Is there a need to increase the dose of efavirenz during concomitant rifampicin-based antituberculosis therapy in sub-Saharan Africa? The HIV-TB pharmagene study

Pharmacogenomics. 2015;16(10):1047-64. doi: 10.2217/pgs.15.35. Epub 2015 Apr 1.

Abstract

Aims: The current HIV treatment guidelines are inconsistent about the need for weight-based efavirenz dose adjustment during rifampicin containing antituberculosis (anti-TB) cotreatment. We investigated effect of rifampicin-based anti-TB cotreatment on plasma efavirenz exposure and treatment outcome, considering effect of CYP2B6 genotype and bodyweight.

Patients & methods: HIV-only (arm 1, n = 285) or TB-HIV (arm 2, n = 208) coinfected patients were enrolled and received efavirenz-based ART alone or with rifampicin-based anti-TB therapy, respectively. Plasma efavirenz concentrations at 4th and 16th weeks, viral load and CD4 cell count at 24th and 48th weeks were determined.

Results: The mean plasma efavirenz concentration at weeks 4 (p = 0.03) and 16 (p = 0.08) was inconsistently higher in arm 2 than arm 1, mainly in CYP2B6*6 carriers. Effect of bodyweight on efavirenz pharmacokinetics was significant only in arm 1, but not in arm 2. Proportion of patients with nondetectable viral load (≤50 copies/ml) at week 24 was higher in arm 1 than arm 2 patients (91.0 vs 76.3%; p = 0.002), but no significant difference was observed at week 48 (89.5 vs 87.8%; p = 0.22).

Conclusion: Rifampicin-based anti-TB cotreatment has no significant influence on long-term efavirenz plasma exposure and efficacy. Hence, there is no need to increase the dose of efavirenz during concomitant rifampicin-based anti-TB cotreatment in the sub-Saharan African population.

Keywords: CYP2B6; Ethiopia; HIV/AIDS; efavirenz; rifampicin; sub-Saharan Africa; treatment guideline; tuberculosis.

Publication types

  • Clinical Trial
  • Comparative Study
  • Multicenter Study
  • Observational Study
  • Research Support, Non-U.S. Gov't

MeSH terms

  • Adult
  • Africa South of the Sahara
  • Alkynes
  • Anti-HIV Agents / administration & dosage*
  • Antibiotics, Antitubercular / therapeutic use*
  • Antiretroviral Therapy, Highly Active / methods
  • Benzoxazines / administration & dosage*
  • CD4 Lymphocyte Count / methods
  • Coinfection / drug therapy
  • Cyclopropanes
  • Cytochrome P-450 CYP2B6 / metabolism
  • Female
  • Genotype
  • HIV Infections / drug therapy*
  • Humans
  • Male
  • Pharmacogenetics / methods
  • Prospective Studies
  • Reverse Transcriptase Inhibitors / administration & dosage*
  • Rifampin / therapeutic use*
  • Tuberculosis / drug therapy*

Substances

  • Alkynes
  • Anti-HIV Agents
  • Antibiotics, Antitubercular
  • Benzoxazines
  • Cyclopropanes
  • Reverse Transcriptase Inhibitors
  • Cytochrome P-450 CYP2B6
  • efavirenz
  • Rifampin