CNS

Opioid Analgesics: Receptor Pharmacology and Clinical Applications


Opioids have rich receptor pharmacology, complex tolerance mechanisms, and high clinical relevance — a reliable exam topic.

Receptor subtypes

  • Mu (μ): analgesia, euphoria, respiratory depression, constipation, miosis
  • Kappa (κ): spinal analgesia, sedation, dysphoria
  • Delta (δ): analgesia, mood modulation

Classification

  • Full agonists: morphine, fentanyl, methadone, tramadol (atypical)
  • Partial agonist: buprenorphine
  • Mixed agonist-antagonist: pentazocine
  • Antagonists: naloxone, naltrexone

Buprenorphine’s high receptor affinity can displace full agonists and precipitate withdrawal — a common vignette.

Tolerance develops to analgesic, euphoric and respiratory effects — but not to constipation and miosis.