Pyrazinamide NEW

Specification

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Key Mechanism of Action

Pyrazinamide is taken up by Mycobacterium tuberculosis (the bacteria that causes TB) and converted to its active form, pyrazinoic acid, by the bacterial enzyme pyrazinamidase.

Pyrazinoic acid disrupts the acid-base balance inside the bacterial cell, inhibits fatty acid synthesis, and damages the bacterial cell membrane, ultimately leading to bacterial death.

It is most effective against M. tuberculosis that resides in the acidic environment of macrophages (immune cells that engulf bacteria), a niche where other first-line TB drugs (e.g., isoniazid, rifampicin) are less potent.

Main Uses

• This combination therapy reduces the risk of drug resistance and ensures complete elimination of the bacteria.

• It is effective for both pulmonary TB (affecting the lungs) and extrapulmonary TB (affecting organs like the lymph nodes, bones, or kidneys).

  Prevention of Tuberculosis (Rarely Used)

  In some cases, it may be part of a preventive therapy regimen for individuals at high risk of developing active TB (e.g., those with latent TB infection and immunocompromise), but this is not a primary indication.

Important Notes

• Drug Resistance: Monotherapy with pyrazinamide is strictly prohibited, as it rapidly leads to the development of resistant M. tuberculosis strains.

• Side Effects: The most common side effect is hyperuricemia (elevated uric acid levels in the blood), which can trigger gout. Other side effects include hepatotoxicity (liver damage), gastrointestinal disturbances, and skin rashes.

• Contraindications: It is contraindicated in patients with severe liver disease or a history of gout, and requires dose adjustment in patients with renal impairment.

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