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CYP2B6 mediates the in vitro hydroxylation of bupropion: potential drug interactions with other antidepressants.
- L. Hesse, K. Venkatakrishnan, D. Greenblatt
- Biology, ChemistryDrug metabolism and disposition: the biological…
- 1 October 2000
Bupropion hydroxylation is mediated almost exclusively by CYP2B6 and can serve as an index reaction reflecting activity of this isoform and suggest a low inhibitory potency versus CYP 2D6, the clinical importance of which is not established.
Midazolam and triazolam biotransformation in mouse and human liver microsomes: relative contribution of CYP3A and CYP2C isoforms.
- M. Perloff, L. V. von Moltke, M. Court, T. Kotegawa, R. Shader, D. Greenblatt
- Biology, ChemistryThe Journal of pharmacology and experimental…
- 1 February 2000
TRZ hydroxylation appears to be CYP3A specific in mice and humans, demonstrating that metabolic profiles of drugs in animals cannot be assumed to reflect human metabolic patterns, even with closely related substrates.
Metabolism of the antidepressant mirtazapine in vitro: contribution of cytochromes P-450 1A2, 2D6, and 3A4.
- E. Störmer, L. V. von Moltke, R. Shader, D. Greenblatt
- BiologyDrug metabolism and disposition: the biological…
- 1 October 2000
Induction/inhibition or genetic polymorphisms of CYP2D6, CYP1A2, and CYP3A4 may affect MIR metabolism, but involvement of several enzymes in different metabolic pathways may prevent large alterations in in vivo drug clearance.
Effect of Age, Gender, and Obesity on Midazolam Kinetics
- D. Greenblatt, D. Abernethy, A. Locniskar, J. Harmatz, R. Limjuco, R. Shader
- Medicine, BiologyAnesthesiology
- 1 July 1984
Midazolam elimination half‐life (t1/2) after iv dosage was significantly prolonged in elderly (aged 60‐74 yr) versus young (24‐33 yr) males and in obese subjects (8.4 vs. 2.7, P < 0.001) and Vd was greater in the obese subjects even after correction for total weight, indicating disproportionate distribution of midAZolam into adipose weight.
Escitalopram (S-citalopram) and its metabolites in vitro: cytochromes mediating biotransformation, inhibitory effects, and comparison to R-citalopram.
- L. V. von Moltke, D. Greenblatt, G. Giancarlo, B. Granda, J. Harmatz, R. Shader
- Biology, MedicineDrug metabolism and disposition: the biological…
- 1 August 2001
S-CT, biotransformed by three CYP isoforms in parallel, is unlikely to be affected by drug interactions or genetic polymorphisms and are also unlikely to cause clinically important drug interactions via CYP inhibition.
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
Midazolam Hydroxylation by Human Liver Microsomes In Vitro: Inhibition by Fluoxetine, Norfluoxetine, and by Azole Antifungal Agents
- L. Moltke, D. Greenblatt, R. Shader
- Biology, ChemistryJournal of clinical pharmacology
- 1 September 1996
Results are consistent with results of other in vitro studies and of clinical studies, indicating that fluoxetine, largely via its metabolite norfluoxettine, may impair clearance of P450‐3A substrates.
Pharmacokinetics of Diphenhydramine and a Demethylated Metabolite Following Intravenous And Oral Administration
- G. Blyden, D. Greenblatt, J. Scavone, R. Shader
- Medicine, ChemistryJournal of clinical pharmacology
- 10 September 1986
Kinetics of diphenhydramine (DP) hydrochloride and a major demethylated metabolite (DMDP) were determined from multiple plasma samples drawn during a 24‐ to 48‐hour period after dosage using a gas chromatographic technique.
Inhibition of Human Cytochrome P450 Isoforms by Nonnucleoside Reverse Transcriptase Inhibitors
In vitro microsomal model provides relevant predictive data on probable drug interactions with NNRTIs when the mechanism is inhibition of CYP‐mediated drug biotransformation, however, the model does not incorporate interactions attributable to enzyme induction.
Population Pharmacokinetics of Methylphenidate in Children with Attention‐Deficit Hyperactivity Disorder
- R. Shader, J. Harmatz, J. Oesterheld, D. Parmelee, F. Sallee, D. Greenblatt
- MedicineJournal of clinical pharmacology
- 1 August 1999
The relatively noninvasive approach used in this study allows the assessment of pharmacokinetic properties of medications under conditions of appropriate clinical use in special populations such as children, adolescents, and the elderly.