ReviewCurrent neuropharmacology2017
Opioids and the Blood-Brain Barrier: A Dynamic Interaction with Consequences on Drug Disposition in Brain.
Review in Current neuropharmacology, 2017. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 53 papers, 1 of them a synthesis 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
53 citing papers in PubMed, 1 synthesis or guideline pooled it, 111 citations in OpenAlex.
- Pooled it
- Brixadi for Stimulant Use Disorder: Evolving Pharmacologic Considerations and Clinical Implications.Advances in therapy · 2026Review
- Modeling insights into potential mechanisms of opioid-induced respiratory depression within medullary and pontine networks.Journal of neurophysiology · 2026Article
- Article
- Methadone and morphine have equivalent analgesic but not reward potency in female mice.Addiction neuroscience · 2025Article
- Comparative analysis of the uptake of the HFluids and barriers of the CNS · 2025Article
- The Rise of Fentanyl: Molecular Aspects and Forensic Investigations.International journal of molecular sciences · 2025Review
- Do P-glycoprotein-mediated drug-drug interactions at the blood-brain barrier impact morphine brain distribution?Journal of pharmacokinetics and pharmacodynamics · 2025Article
- Fentanyl dosage for preterm infants suggested by a pharmacokinetic, -dynamic, and -genetic model.Pediatric research · 2025Article
- Active CNS delivery of oxycodone in healthy and endotoxemic pigs.Fluids and barriers of the CNS · 2024Article
- Cocaine regulates antiretroviral therapy CNS access through pregnane-x receptor-mediated drug transporter and metabolizing enzyme modulation at the blood brain barrier.Fluids and barriers of the CNS · 2024Article
- Xixin Decoction's novel mechanism for alleviating Alzheimer's disease cognitive dysfunction by modulating amyloid-β transport across the blood-brain barrier to reduce neuroinflammation.Frontiers in pharmacology · 2024Article
- Tramadol induces apoptosis, inflammation, and oxidative stress in rat choroid plexus.Metabolic brain disease · 2023Article
- Glymphatic-System Function Is Associated with Addiction and Relapse in Heroin Dependents Undergoing Methadone Maintenance Treatment.Brain sciences · 2023Article
- ABCB1 and ABCG2 Regulation at the Blood-Brain Barrier: Potential New Targets to Improve Brain Drug Delivery.Pharmacological reviews · 2023Review
- Personalized Medicine in Cancer Pain Management.Journal of personalized medicine · 2023Review
- The Pharmacokinetics of Subcutaneous Methylnaltrexone Bromide in Rhesus Macaques (Journal of the American Association for Laboratory Animal Science : JAALAS · 2023Article
- Effect of common OPRM1, COMT, SLC6A4, ABCB1, and CYP2B6 polymorphisms on perioperative analgesic and propofol demands on patients subjected to thyroidectomy surgery.Pharmacological reports : PR · 2023Article
- Drug Permeability: From the Blood-Brain Barrier to the Peripheral Nerve Barriers.Advanced therapeutics · 2023Article
- Oxycodone, an opioid like the others?Frontiers in psychiatry · 2023Review
Corrections and comments
PubMed lists nothing against this paper. Absence here is not a guarantee, only a check that was made.
Authors and funding
4 authors at 2 institutions in 2 countries.
Funding
No grant is acknowledged in the PubMed record.
Abstract
backgroundOpioids are widely used in pain management, acting via opioid receptors and/or Toll-like receptors (TLR) present at the central nervous system (CNS). At the blood-brain barrier (BBB), several influx and efflux transporters, such as the ATP-binding cassette (ABC) P-glycoprotein (P-gp, ABCB1), Breast Cancer Resistance Protein (BCRP, ABCG2) and multidrug resistance-associated proteins (MRP, ABCC) transporters, and solute carrier transporters (SLC), are responsible for the transport of xenobiotics from the brain into the bloodstream or vice versa.
objectiveABC transporters export several clinically employed opioids, altering their neuropharmacokinetics and CNS effects. In this review, we explore the interactions between opioids and ABC transporters, and decipher the molecular mechanisms by which opioids can modify their expression at the BBB.
resultsP-gp is largely implicated in the brain-to-blood efflux of opioids, namely morphine and oxycodone. Long-term exposure to morphine and oxycodone has proven to up-regulate the expression of ABC transporters, such as P-gp, BCRP and MRPs, at the BBB, which may lead to increased tolerance to the antinociceptive effects of such drugs. Recent studies uncover two mechanisms by which morphine may up-regulate P-gp and BCRP at the BBB: 1) via a glutamate, NMDA-receptor and COX-2 signaling cascade, and 2) via TLR4 activation, subsequent development of neuroinflammation, and activation of NF-kB, presumably via glial cells.
conclusionThe BBB-opioid interaction can culminate in bilateral consequences, since ABC transporters condition the brain disposition of opioids, while opioids also affect the expression of ABC transporters at the BBB, which may result in increased CNS drug pharmacoresistance.
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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.