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Review ArticleReview Article

Pharmacology and Therapeutics of Bronchodilators

Mario Cazzola, Clive P. Page, Luigino Calzetta and M. Gabriella Matera
David R. Sibley, ASSOCIATE EDITOR
Pharmacological Reviews July 2012, 64 (3) 450-504; DOI: https://doi.org/10.1124/pr.111.004580
Mario Cazzola
Department of Internal Medicine, Unit of Respiratory Clinical Pharmacology, University of Rome ‘Tor Vergata,’ Rome, Italy (M.C., L.C.); Department of Pulmonary Rehabilitation, San Raffaele Pisana Hospital, Istituto di Ricovero e Cura a Carattere Scientifico, Rome, Italy (M.C., L.C.); Sackler Institute of Pulmonary Pharmacology, Institute of Pharmaceutical Science, King's College London, London, UK (C.P.P., L.C.); and Department of Experimental Medicine, Unit of Pharmacology, Second University of Naples, Naples, Italy (M.G.M.)
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Clive P. Page
Department of Internal Medicine, Unit of Respiratory Clinical Pharmacology, University of Rome ‘Tor Vergata,’ Rome, Italy (M.C., L.C.); Department of Pulmonary Rehabilitation, San Raffaele Pisana Hospital, Istituto di Ricovero e Cura a Carattere Scientifico, Rome, Italy (M.C., L.C.); Sackler Institute of Pulmonary Pharmacology, Institute of Pharmaceutical Science, King's College London, London, UK (C.P.P., L.C.); and Department of Experimental Medicine, Unit of Pharmacology, Second University of Naples, Naples, Italy (M.G.M.)
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Luigino Calzetta
Department of Internal Medicine, Unit of Respiratory Clinical Pharmacology, University of Rome ‘Tor Vergata,’ Rome, Italy (M.C., L.C.); Department of Pulmonary Rehabilitation, San Raffaele Pisana Hospital, Istituto di Ricovero e Cura a Carattere Scientifico, Rome, Italy (M.C., L.C.); Sackler Institute of Pulmonary Pharmacology, Institute of Pharmaceutical Science, King's College London, London, UK (C.P.P., L.C.); and Department of Experimental Medicine, Unit of Pharmacology, Second University of Naples, Naples, Italy (M.G.M.)
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M. Gabriella Matera
Department of Internal Medicine, Unit of Respiratory Clinical Pharmacology, University of Rome ‘Tor Vergata,’ Rome, Italy (M.C., L.C.); Department of Pulmonary Rehabilitation, San Raffaele Pisana Hospital, Istituto di Ricovero e Cura a Carattere Scientifico, Rome, Italy (M.C., L.C.); Sackler Institute of Pulmonary Pharmacology, Institute of Pharmaceutical Science, King's College London, London, UK (C.P.P., L.C.); and Department of Experimental Medicine, Unit of Pharmacology, Second University of Naples, Naples, Italy (M.G.M.)
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David R. Sibley
Department of Internal Medicine, Unit of Respiratory Clinical Pharmacology, University of Rome ‘Tor Vergata,’ Rome, Italy (M.C., L.C.); Department of Pulmonary Rehabilitation, San Raffaele Pisana Hospital, Istituto di Ricovero e Cura a Carattere Scientifico, Rome, Italy (M.C., L.C.); Sackler Institute of Pulmonary Pharmacology, Institute of Pharmaceutical Science, King's College London, London, UK (C.P.P., L.C.); and Department of Experimental Medicine, Unit of Pharmacology, Second University of Naples, Naples, Italy (M.G.M.)
Roles: ASSOCIATE EDITOR
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Abstract

Bronchodilators are central in the treatment of of airways disorders. They are the mainstay of the current management of chronic obstructive pulmonary disease (COPD) and are critical in the symptomatic management of asthma, although controversies around the use of these drugs remain. Bronchodilators work through their direct relaxation effect on airway smooth muscle cells. at present, three major classes of bronchodilators, β2-adrenoceptor (AR) agonists, muscarinic receptor antagonists, and xanthines are available and can be used individually or in combination. The use of the inhaled route is currently preferred to minimize systemic effects. Fast- and short-acting agents are best used for rescue of symptoms, whereas long-acting agents are best used for maintenance therapy. It has proven difficult to discover novel classes of bronchodilator drugs, although potential new targets are emerging. Consequently, the logical approach has been to improve the existing bronchodilators, although several novel broncholytic classes are under development. An important step in simplifying asthma and COPD management and improving adherence with prescribed therapy is to reduce the dose frequency to the minimum necessary to maintain disease control. Therefore, the incorporation of once-daily dose administration is an important strategy to improve adherence. Several once-daily β2-AR agonists or ultra-long-acting β2-AR-agonists (LABAs), such as indacaterol, olodaterol, and vilanterol, are already in the market or under development for the treatment of COPD and asthma, but current recommendations suggest the use of LABAs only in combination with an inhaled corticosteroid. In addition, some new potentially long-acting antimuscarinic agents, such as glycopyrronium bromide (NVA-237), aclidinium bromide, and umeclidinium bromide (GSK573719), are under development, as well as combinations of several classes of long-acting bronchodilator drugs, in an attempt to simplify treatment regimens as much as possible. This review will describe the pharmacology and therapeutics of old, new, and emerging classes of bronchodilator.

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  • This article is available online at http://pharmrev.aspetjournals.org.

    http://dx.doi.org/10.1124/pr.111.004580.

  • © 2012 by The American Society for Pharmacology and Experimental Therapeutics
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Pharmacological Reviews: 64 (3)
Pharmacological Reviews
Vol. 64, Issue 3
1 Jul 2012
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Review ArticleReview Article

PHARMACOLOGY AND THERAPEUTICS OF BRONCHODILATORS

Mario Cazzola, Clive P. Page, Luigino Calzetta and M. Gabriella Matera
Pharmacological Reviews July 1, 2012, 64 (3) 450-504; DOI: https://doi.org/10.1124/pr.111.004580

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Review ArticleReview Article

PHARMACOLOGY AND THERAPEUTICS OF BRONCHODILATORS

Mario Cazzola, Clive P. Page, Luigino Calzetta and M. Gabriella Matera
Pharmacological Reviews July 1, 2012, 64 (3) 450-504; DOI: https://doi.org/10.1124/pr.111.004580
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  • Article
    • Abstract
    • I. Introduction: The Physiological Rationale for Using Bronchodilators
    • II. β-Adrenergic Receptor Agonists
    • III. Muscarinic Acetylcholine Receptor Antagonists
    • IV. Xanthines
    • V. Novel Classes of Bronchodilators
    • VI. Combination Therapy
    • VII. Controversies Surrounding Bronchodilators
    • VIII. The Role of Bronchodilators in the Management of Asthma and Chronic Obstructive Pulmonary Disease
    • IX. The Use of Bronchodilators in Special Populations
    • X. Pharmacogenetics of Airway Obstruction and the Future
    • Authorship Contributions
    • Footnotes
    • References
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