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A method for estimating the probability of adverse drug reactions
TLDR
It was shown that the ADR probability scale has consensual, content, and concurrent validity and may be applicable to postmarketing drug surveillance.
Evaluation of 3'-azido-3'-deoxythymidine, morphine, and codeine as probe substrates for UDP-glucuronosyltransferase 2B7 (UGT2B7) in human liver microsomes: specificity and influence of the UGT2B7*2
TLDR
Although both AZT and morphine can serve as in vitro probe substrates for UGT2B7, AZT appears to be more selective than morphine.
Effects of the Antifungal Agents on Oxidative Drug Metabolism
TLDR
The interactions of ketoconazole with cyclosporin and tacrolimus have been applied for therapeutic purposes to allow a lower dosage and cost of the immunosuppressant and a reduced risk of fungal infections.
CYP2B6 mediates the in vitro hydroxylation of bupropion: potential drug interactions with other antidepressants.
TLDR
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.
In vitro metabolism of midazolam, triazolam, nifedipine, and testosterone by human liver microsomes and recombinant cytochromes p450: role of cyp3a4 and cyp3a5.
TLDR
CYP3A4 and CYP3A5 both contribute to midazolam, triazol am, testosterone, and nifedipine biotransformation in HLMs, with CYP 3A5 being metabolically less active than CYP2A4 in general.
Human Drug Metabolism and the Cytochromes P450: Application and Relevance of In Vitro Models
TLDR
This review evaluates the major human hepatic drug‐metabolizing CYP enzymes and their clinically relevant substrates, inhibitors, and inducers and discusses the molecular bases and clinical implications of genetic polymorphisms that affect the CYPs.
Effect of Obesity on the Pharmacokinetics of Drugs in Humans
TLDR
Clinicians should design treatment regimens that account for any significant differences in the CL and Vd in the obese, using a size descriptor that corrects for differences in absolute CL between obese and non-obese individuals.
Pharmacogenetic determinants of interindividual variability in bupropion hydroxylation by cytochrome P450 2B6 in human liver microsomes.
TLDR
The results of this study indicate that interindividual variability in bupropion hydroxylation is a consequence of interactions between environmental and genetic influences on CYP2B6 gene function.
Apparent mechanism-based inhibition of human CYP2D6 in vitro by paroxetine: comparison with fluoxetine and quinidine.
TLDR
Spectral scanning of CYP2D6 with paroxetine yielded an increase in absorbance at 456 nm suggesting parxetine inactivation of cytochrome P450 2D6 via the formation of a metabolite intermediate complex, consistent with the metabolism of the methylenedioxy substituent in par oxetine.
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