Glycopyrronium

Glycopyrronium, also known as NVA237 or glycopyrrolate, is a racemic mixture of two enantiomers. They are both quaternary ammonium compounds and long acting muscarinic antagonists. It is one of the most commonly prescribed anticholinergic medications. Early research into glycopyrronium use was for its indication as an adjunct therapy in the treatment of peptic ulcers. Later research, taking advantage of the systemic distribution of muscarinic receptors through the body, found that glycopyrronium could also be used for reducing sweat gland, oral, airway, and gastric secretions; as well as reducing cardiac inhibitory reflexes; and reducing bronchoconstriction in COPD. Glycopyrronium is commonly prescribed as a first line treatment for a wide variety indications and is considered to have a wider therapeutic window than tiotropium.

Glycopyrronium was originally granted FDA approval on 11 August 1961.

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. A glycopyrronium intravenous and intramuscular injection is indicated in adults and pediatric patients to reduce the volume and acidity of gastric secretions, reduce airway secretions, and block cardiac inhibitory reflexes during the induction of anesthesia and intubation; to treat surgically-induced, drug-induced, or vagal reflex associated arrhythmias intraoperatively; and to prevent peripheral muscarinic effects of cholinergic drugs. The same injection is indicated in adults as an adjunct therapy in the treatment of peptic ulcers, as is an orally disintegrating tablet formulation. An oral solution is indicated to treat excessive drooling associated with neurologic conditions in patients aged 3-16 years. Glycopyrronium and budesonide can be formulated with formoterol fumarate for the maintenance of COPD.