Glycopyrronium Tosylate (Monograph)

Brand name: Qbrexza
Drug class: Astringents

Medically reviewed by Drugs.com on May 10, 2024. Written by ASHP.

Introduction

Anticholinergic agent.

Uses for Glycopyrronium Tosylate

Primary Axillary Hyperhidrosis

Treatment of primary axillary hyperhidrosis.

May be considered for first-line therapy or for use in patients who have had an unsatisfactory response to antiperspirants containing aluminum or zirconium salts. Other second-line treatment options include botulinum toxin injections and microwave thermolysis. An adequate trial of such therapy usually is recommended before systemic oral drug therapy, local sweat gland ablation, or sympathectomy is considered.

Glycopyrronium Tosylate Dosage and Administration

Administration

Topical Administration

Apply topically using an absorbent polypropylene pad (cloth) that has been premoistened with a solution containing 2.4% glycopyrronium.

For topical external use only. Apply to clean dry skin in the axillary area only. Do not apply to other body areas or to broken skin. Do not cover treated areas with occlusive dressings.

May cause temporary mydriasis and blurred vision if contact with the eyes occurs; take care to avoid transferring solution to the periocular area.

Prior to application, tear open a pouch containing a single cloth premoistened with glycopyrronium 2.4% solution, pull out and unfold the cloth, then wipe it once across one entire axilla and then across the other axilla. Do not reuse the cloth.

Wash hands with soap and water immediately after applying solution and discarding the cloth.

Dosage

Available as glycopyrronium tosylate; concentration expressed in terms of glycopyrronium.

Pediatric Patients

Primary Axillary Hyperhidrosis

Topical

Pediatric patients ≥9 years of age: Wipe one cloth premoistened with glycopyrronium 2.4% solution across both axillae one time once daily.

Adults

Primary Axillary Hyperhidrosis

Topical

Wipe one cloth premoistened with glycopyrronium 2.4% solution across both axillae one time once daily.

Prescribing Limits

Pediatric Patients

Primary Axillary Hyperhidrosis

Topical

Pediatric patients ≥9 years of age: Do not apply more frequently than once every 24 hours.

Adults

Primary Axillary Hyperhidrosis

Topical

Do not apply more frequently than once every 24 hours.

Special Populations

No special population dosage recommendations.

Cautions for Glycopyrronium Tosylate

Contraindications

• Medical conditions potentially exacerbated by increased anticholinergic activity (e.g., glaucoma, paralytic ileus, unstable cardiovascular status in patients with acute hemorrhage, severe ulcerative colitis, toxic megacolon complicating ulcerative colitis, myasthenia gravis, Sjögren’s syndrome).

Warnings/Precautions

GU Disorders

Use with caution in patients with current or prior documented urinary retention. Be alert for manifestations of urinary retention (e.g., difficulty passing urine, distended bladder), especially in individuals with prostatic hyperplasia or bladder neck obstruction, and discontinue use immediately if such manifestations develop. Clinical trials did not include patients with a history of urinary retention.

Thermoregulatory Effects

At hot or very warm environmental temperatures, heat illness (e.g., hyperpyrexia, heat stroke) due to decreased sweating reported with use of anticholinergic drugs. Be alert for a generalized lack of sweating when exposed to such conditions. Advise patients to avoid use if not sweating in hot or very warm temperatures.

Ocular Effects

Transient blurred vision reported following topical application. Performance of activities requiring visual acuity (e.g., operating machinery, driving a motor vehicle, performing hazardous work) may be impaired. If blurred vision occurs, discontinue use until symptoms resolve.

Flammability

Qbrexza cloths premoistened with glycopyrronium tosylate solution are flammable; do not expose to excessive heat or flames.

Specific Populations

Pregnancy

No available data regarding topical glycopyrronium use in pregnant women by which to establish a drug-associated risk for adverse developmental outcomes.

No adverse embryofetal developmental effects observed with IV glycopyrrolate (glycopyrronium bromide) in rabbits. No increase in incidence of gross external or visceral defects observed with oral glycopyrrolate in rats. 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 2.4% solution.

Lactation

Not known whether topically administered glycopyrronium or its metabolites distribute into milk, affect breast-fed infants, or affect milk production.

Consider developmental and health benefits of breast-feeding along with the mother's clinical need for topical glycopyrronium and any potential adverse effects on the breast-fed infant from the drug or underlying maternal condition.

Pediatric Use

Safety and efficacy not established in pediatric patients <9 years of age. Use for topical treatment of primary axillary hyperhidrosis in pediatric patients ≥9 years of age supported by evidence from 2 clinical trials that included 34 pediatric patients ≥9 years of age.

Geriatric Use

Insufficient experience in patients ≥65 years of age to determine whether geriatric patients respond differently than younger individuals.

