Use in conjunction with at least one other antituberculosis agent in the treatment of clinical tuberculosis.
藥理
Pyrazinamide, a derivative of niacinamide, is a synthetic antituberculosis agent. Pyrazinamide may be bacteriostatic or bactericidal in action, depending on the concentration of the drug attained at the site of the infection and the susceptibility of the infecting organism.
藥動學
Pyrazinamide is well absorbed from the GI tract. Pyrazinamide is widely distributed into body tissues and fluids including the liver, lungs, and CSF. Pyrazinamide is hydrolyzed in the liver to pyrazinoic acid, the major active metabolite; some hydrolysis may also occur in the stomach and bladder. Within 24 hours, approximately 70% of an oral dose of pyrazinamide is excreted in urine, mainly by glomerular filtration. About 4–14% of the dose is excreted as unchanged drug; the remainder is excreted as metabolites. The plasma half-life of pyrazinamide is 9–10 hours in patients with normal renal and hepatic function. The plasma half-life of the drug may be prolonged in patients with impaired renal or hepatic function.
禁忌症
Patients with severe hepatic damage, renal failure, gout.
懷孕分類
C
哺乳分類
Because pyrazinamide is distributed into milk in small amounts, a decision should be made whether to discontinue nursing or the drug, taking into account the importance of the drug to the woman.
Tuberculosis, treatment, drug-susceptible: Once-daily therapy:
40 to 55 kg: 1 g once daily. Note: The preferred frequency of administration is once daily; however, 5-days per week administration by directly-observed therapy (DOT) is an acceptable alternative.
56 to 75 kg: 1.5 g once daily.
76 to 90 kg: 2 g once daily. Three-times-weekly DOT:
40 to 55 kg: 1.5 g 3 times weekly.
56 to 75 kg: 2.5 g 3 times weekly.
76 to 90 kg: 3 g 3 times weekly. Twice-weekly DOT:
40 to 55 kg: 2 g twice weekly.
56 to 75 kg: Oral: 3 g twice weekly.
76 to 90 kg: Oral: 4 g twice weekly. 4-month rifapentine-moxifloxacin–based regimen:
40 to <55 kg: Oral: 1 g once daily.
≥55 to 75 kg: Oral: 1.5 g once daily.
>75 kg: Oral: 2 g once daily. Tuberculosis, treatment, drug-resistant (alternative agent) : 25 to 40 mg/kg once daily.
小兒調整劑量
(Younger than 15 years and 40 kg or less) Intensive phase: 30 to 40 mg/kg orally once daily for 8 weeks (56 doses) or 5 days per week for 8 weeks (40 doses); give in combination with isoniazid 10 to 15 mg/kg orally/IM once daily or 5 days per week, rifampin 10 to 20 mg/kg orally/IV once daily or 5 days per week, and ethambutol 15 to 25 mg/kg orally once daily or 5 days per week
(15 years or older or 40 to 55 kg) Intensive phase: 1000 mg orally once daily for 8 weeks (56 doses) or 5 days per week for 8 weeks (40 doses); give in combination with isoniazid 300 mg (about 5 mg/kg) orally/IM once daily or 5 days per week, rifampin 600 mg (about 10 mg/kg) orally/IV once daily or 5 days per week, and ethambutol 800 mg orally once daily or 5 days per week
(15 years or older or 56 to 75 kg) Intensive phase: 1500 mg orally once daily for 8 weeks (56 doses) or 5 days per week for 8 weeks (40 doses); give in combination with isoniazid 300 mg (about 5 mg/kg) orally/IM once daily or 5 days per week, rifampin 600 mg (about 10 mg/kg) orally/IV once daily or 5 days per week, and ethambutol 1200 mg orally once daily or 5 days per week
(15 years or older or 76 to 90 kg) Intensive phase: 2000 mg orally once daily for 8 weeks (56 doses) or 5 days per week for 8 weeks (40 doses); give in combination with isoniazid 300 mg (about 5 mg/kg) orally/IM once daily or 5 days per week, rifampin 600 mg (about 10 mg/kg) orally/IV once daily or 5 days per week, and ethambutol 1600 mg orally once daily or 5 days per week
腎功能調整劑量
CrCl ≥30 mL/minute: No dosage adjustment necessary.
CrCl <30 mL/minute:
Tuberculosis, treatment (drug-susceptible) :
40 to 55 kg: 1 g 3 times weekly.
56 to 75 kg: 1.5 g 3 times weekly.
76 to 90 kg: 2 g 3 times weekly. Tuberculosis, treatment (drug-resistant) (alternative agent) : 25 to 40 mg/kg 3 times weekly.