Pyrafat - General Information:A pyrazine that is used therapeutically as an antitubercular agent. [PubChem]
Pharmacology:Pyrafat 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.
Pyrafat for patients
Pyrazinamide has been reported to interfere with ACETEST® and KETOSTIX® urine tests to produce a pink-brown color. 5
Pyrazinamide is contraindicated in persons:
- with severe hepatic damage.
- who have shown hypersensitivity to it.
- with acute gout.
Additional information about PyrafatPyrafat Indication: For the initial treatment of active tuberculosis in adults and children when combined with other antituberculous agents.
Mechanism Of Action: Pyrafat 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 Pyrafat decreases the effect of cyclosporine
Food Interactions: Not Available
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)
Half Life: 9-10 hours (normal conditions)
Dosage Forms of Pyrafat: Tablet Oral
Chemical IUPAC Name: pyrazine-2-carboxamide
Chemical Formula: C5H5N3O
Pyrazinamide on Wikipedia: http://en.wikipedia.org/wiki/Pyrazinamide
Organisms Affected: Mycobacterium tuberculosis
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