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Pyrazinamide Data - Uses, Dosage, Drug class, Brand name, Warnings, etc



Pharmacology Pyrazinamide is a synthetic analogue of niacinamide, active only against mycobacteria.
Mode of action unknown; most effective at acidic pH, targeting intracellular organisms.
Resistance develops rapidly when used alone; no cross-resistance with isoniazid.
Adult Dosage PO for latent tuberculosis infection:
- Daily: 15–20 mg/kg/day (max 2 g) with rifampin 10 mg/kg/day (max 600 mg) as a single dose for 2 months
- Twice weekly (DOT): 50 mg/kg/dose (max 4 g) with rifampin 10 mg/kg/dose (max 600 mg) for 2–3 months
PO for active tuberculosis:
- See isoniazid dosage for combination regimens
Dosage Forms - Tablet: 500 mg
- Combination Tablet (Rifater): Pyrazinamide 300 mg + isoniazid 50 mg + rifampin 120 mg
Pharmacokinetics Absorption:
- Well absorbed from GI tract
Peak Serum Concentration:
- 40–50 mg/L (0.3–0.4 mmol/L) 2 hr post 1 g dose
- 20–60 mg/L (163–488 µmol/L) 2 hr post 1–2 g dose (adequate absorption)
Excretion:
- Parent compound and metabolites primarily in urine
Adverse Reactions Frequent:
- Hyperuricemia (due to metabolite inhibition of uric acid excretion)
Occasional:
- Dose-dependent hepatotoxicity
- 1–5% of patients on isoniazid-rifampin-pyrazinamide regimens show hepatic enzyme elevations
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