The pharmacokinetics of enteral antituberculosis drugs in patients requiring intensive care

S Afr Med J. 2013 Apr 5;103(6):394-8. doi: 10.7196/samj.6344.

Abstract

Background: There is a paucity of data on the pharmacokinetics of fixed-dose combination enteral antituberculosis treatment in critically ill patients.

Objectives: To establish the pharmacokinetic profile of a fixed-dose combination of rifampicin, isoniazid, pyrazinamide and ethambutol given according to weight via a nasogastric tube to patients admitted to an intensive care unit (ICU).

Methods: We conducted a prospective, observational study on 10 patients (mean age 32 years, 6 male) admitted to an ICU and treated for tuberculosis (TB). Serum concentrations of the drugs were determined at eight predetermined intervals over 24 hours by means of high-performance liquid chromatography.

Results: The therapeutic maximum plasma concentration (Cmax) for rifampicin at time to peak concentration was achieved in only 4 patients, whereas 2 did not achieve therapeutic Cmax for isoniazid. No patient reached sub-therapeutic Cmax for pyrazinamide (6 were within and 4 above therapeutic range). Three patients reached sub-therapeutic Cmax for ethambutol, and 6 patients were within and 1 above the therapeutic range. Patients with a sub-therapeutic rifampicin level had a higher mean Acute Physiology and Chronic Health Evaluation II (APACHE II) score (p=0.03) and a lower estimated glomerular filtration rate (GFR) (p=0.03).

Conclusions: A fixed-dose combination tablet, crushed and mixed with water, given according to weight via a nasogastric tube to patients with TB admitted to an ICU resulted in sub-therapeutic rifampicin plasma concentrations in the majority of patients, whereas the other drugs had a more favourable pharmacokinetic profile. Patients with a sub-therapeutic rifampicin concentration had a higher APACHE II score and a lower estimated GFR, which may contribute to suboptimal outcomes in critically ill patients. Studies in other settings have reported similar proportions of patients with 'sub-therapeutic' rifampicin concentrations.

MeSH terms

  • APACHE
  • Adult
  • Antitubercular Agents / pharmacokinetics*
  • Area Under Curve
  • Chromatography, High Pressure Liquid
  • Drug Therapy, Combination
  • Female
  • Glomerular Filtration Rate
  • Humans
  • Intensive Care Units*
  • Male
  • Prospective Studies
  • South Africa / epidemiology
  • Tablets
  • Tuberculosis, Pulmonary / drug therapy*

Substances

  • Antitubercular Agents
  • Tablets