rate of risperidone hydroxylation was elevated in NFIB rs28379954 T>C carriers among CYP2D6 normal metabolizers, resulting in a similar rate of drug metabolism to what is observed in CYP2D6 ultrarapid metabolizers, with no such effect observed in CYP2D6 poor metabolizers lacking functional enzyme...
CYP enzyme activities were measured by means of the metabolic ratios of sparteine (CYP2D6), endogenous cortisol metabolism (CYP3A4), and caffeine (CYP1A2), as well as by the S/R ratio of mephenytoin (CYP2C19) and antipyrine clearance. The metabolic ratio of sparteine increased after 24 ...
Hepatic CYP enzyme activity was measured before departure, at 24 and 96 hours after arrival to high-altitude location, and at 1 month after return to sea level. CYP enzyme activities were measured by means of the metabolic ratios of sparteine (CYP2D6), endogenous cortisol metabolism (CYP3A4)...
Similar metabolic activities were found for the long-term models HepaRG, HREL, and HepatoPac and the short-term suspension cultures when averaged across all 11 enzyme markers, although differences were seen in the activities of CYP2D6 and non-CYP enzymes. For iCell and HepG2, the metabolic ...
the use ofabacavirin patients with moderate-to-severe hepatic dysfunction is contraindicated. The use of abacavir withribavirinorganciclovircan increase the likelihood of mitochondrial, hepatic, andpancreatic toxicities. Abacavir is not a substrate or inhibitor of the CYP450 enzyme complex, can be taken...
5). Several models, such as a recombinant CYP expression system, microsomes, have been employed to enhance drug metabolism capabilities, although the in vitro metabolic activation system cannot fully replicate the intricate drug metabolism observed in in vivo testing38. Among these systems, recombinant...
Involvement of CYP3A4 and CYP2D6 in the Metabolism of Haloperidol 1. Human cytochrome P450 (CYP) isoenzymes expressed in a human cell line were used to elucidate their involvement in the metabolism of haloperidol (HAL).2... F Jian,GB Baker,PH Silverstone,... - 《Cellular & Molecular Neur...
13 Mice expressing human CYP2D6 and CYP3A4 have been successfully generated; however, many other components of human drug metabolism and transport might be important for consideration in such a holistic model to adequately represent the interplay of drug metabolism in man. Large species differences ...
Over the past two decades, the pig has gained attention as a potential model for human drug metabolism. Cytochrome P450 enzymes (CYP450), a superfamily of biotransformation enzymes, are pivotal in drug metabolism. Porcine CYP450 has been demonstrated to
The hepatic clearance and drug-drug interactions of luteolin and apigenin were studied by using primary cultured rat hepatocytes. Luteolin and apigenin experienced extensive first-pass metabolism. The elimination percent of luteolin and apigenin was found to be 91.9% and 86.7% after 120 min of incuba...