Glycopyrrolate

Glycopyrrolate is an antagonist of muscarinic acetylcholine receptors (mAChRs; K_is = 0.42, 1.77, 0.52, 0.78, and 1.29 nM for the M₁-M₅ receptors, respectively).¹ It induces relaxation of precontracted isolated human bronchi when used at concentrations of 0.01, 0.1, or 1 µM.² Glycopyrrolate reduces post-prandial gastric antral motility in dogs when administered at a dose of 0.01 mg/kg.³ It inhibits salivation in a rat model of sialorrhea induced by pilocarpine with an ED₅₀ value of 0.74 µg/kg.² Formulations containing glycopyrrolate have been used in the treatment of sialorrhea, peptic ulcers, and chronic obstructive pulmonary disease (COPD).

WARNING This product is not for human or veterinary use.

1. Gavaldà, A., Ramos, I., Carcasona, C., et al. The in vitro and in vivo profile of aclidinium bromide in comparison with glycopyrronium bromide. Pulm. Pharmacol. Ther. 28(2), 114-1121 (2014).

2. Rogliani, P., Calzetta, L., Ora, J., et al. Pharmacological assessment of the onset of action of aclidinium and glycopyrronium versus tiotropium in COPD patients and human isolated bronchi. Eur. J. Pharmacol. 761, 383-390 (2015).

3. Burger, D.M., Wiestner, T., Hubler, M., et al. Effect of anticholinergics (atropine, glycopyrrolate) and prokinetics (metoclopramide, cisapride) on gastric motility in beagles and labrador retrievers. J. Vet. Med. A Physiol. Pathol. Clin. Med. 53(2), 97-107 (2006).