Clinical data | |
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Trade names | Robinul, Cuvposa, Seebri, others |
Other names | glycopyrrolate ( USAN US) |
AHFS/ Drugs.com | Monograph |
MedlinePlus | a602014 |
License data | |
Pregnancy category |
|
Routes of administration | By mouth, intravenous, inhalation, topical, injection, subcutaneous |
Drug class | Antimuscarinic agent |
ATC code | |
Legal status | |
Legal status | |
Pharmacokinetic data | |
Elimination half-life | 0.6–1.2 hours |
Excretion | 85% Kidney, unknown amount in the bile |
Identifiers | |
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CAS Number |
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PubChem CID | |
IUPHAR/BPS | |
DrugBank |
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ChemSpider | |
UNII |
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KEGG | |
ChEBI | |
ChEMBL |
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CompTox Dashboard ( EPA) | |
ECHA InfoCard | 100.008.990 |
Chemical and physical data | |
Formula | C19H28BrNO3 |
Molar mass | 398.341 g·mol−1 |
3D model ( JSmol) |
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(what is this?) (verify) |
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 is given by mouth, [8] via intravenous injection, on the skin, [9] and 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).
The most common side effects include irritability, flushing, blocked nose, reduced secretions in the airways, dry mouth, constipation, diarrhea, vomiting and inability to completely empty the bladder (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 US 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]
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 bradycardia, which often will also increase the blood pressure.
It is also used to reduce excessive saliva ( sialorrhea), [7] [15] [16] [17] and to treat Ménière's disease. [18]
It has been used topically and orally to treat hyperhidrosis, in particular, gustatory hyperhidrosis. [19] [20]
In inhalable form 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. [21] [22]
Dry mouth, urinary retention, headaches, vomiting, diarrhea, constipation, blurry vision are possible side effects of the medication. [13]
Glycopyrronium competitively blocks muscarinic receptors, [13] [23] thus inhibiting cholinergic transmission.
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. [24]
It has been studied in asthma. [25] [26]
Clinical data | |
---|---|
Trade names | Robinul, Cuvposa, Seebri, others |
Other names | glycopyrrolate ( USAN US) |
AHFS/ Drugs.com | Monograph |
MedlinePlus | a602014 |
License data | |
Pregnancy category |
|
Routes of administration | By mouth, intravenous, inhalation, topical, injection, subcutaneous |
Drug class | Antimuscarinic agent |
ATC code | |
Legal status | |
Legal status | |
Pharmacokinetic data | |
Elimination half-life | 0.6–1.2 hours |
Excretion | 85% Kidney, unknown amount in the bile |
Identifiers | |
| |
CAS Number |
|
PubChem CID | |
IUPHAR/BPS | |
DrugBank |
|
ChemSpider | |
UNII |
|
KEGG | |
ChEBI | |
ChEMBL |
|
CompTox Dashboard ( EPA) | |
ECHA InfoCard | 100.008.990 |
Chemical and physical data | |
Formula | C19H28BrNO3 |
Molar mass | 398.341 g·mol−1 |
3D model ( JSmol) |
|
| |
| |
(what is this?) (verify) |
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 is given by mouth, [8] via intravenous injection, on the skin, [9] and 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).
The most common side effects include irritability, flushing, blocked nose, reduced secretions in the airways, dry mouth, constipation, diarrhea, vomiting and inability to completely empty the bladder (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 US 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]
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 bradycardia, which often will also increase the blood pressure.
It is also used to reduce excessive saliva ( sialorrhea), [7] [15] [16] [17] and to treat Ménière's disease. [18]
It has been used topically and orally to treat hyperhidrosis, in particular, gustatory hyperhidrosis. [19] [20]
In inhalable form 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. [21] [22]
Dry mouth, urinary retention, headaches, vomiting, diarrhea, constipation, blurry vision are possible side effects of the medication. [13]
Glycopyrronium competitively blocks muscarinic receptors, [13] [23] thus inhibiting cholinergic transmission.
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. [24]
It has been studied in asthma. [25] [26]