Adrenergic Antagonists · Pharmacology

What is the physiological significance of 'Intrinsic Sympathomimetic Activity' (ISA) in beta-blockers like Pindolol?

  1. They cause total blockade of the receptor regardless of the ligand concentration present
  2. They only work when the patient is exercising
  3. They irreversibly destroy the beta receptor
  4. They act as partial agonists, causing less resting bradycardia than pure antagonists
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Correct answer: They act as partial agonists, causing less resting bradycardia than pure antagonists

Beta-blockers with ISA slightly stimulate the receptor while simultaneously blocking the binding of more potent endogenous catecholamines. This results in a lower risk of extreme bradycardia at rest compared to drugs like propranolol.

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