Hepatotoxicity
Like other anticholinergic agents, glycopyrrolate has not been linked to episodes of liver enzyme elevations or clinically apparent liver injury. A major reason for its safety may relate to the low daily dose.
References on the safety and potential hepatotoxicity of anticholinergics are given together after the Overview section on Anticholinergic Agents.
Drug Class: Gastrointestinal Agents; Anticholinergic Agents

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Effects During Pregnancy and Lactation
◉ Summary of Use during Lactation
No information is available on the use of glycopyrrolate during breastfeeding. Because glycopyrrolate is a quaternary ammonium compound, it is not likely to be absorbed and reach the bloodstream of the infant, especially when given by inhalation or topically on the skin. Long-term oral use of glycopyrrolate might reduce milk production or milk letdown, but a single dose is unlikely to interfere with breastfeeding. During long-term use, observe for signs of decreased lactation such as poor weight gain.
◉ Effects in Breastfed Infants
Relevant published information was not found as of the revision date.
◉ Effects on Lactation and Breastmilk
Relevant published information in nursing mothers was not found as of the revision date. Anticholinergics can inhibit lactation in animals, apparently by inhibiting growth hormone and oxytocin secretion. Anticholinergic drugs can also reduce serum prolactin in nonnursing women. The prolactin level in a mother with established lactation may not affect her ability to breastfeed.

[1]. Effects of (a Combination of) the Beta2-Adrenoceptor Agonist Indacaterol and the Muscarinic Receptor Antagonist Glycopyrrolate on Intrapulmonary Airway Constriction . Cells, 2021, 10(5): 1237.

[2]. Dose effect and benefits of glycopyrrolate in the treatment of bradycardia in anesthetized dogs . The Canadian Veterinary Journal, 1999, 40(5): 327.

[3]. Glycopyrrolate causes prolonged bronchoprotection and bronchodilatation in patients with asthma . Chest, 2005, 128(4): 1974-1979.

Glycopyrronium bromide is a quaternary ammonium salt composed of 3-{[cyclopentyl(hydroxy)phenylacetyl]oxy}-1,1-dimethylpyrrolidin-1-ium and bromide ions in a 1:1 ratio. It is a quaternary ammonium salt and an organic bromide salt.
Glycopyrrolate is an anticholinergic agent used to treat gastrointestinal conditions associated with intestinal spasm and to decrease secretions during anesthesia. Glycopyrrolate has not been implicated in causing liver enzyme elevations or clinically apparent acute liver injury.
Glycopyrrolate is a synthetic quaternary ammonium that is an anticholinergic agent with antispasmodic activity. Glycopyrrolate competitively binds to peripheral muscarinic receptors in the autonomic effector cells of, and inhibits cholinergic transmission in smooth muscle, cardiac muscle, the sinoatrial (SA) node, the atrioventricular (AV) node, exocrine glands and in the autonomic ganglia. Blockage of cholinergic transmission, in smooth muscle cells located in the gastrointestinal tract and the bladder, causes smooth muscle relaxation and prevents the occurrence of painful spasms. In addition, glycopyrrolate inhibits the release of gastric, pharyngeal, tracheal, and bronchial secretions.
A muscarinic antagonist used as an antispasmodic, in some disorders of the gastrointestinal tract, and to reduce salivation with some anesthetics.

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Drug Indication
Symptomatic treatment of severe sialorrhoea (chronic pathological drooling) in children and adolescents aged 3 years and older with chronic neurological disorders.
Seebri Breezhaler is indicated as a maintenance bronchodilator treatment to relieve symptoms in adult patients with chronic obstructive pulmonary disease (COPD).
Enurev Breezhaler is indicated as a maintenance bronchodilator treatment to relieve symptoms in adult patients with chronic obstructive pulmonary disease (COPD).
Tovanor Breezhaler is indicated as a maintenance bronchodilator treatment to relieve symptoms in adult patients with chronic obstructive pulmonary disease (COPD).
Treatment of hyperhidrosis
Treatment of sialorrhoea
Treatment of sialorrhoea
Chronic obstructive pulmonary disease

C19H28BRNO3

398.3345

397.125

596-51-0

Glycopyrrolate-d5 bromide;(R,R)-Glycopyrrolate;475468-09-8

11693

White to off-white solid powder

193 - 194.5ºC

1

4

5

24

424

0

VPNYRYCIDCJBOM-UHFFFAOYSA-M

InChI=1S/C19H28NO3.BrH/c1-20(2)13-12-17(14-20)23-18(21)19(22,16-10-6-7-11-16)15-8-4-3-5-9-15;/h3-5,8-9,16-17,22H,6-7,10-14H2,1-2H3;1H/q+1;/p-1

(1,1-dimethylpyrrolidin-1-ium-3-yl) 2-cyclopentyl-2-hydroxy-2-phenylacetate;bromide

2934.99.9001

Powder      -20°C    3 years

                     4°C     2 years

In solvent   -80°C    6 months

                  -20°C    1 month

Note: Please store this product in a sealed and protected environment, avoid exposure to moisture.

Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)

H2O : ~100 mg/mL (~251.05 mM)
DMSO : ~100 mg/mL (~251.05 mM)

Solubility in Formulation 1: ≥ 2.5 mg/mL (6.28 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL.
Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution.

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Solubility in Formulation 2: ≥ 2.5 mg/mL (6.28 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution.

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Solubility in Formulation 3: ≥ 2.5 mg/mL (6.28 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly.

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Solubility in Formulation 4: 50 mg/mL (125.52 mM) in PBS (add these co-solvents sequentially from left to right, and one by one), clear solution; with ultrasonication.

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 (Please use freshly prepared in vivo formulations for optimal results.)