ACITRETIN BIOTRANSFORMATION INTO ETRETINATE - ROLE OF ETHANOL ON IN-VITRO HEPATIC-METABOLISM

The aim of this study was to investigate the possible esterification o f acitretin into etretinate by using hepatocytes in primary culture fr om the rat, monkey, dog and man. With rat and human hepatocytes, etret inate was detectable only when ethanol was co-administered with acitre tin. With monkey and dog cells, traces of etretinate were found withou t ethanol addition, but the esterification of acitretin was highly enh anced by ethanol. The metabolic profile was not changed when cells wer e pre-incubated with ethanol. Therefore acitretin seems to act rather as a substrate than an enzymatic inducer.