Pharmaceutical Chemistry Medicinal Chemistry of Drug Classes

Analgesics: Opioid and Non-Opioid

Topic overview

Start with the big picture

Opioid analgesics are organized by core scaffolds, including phenanthrene or morphinan, 4-anilidopiperidine, and diphenylpropylamine structures. The lesson preview highlights features linked to μ-receptor activity, such as the C3 phenolic group and nitrogen substitution, and considers how chemical modifications and metabolism affect activity. Non-opioid analgesics include NSAIDs, acetaminophen, and centrally acting agents. Within NSAIDs, the source outlines the acidic and hydrophobic features associated with COX inhibition and distinguishes arylpropionates, arylacetic acids, coxibs, and salicylates by their structural characteristics. Together, these comparisons connect medicinal-chemistry concepts to the different ways analgesic classes interact with their targets.

Learning objectives

What you'll learn

  • Identify the major opioid scaffold families and representative examples.
  • Describe structural features associated with μ-opioid receptor agonism.
  • Explain how opioid substitutions and metabolism can influence activity.
  • Distinguish NSAID subclasses by their characteristic structural features.
  • Summarize the chemical rationale for COX-2 selectivity in coxibs.
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