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Beta blockers

Last updated: August 7, 2021

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Beta blockers are a group of drugs that inhibit the sympathetic activation of β-adrenergic receptors. Cardioselective blockers (e.g., atenolol, bisoprolol) primarily block β1 receptors in the heart, causing decreased heart rate, cardiac contractility, cardiac workload, and AVN conduction. Nonselective beta blockers (e.g., pindolol, propranolol) inhibit all β receptors and may cause bronchoconstriction, peripheral vasoconstriction, and metabolic imbalances (e.g., hypoglycemia and hyperglycemia, hypertriglyceridemia) in addition to cardiac effects. Cardioselective beta blockers have a lower side-effect profile and are preferred in the management of coronary heart disease, compensated heart failure, acute coronary syndrome, and certain types of arrhythmias. Propranolol, a nonselective beta blocker, is the first-line drug in the management of essential tremor, portal hypertension, migraine prophylaxis, and thyroid storm. Beta blockers are contraindicated in patients with symptomatic bradycardia, AV block, decompensated heart failure, and asthma. Initiation and cessation of beta-blocker therapy should always be gradual to avoid side effects or symptoms of withdrawal (e.g., rebound tachycardia, hypertension, acute cardiac death).

Characteristics of beta blockers
Type Agents Effects Side effects Indications
Cardioselective beta blockers (β1 selective) With intrinsic sympathomimetic activity (ISA)
  • Acebutolol
  • Celiprolol
Without ISA
  • Atenolol [4]
  • Metoprolol
  • Esmolol
  • Bisoprolol
  • Betaxolol
  • Bevantolol
  • Nebivolol
Nonselective beta blockers1, β2, and β3 receptors) With ISA
  • Pindolol
  • Penbutolol
  • Oxprenolol
  • Block β1, β2, and β3 receptors
  • Sotalol also blocks cardiac potassium channels (antiarrhythmic effect).
Without ISA
  • Propranolol
  • Nadolol
  • Sotalol
  • Timolol
  • Tertalol
With additional α-blocking action
  • Labetalol
  • Bucindolol
  • Carvedilol [5]

With the exception of nebivolol, all cardioselective beta blockers begin with the letters A to M (B1 = first half of the alphabet). Except for beta blockers with alpha-blocking action, all noncardioselective beta blockers begin with the letters N to Z (B2 = second half of the alphabet).

References[6][7][8][9][10]

Beta blockers competitively bind to and block β-adrenergic receptors, thereby inhibiting sympathetic (adrenergic and/or noradrenergic) stimulation of β receptors. See “The sympathetic vs. parasympathetic nervous system” for details regarding the effects of β-adrenergic stimulation.

Effects of β-adrenergic blockade

Overview of β-adrenergic blockade [3]
Types of β receptors Main site of action Effects of β-adrenergic blockade
β1
  • Anti-ischemic effect: β1 blockade → heart rate and ↓ cardiac contractility ↓ blood pressure (BP) and ↓ oxygen consumption by the heart anti-ischemic effect
  • Antiarrhythmic effect: β1 blockade → AVN conduction, AVN refractory time, and heart rate anti-arrhythmic effect
  • Anti-remodeling effect
β2
  • ↓ Glucose uptake (insulin sensitivity)
β3

Beta blockers competitively inhibit adrenergic substances (e.g., adrenaline, noradrenaline) at β receptors.
A rule to remember the main effector organs for β receptors: There is 1 heart (β1 blockers act on the heart) and 2 lungs (β2 blockers affect bronchial smooth muscles).

Intrinsic sympathomimetic activity (ISA) [6][8]

Pharmacokinetics of beta blockers
Lipophilic agents Hydrophilic agents Mixed
Properties
  • Undergo hepatic clearance
  • Penetrate the blood-brain-barrier → central/neurological adverse effects (esp. nightmares and insomnia)
  • Long-acting: most require a single dose per day
Agents

References:[3]

Overview

Beta blockers adverse effects
Type of beta blockers Organ system Effects

Nonselective beta blockers and cardioselective beta blockers

(β1-receptor and β2-receptor blockade)

Cardiac

CNS [17][18]

Cutaneous

Nonselective beta blockers

(β2-receptor blockade)

Pulmonary
Peripheral vasculature
Metabolic

Beta blockers should be introduced gradually with slow increases in dosage and slowly tapered off when no longer needed.

A number of beta blockers (e.g., metoprolol, carvedilol) are metabolized by CYP2D6. Genetic polymorphisms of CYP2D6 (e.g., ultra-rapid metabolization, poor metabolization) can influence adverse effects and tolerated doses. [24]

Beta-blocker overdose

Beta-blocker withdrawal

Caused by the sudden termination of beta blockers

We list the most important adverse effects. The selection is not exhaustive.

Cardiovascular indications

Specific indications for propranolol

Miscellaneous

Contraindications to beta blockers
Absolute contraindications Relative contraindications

We list the most important contraindications. The selection is not exhaustive.

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