Opiate receptor pharmacology
Download
1 / 9

Opiate Receptor Pharmacology - PowerPoint PPT Presentation


  • 478 Views
  • Updated 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

PowerPoint Slideshow about 'Opiate Receptor Pharmacology' - KeelyKia


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
Opiate receptor pharmacology l.jpg

Opiate Receptor Pharmacology

Donald R. Wesson, MD



Schematic of mu opiate receptor l.jpg
Schematic of Mu Opiate Receptor

Source: Goodman and Gillman 9th ed, p. 526


Receptor binding at mu receptor l.jpg

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


Effect of common opiates at mu receptor l.jpg

Heroin, morphine, methadone

Buprenorphine

Naltrexone

Nalmefene

Agonists

Partial Agonist

Antagonist

Effect of Common Opiates at Mu Receptor


Buprenorphine pharmacology l.jpg
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


Buprenorphine pharmacology8 l.jpg
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)


ad