| |  Online-Ressource |
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| Verfasst von: | Mikus, Gerd [VerfasserIn]  |
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| | Heinrich, Tilman [VerfasserIn] |
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| | Bödigheimer, Julia [VerfasserIn] |
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| | Röder, Claudia Stephanie [VerfasserIn] |
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| | Matthée, Anne-Kathrin [VerfasserIn] |
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| | Weiß, Johanna [VerfasserIn] |
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| | Burhenne, Jürgen [VerfasserIn] |
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| | Haefeli, Walter E. [VerfasserIn] |
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| Titel: | Semisimultaneous midazolam administration to evaluate the time course of CYP3A activation by a single oral dose of efavirenz |
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| Verf.angabe: | Gerd Mikus, Tilman Heinrich, Julia Bödigheimer, Claudia Röder, Anne-Kathrin Matthee, Johanna Weiss, Jürgen Burhenne, and Walter E. Haefeli |
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| E-Jahr: | 2017 |
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| Jahr: | July 2017 |
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| Umfang: | 7 S. |
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| Fussnoten: | Gesehen am 31.10.2018 |
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| Titel Quelle: | Enthalten in: Journal of clinical pharmacology |
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| Ort Quelle: | Hoboken, NJ : Wiley, 1961 |
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| Jahr Quelle: | 2017 |
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| Band/Heft Quelle: | 57(2017), 7, Seite 899-905 |
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| ISSN Quelle: | 1552-4604 |
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| Abstract: | This study aimed to assess whether a single oral dose of the nonnucleoside reverse transcriptase inhibitor efavirenz can alter CYP3A in vivo. In 12 healthy participants individual CYP3A activity was quantified using a semisimultaneous methodology (midazolam orally and 6 hours later intravenously) both alone and during a period of 22 days after a single oral dose of 400 mg efavirenz. Twelve hours after efavirenz administration, midazolam apparent oral clearance was significantly increased by 70%, and midazolam systemic clearance after intravenous administration was significantly increased by 27%. Similar effects were still present on day 6, after which midazolam clearances slowly returned to baseline on day 22. At least on day 1, the midazolam clearance increase is consistent with the in vitro observed CYP3A activation. The onset of an efavirenz treatment will almost immediately result in enhanced elimination of CYP3A substrates. |
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| DOI: | doi:10.1002/jcph.879 |
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| URL: | Bitte beachten Sie: Dies ist ein Bibliographieeintrag. Ein Volltextzugriff für Mitglieder der Universität besteht hier nur, falls für die entsprechende Zeitschrift/den entsprechenden Sammelband ein Abonnement besteht oder es sich um einen OpenAccess-Titel handelt.
Volltext ; Verlag: http://dx.doi.org/10.1002/jcph.879 |
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| | Volltext: https://accp1.onlinelibrary.wiley.com/doi/abs/10.1002/jcph.879 |
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| | DOI: https://doi.org/10.1002/jcph.879 |
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| Datenträger: | Online-Ressource |
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| Sprache: | eng |
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| Sach-SW: | CYP3A |
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| | efavirenz |
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| | enzyme activation |
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| | midazolam |
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| K10plus-PPN: | 1582451400 |
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| Verknüpfungen: | → Zeitschrift |
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Semisimultaneous midazolam administration to evaluate the time course of CYP3A activation by a single oral dose of efavirenz / Mikus, Gerd [VerfasserIn]; July 2017 (Online-Ressource)
