Pharmacology
β-blockers — selectivity, ISA, ABCs of side effects
Pharmacology

β-blockers — selectivity, ISA, ABCs of side effects

Cardioselective vs non-selective, with the indications and contraindications that matter.

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◆Classes

  • •β1-selective (cardioselective): metoprolol, atenolol, bisoprolol, esmolol, nebivolol — preferred in COPD, DM, PAD
  • •Non-selective (β1+β2): propranolol, nadolol, timolol — useful in migraine, essential tremor, performance anxiety
  • •Mixed α+β: labetalol, carvedilol — labetalol for hypertensive emergency (incl pregnancy), carvedilol for HFrEF
  • •ISA (intrinsic sympathomimetic activity): pindolol, acebutolol — less bradycardia; avoid post-MI

◆Major indications

  • •HFrEF: carvedilol, metoprolol succinate (NOT tartrate), bisoprolol → mortality benefit
  • •Post-MI: any β-blocker × at least 1 yr
  • •Rate control AFib: metoprolol or atenolol
  • •Migraine prophylaxis: propranolol, metoprolol
  • •Essential tremor: propranolol
  • •Performance anxiety: propranolol PRN (short-acting)
  • •Hyperthyroidism (until antithyroid takes effect): propranolol
  • •Variceal bleeding prophylaxis (cirrhosis): nadolol, propranolol
  • •Pheochromocytoma: AFTER α-blockade (phenoxybenzamine) — never first

◆Side effects (ABCDE)

  • •Asthma / bronchospasm (especially non-selective)
  • •Bradycardia, heart block
  • •Claudication / cold extremities (worsen PAD)
  • •Depression, fatigue, sexual dysfunction
  • •Erectile dysfunction; masks hypoglycemia symptoms (sweating preserved; tachycardia masked) in diabetics

◆Contraindications / caveats

  • •Asthma: avoid non-selective; cardioselective at low dose OK in COPD
  • •Decompensated HF: hold; restart slowly when euvolemic
  • •2nd/3rd degree AV block (without pacer)
  • •Cocaine intoxication: unopposed α → AVOID β-blockers; use benzos, phentolamine if HTN crisis
  • •Pheochromocytoma: phenoxybenzamine first, then β-blocker

◆Overdose

  • •Bradycardia + hypotension; hypoglycemia, seizures
  • •Treatment: IV fluids, atropine, glucagon (drug of choice), high-dose insulin / euglycemia, calcium, lipid emulsion in severe
  • •Pacing if refractory bradycardia

High-yield pearls

  • ◆HFrEF: only carvedilol, metoprolol SUCCINATE, and bisoprolol have mortality benefit
  • ◆Cocaine chest pain: NO β-blocker (use benzos + nitrate); 'unopposed α' risk historically taught — modern evidence less clear, board answer = avoid
  • ◆Pheochromocytoma needs α-blockade FIRST (phenoxybenzamine), then β to prevent hypertensive crisis
  • ◆Glucagon is the antidote for β-blocker AND calcium-channel blocker overdose (via cAMP)
Quick check

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