Pharmacokinetics and Pharmacodynamics of Intensive Antituberculosis Treatment of Tuberculous Meningitis

Clin Pharmacol Ther. 2020 Apr;107(4):1023-1033. doi: 10.1002/cpt.1783. Epub 2020 Feb 29.

Abstract

The most effective antituberculosis drug treatment regimen for tuberculous meningitis is uncertain. We conducted a randomized controlled trial comparing standard treatment with a regimen intensified by rifampin 15 mg/kg and levofloxacin for the first 60 days. The intensified regimen did not improve survival or any other outcome. We therefore conducted a nested pharmacokinetic/pharmacodynamic study in 237 trial participants to define exposure-response relationships that might explain the trial results and improve future therapy. Rifampin 15 mg/kg increased plasma and cerebrospinal fluid (CSF) exposures compared with 10 mg/kg: day 14 exposure increased from 48.2 hour·mg/L (range 18.2-93.8) to 82.5 hour·mg/L (range 8.7-161.0) in plasma and from 3.5 hour·mg/L (range 1.2-9.6) to 6.0 hour·mg/L (range 0.7-15.1) in CSF. However, there was no relationship between rifampin exposure and survival. In contrast, we found that isoniazid exposure was associated with survival, with low exposure predictive of death, and was linked to a fast metabolizer phenotype. Higher doses of isoniazid should be investigated, especially in fast metabolizers.

Publication types

  • Randomized Controlled Trial
  • Research Support, Non-U.S. Gov't

MeSH terms

  • Adult
  • Antitubercular Agents / administration & dosage*
  • Antitubercular Agents / blood*
  • Double-Blind Method
  • Drug Therapy, Combination
  • Female
  • Humans
  • Levofloxacin / administration & dosage
  • Levofloxacin / blood
  • Male
  • Rifampin / administration & dosage
  • Rifampin / blood
  • Treatment Outcome
  • Tuberculosis, Meningeal / blood*
  • Tuberculosis, Meningeal / diagnosis
  • Tuberculosis, Meningeal / drug therapy*

Substances

  • Antitubercular Agents
  • Levofloxacin
  • Rifampin

Associated data

  • ISRCTN/ISRCTN61649292