Description of the active substance:
This information is a reference and it is not enough that the drug has been prescribed by a doctor ..
PHARMACHOLOGIC EFFECT
Synthetic antituberculous agent of the II series. The mechanism of action is not exactly known. It has bacteriostatic or bactericidal action depending on its concentration and sensitivity of the microorganism. It penetrates well into the centers of tuberculous lesion.
PHARMACOKINETICS
After ingestion, pyrazinamide is rapidly absorbed from the digestive tract. C max in blood plasma is achieved after 2 hours and is about 35 Ојg / ml at a dose of 1.5 g and 66 Ојg / ml at a dose of 2 g. Pyrazinamide is widely distributed in tissues and body fluids, it penetrates through the BBB.
Metabolized mainly in the liver by hydrolysis with the formation of pyrazinic acid, the main metabolite, which is gradually hydroxylated to 5-hydrosipyrazinic acid.
T 1/2 from the blood plasma is about 9-10 hours.
It is excreted mainly by the kidneys by glomerular filtration. About 70% is found in urine within 24 hours mainly in the form of metabolites and 4-14% - in the form of an unchanged substance.
INDICATIONS
Tuberculosis (as part of combination therapy).
DOSING MODE
Inside adults and children - 15-25 mg / kg 1 time / day or 50-70 mg / kg 2-3 times a week.
Maximum doses: for adults and children, the daily dose is 2 g for 1 time / day, 3 g for 3 times a week, 4 g for 2 times a week.
SIDE EFFECT
On the part of the digestive system: a violation of the liver, nausea, vomiting, diarrhea.
Allergic reactions: skin rash, itching, arthralgia.
Other: hyperuricemia, exacerbation of gout; rarely - photosensitivity.
CONTRAINDICATIONS
Disorders of liver function, hypersensitivity to pyrazinamide.
PREGNANCY AND LACTATION
Adequate and strictly controlled clinical trials of the safety of pyrazinamide during pregnancy and lactation (breastfeeding) were not conducted. However, with the development of resistance to isoniazid, rifampicin and ethambutol, a discussion of the use of pyrazinamide in pregnant women is possible.
Pyrazinamide in small amounts excreted in breast milk.
APPLICATION FOR VIOLATIONS OF THE FUNCTION OF KIDNEYS
Contraindicated in violations of liver function.
APPLICATION FOR CHILDREN
The application is possible according to the dosing regimen.
SPECIAL INSTRUCTIONS
When monotherapy with pyrazinamide rapidly develops resistance to mycobacteria, and therefore pyrazinamide is usually used in combination with other antituberculosis drugs.
Pyrazinamide is removed from the body by dialysis.
With prolonged use, it is advisable to monitor the activity of hepatic transaminases and the content of uric acid in the blood regularly (once a month).
DRUG INTERACTION
Pyrazinamide reduces the concentration of cyclosporine in the blood plasma.
Pyrazinamide increases the concentration of uric acid in the blood plasma and reduces the effectiveness of antidotal drugs (allopurinol, sulfinpyrazone) with simultaneous application.
