Concentrations of rifampicin in pre-dose samples in patients with pulmonary tuberculosis

Rifampicin is used in both phases of treatment for tuberculosis. In chronic use, the short half-life and the self-induction of metabolism can decrease the levels of the drug below the minimal inhibitory concentration. The aim of the study was to investigate whether plasma concentrations of rifampicin are sustained above 0.5 μg/mL in patients with tuberculosis using 600 mg/day. Rifampicin was measured in plasma by high-performance liquid chromatography and a sputum smear microscopy was performed in all days of the study. A total of 44 male patients completed the study. On days 31, 61 and 91, the mean plasma concentrations of rifampicin were 0.6 (0.5) μg/mL, 0.55 (0.5) μg/mL and 0.46 (0.4) μg/mL. There was a high variation of rifampicin levels leading to a high percentage of samples with concentrations below 0.5 μg/mL. There was no significant association between the frequency of samples with drug levels below 0.5 μg/mL with the conversion of the sputum microscopy. These data suggest that pre-doses samples offer limited information on the exposure of M. tuberculosis to rifampicin.