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Glycopyrronium

Class: Skin and Mucous Membrane Agents, Miscellaneous
Chemical Name: [(3R)-1,1-dimethylpyrrolidin-1-ium-3-yl] (2S)-2-cyclopentyl-2-hydroxy-2-phenylacetate;[(3S)-1,1-dimethylpyrrolidin-1-ium-3-yl] (2R)-2-cyclopentyl-2-hydroxy-2-phenylacetate
Molecular Formula: C38H56N2O6+2
Brands: Qbrexza

Medically reviewed by Drugs.com. Last updated on Aug 17, 2020.

Introduction

Glycopyrronium tosylate is a skin or mucous membrane agent.

Uses for Glycopyrronium

Glycopyrronium tosylate has the following uses:

Glycopyrronium tosylate is an anticholinergic indicated for topical treatment of primary axillary hyperhidrosis in adults and pediatric patients 9 years of age and older.1

Glycopyrronium Dosage and Administration

General

Glycopyrronium tosylate is available in the following dosage form(s) and strength(s):

Cloth: Single-use cloth pre-moistened with 2.4% glycopyrronium solution.1

Dosage

It is essential that the manufacturer's labeling be consulted for more detailed information on dosage and administration of this drug. Dosage summary:

  • Glycopyrronium tosylate is for topical use in the underarm area only and not for use in other body areas.1

  • Wash hands immediately with soap and water after applying and discarding the glycopyrronium tosylate cloth. Glycopyrronium tosylate may cause temporary dilation of the pupils and blurred vision if it comes in contact with the eyes. Avoid transfer of glycopyrronium tosylate to the periocular area.1

  • Do not apply glycopyrronium tosylate to broken skin. Avoid using glycopyrronium tosylate with occlusive dressings.1

Pediatric Patients

Children 9 years of age and older: Glycopyrronium tosylate should be applied to clean dry skin on the underarm areas once daily. Glycopyrronium tosylate should not be used more frequently than once every 24 hours.1

Tear open the pouch and pull out the cloth, unfold the cloth, and wipe it across one entire underarm once. Using the same cloth, wipe the other underarm once. A single cloth should be used to apply glycopyrronium tosylate to both underarms.1

Adults

Glycopyrronium tosylate should be applied to clean dry skin on the underarm areas once daily. Glycopyrronium tosylate should not be used more frequently than once every 24 hours.1

Tear open the pouch and pull out the cloth, unfold the cloth, and wipe it across one entire underarm once. Using the same cloth, wipe the other underarm once. A single cloth should be used to apply glycopyrronium tosylate to both underarms.1

Cautions for Glycopyrronium

Contraindications

Glycopyrronium tosylate is contraindicated in patients with medical conditions that can be exacerbated by the anticholinergic effect of glycopyrronium tosylate (e.g., glaucoma, paralytic ileus, unstable cardiovascular status in acute hemorrhage, severe ulcerative colitis, toxic megacolon complicating ulcerative colitis, myasthenia gravis, Sjogren’s syndrome).1

Warnings/Precautions

Worsening of Urinary Retention

Glycopyrronium tosylate should be used with caution in patients with a history or presence of documented urinary retention. Prescribers and patients should be alert for signs and symptoms of urinary retention (e.g., difficulty passing urine, distended bladder), especially in patients with prostatic hypertrophy or bladder-neck obstruction. Instruct patients to discontinue use immediately and consult a physician should any of these signs or symptoms develop.1

Patients with a history of urinary retention were not included in the clinical studies.1

Control of Body Temperature

In the presence of high ambient temperature, heat illness (hyperpyrexia and heat stroke due to decreased sweating) can occur with the use of anticholinergic drugs such as glycopyrronium tosylate. Advise patients using glycopyrronium tosylate to watch for generalized lack of sweating when in hot or very warm environmental temperatures and to avoid use if not sweating under these conditions.1

