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

Composition:Each tablet contains:
active substance: pyrazinamide - 500 mg;
Excipients: starch, microcrystalline cellulose, povidone, magnesium stearate, silicon dioxide colloid, sodium starch glycolate, talc purified.

Description:Round flat tablets are white, with a risk on one side.

Pharmacotherapeutic group:Anti-tuberculosis drug.

ATX: & nbsp

J.04.A.K.01 Pyrazinamide

Pharmacodynamics:Has a bacteriostatic or bactericidal effect depending on the concentration and sensitivity of the microorganism.More active in tuberculostatic activity than para-aminosalicylic acid, 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. In the course of treatment, the development of resistance is possible, the probability of which decreases when combined with other antituberculous drugs.

Pharmacokinetics:Pyrazinamide well absorbed from the gastrointestinal tract. After oral administration of a dose of 500 mg to adults, 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 into tissues and body fluids including the liver, lungs, cerebrospinal fluid. The connection with plasma proteins is 10-20%. Metabolised in the liver, where an active metabolite (pyrazinic acid) is first formed, which later turns into an inactive metabolite - 5-
hydroxypyrazinoic acid. The half-life period is 8-9 hours.
It is excreted by the kidneys: in unmodified form - 3%, in the form of pyrazinic acid -33%, in the form of other metabolites - 36%.
Removed during hemodialysis.

Indications:Apply the drug with a therapeutic purpose for the appointment of a doctor for tuberculosis.
In combination with other anti-tuberculosis drugs are prescribed in the following cases:
- pulmonary tuberculosis;
- tuberculous meningitis;
- tuberculosis of bones;
tuberculosis of urogenital organs.

Contraindications:- individual intolerance;
- liver disease;
-gout;
- Hyperuricemia;
- Pregnancy, lactation;
- Children's age under 3 years (for this dosage form).

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 elderly people, the drug should be administered every other day at a dose of 15 mg / kg.
Children are prescribed 15-20 mg / kg once a day (the maximum dose is up 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:On the part of the digestive system: nausea, vomiting, diarrhea, "metallic" taste in the mouth, impaired liver function (decreased appetite, liver tenderness, hepatomegaly, jaundice, yellow atrophy of the liver); exacerbation of peptic ulcer.
From the side of the central nervous system: dizziness, headache, sleep disturbances, increased excitability, depression; in some cases - hallucinations, convulsions, confusion.
On the part of the hematopoiesis and hemostasis system: thrombocytopenia, sideroblastic anemia, erythrocyte vacuolization, porphyria, hypercoagulation, splenomegaly.
From the musculoskeletal system: arthralgia. myalgia.
From the side of 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: a violation of liver function, an increase in the severity of side effects from the central nervous system.
Treatment: symptomatic.

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).
The likelihood of developing a hepatotoxic effect of the drug is increased when combined with rifampicin. When used simultaneously with drugs that block tubular secretion, it is possible to reduce excretion and, consequently, to increase toxic reactions.
Strengthens the anti-tuberculosis effect of ofloxacin and lomefloxacin.

Special instructions:With long-term treatment, it is necessary to monitor the activity of alanine aminotransferase and the content of uric acid in the blood once a month.
In patients with diabetes, the risk of hypoglycemia increases.

Form release / dosage:Tablets of 500 mg.

Packaging:10 tablets per strips of aluminum foil.For 10 strips in a cardboard pack together with instructions for use.

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 the drug after the expiration date.

Terms of leave from pharmacies:On prescription

Registration number:LSR-005226/09

Date of registration:30.06.2009

The owner of the registration certificate:FORTYUN MED, LTD FORTYUN MED, LTD Russia

Manufacturer: & nbsp

LINCOLN PHARMACEUTICALS, Ltd. India

Information update date: & nbsp29.07.2015

Illustrated instructions

Instructions

Pyrazinamide (Pyrazinamide)