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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)

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opiate receptor pharmacology

Opiate Receptor Pharmacology

Donald R. Wesson, MD

schematic of mu opiate receptor
Schematic of Mu Opiate Receptor

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

receptor binding at mu receptor
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
Heroin, morphine, methadone

Buprenorphine

Naltrexone

Nalmefene

Agonists

Partial Agonist

Antagonist

Effect of Common Opiates at Mu Receptor
buprenorphine pharmacology
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
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)
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