Once-daily glycopyrronium via the Breezhaler® device for the treatment of COPD: pharmacological and clinical profile

Expert Rev Clin Pharmacol. 2013 Sep;6(5):503-17. doi: 10.1586/17512433.2013.828419. Epub 2013 Aug 24.

Abstract

In the management of chronic obstructive pulmonary disease (COPD), there is an unmet medical need for effective bronchodilator treatments that not only have a fast onset of action, but also a long duration of action and are delivered using a simple, easy-to-use device. Long-acting muscarinic antagonists such as glycopyrronium and tiotropium, along with long-acting beta-2 agonists such as indacaterol, formoterol and salmeterol are the pillars of pharmacological therapy for the long-term management of patients with COPD. Glycopyrronium, the quaternary ammonium ion of glycopyrronium bromide, acts as a competitive antagonist by selectively binding to the muscarinic receptors in the bronchial smooth musculature, thus inhibiting acetylcholine-mediated bronchoconstriction. Glycopyrronium is an inhaled once-daily long-acting muscarinic antagonist recently approved for the maintenance treatment of patients with COPD. Glycopyrronium is administered by a single-dose, dry-powder inhaler, the Breezhaler® device, designed specifically to have a low internal resistance, be easy to use and confirm efficient drug delivery in patients with a wide range of COPD severities, irrespective of the age. Glycopyrronium has been shown to provide rapid and sustained improvements in lung function, dyspnea, health status, exercise endurance and exacerbation risk and an acceptable safety and tolerability profile.

Publication types

  • Research Support, Non-U.S. Gov't
  • Review

MeSH terms

  • Administration, Inhalation
  • Animals
  • Clinical Trials as Topic
  • Drug Administration Schedule
  • Dry Powder Inhalers*
  • Glycopyrrolate / administration & dosage
  • Glycopyrrolate / adverse effects
  • Glycopyrrolate / pharmacokinetics
  • Glycopyrrolate / therapeutic use*
  • Humans
  • Molecular Structure
  • Muscarinic Antagonists / administration & dosage
  • Muscarinic Antagonists / adverse effects
  • Muscarinic Antagonists / pharmacokinetics
  • Muscarinic Antagonists / therapeutic use*
  • Pulmonary Disease, Chronic Obstructive / drug therapy*
  • Treatment Outcome

Substances

  • Muscarinic Antagonists
  • Glycopyrrolate