[Etravirine drug interactions]

Enferm Infecc Microbiol Clin. 2009 Dec:27 Suppl 2:27-31. doi: 10.1016/S0213-005X(09)73216-1.
[Article in Spanish]

Abstract

Etravirine (ETR) belongs to the family of non-nucleoside analogue reverse transcriptase inhibitors (NNRTIs), with antiviral activity in patients with resistance to first-generation NNRTIs. The drug interactions caused by ETR are due to its dual effect on the CYP450 system. ETR acts as an inducer of CYP3A4 and inhibitor of CYP2C9 and CYP2C19. This drug shows few clinically significant drug interactions, the most important of which involve the unboosted protease inhibitors, the NNRTIs efavirenz and nevirapine, full-dose ritonavir and tipranavir/ritonavir. Interaction with fosamprenavir/ritonavir is not clinically significant, although their plasma levels vary slightly when used in combination with ETR. ETR shows no interactions with darunavir/ritonavir.

Publication types

  • Review

MeSH terms

  • Analgesics / pharmacology
  • Anesthetics / pharmacology
  • Anti-HIV Agents / administration & dosage
  • Anti-HIV Agents / pharmacokinetics
  • Anti-HIV Agents / pharmacology*
  • Anti-HIV Agents / therapeutic use
  • Anti-Infective Agents / pharmacology
  • Anticonvulsants / pharmacology
  • Antiretroviral Therapy, Highly Active
  • Aryl Hydrocarbon Hydroxylases / antagonists & inhibitors*
  • Biotransformation / drug effects*
  • Contraceptives, Oral, Hormonal / pharmacology
  • Contraindications
  • Cytochrome P-450 CYP2C19
  • Cytochrome P-450 CYP2C9
  • Cytochrome P-450 CYP3A / biosynthesis*
  • Cytochrome P-450 CYP3A / genetics
  • Drug Interactions
  • Drug Therapy, Combination
  • Enzyme Induction / drug effects
  • HIV Infections / drug therapy*
  • HIV Protease Inhibitors / administration & dosage
  • HIV Protease Inhibitors / pharmacokinetics
  • HIV Protease Inhibitors / pharmacology
  • HIV Reverse Transcriptase / antagonists & inhibitors*
  • HIV-1 / drug effects
  • Humans
  • Microsomes, Liver / drug effects*
  • Microsomes, Liver / enzymology
  • Nitriles
  • Piperazines / administration & dosage
  • Piperazines / pharmacology
  • Purines / administration & dosage
  • Purines / pharmacology
  • Pyridazines / administration & dosage
  • Pyridazines / pharmacokinetics
  • Pyridazines / pharmacology*
  • Pyridazines / therapeutic use
  • Pyrimidines
  • Reverse Transcriptase Inhibitors / administration & dosage
  • Reverse Transcriptase Inhibitors / pharmacokinetics
  • Reverse Transcriptase Inhibitors / pharmacology*
  • Reverse Transcriptase Inhibitors / therapeutic use
  • Sildenafil Citrate
  • Sulfones / administration & dosage
  • Sulfones / pharmacology

Substances

  • Analgesics
  • Anesthetics
  • Anti-HIV Agents
  • Anti-Infective Agents
  • Anticonvulsants
  • Contraceptives, Oral, Hormonal
  • HIV Protease Inhibitors
  • Nitriles
  • Piperazines
  • Purines
  • Pyridazines
  • Pyrimidines
  • Reverse Transcriptase Inhibitors
  • Sulfones
  • etravirine
  • Sildenafil Citrate
  • CYP2C9 protein, human
  • Cytochrome P-450 CYP2C9
  • Aryl Hydrocarbon Hydroxylases
  • CYP2C19 protein, human
  • Cytochrome P-450 CYP2C19
  • Cytochrome P-450 CYP3A
  • CYP3A4 protein, human
  • reverse transcriptase, Human immunodeficiency virus 1
  • HIV Reverse Transcriptase