Pharmacology · Autonomic Nervous System (Cholinergic, Anticholinergic, Sympathomimetics, Sympatholytics)

A 65-year-old with heart failure on carvedilol develops worsening bronchospasm. Switching to metoprolol succinate reduces bronchospasm. The property of metoprolol that accounts for this differential effect is:

  • A Intrinsic sympathomimetic activity at beta-2 receptors
  • B Additional alpha-1 blockade that bronchodilates via vascular unloading
  • C Selective blockade of cardiac beta-1 receptors with relative sparing of beta-2 receptors
  • D Membrane-stabilizing activity that prevents reflex bronchospasm
Correct answer: C. Selective blockade of cardiac beta-1 receptors with relative sparing of beta-2 receptors

Explanation

Metoprolol is a cardioselective (beta-1 selective) blocker with approximately 75-fold greater affinity for beta-1 than beta-2 receptors. Carvedilol is a non-selective beta blocker (plus alpha-1 blockade) with equal beta-1 and beta-2 blockade, precipitating bronchoconstriction via beta-2 receptor antagonism in airways. Cardioselectivity is relative and dose-dependent but clinically meaningful at standard therapeutic doses.

Reference: KD Tripathi, Essentials of Medical Pharmacology, 8th ed.

High-yield for: NEET PGINI-CETNExTFMGEUSMLEPLABMRCP

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