en
Scientific article
Open access
English

Geneva Cocktail for Cytochrome P450 and P-glycoprotein Activity Assessment Using Dried Blood Spots

Published inClinical pharmacology and therapeutics, vol. 96, no. 3, p. 349-359
Publication date2014
Abstract

The suitability of the capillary dried blood spot (DBS) sampling method was assessed for simultaneous phenotyping of cytochrome P450 (CYP) enzymes and P-glycoprotein (P-gp) using a cocktail approach. Ten volunteers received an oral cocktail capsule containing low doses of the probes bupropion (CYP2B6), flurbiprofen (CYP2C9), omeprazole (CYP2C19), dextromethorphan (CYP2D6), midazolam (CYP3A), and fexofenadine (P-gp) with coffee/Coke (CYP1A2) on four occasions. They received the cocktail alone (session 1), and with the CYP inhibitors fluvoxamine and voriconazole (session 2) and quinidine (session 3). In session 4, subjects received the cocktail after a 7-day pretreatment with the inducer rifampicin. The concentrations of probes/metabolites were determined in DBS and plasma using a single liquid chromatography-tandem mass spectrometry method. The pharmacokinetic profiles of the drugs were comparable in DBS and plasma. Important modulation of CYP and P-gp activities was observed in the presence of inhibitors and the inducer. Minimally invasive one- and three-point (at 2, 3, and 6 h) DBS-sampling methods were found to reliably reflect CYP and P-gp activities at each session.Clinical Pharmacology & Therapeutics (2014); advance online publication 7 May 2014. doi:10.1038/clpt.2014.83.

Citation (ISO format)
BOSILKOVSKA WEISSKOPF, Marija et al. Geneva Cocktail for Cytochrome P450 and P-glycoprotein Activity Assessment Using Dried Blood Spots. In: Clinical pharmacology and therapeutics, 2014, vol. 96, n° 3, p. 349–359. doi: 10.1038/clpt.2014.83
Main files (1)
Article (Published version)
accessLevelPublic
Identifiers
ISSN of the journal0009-9236
778views
306downloads

Technical informations

Creation05/19/2014 4:25:00 PM
First validation05/19/2014 4:25:00 PM
Update time03/14/2023 9:15:16 PM
Status update03/14/2023 9:15:16 PM
Last indexation01/16/2024 10:42:54 AM
All rights reserved by Archive ouverte UNIGE and the University of GenevaunigeBlack