Operating Machinery or an Automobile

Transient blurred vision may occur with use of glycopyrronium tosylate. If blurred vision occurs, the patient should discontinue use until symptoms resolve. Patients should be warned not to engage in activities that require clear vision, such as operating a motor vehicle or other machinery or performing hazardous work, until the symptoms have resolved.1

Specific Populations

Pregnancy

Risk Summary: There are no available data on glycopyrronium tosylate use in pregnant women to inform a drug-associated risk for adverse developmental outcomes. In pregnant rats, daily oral administration of glycopyrrolate (glycopyrronium bromide) during organogenesis did not result in an increased incidence of gross external or visceral defects. When glycopyrrolate was administered intravenously to pregnant rabbits during organogenesis, no adverse effects on embryo-fetal development were seen. The available data do not support relevant comparisons of systemic glycopyrronium exposures achieved in the animal studies to exposures observed in humans after topical use of glycopyrronium tosylate.1

The estimated background risks of major birth defects and miscarriage for the indicated population are unknown. In the U.S. general population, the estimated background risk of major birth defects and miscarriage in clinically recognized pregnancies is 2-4% and 15-20%, respectively.1

Animal Data: Glycopyrrolate was orally administered to pregnant rats at dosages of 50, 200, and 400 mg/kg/day during the period of organogenesis. Glycopyrrolate had no effect on maternal survival, but significantly reduced mean maternal body weight gain over the period of dosing at all dosages evaluated. Mean fetal weight was significantly reduced in the 200 and 400 mg/kg/day dose groups. There were two litters with all resorbed fetuses in the 400 mg/kg/day dose group. There were no effects of treatment on the incidence of gross external or visceral defects. Minor treatment-related skeletal effects included reduced ossification of various bones in the 200 and 400 mg/kg/day dose groups; these skeletal effects were likely secondary to maternal toxicity.1

Glycopyrrolate was intravenously administered to pregnant rabbits at dosages of 0.1, 0.5, and 1.0 mg/kg/day during the period of organogenesis. Glycopyrrolate did not affect maternal survival under the conditions of this study. Mean maternal body weight gain and mean food consumption over the period of dosing were lower than the corresponding control value in the 0.5 and 1.0 mg/kg/day treatment groups. There were no effects of treatment on fetal parameters, including fetal survival, mean fetal weight, and the incidence of external, visceral, or skeletal defects.1

Female rats that were pregnant or nursing were orally dosed with glycopyrrolate daily at dosages of 0, 50, 200, or 400 mg/kg/day, beginning on day 7 of gestation, and continuing until day 20 of lactation. Mean body weight of pups in all treatment groups was reduced compared to the control group during the period of nursing, but eventually recovered to be comparable to the control group, post-weaning. No other notable delivery or litter parameters were affected by treatment in any group, including no effects on mean duration of gestation or mean numbers of live pups per litter. No treatment-related effects on survival or adverse clinical signs were observed in pups. There were no effects of maternal treatment on behavior, learning, memory, or reproductive function of pups.1

Lactation

There are no data on the presence of glycopyrrolate or its metabolites in human milk, the effects on the breastfed infant, or the effects on milk production. The developmental and health benefits of breastfeeding should be considered along with the mother’s clinical need for glycopyrronium tosylate and any potential adverse effects on the breastfed infant from glycopyrronium tosylate or from the underlying maternal condition.1

Pediatric Use

The safety, effectiveness, and pharmacokinetics of glycopyrronium tosylate have been established in pediatric patients age 9 years and older for topical treatment of primary axillary hyperhidrosis. Use of glycopyrronium tosylate in this age group is supported by evidence from two multicenter, randomized, double-blind, parallel-group, vehicle-controlled 4-week trials which included 34 pediatric subjects 9 years and older.1

The safety and effectiveness of glycopyrronium tosylate have not been established in pediatric patients under 9 years of age.1

Geriatric Use

Clinical trials of glycopyrronium tosylate did not include sufficient numbers of subjects age 65 years and older to determine whether they respond differently from younger subjects.1

