pyrazinamiidiin

Pyrazinamide is a synthetic antibiotic belonging to the pyrazinamide class of drugs and is widely used in the treatment of tuberculosis. It was first discovered and approved by the United States Food and Drug Administration in 1968. The drug is available in oral dosage forms, including tablets and liquid preparations, and is additionally used in the form of a dosage rectangle with a co-formulated rifampin and isoniazid. Pyrazinamide is also marketed alone or in combination with other antitubercular agents in several countries under various trade names.

The mechanism of action of pyrazinamide is not fully understood. It is thought to be related to its active form, pyrazinoic acid, which accumulates inside Mycobacterium tuberculosis. The acid form interferes with mycobacterial cell processes by undermining membrane lipid transport, causing an energy crisis and subsequent cell death, or by altering membrane enzyme function. The drug is specifically effective against the dormant, metabolically sluggish form of the pathogen that later becomes active, reducing treatment duration and preventing relapse.

Treatment guidelines recommend that pyrazinamide be used as a component of a four-drug regimen during the initial phase of therapy. The standard dose for adults is 15–20 mg/kg/day orally, typically divided into two or three daily doses. Pyrazinamide is generally administered for 2–4 months in combination therapy and is usually not prescribed as a single-agent treatment. It is metabolised in the liver via glucuronidation, and the drug is excreted via the kidneys, primarily unchanged.

Common adverse effects of pyrazinamide include hepatotoxicity, which can lead to transaminase elevation or, in rare cases, severe liver injury. Sore throat and gynecomastia may occur, and the drug can produce a tingling sensation (paresthesia) in the hands and feet. Patients with pre‑existing liver disease or poor liver function are advised to undergo close monitoring while on pyrazinamide therapy. Avoid carrying the drug in a bag or compartment where it may be accidentally taken for other types of medications to prevent unnecessary toxic exposure.