Legal status US: ℞-only PubChem CID 11693 | CAS Number 51186-83-5 | |
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Trade names Robinul (tablets, intravenous), Seebri (inhalation), others Pregnancy
category US: B (No risk in non-human studies) ATC code A03AB02 (WHO) R03BB06 (WHO) | ||
Glycopyrronium bromide is a medication of the muscarinic anticholinergic group. It does not cross the blood–brain barrier and consequently has no to few central effects. A synthetic quaternary amine, it is available in oral and intravenous forms and as inhalation. It was developed by Sosei and licensed to Novartis in 2005. The cation, which is the active moiety, is called glycopyrronium (INN) or glycopyrrolate (USAN).
Contents
Medical uses
In anesthesia, glycopyrronium injection can be used as a preoperative medication in order to reduce salivary, tracheobronchial, and pharyngeal secretions, as well as decreasing the acidity of gastric secretion. It is also used in conjunction with neostigmine, a neuromuscular blocking reversal agent, to prevent neostigmine's muscarinic effects such as bradycardia.
It is also used to reduce excessive saliva (sialorrhea), and Ménière's disease.
It decreases acid secretion in the stomach and so may be used for treating stomach ulcers, in combination with other medications.
It has been used topically and orally to treat hyperhidrosis, in particular, gustatory hyperhidrosis.
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.
Side effects
Since glycopyrronium reduces the body's sweating ability, it can even cause hyperthermia and heat stroke in hot environments. Dry mouth, difficulty urinating, headaches, diarrhea and constipation are also observed side effects of the medication. The medication also induces drowsiness or blurred vision, an effect exacerbated by the consumption of alcohol.
Mechanism of action
Glycopyrronium blocks muscarinic receptors, thus inhibiting cholinergic transmission.
Pharmacokinetics
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 tendency of glycopyrronium followed a tri-exponential equation, followed 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.
Research
It has been studied in asthma.