Glycopyrronium bromide
Anticholinergic
From Wikipedia, the free encyclopedia
Glycopyrronium bromide is a medication of the muscarinic anticholinergic group.[7] It does not cross the blood–brain barrier and consequently has few to no central effects. It can be administered orally,[8] intravenously, topically,[9] or via inhalation.[4][5][6] It is a synthetic quaternary ammonium compound.[2] The cation, which is the active moiety, is called glycopyrronium (INN)[10] or glycopyrrolate (USAN).
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| Pronunciation | /ˌɡlaɪkoʊpaɪˈroʊniʌmˈbroʊmaɪd/ gly-koh-py-ROH-nee-um BROH-myd |
| Trade names | Robinul, Cuvposa, Seebri, others |
| Other names | glycopyrrolate (USAN US) |
| AHFS/Drugs.com | Monograph |
| MedlinePlus | a602014 |
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| Routes of administration | By mouth, intravenous, inhalation, topical, injection, subcutaneous |
| Drug class | Antimuscarinic (peripherally-selective) |
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| Elimination half-life | 0.6–1.2 hours |
| Excretion | 85% Kidney, unknown amount in the bile |
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| ECHA InfoCard | 100.008.990 |
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| Formula | C19H28BrNO3 |
| Molar mass | 398.341 g·mol−1 |
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The most common side effects include irritability, flushing, nasal congestion, reduced secretions in the airways, dry mouth, constipation, diarrhea, nausea and vomiting, and urinary retention.[7]
In September 2012, glycopyrronium was approved for medical use in the European Union.[4] In June 2018, glycopyrronium was approved by the U.S. Food and Drug Administration (FDA) to treat excessive underarm sweating, becoming the first drug developed specifically to reduce excessive sweating.[11] It is on the World Health Organization's List of Essential Medicines.[12]
Medical uses
Glycopyrronium was first used in 1961 to treat peptic ulcers. Since 1975, intravenous glycopyrronium has been used before surgery to reduce salivary, tracheobronchial, and pharyngeal secretions.[13] It is also used in conjunction with neostigmine, a neuromuscular blocking reversal agent, to prevent neostigmine's muscarinic effects such as bradycardia.[14] It can be administered to raise the heart rate in reflex bradycardia as a result of a vasovagal reaction, which often will also increase the blood pressure.[15]
It is also used to reduce excessive saliva (sialorrhea),[7][16][17][18] and to treat Ménière's disease.[19]
It has been used topically and orally to treat hyperhidrosis, in particular, gustatory hyperhidrosis and generalized hyperhidrosis.[20][21]
When inhaled, it is used to treat chronic obstructive pulmonary disease (COPD).[4][5][6] Doses for inhalation are much lower than oral ones, so that swallowing a dose will not have an effect.[22][23]
Side effects
Dry mouth, urinary retention, headaches, vomiting, diarrhea, constipation, and blurry vision are possible side effects of the medication.[13]
Pharmacology
Mechanism of action
Glycopyrronium competitively blocks muscarinic receptors,[13][24] 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 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.[25]
