Pyrazinamide - instructions for use, dose, side effects, contraindications

Composition:Composition per one tablet.
Active substance:
Pyrazinamide (Lupine Lid, India / Kalix Chemicals & Pharmaceuticals Limited, India) -500 mg;
Excipients:
Potato starch is 32.30 mg;
Gelatin-11.54 mg;
Carboxymethyl starch sodium (primogel) -3.85 mg;
Silica colloidal dioxide (Aerosil brand A 300) -8.46 mg;
Magnesium stearate 3.85 mg
Weight of the tablet -560 mg

Description:Tablets of white or almost white color are round, flat-cylindrical with a risk on one side with bevelled edges.

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 administered orally during or after meals once a day, preferably at breakfast with a small amount of 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: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 with other drugs
Pyrazinamide is combined with other anti-tuberculosis 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:Primary packaging of medicinal
preparation.
For 10 tablets in a contour mesh box made of polyvinylchloride film and aluminum foil printed lacquered.
For 50 or 100 tablets are placed in a can of polymer with a lid pulled with the control of the first opening. Free space is filled with cotton wool.On cans are labeled with paper label or from polymer materials, self-adhesive.
For 500 tablets (for hospitals), put in a polymer jar with a lid pulled with a control
first autopsy. Free space is filled with cotton wool. Labels are applied to cans from paper label or written or from polymer materials, self-adhesive.
Secondary packaging of medicinal product.
For 5 or 10 out-of-round cell packs, together with the instructions for use, they are placed in a pack of cardboard for consumer containers. Banks, together with an equal number of instructions for use, are placed in a group package.

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:4 years. Do not use after the time specified on the package.

Terms of leave from pharmacies:On prescription

Registration number:LSR-001810/08

Date of registration:17.03.2008

The owner of the registration certificate:FARMSINTEZ, PAO FARMSINTEZ, PAO Russia

Manufacturer: & nbsp

FARMSINTEZ, JSC Russia

Representation: & nbspFARMSINTEZ, PAO FARMSINTEZ, PAO Russia

Information update date: & nbsp31.07.2015

Illustrated instructions

Instructions

Pyrazinamide (Pyrazinamide)