Theoretical calculation of triazolam hydroxylation and endogenous steroid inhibition in the active site of CYP3A4

Effect of active infection on cytochrome P450‐mediated metabolism of cyclosporine in renal transplant patients

“…Concerning cytokines released during inflammatory conditions, a stimulation of the hypothalamus pituitary‐adrenal axis also occurs by factors produced at inflamed area, promoting an increase in corticosteroid secretion during early stage of the inflammatory response . These endogenous steroids are metabolized by CYP3A4 and may competitively inhibit drug metabolism catalyzed by CYP3A4 .…”

An epoxidation mechanism of carbamazepine by CYP3A4

“…27 It oxidizes more than half of the medicines that are metabolized by CYP, especially macrolides, steroids and anti-epilepsy medicines. 28,29 Thus, investigation of the mechanism of drug metabolism by human CYP3A4 is important and will be helpful for the development of various types of pharmaceutics in the future.…”

Primary hepatocytes as an useful bioassay to characterize metabolism and bioactivity of illicit steroids in cattle

“…The former refers to competition of two substrates for CYP3A4, while the second one lies in the formation of a stable intermediate-metabolite complex, with an irreversible loss of catalytic function and reduced clearance of other CYP3A substrates (Polasek and Miners, 2006;Zhou, 2008). Differences in the interaction between the steroid and the CYP3A active site have also been considered to explain the steroid inhibitory effects on CYP3A4dependent TST hydroxylation (Torimoto et al, 2007). Taken together, these evidences would be helpful to justify the inhibitory effect of ADD, BOLD and DHEA on CYP3Adependent TST hydroxylation here observed.…”