Pyrazinamide
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Clinical Pharmacology
PIRAZINAMID is a synthetic II row tuberculosis remedy. The mechanism of action is unknown. It has a bacteriostatic or bactericidal effect depending on its concentration and sensitivity of the microorganism. It penetrates well into the lesions of the tuberculous lesion.
Indications
Tuberculosis (as part of combination therapy).
Composition
Pyrazinamide.
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Dosage and Administration
Inside adults and children - 15-25 mg / kg 1 time / day. or at 50-70 mg / kg 2-3 times a week.
Maximum doses: for adults and children, the daily dose is 2 g when taken 1 time / day., 3 g when taken 3 times a week, 4 g when taken 2 times a week.
Adverse reactions
From the digestive system: abnormal liver function, nausea, vomiting, diarrhea.
Allergic reactions: skin rash, itching, arthralgia.
Other: hyperuricemia, aggravation of gout; rarely - photosensitization.
Contraindications
Liver dysfunction, hypersensitivity to pyrazinamide.
Drug interactions
Pyrazinamide reduces plasma cyclosporine concentrations.
Pyrazinamide increases plasma uric acid levels and reduces the effectiveness of anti-arthritic drugs (allopurinol, sulfinpyrazon), while simultaneous use.
Pregnancy and Lactation
Adequate and strictly controlled clinical studies of the safety of the use of pyrazinamide during pregnancy and lactation (breastfeeding) have not been conducted. However, with the development of resistance to isoniazid, rifampicin and ethambutol, it is possible to discuss the use of pyrazinamide in pregnant women.
Pyrazinamide in small quantities excreted in breast milk.
Special instructions
With monotherapy to pyrazinamide, resistance of mycobacteria rapidly develops, and therefore pyrazinamide is usually used in combination with other anti-tuberculosis drugs.
Pyrazinamide is excreted by dialysis.
With prolonged use, it is advisable regularly (1 time per month) to monitor the activity of hepatic transaminases and the content of uric acid in the blood.
- Brand name: Pyrazinamide
- Active ingredient: Pyrazinamide
- Dosage form: Pills.
- Manufacturer: Ozone
- Country of Origin: Russia
- Pyrazinamide-induced sideroblastic anemia
- Specificity and Mechanism of Acinetobacter baumanii Nicotinamidase: Implications for Activation of the Front-Line Tuberculosis Drug Pyrazinamide
- Potential Tuberculostatic Agent: Micelle-forming Pyrazinamide Prodrug
- Comments on the use of pyrazinamide
- Metabolic disposition of pyrazinamide in the rat: Identification of a novel in vivo metabolite common to both rat and human
- Investigation of the effects of concomitant caffeine administration on the metabolic disposition of pyrazinamide in rats
- The Effect of pyrazinamide and rifampicin on isoniazid metabolism in rats
- The effect of rifampicin and pyrazinamide on isoniazid pharmacokinetics in rats
- ChemInform Abstract: New Derivatives of Isoniazide, Pyrazinamide, and 2-Aminobutanol and Their Antitubercular Activity.
- ChemInform Abstract: Catalytic Synthesis of Pyrazinamide from 2,5-Dimethylpyrazine.
- Synthesis and in vitro Anti-Tuberculosis Activity of Amidine and Hydrazidine Analogues of Pyrazinamide and Isoniazid.
- Deleterious influence of pyrazinamide on the outcome of patients with fulminant or subfulminant liver failure during antituberculous treatment including isoniazid
- Biowaiver monographs for immediate release solid oral dosage forms: Pyrazinamide
- Polarographic determination of pyrazinamide serum and plasma concentrations in the presence of isoniazid
- Construction and properties of a pyrazinamide-selective biosensor using chemoreceptor structures from crayfish
- Crayfish walking leg neuronal biosensor for the detection of pyrazinamide and selected local anesthetics
- Liquid chromatographic assay for the simultaneous determination of pyrazinamide and rifampicin in serum samples from patients with tuberculosis meningitis
- Rapid and simultaneous determination of pyrazinamide and its major metabolites in human plasma by high-performance liquid chromatography
- Microdétermination du pyrazinamide et de ses métabolites (acide pyrazinoïque, acide hydroxy-5-pyrazinoïque, hydroxy-5-pyrazinamide, acide pyrazinurique) plasmatiques et urinaires par chromatographie en phase liquide
- Identification of 5-hydroxypyrazinamide isolated from urine of subjects given pyrazinamide
- Comprehensive assay for pyrazinamide, rifampicin and isoniazid with its hydrazine metabolites in human plasma by column liquid chromatography
- Comparative bioavailability of rifampicin, isoniazid and pyrazinamide from a four drug fixed dose combination with separate formulations at the same dose levels
- Biological evaluation of pyrazinamide liposomes for treatment of Mycobacterium tuberculosis
- Peruvian and globally reported amino acid substitutions on the Mycobacterium tuberculosis pyrazinamidase suggest a conserved pattern of mutations associated to pyrazinamide resistance