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Updated: Jun 8 2021


  • Competitive vs. noncompetitive antagonist
    • Competitive
      • shifts agonist curve to the right
        • characteristics
          • resembles substrate [S]
          • blocks active site and can be overcome by ↑ [S]
          • ↓ potency, ↑ Km, and Vmax is unchanged
    • Noncompetitive antagonist
      • shifts agonist curve downward
      • characteristics
        • does not resemble [S]
        • does not block active site, therefore no ↑ [S] can overcome effect
        • ↓ efficacy and potency, ↓ Vmax, and Km is unchanged
        • ↑ EC50 of agonist (half maximally effective concentration for producing a given effect)
  • Agonist vs. partial agonist
    • Agonist
      • acts on the receptor and triggers a full response (100% effect)
    • Partial agonist
      • acts on the same receptor as the full agonist
      • ↓ efficacy, independent of dose
      • may be more potent, less potent, or equally potent
        • potency is an independent factor
      • can compete with full agonist to inhibit some of the response of the full agonist
  • Synergism & Potentiation
    • Synergism
      • the combined action of two drugs is greater than the activity of either alone (in total)
        • for example: monobactams and aminoglycosides
    • Potentiation
      • drug A is required for the full effect of drug B to occur, but drug A itself does not have much of an effect (unlike synergism)
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