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Pyrazinamide information from DrugsUpdate  

See Available Brands of Pyrazinamide in India

P - Contraindicated in pregnancy
L - Caution when used during lactation

Pyrazinamide is a drug used to treat tuberculosis. The drug is largely bacteriostatic, but can be bacteriocidal on actively replicating tuberculosis bacteria.

Pharmacodynamics

Pharmacokinetics

Pyrazinamide has bactericidal action against M. tuberculosis in acid environment present in macrophages and inflammed tissue. Together with rifampicin provides greatest sterilising action with reduction in relapse rate. Reduces tubular secretion of uric acid.

Absorption
Readily absorbed from the GI tract (oral); peak plasma concentrations after 2 hours.

Distribution

Body fluids and tissues (wide), CSF, enters breast milk.

Metabolism

Hepatic; hydrolysed to pyrazinoic acid (active) then hydroxylated to 5-hydroxypyrazinoic acid (major excretory product).

Excretion

Via urine by glomerular filtration (70% as metabolites, 4-14% as unchanged); 9-10 hours (elimination half-life), removed by dialysis.

Pyrazinamide Indications / Pyrazinamide Uses

Information Not Available

Pyrazinamide Adverse Reactions / Pyrazinamide Side Effects

Hepatotoxicity (hepatomegaly, splenomegaly and jaundice may develop and in rare case fulminating acute yellow atrophy and death). Anorexia, nausea, vomiting, arthralgia, malaise, fever, hyperuricaemia, abnormal LFT, skin rashes.

Potentially Fatal: Severe liver damage, fulminant hepatitis.

Precautions

Pyrazinamide inhibits renal excretion of urates, frequently resulting in hyperuricemia which is usually asymptomatic. If hyperuricemia is accompanied by acute gouty arthritis, Pyrazinamide should be discontinued.

Pyrazinamide should be used with caution in patients with a history of diabetes mellitus, as management may be more difficult.

Primary resistance of M. tuberculosis to Pyrazinamide is uncommon. In cases with known or suspected drug resistance, in vitro susceptibility tests with recent cultures of M. tuberculosis against Pyrazinamide and the usual primary drugs should be performed. There are few reliable in vitro tests for Pyrazinamide resistance. A reference laboratory capable of performing these studies must be employed.

Special Precautions

Diabetes, renal failure, history of gout, children. Monitor liver function and serum uric acid regularly.

Other Drug Interactions

Excretion may be blocked by probenecid

Other Interactions

Information Not Available

Dosage

Oral
Tuberculosis
Adult: As part of a mulitdrug regimen, 20-25 mg/kg (max: 2 g) daily or 1.5-3 g 3 times weekly.
Child: As part of a mulitdrug regimen, 35 mg/kg daily or 50 mg/kg 3 times weekly or 75 mg/kg twice weekly. Max dose: 3 g daily.
Renal impairment: May need dose reduction.

Food(before/after)

Should be taken with food

List of Contraindications

Pyrazinamide and Pregnancy

Contraindicated in pregnancy

Category C: Either studies in animals have revealed adverse effects on the foetus (teratogenic or embryocidal or other) and there are no controlled studies in women or studies in women and animals are not available. Drugs should be given only if the potential benefit justifies the potential risk to the foetus.

Pyrazinamide and Lactation

Caution when used in lactation


Excreted in breast milk

Pyrazinamide and Children

Use only if therapy is essential


Appears to be well tolerated in children

Pyrazinamide and Geriatic

Use with caution, usually starting at the low end of the dosage range, because of the greater frequency of decreased hepatic, renal, or cardiac function, and concomitant diseases or other drug therapy.

Pyrazinamide and Other Contraindications

Hypersensitivity; existing liver disease; acute gout or hyperuricaemia. Porphyria. Pregnancy and lactation.

Storage

Oral
Store at 15-30°C.

Lab interference

Oral
Store at 15-30°C.

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