Insights into the pharmacokinetic properties of antitubercular drugs

Expert Opin Drug Metab Toxicol. 2016 Jul;12(7):765-78. doi: 10.1080/17425255.2016.1183643. Epub 2016 May 17.

Abstract

Introduction: The furiously advancing cases of multidrug-resistant tuberculosis (TB) along with the recent emergence of total drug resistant TB and TB-AIDS comorbidity present an increased threat to global public health. Knowledge of pharmacokinetic properties helps in selecting an appropriate anti-TB dosage regimen to achieve optimal results in patients.

Areas covered: This article provides a brief compilation of the information available regarding published pharmacokinetic data for anti-TB drugs and may act as a single window for investigators/medical practitioners in this field. The information regarding absorption, tissue distribution, elimination and pharmacokinetic interactions of the first- and second-line anti-TB drugs and candidate drugs under clinical trials is discussed.

Expert opinion: Pharmacokinetic properties such as poor absorption, too short biological half-life, extensive first-pass metabolism, drug-food and drug-drug related interactions are not attractive for prospective anti-TB drugs and significantly contribute to treatment failure and further resistance. The long duration, monotonous and multidrug treatment plan leads to poor patient compliance and resulted in a greater occurrence of anti-TB drug resistance worldwide. Few new agents, which are in development phase, are considering the aspect of shortening duration of the treatment regimen and provide a boost in therapy that is sorely needed.

Keywords: Anti-TB; absorption; distribution; excretion; metabolism.

Publication types

  • Review

MeSH terms

  • Acquired Immunodeficiency Syndrome / complications
  • Animals
  • Antitubercular Agents / pharmacokinetics*
  • Antitubercular Agents / therapeutic use
  • Drug Interactions
  • Drug Resistance, Multiple, Bacterial
  • Food-Drug Interactions
  • Global Health*
  • Half-Life
  • Humans
  • Medication Adherence
  • Public Health
  • Tissue Distribution
  • Tuberculosis, Multidrug-Resistant / drug therapy*
  • Tuberculosis, Multidrug-Resistant / epidemiology

Substances

  • Antitubercular Agents