or after a meal, once a day, preferably at breakfast with a little water.
    Adults appoint 25-30 mg / kg body weight, which corresponds to those with a body weight of less than 50 kg - 1.5 g and for individuals with a body weight of more than 50 kg - 2 g.
    The maximum daily dose is 2.5 g.
    In case of unsatisfactory portability Pyrazinamide appoint 2-3 reception. In elderly and senile patients, the daily dose of pyrazinamide should not exceed 15 mg / kg of body weight. In these cases, the drug should be administered every other day.
    Children are prescribed 15-20 mg / kg once a day (maximum to 1.5 g per day).
    Pyrazinamide is used in combination with aminoglycosides (streptomycin or kanamycin in a dose of 15 mg / kg), isoniazid (10 mg / kg), rifampicin (10 mg / kg).
    The course of treatment is 3 months.

    Side effects:From the gastrointestinal tract: nausea, vomiting, diarrhea, lack of appetite, unpleasant metallic taste in the mouth, epigastric pain. Violation of the function of the liver. Exacerbation of peptic ulcer.
    From the central nervous system: with prolonged use - headache, dizziness, increased excitability, depression, sleep disturbance, weakness; in some cases - confusion, hallucinations, convulsions;
    On the part of the hematopoiesis and hemostasis system: thrombocytopenia, sideroblastic anemia, erythrocyte vacuolisation, porphyria, hypercoagulation, splenomegaly;
    From the musculoskeletal system: myalgia;
    From the urinary system: dysuria, interstitial nephritis;
    Other: hyperthermia, acne, increased serum iron concentration.
    Possible allergic reactions, arthralgia, hyperuricemia, exacerbation of gout, photosensitivity. There is evidence of a delay in the body under the influence of pyrazinamide, uric acid, and possibly the appearance of arthritic pain in the joints.Therefore, it is advisable to monitor the activity of hepatic transaminases and the content of uric acid in the blood regularly (at least once a month).
    Possible development of hypoglycemia in patients with diabetes mellitus.
    With prolonged use may have toxic effects on the liver.

    Overdose:Symptoms of an overdose: nausea, vomiting, abdominal pain, jaundice, increased liver enzymes, acute pulmonary edema, impaired consciousness, coma, convulsions, respiratory failure, hyperglycemia, metabolic ketoacidosis.
    Treatment: gastric lavage with the introduction of activated carbon, forced diuresis, general measures to maintain vital functions, hemodialysis.

    Interaction:Pyrazinamide are combined with other antituberculosis drugs. In particular, with chronic destructive forms it is recommended to combine it with rifampicin (pronounced effect) or ethambutol (better tolerability). Strengthens the anti-tuberculosis effect of ofloxacin and lomefloxacin.
    The likelihood of developing a hepatotoxic effect of the drug is increased when combined with rifampicin.With simultaneous application with probenecid, a decrease in excretion and, consequently, an increase in toxic reactions is possible.

    Form release / dosage:Tablets 500 mg.

    Packaging:For 10 tablets in a contour mesh box made of polyvinylchloride film and aluminum foil printed lacquered.
    For 50 or 100 tablets in a jar of light-protective glass or in a can of polymer or a polymer bottle.
    Each jar, bottle, 5 or 10 contour mesh packages together with the instruction for use is placed in a pack of cardboard

    Storage conditions:List B. In a dry, 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 time specified on the package.

    Terms of leave from pharmacies:On prescription
    Registration number:LSR-002874/08
    Date of registration:18.04.2008
    The owner of the registration certificate:NORTH STAR, CJSC NORTH STAR, CJSC Russia
    Manufacturer: & nbsp
    Representation: & nbspNORTH STAR CJSC NORTH STAR CJSC Russia
    Information update date: & nbsp30.07.2015
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