Active substancePyrazinamidePyrazinamide
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  • Dosage form: & nbspPills

    Composition:Each tablet contains:
    active substance: pyrazinamide 0.5 g
    Excipients: potato starch, potato pregelatinized starch, gelatin, silicon dioxide colloid (aerosil), microcrystalline cellulose, croscarmellose sodium (impellose), talc, magnesium stearate.

    Description:Tablets are white or white with a creamy shade of color flat-cylindrical with a facet and with a risk. "Marble" is allowed.

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

    J.04.A.K.01   Pyrazinamide

    Pharmacodynamics:Pyrazinamide is a synthetic antituberculous agent. It acts on intracellularly located mycobacteria. Has a bacteriostatic or bactericidal effect depending on the concentration and sensitivity of the microorganism. It operates on mycobacteria, resistant to other anti-tuberculosis drugs of the II series. The drug penetrates well into the centers of tuberculous lesion. The activity does not decrease in the acidic environment of caseous masses, in connection with which pyrazinamide often prescribed for caseous lymphadenitis, tuberculomas and caseous-pneumonic processes. More active on tuberculostatic activity than PASK, inferior to isoniazid, streptomycin, rifampicin.
    In the course of treatment, the development of resistance is possible, the probability of which decreases when combined with other anti-tuberculosis drugs.

    Pharmacokinetics:Pyrazinamide quickly and completely absorbed from the gastrointestinal tract. After ingestion of an adult dose of 500 mg peak pyrazinamide concentration in 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. .
    It penetrates well into tissues and body fluids, including the liver, lungs, cerebrospinal fluid. Approximately 50% binds to blood plasma proteins. The half-life is 8-10 hours for those patients whose liver and kidney function are not impaired. Within 24 hours, about 70% of the oral dose is excreted by the kidneys (4-14% of the dose is released in unchanged form, in the form of pyrazinic acid -33%, in the form of other metabolites - 36%). Removed during hemodialysis.

    Indications:Tuberculosis.

    Contraindications:- individual intolerance;
    - liver disease;
    - gout;
    - Hyperuricemia;
    - Pregnancy, lactation.

    Dosing and Administration:Inside, during or after a meal, once a day, preferably at breakfast with a little water.
    Adults appoint 15-30 mg / kg body weight (for individuals with a body weight of less than 50 kg - 1.5 g, more than 50 kg - 2 g). In case of unsatisfactory tolerability, the drug is prescribed in 2-3 divided doses of 5-8.75 mg / kg every 6 hours or 6.7-11.7 mg / kg every 8 hours. It can be administered at 90 mg / kg once a week or 50-70 mg / kg 2-3 times a week (2-2.5 g 3 times a week, or 2-2.5 g 3 times a week, or 3-3.5 g 2 times in Week). The maximum daily dose is 2.5 g (3 g when taken 3 times a week, 4 g when taken 2 times a week).The course of treatment is from 3 months to 2 years.
    In elderly and senile patients, the daily dose of pyrazinamide should not exceed 15 mg / kg. In these cases, the drug should be administered every other day. Children are prescribed 15-20 mg / kg once a day; the maximum daily dose is 1.5 g. If necessary, the tablet can be crushed and mixed with a small amount of water. Pyrazinamide are used in combination with aminoglycosides (streptomycin or kanamycin at a dose of 15 mg / kg), isoniazid (10 mg / kg), rifampicin (10 mg / kg).

    Side effects:From the gastrointestinal tract: nausea, vomiting, diarrhea, "metallic" taste in the mouth, epigastric pain, impaired liver function (decreased appetite, liver tenderness, hepatomegaly, jaundice, yellow atrophy of the liver); exacerbation of peptic ulcer.
    From the central nervous system: headache, dizziness, increased excitability, depression, sleep disturbance, weakness; in some cases - confusion, hallucinations, convulsions.
    On the part of the organs of hematopoiesis and the system of hemostasis: thrombocytopenia, sideroblastic anemia, erythrocyte vacuolization, porphyria, hypercoagulation, splenomegaly.
    From the musculoskeletal system: arthralgia, myalgia.
    From the urinary system: dysuria, interstitial nephritis.
    Allergic reactions: skin rash, hives.
    Other: hyperthermia, acne, hyperuricemia, exacerbation of gout, photosensitivity, increased serum iron concentration.

    Overdose:Symptoms: 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 combined with other antituberculous drugs: in chronic destructive forms pyrazinamide it is recommended to combine with rifampicin (pronounced effect) or ethambutol (better tolerability). The likelihood of developing a hepatoxic effect of the drug is increased when combined with rifampicin. When used simultaneously with drugs that block tubular secretion,it is possible to reduce their excretion and intensify toxic reactions. Strengthens the anti-tuberculosis effect of ofloxacin and lomefloxacin.

    Special instructions:It is advisable regularly (at least once a month) to monitor the activity of "liver" transaminases and the content of uric acid in the blood.
    Possible development of hypoglycemia in patients with diabetes mellitus.

    Form release / dosage:Tablets 0.5 g.

    Packaging:For 10 tablets in a planar cell package.
    For 100 tablets in a polymer bank.
    The polymer bank or 10 contour mesh packages together with instructions for use 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:P N001507 / 01
    Date of registration:13.08.2008
    The owner of the registration certificate:NIZHFARM, JSC NIZHFARM, JSC Russia
    Manufacturer: & nbsp
    Representation: & nbspMAKIZ-PHARMA, LLCMAKIZ-PHARMA, LLCRussia
    Information update date: & nbsp30.07.2015
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