What is the drug pyrazinamide used to treat?

Pyrazinamide kills or stops the growth of certain bacteria that cause tuberculosis (TB). It is used with other drugs to treat tuberculosis. This medication is sometimes prescribed for other uses; ask your doctor or pharmacist for more information.

What is the structure of pyrazinamide?

C5H5N3OPyrazinamide / Formula

Who discovered pyrazinamide?

As previously described, pyrazinamide (PZA) (Fig. 1(2)) emerged as an outgrowth of research conducted by Vital Chorine who discovered the ability of subcutaneous nicotinamide to prolong survival of Mtb-infected guinea pigs (Chorine 1945).

What is the meaning of pyrazinamide?

A synthetic pyrazinoic acid amide derivative with bactericidal property. Pyrazinamide is particularly active against slowly multiplying intracellular bacilli (unaffected by other drugs) by an unknown mechanism of action.

How is pyrazinamide metabolized?

Pyrazinamide, an antituberculous agent, is transformed to pyrazinoic acid in the human body and then excreted in the urine (1). Al- though other metabolites have been demon- strated, their amounts were minimal (2), and pyrazinoic acid is the sole main metabolite of pyrazinamide in humans and in laboratory animals.

Why pyrazinamide is a prodrug?

Pyrazinamide is a prodrug that stops the growth of M. tuberculosis. Pyrazinamide diffuses into the granuloma of M. tuberculosis, where the tuberculosis enzyme pyrazinamidase converts pyrazinamide to the active form pyrazinoic acid.

How does pyrazinamide cause hepatotoxicity?

The mechanism of hepatic injury by pyrazinamide is not known, but the drug is extensively metabolized by the liver and injury may be caused by a metabolic intermediate. Hepatotoxicity from pyrazinamide appears to be more frequent with higher doses, suggesting a direct toxic effect, at least in part.

Is pyrazinamide bacteriostatic or bactericidal?

Pyrazinamide is bactericidal for M. tuberculosis, particularly when bacilli are found inside macrophages or other similarly acidic environments. Pyrazinamide exerts maximal effect during the first 2 months of therapy, and its use allows treatment duration to be shortened to 6 months.

What are the contraindications of pyrazinamide?

The following conditions are contraindicated with this drug….Who should not take PYRAZINAMIDE?

• diabetes.
• a type of joint disorder due to excess uric acid in the blood called gout.
• porphyria.
• alcoholism.
• severe liver disease.

Is pyrazinamide more hepatotoxic than isoniazid?

Results. Preventive treatment with rifampin-pyrazinamide caused severe hepatotoxicity more often than did preventive treatment with isoniazid (odds ratio [OR], 2.61; 95% confidence interval [CI], 1.26–5.39; P = . 012), especially in patients <25 years old.