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Adrenergic beta-2 Receptor Agonists

AMD:CLASS:00995 · English

Adrenergic beta-2 Receptor Agonists

Overview

Overview
Beta-2 receptor agonists relax airway smooth muscle and are central bronchodilators for asthma and COPD. They differ mainly by onset and duration rather than by an absolute difference in receptor selectivity.
Source [1]

Classification

Key statement
Classification
Short-acting agents include salbutamol and terbutaline. Long-acting agents include formoterol and salmeterol, while ultra-long-acting agents used mainly in COPD include indacaterol, olodaterol and vilanterol.
Source [1]

Mechanism of action

Mechanism of action
Beta-2 receptors couple to Gs and increase cyclic AMP, promoting smooth-muscle relaxation. In skeletal muscle and liver, beta-2 stimulation contributes to tremor, glycogenolysis, insulin release and intracellular potassium shift.
Source [1]

Important members

Important members
Salbutamol, terbutaline, formoterol, salmeterol, indacaterol, olodaterol and vilanterol are important examples. Ritodrine is an older uterine relaxant with limited use.
Source [1]

Clinical uses

Clinical uses
Short-acting inhaled beta-2 agonists provide rapid relief of bronchospasm. Long-acting agents are maintenance bronchodilators; in asthma they are used within an inhaled-corticosteroid-containing strategy, while COPD regimens follow symptom and exacerbation assessment.
Source [1]

Adverse effects

Adverse effects
Tremor, palpitations, tachycardia, nervousness, headache, hyperglycaemia and hypokalaemia may occur. Excessive use can cause arrhythmia and lactic acidosis and may signal poorly controlled airway disease.
Source [1]

Contraindications and precautions

Contraindications and precautions
Use cautiously in significant tachyarrhythmia, unstable cardiovascular disease, hyperthyroidism and hypokalaemia. Long-acting beta-2 agonist monotherapy is not appropriate controller treatment for asthma.
Source [1]

References

  1. Hsu E, Bajaj T. Beta2-Agonists. NCBI Bookshelf. Updated 2023. SOURCE:NCBI:BETA2_AGONISTS:2023