Renal Impairment

Elimination of IV glycopyrronium in patients with renal failure is severely impaired. Pharmacokinetics of topical glycopyrronium in patients with renal impairment not determined.

Common Adverse Effects

Topical therapy of primary axillary hyperhidrosis (≥2%): Dry mouth, mydriasis, oropharyngeal pain, headache, urinary hesitation, blurred vision, nasal dryness, dry throat, dry eye, dry skin, constipation. Adverse local effects (e.g., erythema, burning/stinging, pruritus) reported in >5% of patients.

Drug Interactions

Topical glycopyrronium not expected to induce CYP isoenzymes 1A2, 2B6, or 3A4 or inhibit CYP isoenzymes 1A2, 2B6, 2C8, 2C9, 2C19, 2D6, or 3A4.

Specific Drugs

Glycopyrronium Tosylate Pharmacokinetics

Absorption

Bioavailability

Following topical application to axillae once daily for 5 days, pharmacokinetic parameters are similar in adults and pediatric patients 10–17 years of age, with no evidence of drug accumulation; peak plasma concentrations average 0.07–0.08 ng/mL and are attained at a median of 1 hour in adults and 1.5 hours in pediatric patients. By comparison, mean plasma concentrations of 0.15–0.38 ng/mL achieved in adults receiving oral glycopyrrolate solution (initial dosage of 1 mg every 8 hours, increased in 1-mg increments every 5 days to a maximum dosage of 3 mg every 8 hours).

Distribution

Extent

Not known whether glycopyrronium or its metabolites distributed into milk.

Elimination

Metabolism

Metabolized to limited extent following IV administration; metabolic pathway not characterized.

Elimination Route

About 85% excreted in urine and <5% present in bile following IV administration after surgery for cholelithiasis; >80% of recovered drug was unchanged.

Special Populations

Hepatic impairment: Pharmacokinetics of glycopyrronium not determined.

Renal impairment: Pharmacokinetics of topical glycopyrronium not determined. Elimination of IV glycopyrronium is severely impaired in patients with renal failure.

Stability

Storage

Topical

Solution on Premoistened Cloth

20–25°C (may be exposed to 15–30°C). Flammable; keep away from heat or flame.

Actions

• Competitively inhibits the action of acetylcholine on structures innervated by postganglionic cholinergic nerves, including sweat glands.

• Exact cause of primary hyperhidrosis not fully established but thought to result from autonomic nervous system dysregulation leading to overstimulation of cholinergic receptors on the eccrine sweat glands. Glycopyrronium reduces rate of sweat secretion by inhibiting the action of acetylcholine on sweat glands.

Advice to Patients

• Advise patients to read the manufacturer's patient information.

• Advise patients to be alert for signs and symptoms of urinary retention (e.g., difficulty passing urine, distended bladder) and instruct them to discontinue use and consult a clinician immediately if such manifestations develop.

• Risk of heat illness; advise patients to be alert for generalized lack of sweating when in hot or very warm environments and to avoid use of glycopyrronium if they are not sweating under these conditions.

• Risk of transient blurred vision; advise patients to contact their clinician if blurred vision occurs and to discontinue use of the drug and avoid activities requiring visual acuity (e.g., driving, operating machinery, hazardous work) until the symptoms resolve.

• Instruct patients regarding appropriate use of topical glycopyrronium, including proper application of the drug using the premoistened cloths and using a single cloth to wipe across each underarm once. Importance of avoiding use of occlusive dressings on treated areas and of not applying the drug to broken skin or to areas other than the axillae; importance of avoiding contact with the eyes and of washing the hands with soap and water immediately after applying the solution and discarding the cloth.

• Advise patients that Qbrexza cloths premoistened with glycopyrronium tosylate solution are flammable and that the preparation should be kept away from excessive heat and flames.

• Importance of women informing clinicians if they are or plan to become pregnant or plan to breast-feed.

• Importance of informing clinicians of existing or contemplated concomitant therapy, including prescription and OTC drugs and dietary or herbal supplements, as well as any concomitant illnesses.

• Importance of informing patients of other important precautionary information. (See Cautions.)

Additional Information

The American Society of Health-System Pharmacists, Inc. represents that the information provided in the accompanying monograph was formulated with a reasonable standard of care, and in conformity with professional standards in the field. Readers are advised that decisions regarding use of drugs are complex medical decisions requiring the independent, informed decision of an appropriate health care professional, and that the information contained in the monograph is provided for informational purposes only. The manufacturer’s labeling should be consulted for more detailed information. The American Society of Health-System Pharmacists, Inc. does not endorse or recommend the use of any drug. The information contained in the monograph is not a substitute for medical care.

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.

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Frequently asked questions

• How do you use a Qbrexza cloth?

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