title: [Etravirine in first-line therapy].
abstract: Etravirine (ETR) is a non-nucleoside reverse transcriptase inhibitor (NNRTI) with a potent and broad in vitro spectrum of activity against HIV-1 and viruses with NNRTI resistances, allowing sequential use of drugs of this family. The potency, efficacy and safety of etravirine have been demonstrated in multi-treated patients, but few data are available on first-line antiretroviral therapy (ART) and the role of this drug in initial treatment phases has not been defined. The presence of primary NNRTI resistances and those acquired during first-line therapy is increasingly frequent. Due to its genetic barrier and efficacy, ETR can form part of a second-line ART regimen in patients with failure to a first-line regimen. In the initial phases, adverse effects continue to be the main reason for modifying ART. ETR has demonstrated safety and tolerability, with no central nervous system adverse effects and a good liver, lipid and gastrointestinal safety profile. As with the other NNRTIs, the most common adverse effect is rash. Because of ETR good tolerability profile, this drug can be considered when a new treatment is required due to adverse effects. Because of the characteristics of ETR the possibility of once-daily administration and dissolution in water, as well as the absence of drug-drug interactions with methadone this drug is especially attractive as a firstline therapy and in patients with poor adherence, such as intravenous drug users receiving methadone treatment.
authors.affiliation: Hospital Universitario Miguel Servet, Zaragoza, España. parazo@salud.aragon.es
authors.forename: Piedad Arazo
authors.initials: PA
authors.lastname: Garcés
authors.forename: Esther Valero
authors.initials: EV
authors.lastname: Tena
mesh_terms: D019380:Anti-HIV Agents / Q000008:administration & dosage / Q000009:adverse effects / Q000493:pharmacokinetics / Q000627:therapeutic use*; D056486:Chemical and Drug Induced Liver Injury / Q000209:etiology; D003875:Drug Eruptions / Q000209:etiology; D004347:Drug Interactions; D024921:Drug Resistance, Multiple, Viral; D015751:Genes, pol / Q000235:genetics; D015658:HIV Infections / Q000150:complications / Q000188:drug therapy*; D054303:HIV Reverse Transcriptase / Q000037:antagonists & inhibitors* / Q000235:genetics; D015497:HIV-1 / Q000187:drug effects* / Q000201:enzymology; D006525:Hepatitis, Viral, Human / Q000150:complications; D006556:Heroin Dependence / Q000150:complications / Q000534:rehabilitation; D006801:Humans; D001523:Mental Disorders / Q000139:chemically induced; D008691:Methadone / Q000493:pharmacokinetics; D015337:Multicenter Studies as Topic / Q000706:statistics & numerical data; D009570:Nitriles; D010349:Patient Compliance; D011724:Pyridazines / Q000008:administration & dosage / Q000009:adverse effects / Q000493:pharmacokinetics / Q000627:therapeutic use*; D011743:Pyrimidines; D016032:Randomized Controlled Trials as Topic / Q000706:statistics & numerical data; D018894:Reverse Transcriptase Inhibitors / Q000008:administration & dosage / Q000009:adverse effects / Q000493:pharmacokinetics / Q000627:therapeutic use*; D015819:Substance Abuse, Intravenous / Q000150:complications / Q000534:rehabilitation
chemical_list: D019380:Anti-HIV Agents; D009570:Nitriles; D011724:Pyridazines; D011743:Pyrimidines; D018894:Reverse Transcriptase Inhibitors; C451734:etravirine; C514824:reverse transcriptase, Human immunodeficiency virus 1; D054303:HIV Reverse Transcriptase; D008691:Methadone