Klin Farmakol Farm. 2009;23(3):108-110

On the possibility of interactions of rocuronium with liver microsomal cytochromes P450

doc. RNDr. Eva Anzenbacherová, CSc¹, Pavel Anzenbacher², Alena Tunková², Milan Adamus³

¹ Ústav lékařské chemie a biochemie, LF UP, Olomouc

² Ústav farmakologie LF UP a FN Olomouc

³ Klinika anesteziologie a resuscitace FN Olomouc

Aim of the study: Aim of the study was to find whether human liver microsomal cytochromes P450 interact with rocuronium in vitro.

Methods: Interaction of rocuronium with microsomal cytochromes P450 was followed spectrophotometrically using difference absorption

spectroscopy. Interaction with cytochrome P450 form CYP3A4 was studied by determination of inhibition of a CYP3A4-specific enzyme

activity (testosterone 6β-hydroxylation) by HPLC.

Results: Rocuronium interacts in vitro with human liver microsomal cytochromes P450 and inhibits effectively the CYP3A4 specific

enzyme activity.

Conclusion: Due to the fact that the CYP3A4 form is known to metabolize steroids and steroid-related compounds there is a possibility

of an influence of rocuronium-CYP3A4 interactions on other processes in the organism. Moreover, a possibility of drug interactions with

concomitantly administered drugs metabolized by CYP3A4 leading to e.g. prolongation of rocuronium effect cannot be excluded.

Keywords: rocuronium, metabolism, CYP3A4, cytochromes P450.

Published: November 6, 2009  Show citation