ReviewCurrent topics in medicinal chemistry2011
Opioid analgesics and P-glycoprotein efflux transporters: a potential systems-level contribution to analgesic tolerance.
Review in Current topics in medicinal chemistry, 2011. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 39 papers.
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
39 citing papers in PubMed, 102 citations in OpenAlex.
- Interactions between long-acting antiretrovirals and opioids: a call for clinical awareness.Clinical microbiology reviews · 2026Review
- Case Report: Adverse reaction to butorphanol in a Collie homozygous for theFrontiers in veterinary science · 2025Article
- Reversing Morphine Induced Tolerance: Insights Into Cetirizine and Green Tea Extract Efficacy.Current therapeutic research, clinical and experimental · 2025Article
- Changes in Expression and Function of Placental and Intestinal P-gp and BCRP Transporters during Pregnancy.International journal of molecular sciences · 2023Review
- Assessment of Drug-Drug Interaction Risk Between Intravenous Fentanyl and the Glecaprevir/Pibrentasvir Combination Regimen in Hepatitis C Patients Using Physiologically Based Pharmacokinetic Modeling and Simulations.Infectious diseases and therapy · 2023Article
- CYP2D in the brain impacts oral hydrocodone analgesia in vivo.Neuropharmacology · 2022Article
- The Impact of P-Glycoprotein on Opioid Analgesics: What's the Real Meaning in Pain Management and Palliative Care?International journal of molecular sciences · 2022Review
- ATP-binding cassette (ABC) drug transporters in the developing blood-brain barrier: role in fetal brain protection.Cellular and molecular life sciences : CMLS · 2022Review
- P-glycoprotein: new insights into structure, physiological function, regulation and alterations in disease.Heliyon · 2022Review
- Morphine Accumulates in the Retina Following Chronic Systemic Administration.Pharmaceuticals (Basel, Switzerland) · 2022Article
- Pharmacogenomics biomarkers for personalized methadone maintenance treatment: The mechanism and its potential use.Bosnian journal of basic medical sciences · 2021Review
- Tolerance to Opioid-Induced Respiratory Depression in Chronic High-Dose Opioid Users: A Model-Based Comparison With Opioid-Naïve Individuals.Clinical pharmacology and therapeutics · 2021Article
- Case Study 7: Transporters Case Studies-In Vitro Solutions for Translatable Outcomes.Methods in molecular biology (Clifton, N.J.) · 2021Article
- Opioid-Mediated HIV-1 Immunopathogenesis.Journal of neuroimmune pharmacology : the official journal of the Society on NeuroImmune Pharmacology · 2020Review
- Opioid Use Disorders in People Living with HIV/AIDS: A Review of Implications for Patient Outcomes, Drug Interactions, and Neurocognitive Disorders.Pharmacy (Basel, Switzerland) · 2020Article
- Personalized pediatric anesthesia and pain management: problem-based review.Pharmacogenomics · 2020Review
- Peripheral Opioid Receptor Antagonists for Opioid-Induced Constipation: A Primer on Pharmacokinetic Variabilities with a Focus on Drug Interactions.Journal of pain research · 2020Review
- Potential Pharmacokinetic Drug-Drug Interactions between Cannabinoids and Drugs Used for Chronic Pain.BioMed research international · 2020Review
- Computational framework for predictive PBPK-PD-Tox simulations of opioids and antidotes.Journal of pharmacokinetics and pharmacodynamics · 2019Article
- Review
Corrections and comments
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Authors and funding
2 authors at 2 institutions in 1 country.
Funding
Abstract
Chronic clinical pain remains poorly treated. Despite attempts to develop novel analgesic agents, opioids remain the standard analgesics of choice in the clinical management of chronic and severe pain. However, mu opioid analgesics have undesired side effects including, but not limited to, respiratory depression, physical dependence and tolerance. A growing body of evidence suggests that P-glycoprotein (P-gp), an efflux transporter, may contribute a systems-level approach to the development of opioid tolerance. Herein, we describe current in vitro and in vivo methodology available to analyze interactions between opioids and P-gp and critically analyze P-gp data associated with six commonly used mu opioids to include morphine, methadone, loperamide, meperidine, oxycodone, and fentanyl. Recent studies focused on the development of opioids lacking P-gp substrate activity are explored, concentrating on structure-activity relationships to develop an optimal opioid analgesic lacking this systems-level contribution to tolerance development. Continued work in this area will potentially allow for delineation of the mechanism responsible for opioid-related P-gp up-regulation and provide further support for evidence based medicine supporting clinical opioid rotation.
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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.