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Glycopyrronium is an anticholinergic agent used to treat hyperhidrosis, severe drooling, COPD, used with other medications to treat ulcers, and used in anesthesia. Glycopyrronium, also known as NVA237 or glycopyrrolate, is a racemic mixture of two enantiomers.
- Mechanism
- Curator reviewed · 13 references
Glycopyrronium is a muscarinic antagonist with the highest affinity for M1 receptors, followed by M3, M2/M4, and M5.
Muscarinic receptors M1 to M4 are found in the lung, although M3 is predominantly responsible for bronchoconstriction and airway secretions. Secretions from salivary and sweat glands, as well as gastric acid secretions, are also predominantly mediated by the M3 receptor. Salivary and gastric acid secretions are also partially mediated by the M1 receptor. Antagonism of these receptors decreases the volume of their respective secretions, and in the case of the gastrointestinal system, reduces the acidity of the stomach.
In the cardiovascular system, muscarinic receptors M1 to M5 are all present, however the function of M5 has not been described in literature. Under normal circumstances, stimulation of the vagal nerve lowers the heart rate, potentially leading to intraoperative bradycardia. Studies in mice suggest that this stimulation is predominantly mediated by the M3 receptor, and mutant knockout mice are not susceptible to these effects.
- Primary indication
- Glycopyrronium formulated as a topical cloth is indicated to treat primary axillary hyperhidrosis in patients ≥9 years, and an inhalational solution is indicated for long term maintenance of airflow obstruction in COPD.Curator reviewed · 19 structured indications
- Formula / weight
- C19H28NO3 · 318.4305 g/mol (avg)
- First approval
- Canada, 2005 · United States, 1961 · European Union, 2016
- Also known as
- Glycopyrrolate · Glycopyrrolate ion · Glycopyrronium ion
- Code names
- DRM-04
Resolves to
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Which drugs share a target with Glycopyrronium, and which of those have an active Phase 3 trial?