Seguridad y tolerabilidad de etravirina

Portilla, Joaquín

doi:10.1016/S0213-005X(09)73215-X

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Resumen

Etravirina (ETR) es el primer representante de una nueva generación de inhibidores de la transcriptasa inversa no análogos de nucleósidos (ITINAN), y está indicado en el tratamiento de pacientes con infección por VIH en situación de fracaso virológico. La dosis recomendada es de 200 mg (2 comprimidos) cada 12 h, después de una comida. La tolerabilidad a ETR es buena, los comprimidos son fácilmente dispersables en agua y ello puede mejorar la deglución de los comprimidos en algunos pacientes. ETR tiene una vida media en plasma de 30-40 h, por ello es un fármaco candidato a pautas de 1 vez al día. El exantema cutáneo es el efecto adverso más frecuente en pacientes que reciben ETR (19%), suele ser leve (grados 1 o 2) y no obliga a suspender el fármaco. Los estudios DUET-1 y 2, que compararon ETR frente a placebo, ambos grupos con darunavir potenciado y terapia optimizada, no demostraron una mayor incidencia de toxicidad hepática, síntomas neuropsiquiátricos, trastornos gastrointestinales o dislipemia aterógena en los pacientes que recibieron ETR. El perfil de seguridad de ETR sugiere que podría utilizarse como fármaco de sustitución en pacientes con toxicidad inducida por ITINAN de primera generación u otros fármacos antirretrovirales.

Palabras clave:

Etravirina

Inhibidores no nucleósidos de la transcriptasa inversa

Infección por VIH

Efectos adversos

Exantema

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.

Key words:

Etravirine

Non-nucleoside reverse transcriptase inhibitors

HIV infection

Adverse effects

Rash

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