Effect of psychotropic medication on the in vitro metabolism of buprenorphine in human cDNA-expressed cytochrome P450 enzymes
European Journal of Clinical Pharmacology, ISSN: 0031-6970, Vol: 62, Issue: 8, Page: 639-643
2006
- 8Citations
- 11Captures
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Example: if you select the 1-year option for an article published in 2019 and a metric category shows 90%, that means that the article or review is performing better than 90% of the other articles/reviews published in that journal in 2019. If you select the 3-year option for the same article published in 2019 and the metric category shows 90%, that means that the article or review is performing better than 90% of the other articles/reviews published in that journal in 2019, 2018 and 2017.
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Metrics Details
- Citations8
- Citation Indexes8
- CrossRef6
- Captures11
- Readers11
- 11
Article Description
Objective: The aim of the present study was to estimate the drug interaction potential of psychtropic medication on buprenorphine (BUP) N-dealkylation using cDNA-expressed cytochrome P450 (CYP) enzymes. Methods: BUP was incubated with psychotropic drugs and cDNA-expressed CYP 3A4 and CYP 2C8 enzymes. Seven substances were screened for their inhibition potency. To check for a mechanism-based component in inhibition, all substances were tested with and without preincubation, respectively. Norbuprenorphine (NBUP) concentrations were determined by liquid chromatography/tandem mass spectrometry, following liquid/liquid extraction. Results: Midazolam and zolpidem demonstrated greatest inhibition in screening experiments. As expected, IC values without preincubation were higher than those after 30-min preincubation, with zolpidem 113.1 μM and midazolam 20.25 μM. Following a 30-min preincubation period in the absence of the probe substrate BUP, the apparent IC values for zolpidem and midazolam were 20.17 μM and 3.5 μM. Conclusion: Both midazolam and zolpidem showed a distinct inhibitory potency towards NBUP formation by CYP 3A4, implicating a decreased conversion of BUP. When preincubated, the inhibitory potency was increased, which strongly suggests a metabolically activated component in inhibition. © Springer-Verlag 2006.
Bibliographic Details
http://www.scopus.com/inward/record.url?partnerID=HzOxMe3b&scp=33746413855&origin=inward; http://dx.doi.org/10.1007/s00228-006-0147-6; http://www.ncbi.nlm.nih.gov/pubmed/16802166; http://link.springer.com/10.1007/s00228-006-0147-6; http://www.springerlink.com/index/10.1007/s00228-006-0147-6; http://www.springerlink.com/index/pdf/10.1007/s00228-006-0147-6; https://dx.doi.org/10.1007/s00228-006-0147-6; https://link.springer.com/article/10.1007/s00228-006-0147-6
Springer Science and Business Media LLC
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