Category:Bronchodilators: Difference between revisions
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The inhaled antimuscarinics returned with a quaternary-amine modification that prevented systemic absorption from the airway. [[Ipratropium|Ipratropium]] bromide (Boehringer Ingelheim, 1976), a quaternary derivative of atropine, was the first inhaled muscarinic antagonist; it provided 6-to-8-hour bronchodilation as a short-acting agent. The [[:Category:Long-acting_muscarinic_antagonists|long-acting muscarinic antagonist]] [[Tiotropium|tiotropium]] (Boehringer Ingelheim, 2002), with its slow off-rate from the M3 receptor, gave once-daily dosing; aclidinium, umeclidinium, and glycopyrronium followed. The LAMAs are now first-line maintenance therapy in COPD and increasingly used as add-on in moderate-to-severe asthma. The combination of a LABA and a LAMA in a single inhaler (umeclidinium/vilanterol, glycopyrronium/indacaterol, tiotropium/olodaterol, others) has become the standard maintenance regimen in moderate COPD; the triple combination of LABA, LAMA, and inhaled corticosteroid (the so-called single-inhaler triple therapy, including fluticasone/umeclidinium/vilanterol and budesonide/glycopyrronium/formoterol) is now the standard for severe COPD with exacerbations and for severe asthma not controlled on dual therapy. | The inhaled antimuscarinics returned with a quaternary-amine modification that prevented systemic absorption from the airway. [[Ipratropium|Ipratropium]] bromide (Boehringer Ingelheim, 1976), a quaternary derivative of atropine, was the first inhaled muscarinic antagonist; it provided 6-to-8-hour bronchodilation as a short-acting agent. The [[:Category:Long-acting_muscarinic_antagonists|long-acting muscarinic antagonist]] [[Tiotropium|tiotropium]] (Boehringer Ingelheim, 2002), with its slow off-rate from the M3 receptor, gave once-daily dosing; aclidinium, umeclidinium, and glycopyrronium followed. The LAMAs are now first-line maintenance therapy in COPD and increasingly used as add-on in moderate-to-severe asthma. The combination of a LABA and a LAMA in a single inhaler (umeclidinium/vilanterol, glycopyrronium/indacaterol, tiotropium/olodaterol, others) has become the standard maintenance regimen in moderate COPD; the triple combination of LABA, LAMA, and inhaled corticosteroid (the so-called single-inhaler triple therapy, including fluticasone/umeclidinium/vilanterol and budesonide/glycopyrronium/formoterol) is now the standard for severe COPD with exacerbations and for severe asthma not controlled on dual therapy. | ||
The methylxanthines (theophylline, aminophylline) are the older oral bronchodilators, derivatives of the natural xanthine caffeine that acts through phosphodiesterase inhibition and adenosine-receptor antagonism. Their narrow therapeutic window (serum levels above 20 mg/L produce nausea, headache, tachyarrhythmia, and seizure), substantial | The methylxanthines (theophylline, aminophylline) are the older oral bronchodilators, derivatives of the natural xanthine caffeine that acts through phosphodiesterase inhibition and adenosine-receptor antagonism. Their narrow therapeutic window (serum levels above 20 mg/L produce nausea, headache, tachyarrhythmia, and seizure), substantial interaction profile (multiple CYP isoforms), and modest bronchodilator effect have progressively narrowed their use to selected patients with refractory disease. [[wikipedia:Roflumilast|Roflumilast]] (Daxas, 2010), an oral PDE4 inhibitor, is an inflammation-modifying medicine in severe COPD rather than a bronchodilator in the conventional sense, but is collected here for its closely related pharmacology. | ||
The pharmacology of the contemporary inhaled bronchodilator is shaped, more than any other class, by the device through which the medicine is delivered. The pressurised metered-dose inhaler (developed by Riker Laboratories in 1956 and the first practical handheld aerosol medicine), the dry-powder inhaler (Spinhaler 1971, Turbuhaler 1988, Diskus 2000), the soft-mist Respimat inhaler, and the nebuliser each deliver a different fraction of the labelled dose to the lung depending on patient inhalation technique. The substantial fraction of clinical "treatment failure" in obstructive airway disease is, on close examination, failure of device technique rather than failure of the medicine, and patient education in inhaler use is part of the clinical pharmacology of this category in a way it is not for any other. | The pharmacology of the contemporary inhaled bronchodilator is shaped, more than any other class, by the device through which the medicine is delivered. The pressurised metered-dose inhaler (developed by Riker Laboratories in 1956 and the first practical handheld aerosol medicine), the dry-powder inhaler (Spinhaler 1971, Turbuhaler 1988, Diskus 2000), the soft-mist Respimat inhaler, and the nebuliser each deliver a different fraction of the labelled dose to the lung depending on patient inhalation technique. The substantial fraction of clinical "treatment failure" in obstructive airway disease is, on close examination, failure of device technique rather than failure of the medicine, and patient education in inhaler use is part of the clinical pharmacology of this category in a way it is not for any other. | ||