|Trade names||Robinul, Cuvposa, Seebri, others|
|Other names||Glycopyrrolate, glycopyrronium bromide, glycopyrronium tosylate|
|Main uses||COPD, excessive saliva|
|Side effects||Dry mouth, urinary retention, blurry vision, large pupils, headache, confusion, sleepiness, constipation|
|By mouth, intravenous, inhaled, topical|
|Chemical and physical data|
|Molar mass||398.341 g·mol−1|
|3D model (JSmol)|
Glycopyrronium, also known as glycopyrrolate, is a medication used to treat COPD, excessive saliva, and excessive sweating. It may be taken by mouth, by injection, applied to the skin, or inhaled. Effects may last for up to 12 hours. It is also available in combination with a long-acting beta-adrenoceptor agonist (LABA) and inhaled steroid.
Common side effects include dry mouth, urinary retention, blurry vision, large pupils, headache, confusion, sleepiness, and constipation. Other side effects may include allergic reactions and bronchospasm. Safety in pregnancy is unclear. It is an antimuscarinic. It does not generally cross the blood–brain barrier.
Glycopyrronium was approved for medical use in the United States in 1961. It is on the World Health Organization's List of Essential Medicines as an alternative to tiotropium. In the United Kingdom a month of inhaled medication costs the NHS about £28 as of 2021. In the United States the tablets are inexpensive.
Intravenous glycopyrronium has been used before surgery to reduce salivary, tracheobronchial, and pharyngeal secretions. It is also used in conjunction with neostigmine, a neuromuscular blocking reversal agent, to prevent neostigmine's muscarinic effects such as bradycardia. It can be administered to raise the heart rate in bradycardia, which often will also increase the blood pressure.
It is also used to reduce excessive saliva (sialorrhea), and Ménière's disease. In end of life care, it may be used to decrease bronchial secretions in people who are no longer able to clear their own airway through insufficient coughing reflex.
In inhalable form it is used to treat chronic obstructive pulmonary disease (COPD). Doses for inhalation are much lower than oral ones, so that swallowing a dose will not have an effect.
For COPD the inhaled form is used at a dose of 44 micrograms once per day.
Dry mouth, urinary retention, headaches, vomiting, diarrhea, constipation, blurry vision are possible side effects of the medication. Since glycopyrronium reduces the body's sweating ability, it can even cause hyperthermia and heat stroke in hot environments. The medication also induces drowsiness, an effect exacerbated by the consumption of alcohol.
Mechanism of action
Glycopyrronium bromide affects the gastrointestinal tracts, liver and kidney but has a very limited effect on the brain and the central nervous system. In horse studies, after a single intravenous infusion, the observed tendencies of glycopyrronium followed a tri-exponential equation, by rapid disappearance from the blood followed by a prolonged terminal phase. Excretion was mainly in urine and in the form of an unchanged drug. Glycopyrronium has a relatively slow diffusion rate, and in a standard comparison to atropine, is more resistant to penetration through the blood-brain barrier and placenta.
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