Gazzaz, Malaz, Kinzig, Martina, Schaeffeler, Elke, Juebner, Martin, Hsin, Chih-hsuan, Li, Xia, Taubert, Max ORCID: 0000-0001-8925-7782, Trueck, Christina, Iltgen-Breburda, Juliane, Kraus, Daria, Queckenberg, Christian, Stoffel, Marc, Schwab, Matthias, Soergel, Fritz and Fuhr, Uwe (2018). Drinking Ethanol Has Few Acute Effects on CYP2C9, CYP2C19, NAT2, and P-Glycoprotein Activities but Somewhat Inhibits CYP1A2, CYP2D6, and Intestinal CYP3A: So What? Clin. Pharmacol. Ther., 104 (6). S. 1249 - 1260. HOBOKEN: WILEY. ISSN 1532-6535

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Abstract

We quantified the effect of acute ethanol exposure (initial blood concentrations 0.7 g/L) on major drug metabolizing enzymes and p-glycoprotein. Sixteen healthy Caucasians participated in a randomized crossover study with repeated administration of either vodka or water. Enzyme/transporter activity was assessed by a cocktail of probe substrates, including caffeine (CYP1A2/NAT2), tolbutamide (CYP2C9), omeprazole (CYP2C19), dextromethorphan (CYP2D6), midazolam (CYP3A), and digoxin (P-glycoprotein). The ratio of AUC(0-t) of dextromethorphan for ethanol/water coadministration was 1.95 (90% confidence interval (CI) 1.48-2.58). The effect was strongest in individuals with a CYP2D6 genotype predicting high activity (n = 7, ratio 2.66, 90% CI 1.65-4.27). Ethanol increased caffeine AUC(0-t) 1.38-fold (90% CI 1.25-1.52) and reduced intestinal midazolam extraction 0.77-fold (90% CI 0.69-0.86). The other probe drugs were not affected by ethanol. The results suggest that acute ethanol intake typically has no clinically important effect on the enzymes/transporters tested.

Item Type: Journal Article
Creators:
CreatorsEmailORCIDORCID Put Code
Gazzaz, MalazUNSPECIFIEDUNSPECIFIEDUNSPECIFIED
Kinzig, MartinaUNSPECIFIEDUNSPECIFIEDUNSPECIFIED
Schaeffeler, ElkeUNSPECIFIEDUNSPECIFIEDUNSPECIFIED
Juebner, MartinUNSPECIFIEDUNSPECIFIEDUNSPECIFIED
Hsin, Chih-hsuanUNSPECIFIEDUNSPECIFIEDUNSPECIFIED
Li, XiaUNSPECIFIEDUNSPECIFIEDUNSPECIFIED
Taubert, MaxUNSPECIFIEDorcid.org/0000-0001-8925-7782UNSPECIFIED
Trueck, ChristinaUNSPECIFIEDUNSPECIFIEDUNSPECIFIED
Iltgen-Breburda, JulianeUNSPECIFIEDUNSPECIFIEDUNSPECIFIED
Kraus, DariaUNSPECIFIEDUNSPECIFIEDUNSPECIFIED
Queckenberg, ChristianUNSPECIFIEDUNSPECIFIEDUNSPECIFIED
Stoffel, MarcUNSPECIFIEDUNSPECIFIEDUNSPECIFIED
Schwab, MatthiasUNSPECIFIEDUNSPECIFIEDUNSPECIFIED
Soergel, FritzUNSPECIFIEDUNSPECIFIEDUNSPECIFIED
Fuhr, UweUNSPECIFIEDUNSPECIFIEDUNSPECIFIED
URN: urn:nbn:de:hbz:38-164786
DOI: 10.1002/cpt.1083
Journal or Publication Title: Clin. Pharmacol. Ther.
Volume: 104
Number: 6
Page Range: S. 1249 - 1260
Date: 2018
Publisher: WILEY
Place of Publication: HOBOKEN
ISSN: 1532-6535
Language: English
Faculty: Unspecified
Divisions: Unspecified
Subjects: no entry
Uncontrolled Keywords:
KeywordsLanguage
HUMAN CYTOCHROME-P450 ISOFORMS; DRUG-DRUG INTERACTIONS; IN-VITRO; COCKTAIL INTERACTION; HEALTHY-VOLUNTEERS; ORGANIC-SOLVENTS; PHARMACOKINETICS; ALCOHOL; DEXTROMETHORPHAN; DIGOXINMultiple languages
Pharmacology & PharmacyMultiple languages
Refereed: Yes
URI: http://kups.ub.uni-koeln.de/id/eprint/16478

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