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pyrazinamide

 

Classes: Antitubercular Agents

Dosing and uses of Pyrazinamide

 

Adult dosage forms and strengths

tablet

  • 500mg

 

Tuberculosis Treatment For HIV Negative

Daily therapy

  • 15-30 mg/kg PO qDay; not to exceed 2 g/day

Twice weekly therapy

  • 50 mg/kg PO twice weekly; not to exceed 2 g/dose

 

Tuberculosis Treatment For HIV Exposed/Infected

20-40 mg/kg/dose PO qDay; not to exceed 2 g/day

 

See Also Combo

With isoniazid & rifampin

 

Other Indications & Uses

Tuberculosis; should always be admin with other anti-TB drugs

 

Pediatric dosage forms and strengths

tablet

  • 500mg

 

Tuberculosis Treatment

Daily therapy

  • 15-30 mg/kg PO qD; not to exceed 2000 mg/day

Twice weekly therapy

  • 50 mg/kg/dose; not to exceed 3000 mg/day

 

Pyrazinamide adverse (side) effects

1-10%

Malaise

Nausea

Vomiting

Anorexia

Arthralgia

Myalgia

 

<1%

Fever

Rash

Itching

Acne

Photosensitivity

Gout

Dysuria

Porphyria

Thrombocytopenia

Hepatotoxicity

Interstitial nephritis

 

Warnings

Contraindications

Severe hepatic damage, acute gout, hypersensitivity

 

Cautions

See pkg insert for complete dosage info

 

Pregnancy and lactation

Pregnancy category: C

Lactation: enters breast milk

 

Pregnancy categories

A: Generally acceptable. Controlled studies in pregnant women show no evidence of fetal risk.

B: May be acceptable. Either animal studies show no risk but human studies not available or animal studies showed minor risks and human studies done and showed no risk.

C: Use with caution if benefits outweigh risks. Animal studies show risk and human studies not available or neither animal nor human studies done.

D: Use in LIFE-THREATENING emergencies when no safer drug available. Positive evidence of human fetal risk.

X: Do not use in pregnancy. Risks involved outweigh potential benefits. Safer alternatives exist.

NA: Information not available.

 

Pharmacology of Pyrazinamide

Absorption: well absorbed

Distribution: widely into body tissues and fluids including liver, lung, and CSF

Relative diffusion from blood into CSF: adequate with or without inflammation (exceeds usual MICs)

CSF:blood level ratio: inflamed meninges: 100%

Protein binding: 50%

Metabolism: hepatic

Half-life elimination: 9-10 hr

Time to peak, serum: within 2 hr

Excretion: urine (4% as unchanged drug)

 

Mechanism of action

Unknown; bacteriostatic or -cidal for Mycobacterium