Effects of injectable propofol emulsion on singlet oxygen released from activated human neutrophils and that chemically generated.

Effects of an injectable emulsion of propofol and its emulsifier on singlet oxygen (1O2) were examined. 1O2 released from activated human neutrophils was detected by chemiluminescence, and chemically generated 1O2 was detected by electron paramagnetic resonance (EPR). Both the propofol emulsion and the emulsifier suppressed 1O2 release from neutrophils.

Impact of CYP2D6*10 on mexiletine pharmacokinetics in healthy adult volunteers.

Objective: In vitro studies with human liver microsomes have suggested that the oxidative conversion of mexiletine (MX) to its metabolites is catalyzed by CYP2D6 and is significantly impaired in microsomes with the CYP2D6*10/*10 genotype. Therefore, we examined the influence of the CYP2D6*10 allele on MX pharmacokinetics in Japanese subjects.

Methods: Subjects with CYP2D6*1/*1 (group *1/*1; n=5), CYP2D6*10/*10 (group *10/*10; n=6) and CYP2D6*5/*10 (group *5/*10; n=4) genotypes received a single 200-mg dose of MX.

Mexiletine carbonyloxy beta-D-glucuronide: a novel metabolite in human urine.

1. The study was performed to isolate and characterize a glucuronic acid conjugate of mexiletine that releases mexiletine on acid hydrolysis from urine samples obtained from healthy volunteers following a single oral dose of mexiletine. 2.

Influence of the CYP2D6*10 allele on the metabolism of mexiletine by human liver microsomes.

Aims: To study the influence of CYP2D6*10 on the formation of p-hydroxymexiletine (PHM) and hydroxymethylmexiletine (HMM) using microsomes from human liver of known genotypes.

Methods: Microsomes from human livers of genotype CYP2D6*1/*1 (n = 5), *1/*10 (n = 6) and *10/*10 (n = 6) were used in this study. The formation of PHM and HMM was determined by high-performance liquid chromatography.

Quantitative prediction of in vivo drug interactions between nevirapine and antifungal agents from in vitro data in rats.

We investigated the effects of ketoconazole (KCZ) and fluconazole (FCZ) on rat liver microsomal nevirapine (NVP) metabolism in vitro and on NVP plasma profiles in vivo in order to determine whether the in vivo drug interactions could be predicted quantitatively from the in vitro data. The Ki values of KCZ and FCZ for NVP 12-hydroxylation were 1.59 microm and 11.