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Bronchodilators relax bronchial smooth muscle and widen the airway. Three drug groups reach that goal by different pathways.
| Group | Target | Result |
|---|---|---|
| Beta₂-adrenergic agonists | Stimulate beta₂ receptors on airway smooth muscle → ↑cyclic AMP | Smooth muscle relaxation; also stabilize mast cells and improve mucociliary clearance |
| Muscarinic antagonists (anticholinergics) | Block acetylcholine at M₃ receptors | Prevent vagally mediated bronchoconstriction and reduce mucus secretion |
| Methylxanthines | Inhibit phosphodiesterase and block adenosine receptors | Modest bronchodilation, increased diaphragm contractility, central respiratory stimulation |
The inhaled route is preferred because it delivers the drug directly to the airway, works faster, and needs a much smaller dose than oral therapy, which lowers systemic adverse effects.
| Drug (generic) | Class | Key use | Key point |
|---|---|---|---|
| Albuterol (salbutamol) — prototype | SABA | Quick relief of bronchospasm; acute asthma and COPD exacerbations; exercise-induced bronchoconstriction | Onset within about 5 minutes, lasts 4–6 hours |
| Levalbuterol | SABA | Same as albuterol | Single-isomer form; similar adverse effects |
| Terbutaline | SABA (inhaled, oral, subcutaneous) | Bronchospasm | Boxed warning: not for prolonged prevention or treatment of preterm labor — injectable not beyond 48–72 hours; oral not for any tocolysis |
| Formoterol | LABA, fast onset | Asthma (always with ICS); COPD maintenance | The only LABA used as a reliever — inside an ICS-formoterol inhaler |
| Salmeterol, vilanterol, olodaterol, indacaterol | LABA | Maintenance twice daily or once daily | Not approved or used as rescue drugs (salmeterol also has a slow onset) |
| Ipratropium — prototype SAMA | Short-acting muscarinic antagonist | COPD relief; add-on in severe acute asthma | Often combined with albuterol in one inhaler or nebule |
| Tiotropium — prototype LAMA | Long-acting muscarinic antagonist | COPD maintenance; add-on in severe asthma (step 5) | Once daily; not for acute relief |
| Umeclidinium, glycopyrronium (glycopyrrolate), aclidinium | LAMA | COPD maintenance | Often in fixed LABA + LAMA combinations |
| Theophylline (oral), aminophylline (IV) | Methylxanthine | Rarely used add-on when other therapy is unavailable or insufficient | Narrow therapeutic range; many interactions |
| Class | Common | Serious |
|---|---|---|
| Beta₂ agonists | Tremor, tachycardia, palpitations, nervousness, headache, insomnia | Hypokalemia, hyperglycemia, lactic acidosis with high-dose repeated nebulization, dysrhythmias, chest pain, paradoxical bronchospasm |
| LABA | As above | Single-ingredient LABA used without ICS in asthma increases the risk of severe attacks and asthma-related death. In 2017 the FDA removed the boxed warning from ICS/LABA combination inhalers because combined use did not show this risk. Single-ingredient LABA products (e.g., salmeterol) still carry the boxed warning (asthma-related death); LABA monotherapy in asthma is contraindicated |
| Muscarinic antagonists | Dry mouth, cough, bitter taste, constipation | Urinary retention, acute angle-closure glaucoma (eye pain, halos, blurred vision) if mist reaches the eyes, paradoxical bronchospasm |
| Methylxanthines | Nausea, vomiting, insomnia, restlessness, headache, diuresis | Tachydysrhythmias, seizures — seizures can occur without earlier gastrointestinal warning signs |
Listed in priority order.
| Toxicity | Findings | Management |
|---|---|---|
| Beta₂-agonist excess | Tachycardia, tremor, agitation, hypokalemia, hyperglycemia, lactic acidosis, dysrhythmias | Stop or reduce the drug, cardiac monitoring, correct potassium carefully (it shifts back when the drug wears off). No specific antidote; beta-blockers are used only by specialists because they can provoke bronchospasm |
| Anticholinergic excess (usually from swallowing or eye exposure) | Dry flushed skin, dilated pupils, urinary retention, confusion, eye pain | Stop the drug; urgent eye assessment for angle-closure glaucoma; supportive care |
| Theophylline toxicity | Levels above about 20 mcg/mL (111 µmol/L): nausea, vomiting, tachycardia, restlessness; higher levels: seizures, ventricular dysrhythmias, hypokalemia, hyperglycemia | Stop the drug; cardiac monitoring; activated charcoal (multiple doses) if airway is protected; antiemetic; benzodiazepines for seizures; hemodialysis for severe toxicity. No specific antidote |
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