[Safety and tolerability of etravirine].

Abstract

Etravirine (ETR) is the first representative of a new generation of non-nucleoside reverse transcriptase inhibitors (NNRTI) and is indicated in patients with HIV infection and virological failure. The recommended dose is 200 mg (two tablets) every 12 hours after a meal. ETR has good tolerability and the tablets can be dissolved in water, which can aid swallowing in some patients. This drug has a plasma half-life of 30-40 hours and consequently is a candidate for once-daily regimens. The most frequent adverse effect is rash (affecting 19% of patients), which is usually mild (grades 1 or 2) and does not lead to drug withdrawal. The DUET 1 and 2 studies, which compared ETR versus placebo, with both groups receiving boosted darunavir and an optimized background regimen, did not demonstrate a higher incidence of liver toxicity, neuropsychiatric symptoms, gastrointestinal disturbances or atherogenic dyslipidemia in patients receiving ETR. The safety profile of ETR suggests that it could be used as a substitute drug in patients with toxicity induced by first-generation NNRTIs or other antiretroviral drugs.

• Authors: Joaquín Portilla
• Journal: Enfermedades infecciosas y microbiologia clinica (Enferm Infecc Microbiol Clin) Vol. 27 Suppl 2 Pg. 21-6 (Dec 2009) ISSN: 0213-005X [Print] Spain
• Vernacular Title: Seguridad y tolerabilidad de etravirina.
• PMID: 20116624 (Publication Type: Journal Article, Review)
• Copyright: 2009 Elsevier España S.L. All rights reserved.

Chemical References

• Anti-HIV Agents
• Nitriles
• Pyridazines
• Pyrimidines
• Reverse Transcriptase Inhibitors
• Sulfonamides
• etravirine
• reverse transcriptase, Human immunodeficiency virus 1
• HIV Reverse Transcriptase
• Darunavir

Topics

• Animals
• Anti-HIV Agents (adverse effects, pharmacology, therapeutic use)
• Chemical and Drug Induced Liver Injury (etiology)
• Darunavir
• Drug Eruptions (etiology)
• Drug Evaluation, Preclinical
• Dyslipidemias (chemically induced)
• Female
• Fetus (drug effects)
• Gastrointestinal Diseases (chemically induced)
• HIV Infections (drug therapy)
• HIV Reverse Transcriptase (antagonists & inhibitors)
• Humans
• Male
• Mental Disorders (chemically induced)
• Multicenter Studies as Topic (statistics & numerical data)
• Nitriles
• Pregnancy
• Pregnancy Complications, Infectious (drug therapy)
• Pyridazines (adverse effects, pharmacology, therapeutic use)
• Pyrimidines
• Quality of Life
• Randomized Controlled Trials as Topic (statistics & numerical data)
• Reverse Transcriptase Inhibitors (adverse effects, pharmacology, therapeutic use)
• Sulfonamides (adverse effects, therapeutic use)