Effect of the inhibition of CYP3A4 or CYP2D6 on the pharmacokinetics and pharmacodynamics of oxycodone

O Kummer, F Hammann, C Moser, O Schaller… - European journal of …, 2011 - Springer
Purpose The main metabolic pathways of oxycodone, a potent opioid analgetic, are N-
demethylation (CYP3A4) to inactive noroxycodone and O-demethylation (CYP2D6) to active …

Effect of inhibition of cytochrome P450 enzymes 2D6 and 3A4 on the pharmacokinetics of intravenous oxycodone: a randomized, three-phase, crossover, placebo …

J Grönlund, TI Saari, NM Hagelberg… - Clinical drug …, 2011 - Springer
Abstract Background and Objective Oxycodone is a μ-opioid receptor agonist that is mainly
metabolized by hepatic cytochrome P450 (CYP) enzymes. Because CYP enzymes can be …

Exposure to oral oxycodone is increased by concomitant inhibition of CYP2D6 and 3A4 pathways, but not by inhibition of CYP2D6 alone

J Grönlund, TI Saari, NM Hagelberg… - British journal of …, 2010 - Wiley Online Library
WHAT IS ALREADY KNOWN ABOUT THIS SUBJECT• Oxycodone is an opioid analgesic
that is metabolized mainly in the liver by cytochrome P450 (CYP) 2D6 and 3A4 enzymes.• …

Effects of blocking CYP2D6 on the pharmacokinetics and pharmacodynamics of oxycodone

T Heiskanen, KT Olkkola, E Kalso - Clinical Pharmacology & …, 1998 - Wiley Online Library
Background Oxycodone is metabolized in the liver by means of O‐demethylation to form
oxymorphone in a reaction catalyzed by the enzyme cytochrome P450 2D6 (CYP2D6). This …

Pharmacokinetics and pharmacodynamics of oral oxycodone in healthy human subjects: role of circulating active metabolites

B Lalovic, E Kharasch, C Hoffer, L Risler… - Clinical …, 2006 - Wiley Online Library
Background In vitro experiments suggest that circulating metabolites of oxycodone are
opioid receptor agonists. Clinical and animal studies to date have failed to demonstrate a …

Effects of itraconazole on the pharmacokinetics and pharmacodynamics of intravenously and orally administered oxycodone

TI Saari, J Grönlund, NM Hagelberg… - European journal of …, 2010 - Springer
Background The aim of this study was to investigate the effects of the cytochrome P450 3A4
(CYP34A) inhibitor itraconazole on the pharmacokinetics and pharmacodynamics of orally …

The effects of CYP2D6 and CYP3A activities on the pharmacokinetics of immediate release oxycodone

CF Samer, Y Daali, M Wagner… - British journal of …, 2010 - Wiley Online Library
Background and purpose: There is high interindividual variability in the activity of drug‐
metabolizing enzymes catalysing the oxidation of oxycodone [cytochrome P450 (CYP) 2D6 …

Contribution of oxycodone and its metabolites to the overall analgesic effect after oxycodone administration

R Klimas, D Witticke, S El Fallah… - Expert opinion on drug …, 2013 - Taylor & Francis
Objective: Oxycodone (OC) is an opioid which exerts its analgesic effect through µ-receptors
in the brain. It is metabolized through CYP450 enzymes and some of the metabolites show …

Cytochrome P450-mediated changes in oxycodone pharmacokinetics/pharmacodynamics and their clinical implications

KC Söderberg Löfdal, ML Andersson, LL Gustafsson - Drugs, 2013 - Springer
In recent years the use of the opioid oxycodone has increased markedly and replacing
morphine as the first-line choice of opioid in several countries. There are formulations for …

[HTML][HTML] Updated clinical pharmacokinetics and pharmacodynamics of oxycodone

M Kinnunen, P Piirainen, H Kokki, P Lammi… - Clinical …, 2019 - Springer
Global oxycodone consumption has increased sharply during the last two decades, and, in
2008, oxycodone consumption surpassed that of morphine. As oxycodone was synthesized …