opiate receptor pharmacology l.
Download
Skip this Video
Loading SlideShow in 5 Seconds..
Opiate Receptor Pharmacology PowerPoint Presentation
Download Presentation
Opiate Receptor Pharmacology

Loading in 2 Seconds...

play fullscreen
1 / 9

Opiate Receptor Pharmacology - PowerPoint PPT Presentation


  • 503 Views
  • Uploaded on

Opiate Receptor Pharmacology. Donald R. Wesson, MD. Opiate Receptors and effect of Agonist. Schematic of Mu Opiate Receptor. Source: Goodman and Gillman 9 th ed, p. 526. Agonist Partial Agonist Antagonists. Morphine-like effect (e.g., heroin, weak binding except for Fentanyl)

loader
I am the owner, or an agent authorized to act on behalf of the owner, of the copyrighted work described.
capcha
Download Presentation

Opiate Receptor Pharmacology


An Image/Link below is provided (as is) to download presentation

Download Policy: Content on the Website is provided to you AS IS for your information and personal use and may not be sold / licensed / shared on other websites without getting consent from its author.While downloading, if for some reason you are not able to download a presentation, the publisher may have deleted the file from their server.


- - - - - - - - - - - - - - - - - - - - - - - - - - E N D - - - - - - - - - - - - - - - - - - - - - - - - - -
    Presentation Transcript
    1. Opiate Receptor Pharmacology Donald R. Wesson, MD

    2. Opiate Receptors and effect of Agonist

    3. Schematic of Mu Opiate Receptor Source: Goodman and Gillman 9th ed, p. 526

    4. Agonist Partial Agonist Antagonists Morphine-like effect (e.g., heroin, weak binding except for Fentanyl) Weak morphine-like effects with strong receptor affinity (e.g., buprenorphine) No effect in absence of an opiate or opiate dependence (e.g., naltrexone) Receptor Binding at Mu receptor

    5. Heroin, morphine, methadone Buprenorphine Naltrexone Nalmefene Agonists Partial Agonist Antagonist Effect of Common Opiates at Mu Receptor

    6. Buprenorphine Pharmacology • Partial agonist at mu receptor • High affinity for mu receptor • Can displace full opiate agonist such as heroin or methadone • Displacement of heroin or methadone by buprenorphine can produce opiate withdrawal symptoms

    7. Buprenorphine Pharmacology • Antagonist at kappa receptor • Poor bio-availability taken orally (extensive first pass metabolism) • Much more bio-available from sublingual mucosa (Peak 2-3 hours following sublingual dose)