Regulation of Receptors

Regulation of receptors involves upregulation or downregulation, affecting drug sensitivity and therapeutic response.

Regulation of Receptors

• Cells dynamically regulate receptors in response to various stimuli to maintain homeostasis.

Key mechanisms include:

Receptors can change in number or sensitivity in response to drug exposure:

1. Upregulation

   • Increase in receptor number or sensitivity.
   • Occurs after prolonged use of antagonists or loss of endogenous ligand.
   • Example: Sudden withdrawal of β-blockers → hypersensitive response.

2. Downregulation

   • Decrease in receptor number or sensitivity.
   • Caused by prolonged exposure to agonists.
   • Example: Continuous use of salbutamol (β2 agonist) → tolerance.

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