No

Antitubercular Agent

Adjunctive treatment of tuberculosis in combination with other antituberculosis agents

C

Severe hepatic damage; hypersensitivity to pyrazinamide or any component; acute gout

Use with caution in patients with renal failure, chronic gout, diabetes mellitus, or porphyria

1% to 10%:

Central nervous system: Malaise

Gastrointestinal: Nausea, vomiting, anorexia

Neuromuscular & skeletal: Arthralgia, myalgia

<1%: Fever, rash, itching, acne, photosensitivity, gout, dysuria, porphyria, thrombocytopenia, hepatotoxicity, interstitial nephritis

Symptoms of overdose include gout, gastric upset, hepatic damage (mild)

Treatment following GI decontamination is supportive

No data reported

Converted to pyrazinoic acid in susceptible strains of Mycobacterium which lowers the pH of the environment; exact mechanism of action has not been elucidated

Bacteriostatic or bactericidal depending on the drug's concentration at the site of infection

Distribution: Widely distributed into body tissues and fluids including the liver, lung, and CSF

Relative diffusion of antimicrobial agents from blood into cerebrospinal fluid (CSF): Adequate with or without inflammation (exceeds usual MICs)

Ratio of CSF to blood level (%): Inflamed meninges: 100

Protein binding: 50%

Metabolism: In the liver

Half-life: 9-10 hours

Time to peak serum concentration: Within 2 hours

Elimination: In urine (4% as unchanged drug)

Oral (calculate dose on ideal body weight rather than total body weight): Note: A four-drug regimen (isoniazid, rifampin, pyrazinamide, and either streptomycin or ethambutol) is preferred for the initial, empiric treatment of TB. When the drug susceptibility results are available, the regimen should be altered as appropriate.

Daily therapy: 15-30 mg/kg/day (maximum: 2 g/day)

Directly observed therapy (DOT): Twice weekly: 50-70 mg/kg (maximum: 4 g)

DOT: 3 times/week: 50-70 mg/kg (maximum: 3 g)

Elderly: Start with a lower daily dose (15 mg/kg) and increase as tolerated

Dosing adjustment in renal impairment: Cl_cr <50 mL/minute: Avoid use or reduce dose to 12-20 mg/kg/day

Dosing adjustment in hepatic impairment: Reduce dose

Periodic liver function tests, serum uric acid, sputum culture, chest x-ray 2-3 months into treatment and at completion

Reacts with Acetest® and Ketostix® to produce pinkish-brown color

May cause drowsiness

None reported

No information available to require special precautions

No effects or complications reported

Take with food for full length of therapy. Do not miss doses and do not discontinue without consulting prescriber. You will need regular medical follow-up while taking this medication. You may experience nausea or loss of appetite; small frequent meals, frequent mouth care, sucking lozenges, or chewing gum may help. Report unusual fever, unresolved nausea or vomiting, change in color of urine, pale stools, easy bruising or bleeding, blood in urine or difficulty urinating, yellowing of skin or eyes, or extreme joint pain. Pregnancy precautions: Inform prescriber if you are or intend to be pregnant.

Monitor periodic liver function tests, serum uric acid

Tablet: 500 mg

Pyrazinamide suspension can be compounded with simple syrup or 0.5% methylcellulose with simple syrup at a concentration of 100 mg/mL; the suspension is stable for 2 months at 4°C or 25°C when stored in glass or plastic bottles

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