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Comparison between cytochrome P450 (CYP) content and relative activity approaches to scaling from cDNA-expressed CYPs to human liver microsomes: ratios of accessory proteins as sources of
Relative activity factors (RAFs) and immunoquantified levels of cytochrome P450 (CYP) isoforms both have been proposed as scaling factors for the prediction of hepatic drug metabolism from studiesExpand
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O- and N-demethylation of Venlafaxine In Vitro by Human Liver Microsomes and by Microsomes from cDNA-Transfected Cells: Effect of Metabolic Inhibitors and SSRI Antidepressants
The biotransformation of venlafaxine (VF) into its two major metabolites, O-desmethylvenlafaxine (ODV) and N-desmethylvenlafaxine (NDV) was studied in vitro with human liver microsomes and withExpand
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Time course of recovery of cytochrome p450 3A function after single doses of grapefruit juice
Components of grapefruit juice may impair the activity of intestinal cytochrome P450 (CYP) 3A enzymes, sometimes resulting in clinically important drug interactions. The time course of recovery fromExpand
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Effect of Age, Gender, and Obesity on Midazolam Kinetics
&NA; The effects of age, sex, and obesity on the kinetics of single intravenous (iv) and oral doses of midazolam were evaluated in healthy volunteers who received 2.5‐5 mg of iv midazolam on oneExpand
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Escitalopram (S-citalopram) and its metabolites in vitro: cytochromes mediating biotransformation, inhibitory effects, and comparison to R-citalopram.
Transformation of escitalopram (S-CT), the pharmacologically active S-enantiometer of citalopram, to S-desmethyl-CT (S-DCT), and of S-DCT to S-didesmethyl-CT (S-DDCT), was studied in human liverExpand
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Inhibition of Human Cytochrome P450 Isoforms by Nonnucleoside Reverse Transcriptase Inhibitors
The capacity of three clinically available nonnucleoside reverse transcriptase inhibitors (NNRTIs) to inhibit the activity of human cytochromes P450 (CYPs) was studied in vitro using human liverExpand
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Population Pharmacokinetics of Methylphenidate in Children with Attention‐Deficit Hyperactivity Disorder
Sources of individual variation in plasma methylphenidate (MP) concentrations during usual clinical use are not established. This was evaluated in a series of patients receiving clinical treatmentExpand
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Midazolam Hydroxylation by Human Liver Microsomes In Vitro: Inhibition by Fluoxetine, Norfluoxetine, and by Azole Antifungal Agents
Biotransformation of the imidazobenzodiazepine midazolam to its α‐hydroxy and 4‐hydroxy metabolites was studied in vitro using human liver microsomal preparations. Formation of α‐hydroxy‐midazolamExpand
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Inhibition of human cytochromes P450 by components of Ginkgo biloba
The extraction, isolation and characterization of 29 natural products contained in Ginkgo biloba have been described, which we have now tested for their in‐vitro capacity to inhibit the five majorExpand
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Protease Inhibitors as Inhibitors of Human Cytochromes P450: High Risk Associated with Ritonavir
Four protease inhibitor antiviral agents (ritonavir, indinavir, nelfinavir, saquinavir) were evaluated as in vitro inhibitors of the activity of six human cytochromes using an in vitro model based onExpand
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