Article information
Resumen
Etravirina (ETR) es un fármaco perteneciente a la familia de los inhibidores de la transcriptasa inversa no análogos de nucleósidos (ITINAN), con actividad antiviral en situaciones de resistencia a los ITINAN de primera generación. Las interacciones farmacológicas producidas por ETR se deben a su efecto dual sobre el sistema CYP450. Es inductor de la actividad de CYP3A4 e inhibidor de la de CYP2C9 y CYP2C19. ETR presenta escasas interacciones farmacológicas clínicamente significativas, entre las que destacan los inhibidores de la proteasa sin potenciar, los ITINAN efavirenz y nevirapina, ritonavir a dosis plena y tipranavir/ritonavir. La interacción con fosamprenavir/ritonavir no es clínicamente significativa, aunque hay una escasa variación de sus valores plasmáticos al administrarse de manera conjunta con ETR. No presenta interacciones con darunavir/ritonavir.
Palabras clave:
Etravirina
Interacciones
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.
Keywords:
Etravirine
Drug interactions
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