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Opiate Receptor Pharmacology

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

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  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)

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