Trial reportBritish journal of pharmacology2010
The effects of CYP2D6 and CYP3A activities on the pharmacokinetics of immediate release oxycodone.
Trial report in British journal of pharmacology, 2010. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 64 papers, 3 of them syntheses that pooled it.
What it found
Each row is one number read from the abstract, on the scale the paper reported it, with its interval. Left of the dashed line favours the treatment, right favours the comparator. Under each row is the sentence it came from. New to these charts? A ten-minute tutorial.
The abstract states no effect estimate the extractor could read, or names no intervention and outcome on the map, so this paper lights no cell and moves no belief. It is still indexed, cited and linked below.
The trial behind it
Trials whose registry record cites this paper, or whose number appears in the abstract. A trial that started after this paper was published is citing it as background, not reporting it.
Neither the registry nor the abstract names a trial number. If this is a trial report, that itself is worth knowing.
Who cites it
64 citing papers in PubMed, 3 syntheses or guidelines pooled it, 163 citations in OpenAlex.
- Executive summary of the guideline for prescribing opioid analgesics for chronic non-cancer pain (third edition) by the Japan Society of Pain Clinicians.Journal of anesthesia · 2025Guideline
- Appraisal and development of evidence-based clinical decision support to enable perioperative pharmacogenomic application.The pharmacogenomics journal · 2021Pooled it
- Complex Drug-Drug-Gene-Disease Interactions Involving Cytochromes P450: Systematic Review of Published Case Reports and Clinical Perspectives.Clinical pharmacokinetics · 2018Pooled it
- Pharmacokinetics and Bioequivalence Evaluation of a New Oxycodone Tamper-Resistant Tablet Administered with an Opioid Antagonist in Patients with Chronic Pain.Clinical drug investigation · 2020Trial
- CYP2D6 pharmacogenetic and oxycodone pharmacokinetic association study in pediatric surgical patients.Pharmacogenomics · 2017Trial
- The effect of grape seed extract on the pharmacokinetics of dextromethorphan in healthy volunteers.European journal of clinical pharmacology · 2013Trial
- Influences on the pharmacokinetics of oxycodone: a multicentre cross-sectional study in 439 adult cancer patients.European journal of clinical pharmacology · 2011Trial
- Genetic polymorphisms and drug interactions modulating CYP2D6 and CYP3A activities have a major effect on oxycodone analgesic efficacy and safety.British journal of pharmacology · 2010Trial
- Retrospective Metabolomics Profiling of Clinical Urine Drug Screen Samples Reveals Features Associated with Opiate Exposure.Metabolites · 2026Article
- Opioid Toxicity Following Concomitant Use of Macrolide Antibiotics with Fentanyl, Hydromorphone, or Oxycodone: A Population-Based Study.Clinical pharmacology and therapeutics · 2026Article
- Nicotine use is Associated With Elevated Risk of Opioid use Disorder Following Total/Hemi Hip Arthroplasty Procedures.Nicotine & tobacco research : official journal of the Society for Research on Nicotine and Tobacco · 2026Article
- Oxycodone: A Pain-Relieving Agent With Cardioprotective Properties Against Myocardial Ischemia-Reperfusion Injury.Cardiovascular therapeutics · 2026Review
- Pharmacogenomic-guided opioid prescribing in hospice: reducing toxicity while maximizing symptom relief.Frontiers in medicine · 2026Review
- Synthesis, Experimental and Computational Evaluation of SERAAK1 as a 5-HTMolecules (Basel, Switzerland) · 2025Article
- Influence of aging on opioid dosing for perioperative pain management: a focus on pharmacokinetics.Journal of anesthesia, analgesia and critical care · 2024Review
- Drug-drug interaction perpetrators of oxycodone in patients with cancer: frequency and clinical relevance.European journal of clinical pharmacology · 2024Article
- Effects of pharmacogenetic profiles on pediatric pain relief and adverse events with ibuprofen and oxycodone.Pain reports · 2023Article
- Oxycodone: A Current Perspective on Its Pharmacology, Abuse, and Pharmacotherapeutic Developments.Pharmacological reviews · 2023Review
- Hydrocodone, Oxycodone, and Morphine Metabolism and Drug-Drug Interactions.The Journal of pharmacology and experimental therapeutics · 2023Review
- Oral oxycodone self-administration leads to features of opioid misuse in male and female mice.Addiction biology · 2023Article
4 more citing papers are in PubMed but not listed here.
Corrections and comments
PubMed lists nothing against this paper. Absence here is not a guarantee, only a check that was made.
Authors and funding
10 authors at 4 institutions in 2 countries.
Funding
No grant is acknowledged in the PubMed record.
Abstract
background and purposeThere is high interindividual variability in the activity of drug-metabolizing enzymes catalysing the oxidation of oxycodone [cytochrome P450 (CYP) 2D6 and 3A], due to genetic polymorphisms and/or drug-drug interactions. The effects of CYP2D6 and/or CYP3A activity modulation on the pharmacokinetics of oxycodone remains poorly explored. EXPERIMENTAL APPROACH: A randomized crossover double-blind placebo-controlled study was performed with 10 healthy volunteers genotyped for CYP2D6 [six extensive (EM), two deficient (PM/IM) and two ultrarapid metabolizers (UM)]. The volunteers randomly received on five different occasions: oxycodone 0.2 mg x kg(-1) and placebo; oxycodone and quinidine (CYP2D6 inhibitor); oxycodone and ketoconazole (CYP3A inhibitor); oxycodone and quinidine+ketoconazole; placebo. Blood samples for plasma concentrations of oxycodone and metabolites (oxymorphone, noroxycodone and noroxymorphone) were collected for 24 h after dosing. Phenotyping for CYP2D6 (with dextromethorphan) and CYP3A (with midazolam) were assessed at each session. KEY
resultsCYP2D6 activity was correlated with oxymorphone and noroxymorphone AUCs and C(max) (-0.71 < Spearman correlation coefficient rhos < -0.92). Oxymorphone C(max) was 62% and 75% lower in PM than EM and UM. Noroxymorphone C(max) reduction was even more pronounced (90%). In UM, oxymorphone and noroxymorphone concentrations increased whereas noroxycodone exposure was halved. Blocking CYP2D6 (with quinidine) reduced oxymorphone and noroxymorphone C(max) by 40% and 80%, and increased noroxycodone AUC(infinity) by 70%. Blocking CYP3A4 (with ketoconazole) tripled oxymorphone AUC(infinity) and reduced noroxycodone and noroxymorphone AUCs by 80%. Shunting to CYP2D6 pathway was observed after CYP3A4 inhibition. CONCLUSIONS AND IMPLICATIONS: Drug-drug interactions via CYP2D6 and CYP3A affected oxycodone pharmacokinetics and its magnitude depended on CYP2D6 genotype.
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What OpenQuestion holds
Registered trials
Read under generation 80e0d062 · epoch 390. Bibliography from PubMed, PubMed Central and OpenAlex; grants from NIH RePORTER; trial links from ClinicalTrials.gov; estimates, votes and beliefs from the OpenQuestion graph.