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Concept
Beta2-adrenergic agonist
Summary
DISPLAYTITLE:Beta2-adrenergic agonist
Beta2-adrenergic agonists, also known as adrenergic β2 receptor agonists, are a class of drugs that act on the β2 adrenergic receptor. Like other β adrenergic agonists, they cause smooth muscle relaxation. β2 adrenergic agonists' effects on smooth muscle cause dilation of bronchial passages, vasodilation in muscle and liver, relaxation of uterine muscle, and release of insulin. They are primarily used to treat asthma and other pulmonary disorders, such as Chronic obstructive pulmonary disease (COPD).
Activation of β adrenergic receptors leads to relaxation of smooth muscle in the lung, and dilation and opening of the airways.
β adrenergic receptors are coupled to a stimulatory G protein of adenylyl cyclase. This enzyme produces the second messenger cyclic adenosine monophosphate (cAMP). In the lung, cAMP decreases calcium concentrations within cells and activates protein kinase A. Both of these changes inactivate myosin light-chain kinase and activate myosin light-chain phosphatase. In addition, β2 agonists open large conductance calcium-activated potassium channels and thereby tend to hyperpolarize airway smooth muscle cells. The combination of decreased intracellular calcium, increased membrane potassium conductance, and decreased myosin light chain kinase activity leads to smooth muscle relaxation and bronchodilation.
Findings indicate that β2 stimulants, especially in parenteral administration such as inhalation or injection, can induce adverse effects:
Tachycardia secondary to peripheral vasodilation and cardiac stimulation (Such tachycardia may be accompanied by palpitations.)
Tremor, excessive sweating, anxiety, insomnia, and agitation
More severe effects include paradoxical bronchospasm, hypokalemia, and in rare cases a myocardial infarction. (More severe effects, such as pulmonary edema, myocardial ischemia, and cardiac arrhythmia, are exceptional.)
Overuse of β2 agonists and asthma treatment without proper inhaled corticosteroid use has been associated with an increased risk of asthma exacerbations and asthma-related hospitalizations.
Official source
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