WHAT ARE BRONCHODILATORS?
Bronchodilators are medications that relax the bronchial muscles. Relaxing these muscles makes the airways larger, allowingair to pass through the lungs easier. This helps people with COPD breathe better. Many different kinds of bronchodilators areavailable. They can be grouped according to how long they work (called short- and long-acting drugs) or the way in which theywiden or dilate the airways (beta-agonists, anticholinergics or theophyllines). While all bronchodilators widen the airways, theywork in different ways to do so. It is therefore possible to combine bronchodilators in order to achieve maximal benefit. Manypeople with COPD experience constant breathing difficulty. Bronchodilators therefore need to be taken regularly to keepbreathing under control, this is called maintenance medication. Conversely, reliever medications are used for temporarybreathless.
What kinds of bronchodilators are there?
The three main groups of bronchodilators are beta-agonists, anticholinergics and theophyllines. Bronchodilators are importantin treating the symptoms of COPD, such as breathlessness, cough and sputum production. People with COPD are generallyprescribed at least one bronchodilator, however, sometimes two or three medications are needed to control symptoms.Bronchodilators can also be used to "relieve" worsening symptoms. Reliever drugs are usually short acting and, therefore, arenot the best way to control day-to-day symptoms. In order to give you regular control or to maintain your breathing, these short-acting bronchodilators would have to be taken frequently, day and night, 24 hours a day. This is not very practical for mostpeople.It is unusual to find two people with COPD on the same program of medication. Some need bronchodilators from only onegroup, while some need bronchodilators from all three groups. For example, a person may need a beta-agonist as well as ananticholinergic and a theophylline drug. The number of different bronchodilators people with COPD need depends on how welltheir symptoms are controlled.
MECHANISM OF BRONCHODILATOR DRUGS
Inhaled allergens stimulate sensory nerve endings called irritant receptors lying below the airwayepithelium.
Stimulation of these irritant receptors causes parasympathetic nerves to release acetylcholine (ACh).
When acetylcholine binds to M3 muscarinic receptors on airway smooth muscle, a series of events isinitiated which results in an increase in intracellular calcium (Ca2+) and smooth muscle contraction(bronchoconstriction or bronchospasm)
Some inflammatory mediators such as histamine (not shown in illustration) can also increaseintracellular calcium and cause bronchospasm.
There are drugs that can be used to counteract this bronchoconstriction
Beta-2 agonist drugs bind to beta-2 receptors on airway smooth muscle and cause an increase in theconcentration of cAMP in the muscle cell which results in smooth muscle relaxation. When airway smoothmuscle relaxes, the diameter of the air passages is enlarged.
Aminophylline blocks the action of phosphodiesterases and prevents the breakdown of cAMP to 5'-AMP. Thisalso has the effect of relaxing smooth muscle and allowing the airways to dilate.
The bronchoconstricting effects of acetylcholine can be blocked by muscarinic antagonists such as ipratropium bromide.Muscarinic antagonists bind to muscarinic receptors and prevent acetylcholine from binding (see illustration).Bronchodilation can also be achieved by alpha-2 agonist drugs that bind to alpha-2 receptors on parasympathetic nervesand prevent acetylcholine from being released. The following schematic illustrates the mechanism of action of the varioustypes of bronchodilator drugs.