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Pezetamid: Full Drug Profile

Medically reviewed by Min Clinic Staff | Updated: January 2026

Pezetamid - General Information

A pyrazine that is used therapeutically as an antitubercular agent. [PubChem]

 

Pharmacology of Pezetamid

Pezetamid kills or stops the growth of certain bacteria that cause tuberculosis (TB). It is used with other drugs to treat tuberculosis. It is a highly specific agent and is active only against Mycobacterium tuberculosis. In vitro and in vivo, the drug is active only at a slightly acid pH.

 

Pezetamid for patients

 

Pezetamid Interactions

Pyrazinamide has been reported to interfere with ACETEST® and KETOSTIX® urine tests to produce a pink-brown color. 5

 

Pezetamid Contraindications

Pyrazinamide is contraindicated in persons:

  • with severe hepatic damage.
  • who have shown hypersensitivity to it.
  • with acute gout.

 

Additional information about Pezetamid

Pezetamid Indication

For the initial treatment of active tuberculosis in adults and children when combined with other antituberculous agents.

Mechanism Of Action
Pezetamid is an important sterilizing drug that shortens tuberculosis (TB) therapy. However, the mechanism of action of pyrazinamide is poorly understood because of its unusual properties. In literature it has been written that the pyrazinoic acid (POA), the active moiety of pyrazinamide, disrupted membrane energetics and inhibited membrane transport function at acid pH in Mycobacterium tuberculosis. The antimycobacterial activity appears to partly depend on conversion of the drug to POA. Susceptible strains of M. tuberculosis produce pyrazinamidase, an enzyme that deaminates pyrazinamide to POA, and the vitro susceptibility of a given strain of the organism appears to correspond to its pyrazinamidase activity. Experimental evidence suggests that pyrazinamide diffuses into M. tuberculosis in a passive manner, is converted into POA by pyrazinamidase, and because of an inefficient efflux system, accumulates in huge amounts in the bacterial cytoplasm. The accumulation of POA lowers the intracellular pH to a suboptimal level that is likely to inactivate a vital target enzyme such as fatty acid synthase.
Drug Interactions
Cyclosporine Pezetamid decreases the effect of cyclosporine
Generic Name
Pyrazinamide
Synonyms
Pyrazinecarboxylic acid amide; Pyrazinecarboxamide; Pyrazinoic acid amide; PZA; Pyrazineamide; Pyrazine carboxylamide; Pyrazinamdie; Pirazinamid; Pirazimida
Drug Category
Antitubercular Agents
Drug Type
Small Molecule; Approved
Other Brand Names containing Pyrazinamide
Aldinamid; Aldinamide; Braccopiral; Corsazinmid; Dipimide; Eprazin; Farmizina; Isopas; Lynamide; Novamid; Pezetamid; Piraldina; Pirilene; Prazina; Pyrafat; Pyramide; Pyrazide; Pyrazinamide BP 2000; Rifater; Rozide; Tebrazid; Tebrazio; Unipyranamide; Zinamide; Zinastat; pms-Pyrazinamide;
Absorption
Rapidly and well absorbed from the gastrointestinal tract.
Toxicity (Overdose)
Side effects include liver injury, arthralgias, anorexia, nausea and vomiting, dysuria,malaise and fever, sideroblastic anemia, adverse effects on the blood clotting mechanism or vascular integrity, and hypersensitivity reactions such as urticaria, pruritis and skin rashes.
Protein Binding
~10% (bound to plasma proteins)
Biotransformation
Hepatic.
Half Life
9-10 hours (normal conditions)
Dosage Forms of Pezetamid
Tablet Oral
Chemical IUPAC Name
pyrazine-2-carboxamide
Chemical Formula
C5H5N3O
Organisms Affected
Mycobacterium tuberculosis