Trial reportEuropean journal of clinical pharmacology2011
Effect of the inhibition of CYP3A4 or CYP2D6 on the pharmacokinetics and pharmacodynamics of oxycodone.
Trial report in European journal of clinical pharmacology, 2011. The graph could read no effect estimate from its abstract, so it casts no vote on the map. It is linked to trial NCT04310579 (Clinical Study to Investigate the Effect of the Combination of Psychotropic Drugs and an Opioid on Ventilation), which is not on this map. Cited by 37 papers, 2 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.
Clinical Study to Investigate the Effect of the Combination of Psychotropic Drugs and an Opioid on Ventilation
Who cites it
37 citing papers in PubMed, 2 syntheses or guidelines pooled it, 85 citations in OpenAlex.
- Oxycodone for cancer-related pain.The Cochrane database of systematic reviews · 2022Pooled it
- Oxycodone for cancer-related pain.The Cochrane database of systematic reviews · 2017Pooled it
- Differential effects of calcium channel blockers combined with various opioids on length of stay in hypertensive cardiac surgery patients: analysis of the MIMIC-IV database.BMC cardiovascular disorders · 2026Article
- Oxycodone: A Pain-Relieving Agent With Cardioprotective Properties Against Myocardial Ischemia-Reperfusion Injury.Cardiovascular therapeutics · 2026Review
- Association of initiating CYP2D6-metabolized opioids with risks of adverse outcomes in older adults receiving antidepressants: A retrospective cohort study.PLoS medicine · 2025Article
- Clinically important pharmacokinetic drug-drug interactions with antibacterial agents.Revista espanola de quimioterapia : publicacion oficial de la Sociedad Espanola de Quimioterapia · 2024Review
- Drug-drug interaction perpetrators of oxycodone in patients with cancer: frequency and clinical relevance.European journal of clinical pharmacology · 2024Article
- Hydrocodone, Oxycodone, and Morphine Metabolism and Drug-Drug Interactions.The Journal of pharmacology and experimental therapeutics · 2023Review
- Importance of cytochrome 3A4 and 2D6-mediated drug-drug interactions in oxycodone consumption among older adults hospitalized for hip fracture: a cross-sectional study.Aging clinical and experimental research · 2023Observational
- Article
- Identification of sex-specific genetic associations in response to opioid analgesics in a White, non-Hispanic cohort from Southeast Minnesota.The pharmacogenomics journal · 2022Article
- Risk of Opioid Overdose Associated With Concomitant Use of Oxycodone and Selective Serotonin Reuptake Inhibitors.JAMA network open · 2022Article
- Effects of sedative psychotropic drugs combined with oxycodone on respiratory depression in the rat.Clinical and translational science · 2021Article
- Contribution of CYP2D6 Functional Activity to Oxycodone Efficacy in Pain Management: Genetic Polymorphisms, Phenoconversion, and Tissue-Selective Metabolism.Pharmaceutics · 2021Review
- Population Pharmacokinetics of Oxycodone and Metabolites in Patients with Cancer-Related Pain.Cancers · 2021Article
- Opioids, Polypharmacy, and Drug Interactions: A Technological Paradigm Shift Is Needed to Ameliorate the Ongoing Opioid Epidemic.Pharmacy (Basel, Switzerland) · 2020Article
- Review
- Updated Clinical Pharmacokinetics and Pharmacodynamics of Oxycodone.Clinical pharmacokinetics · 2019Review
- PharmGKB summary: oxycodone pathway, pharmacokinetics.Pharmacogenetics and genomics · 2018Article
- Creatinine-Based Renal Function Estimates and Dosage of Postoperative Pain Management for Elderly Acute Hip Fracture Patients.Pharmaceuticals (Basel, Switzerland) · 2018Article
Corrections and comments
PubMed lists nothing against this paper. Absence here is not a guarantee, only a check that was made.
Authors and funding
6 authors at 1 institution in 1 country.
Funding
No grant is acknowledged in the PubMed record.
Abstract
purposeThe main metabolic pathways of oxycodone, a potent opioid analgetic, are N-demethylation (CYP3A4) to inactive noroxycodone and O-demethylation (CYP2D6) to active oxymorphone. We performed a three-way, placebo-controlled, double-blind cross-over study to assess the pharmacokinetic and pharmacodynamic consequences of drug interactions with oxycodone.
methodsThe 12 participants (CYP2D6 extensive metabolizers) were pre-treated with placebo, ketoconazole or paroxetine before oral oxycodone ingestion (0.2 mg/kg).
resultsPre-treatment with ketoconazole increased the AUC for oxycodone 2- to 3-fold compared with placebo or paroxetine. In combination with placebo, oxycodone induced the expected decrease in pupil diameter. This decrease was accentuated in the presence of ketoconazole, but blunted by paroxetine. In comparison to pre-treatment with placebo, ketoconazole increased nausea, drowsiness, and pruritus associated with oxycodone. In contrast, the effect of pre-treatment with paroxetine on the above-mentioned adverse events was not different from that of placebo. Ketoconazole increased the analgetic effect of oxycodone, whereas paroxetine was not different from placebo.
conclusionsInhibition of CYP3A4 by ketoconazole increases the exposure and some pharmacodynamic effects of oxycodone. Paroxetine pretreatment inhibits CYP2D6 without inducing relevant changes in oxycodone exposure, and partially blunts the pharmacodynamic effects of oxycodone due to intrinsic pharmacological activities. Pharmacodynamic changes associated with CYP3A4 inhibition may be clinically important in patients treated with oxycodone.
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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.