Efavirenz intoxication due to a new CYP2B6 constellation

Antivir Ther. 2013;18(5):739-43. doi: 10.3851/IMP2571. Epub 2013 May 2.

Abstract

Here, we describe severe neuropsychiatric symptoms in an HIV-positive Asian man with extremely high efavirenz plasma levels while receiving standard treatment with efavirenz/tenofovir/emtricitabine fixed-dose regimen. Genetic examination revealed compound homozygosity for loss-of-function alleles of CYP2B6, including coding for a rare truncated protein. Neuropsychiatric symptoms resolved completely after efavirenz discontinuation.

Publication types

  • Case Reports

MeSH terms

  • Adult
  • Alkynes
  • Alleles
  • Anti-HIV Agents / pharmacokinetics*
  • Anti-HIV Agents / therapeutic use
  • Aryl Hydrocarbon Hydroxylases / genetics
  • Aryl Hydrocarbon Hydroxylases / metabolism*
  • Benzoxazines / metabolism*
  • Cyclopropanes
  • Cytochrome P-450 CYP2B6
  • Genotype
  • HIV Infections / drug therapy
  • HIV Infections / enzymology
  • HIV Infections / genetics
  • HIV-1
  • Humans
  • Male
  • Pharmacogenetics
  • Polymorphism, Single Nucleotide
  • Reverse Transcriptase Inhibitors / pharmacokinetics*
  • Reverse Transcriptase Inhibitors / therapeutic use

Substances

  • Alkynes
  • Anti-HIV Agents
  • Benzoxazines
  • Cyclopropanes
  • Reverse Transcriptase Inhibitors
  • Aryl Hydrocarbon Hydroxylases
  • CYP2B6 protein, human
  • Cytochrome P-450 CYP2B6
  • efavirenz