Pyrazinamidum

General characteristics. Structure:

Active agent: Pyrazinamidum of 500 mg;

Description: tablets of white or almost white color, round, a ploskotsilindrichesky form, with a facet from two parties and risky on the one hand.

Pharmacological properties:

Pharmacodynamics. Pyrazinamidum — a synthetic antituberculous remedy. Has bacteriostatic or bactericidal effect depending on concentration and sensitivity of a microorganism. Is more active on tuberculostatic activity, than PASK though concedes to an isoniazid, streptomycin, rifampicin. Affects the mycobacteria steady against other antitubercular drugs II of a row. Drug well gets into the centers of tubercular defeat. Its activity does not decrease in acid medium of caseous masses in this connection it is often appointed at caseous lymphadenites, tuberkuloma and caseous and pneumonic processes.

Pharmacokinetics. Pyrazinamidum is well soaked up from digestive tract. After intake by the adult of a dose of 500 mg, the peak of concentration of Pyrazinamidum in a blood plasma within 9-12 mkg/ml is reached within 2 hours, 7 mkg/ml — in 8 hours and 2 mkg/ml in 24 hours. Pyrazinamidum gets into fabrics and fluid mediums of an organism, including a liver, lungs, cerebrospinal liquid. About 50% contact proteins of plasma. The elimination half-life makes 9-10 hours at those patients, functions of a liver and which kidneys are not broken. Within 24 hours, about 70% of a peroral dose are allocated with kidneys. About 4-14% of a dose are allocated in an invariable look. The remains are allocated as metabolites.

Indications to use:

It is applied to treatment of tuberculosis. In a combination with other antitubercular drugs appoint in the following cases:

- teberkulezny meningitis;

- tuberculosis of bones;

- urinogenital tuberculosis;

Route of administration and doses:

Drug is used inside in time or after food, once a day, it is more preferable during a breakfast with a small amount of water.
The adult appoint 25-30 mg/kg of body weight that there correspond for persons with body weight less than 50 kg — 1,5 g and for persons with body weight more than 50 kg — 2 g. The maximum daily dose — 2,5 g. In case of unsatisfactory portability Pyrazinamidum is appointed in 2-3 receptions. At persons of advanced and senile age the daily dose of Pyrazinamidum should not exceed 15 mg/kg of weight. In these cases it is reasonable to appoint drug every other day.
To children appoint 15-20 mg/kg once a day (as much as possible to 1,5 g a day). Pyrazinamidum is applied in a combination with aminoglycosides (streptomycin or Kanamycinum in a dose of 15 mg/kg), an isoniazid (10 mg/kg), rifampicin (10 mg/kg). Course of treatment 3 months.

Features of use:

There are no data.

Side effects:

- From digestive tract: nausea, vomiting, diarrhea, lack of appetite, unpleasant metal smack in a mouth, epigastric pains. Abnormal liver function. Aggravation of a round ulcer.
- From the central nervous system: at prolonged use — a headache, dizziness, a hyperexcitability, depressions, a sleep disorder, weakness; in some cases — confusion of consciousness, a hallucination, spasm;
- From bodies of a hemopoiesis and system of a hemostasis: thrombocytopenia, sideroblastny anemia, vacuolation of erythrocytes, porphyria, hypercoagulation, splenomegaly;
- From a musculoskeletal system: mialgiya;
- From an urinary system: dysuria, intersticial nephrite;
- Other: hyperthermia, acne, increase in concentration of serumal iron. Allergic reactions, arthralgias, a hyperuricemia, an exacerbation of gout, a photosensitization are possible. There are data on a delay in an organism under the influence of Pyrazinamidum of uric acid and emergence in joints of pains of gouty character is possible. Therefore it is reasonablly regular (at least 1 time a month) to control activity of hepatic transaminases and content of uric acid in blood. Development of a hypoglycemia in patients with a diabetes mellitus is possible. At prolonged use can have toxic effect on a liver.

Interaction with other medicines:

Pyrazinamidum is combined with other antitubercular drugs. In particular, at chronic destructive forms it is recommended to combine it with rifampicin (the expressed effect) or Ethambutolum (portability is better). Strengthens antitubercular action of an ofloksatsin and lomefloksatsin. The probability of development of a hepatotoxic action of drug increases at combined use with rifampicin. At simultaneous use with test-netsidom decrease in excretion and thereof, strengthening toxic, reactions is possible.

Contraindications:

— individual intolerance;
— liver diseases;
— gout;
— hyperuricemia;
— pregnancy, lactation;
— children's age up to 3 years.

Overdose:

Overdose symptoms: nausea, vomiting, abdominal pains, jaundice, increase in level of liver enzymes, acute fluid lungs, consciousness disturbance, coma, spasms, breath disturbance, hyperglycemia, metabolic ketoacidosis.
Treatment: a gastric lavage with introduction in absorbent carbon, an artificial diuresis, general measures on maintenance of the vital functions, a hemodialysis.

Storage conditions:

List B. To store in the dry, protected from light place at a temperature not above 25 °C. To store in the place, unavailable to children.

Issue conditions:

According to the recipe

Packaging:

Tablets of 500 mg.
On 10 tablets in a blister strip packaging from a film of the polyvinyl chloride and printing aluminum foil varnished.
On 100, 200, 300, 400, 500 or 1000 tablets in a container polymeric for medicines.
One container or 10, 20, 30, 40, 50 or 100 blister strip packagings together with the application instruction place in a pack from a cardboard.