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Pyrazinamide deamidase activity in tuberculous disease
The American Review of Respiratory Disease
|July 1, 1981
Summary
Tuberculosis does not suppress pyrazinamide deamidase activity. Serum pyrazinamide concentrations and half-lives were similar in patients with active tuberculosis and healthy controls, indicating consistent drug metabolism.
Area of Science:
- Pharmacology
- Infectious Diseases
- Tuberculosis Research
Background:
- Tuberculosis treatment relies on drugs like pyrazinamide.
- Pyrazinamide's efficacy depends on its conversion to pyrazinoic acid by pyrazinamide deamidase.
- Understanding pyrazinamide metabolism in active tuberculosis is crucial for treatment optimization.
Purpose of the Study:
- To determine if active tuberculosis suppresses pyrazinamide deamidase activity.
- To compare pyrazinamide pharmacokinetics between tuberculosis patients and healthy individuals.
Main Methods:
- Administered a 40 mg/kg dose of pyrazinamide to 10 patients with active pulmonary tuberculosis and 10 healthy controls.
- Measured serial serum concentrations of pyrazinamide over time.
- Calculated pyrazinamide half-lives in both groups.
Main Results:
- Serum pyrazinamide concentrations were comparable between tuberculosis patients and control subjects.
- Pyrazinamide half-lives were similar in both groups.
- No significant difference in pyrazinamide metabolism was observed.
Conclusions:
- Active tuberculosis does not appear to suppress pyrazinamide deamidase activity.
- Pyrazinamide pharmacokinetics remain consistent in patients with active tuberculosis.
- This suggests reliable pyrazinamide efficacy in treating tuberculosis.