Renal Impairment

The elimination of glycopyrronium is severely impaired in patients with renal failure.1

Common Adverse Effects

Most common adverse reactions (incidence ≥2%) are dry mouth, mydriasis, oropharyngeal pain, headache, urinary hesitation, vision blurred, nasal dryness, dry throat, dry eye, dry skin, constipation. Local skin reactions, including erythema, burning/stinging and pruritus were also common (>5%).1

Drug Interactions

Specific Drugs

It is essential that the manufacturer's labeling be consulted for more detailed information on interactions with this drug, including possible dosage adjustments. Interaction highlights:

Coadministration of glycopyrronium tosylate with anticholinergic medications may result in additive interaction leading to an increase in anticholinergic adverse effects. Avoid coadministration of glycopyrronium tosylate with other anticholinergic-containing drugs.1

Actions

Mechanism of Action

Glycopyrronium is a competitive inhibitor of acetylcholine receptors that are located on certain peripheral tissues, including sweat glands. In hyperhidrosis, glycopyrronium inhibits the action of acetylcholine on sweat glands, reducing sweating.1

Advice to Patients

Patient Counseling Information

Advise the patient to read the FDA-approved patient labeling.1

Instruct patients to be alert for signs and symptoms of urinary retention (e.g., difficulty passing urine, distended bladder). Instruct patients to discontinue use and consult a physician immediately should any of these signs or symptoms develop.1

In the presence of high ambient temperature, heat illness due to decreased sweating can occur with the use of anticholinergic drugs such as glycopyrronium tosylate. Advise patients using glycopyrronium tosylate to watch for generalized lack of sweating when in hot or very warm environmental temperatures and to avoid use if not sweating under these conditions.1

Transient blurred vision may occur with glycopyrronium tosylate. If this occurs, instruct patients to contact their healthcare provider, discontinue use of glycopyrronium tosylate, and avoid operating a motor vehicle or other machinery, or performing hazardous work until symptoms resolve.1

It is important for patients to understand how to correctly apply glycopyrronium tosylate.1

Instruct patients to use one cloth to apply glycopyrronium tosylate to both axillae by wiping the cloth across one underarm one time.1 Using the same cloth, apply the medication to the other underarm one time.1

Inform patients that glycopyrronium tosylate can cause temporary dilation of the pupils and blurred vision if it comes in contact with the eyes.1

Instruct patients to wash their hands with soap and water immediately after discarding the used cloth.1

Remind patients not to apply glycopyrronium tosylate to other body areas or to broken skin. Instruct patients to avoid using glycopyrronium tosylate with occlusive dressings.1

Glycopyrronium tosylate is flammable; avoid use near heat or flame.1

Additional Information

AHFSfirstRelease. For additional information until a more detailed monograph is developed and published, the manufacturer's labeling should be consulted. It is essential that the manufacturer's labeling be consulted for more detailed information on usual uses, dosage and administration, cautions, precautions, contraindications, potential drug interactions, laboratory test interferences, and acute toxicity.

Preparations

Excipients in commercially available drug preparations may have clinically important effects in some individuals; consult specific product labeling for details.

Please refer to the ASHP Drug Shortages Resource Center for information on shortages of one or more of these preparations.

Glycopyrronium Tosylate

Routes

Dosage Forms

Strengths

Brand Names

Manufacturer

Topical

Cloth

2.4 g/100 g

Qbrexza

Dermira

AHFS Drug Information. © Copyright 2021, Selected Revisions August 27, 2018. American Society of Health-System Pharmacists, Inc., 4500 East-West Highway, Suite 900, Bethesda, Maryland 20814.

References

1. Dermira, Inc. Qbrexza (glycopyrronium) TOPICAL prescribing information. 2018 Aug. http://dailymed.nlm.nih.gov/dailymed/drugInfo.cfm?setid=6b985380-1256-4fb3-b89a-6df2c6a6d12e

Frequently asked questions