[Safety and tolerability of etravirine].
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.
Portilla
Joaquín
J
Hospital General Universitario de Alicante, España. portilla_joa@gva.es
D000818:Animals; D019380:Anti-HIV Agents / Q000009:adverse effects* / Q000494:pharmacology / Q000627:therapeutic use; D056486:Chemical and Drug Induced Liver Injury / Q000209:etiology; D000069454:Darunavir; D003875:Drug Eruptions / Q000209:etiology; D004353:Drug Evaluation, Preclinical; D050171:Dyslipidemias / Q000139:chemically induced; D005260:Female; D005333:Fetus / Q000187:drug effects; D005767:Gastrointestinal Diseases / Q000139:chemically induced; D015658:HIV Infections / Q000188:drug therapy*; D054303:HIV Reverse Transcriptase / Q000037:antagonists & inhibitors*; D006801:Humans; D008297:Male; D001523:Mental Disorders / Q000139:chemically induced; D015337:Multicenter Studies as Topic / Q000706:statistics & numerical data; D009570:Nitriles; D011247:Pregnancy; D011251:Pregnancy Complications, Infectious / Q000188:drug therapy; D011724:Pyridazines / Q000009:adverse effects* / Q000494:pharmacology / Q000627:therapeutic use; D011743:Pyrimidines; D011788:Quality of Life; D016032:Randomized Controlled Trials as Topic / Q000706:statistics & numerical data; D018894:Reverse Transcriptase Inhibitors / Q000009:adverse effects* / Q000494:pharmacology / Q000627:therapeutic use; D013449:Sulfonamides / Q000009:adverse effects / Q000627:therapeutic use
D019380:Anti-HIV Agents; D009570:Nitriles; D011724:Pyridazines; D011743:Pyrimidines; D018894:Reverse Transcriptase Inhibitors; D013449:Sulfonamides; C451734:etravirine; C514824:reverse transcriptase, Human immunodeficiency virus 1; D054303:HIV Reverse Transcriptase; D000069454:Darunavir