COPD new drugs new devices
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This document discusses the pharmacological treatment of COPD, classifying medications by class. It describes long-acting bronchodilators including LAMAs which block acetylcholine-mediated bronchoconstriction and LABAs which directly relax airway smooth muscle. It also discusses fixed-dose combination LABA/LAMA inhalers, ICS/LABA inhalers, and the PDE-4 inhibitor Roflumilast which reduces inflammation but has no direct bronchodilator effect.
COPD new drugs new devices
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- 7. 7 Pharmacological treatment of COPD (Lots of inhalers, lots of names…)
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- 9. 9 More useful to classify in terms of classes
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- 11. Children’s Healthcare of Atlanta
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- 30. 30 Long-Acting Bronchodilators • LAMAs • Block acetylcholine- mediated bronchoconstriction (via M3 receptors) – Tiotropium – Aclidinium – Glycopyrronium (glycopyrrolate) – Umeclidinium • LABAs • Direct relaxant activity on airway smooth muscle (via β2 adrenoceptors) – Formoterol – Salmeterol – Indacaterol – Oldaterol – Vilanterol
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- 32. 32 LABA DPI Diskus Serevent® (salmeterol) DPI Aerolizer Foradil® (formoterol) DPI Breezhaler Onbrez® (indacaterol) SMI Respimat Striverdi® (Olodaterol)
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- 42. 42 LAMA DPI HandiHaler/ SMI Respimat Spiriva® (tiotropium) DPI Breezhaler Seebri® (glycopyrronium) DPI Genuair Eklira® (aclidinium) DPI Ellipta Incruse® (umeclidinium) LAMA inhalers for COPD
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- 50. Children’s Healthcare of Atlanta Proskocil BJ et al. Proc Am Thorac Soc. 2005;2(4):305-310. SMC relaxationSMC contraction M3- muscarinic receptors Beta Agonists (LABA)Antocholinergics (LAMA) β2-adrenergic receptors Mechanisms of action of bronchodilators on airway smooth muscle
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- 52. 52 Fixed-dose combination LABA/LAMA DPI Ellipta Anoro® (vilanterol/umeclidinium) DPI Breezhaler Ultibro® (indacaterol/glycopyrronium) SMI Respimat Inspiolto® (olodaterol/tiotropium) DPI Genuair Duaklir® (formoterol/aclidinium) Combination LABA/LAMA inhalers for COPD
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- 62. 62 ICS/LABA DPI Diskus Advair® (Fluticasone/salmeterol) DPI Turbuhaler Symbicort® (Budesonide/formoterol) DPI Ellipta Relvar® (Fluticasone/vilanterol)
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- 64. 64 Diskus
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- 77. 77 Phosphodiesterase-4 inhibitor: Roflumilast (Daliresp) i. Indication: As a daily treatment to reduce the risk of COPD exacerbations in patients with severe COPD (FEV1 less than 50% of predicted) associated with chronic bronchitis and a history of frequent exacerbations. ii. Mechanism: Reduces inflammation through inhibition of the breakdown of intracellular cyclic adenosine monophosphate; no direct bronchodilator activity page
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- 80. 80 iii. Dose: 500 mcg orally once daily iv. Contraindications: Moderate to severe liver impairment; use in nursing mothers v. Precautions: Weight loss (monitor); psychiatric events including suicidality (monitor; weigh risk/benefit ratio in patients with preexisting psychiatric illness). Twenty percent of patients studied had weight loss of 5%–10% of body weight, compared with 7% with placebo; average weight loss was 2 kg.
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- 83. 83 vi. Adverse reactions: Diarrhea, weight loss or decreased appetite, nausea, headache, back pain, influenza, insomnia, and dizziness vii. Drug interactions: Use with strong cytochrome P450 (CYP) enzyme inducers is not recommended (e.g., rifampin, phenobarbital, carbamazepine, phenytoin); use with CYP3A4 inhibitors or dual inhibitors of CYP3A4 and CYP1A2 (e.g., erythromycin, ketoconazole, fluvoxamine) increases roflumilast exposure and adverse effects (risk/benefit ratio must be weighed).
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