Glycopyrronium is an anticholinergic agent indicated for topical treatment of primary axillary hyperhidrosis in adults and pediatric patients 9 years of age and older. The product is available as a pre-moistened cloth that should be apply no more frequently than once every 24 hours. Patients who apply the drug in the presence of high ambient temperature may be at increased risk for heat illness (e.g., hyperpyrexia, heat stroke). Instruct drug recipients to watch for a generalized lack of sweating when in hot or very warm environments, and to avoid use if not sweating in these conditions. Use of the drug should also be avoided in patients with medical conditions that may be exacerbated by the anticholinergic actions of glycopyrronium.
General Administration Information
For storage information, see the specific product information within the How Supplied section.
Route-Specific Administration
Topical Administration
Other Topical Formulations
Pre-moistened Cloth
-Apply to the underarm (axillary) areas only; do not use on other areas of the body. Clean and dry treatment area before application. Do not apply to broken skin or cover with occlusive dressing.
-Avoid contact with the periocular area. Temporary dilation of the pupils and blurred vision may occur if it comes in contact with the eyes.
-Tear open the pouch and remove the cloth.
-Unfold the cloth, and wipe it across the entire underarm once. Using the same cloth, wipe the other underarm once.
-Immediately discard the cloth in the household trash out of reach of children and others.
-Wash hands with soap and water.
Local adverse reactions experienced by recipients of glycopyrronium during clinical trials included erythema (2.4% to 17%), skin irritation (6.4% to 14.1%), pruritus (3.8% to 8.1%), contact dermatitis (3.8%), rash (3.8%), and xeroderma (2.2%).
Occurring in 16.9% to 24.2% of glycopyrronium recipients, xerostomia was the most frequently reported adverse reaction during clinical trials. Other gastrointestinal adverse reactions experienced by study patients included oropharyngeal pain (5.7%), pharyngitis (2.2% to 5.8%), dry throat (2.6%), and constipation (2.0%).
Ophthalmic adverse reactions reported by recipients of glycopyrronium during clinical trials included mydriasis (5.3% to 6.8%), blurred vision (3.5% to 6.7%), and xerophthalmia (2.4% to 2.9%).
During clinical trials, 3.5% to 4.2% of patients treated with glycopyrronium developed urinary retention. New onset urinary retention has also been reported during postmarketing use of the drug.
Headache (5%) and nasal dryness (2.6% to 3.6%) were reported by glycopyrronium recipients during clinical trials.
Glycopyrronium is contraindicated for use in patients with glaucoma because it produces mydriasis which can increase intraocular pressure.
The anticholinergic actions of glycopyrronium may exacerbate the dry eyes and mouth effects experienced by patients with Sjogren's syndrome; therefore, use of glycopyrronium is contraindicated in patients with Sjogren's syndrome. In addition, drug induced dry eyes may cause irritation for wearers of contact lenses. Use of lubricating drops may be necessary.
Glycopyrronium is contraindicated in patients with myasthenia gravis because the drug competes with the small amount of acetylcholine that has potential to act in the body.
The anticholinergic effects of glycopyrronium on the gastrointestinal tract may exacerbate some gastrointestinal disorders. For this reason, use of glycopyrronium is contraindicated in patients with paralytic ileus, severe ulcerative colitis, and toxic megacolon complicating ulcerative colitis.
Use of glycopyrronium is contraindicated in patients with unstable cardiovascular status due to hemorrhagic shock. Glycopyrronium, like other anticholinergic drugs, may cause tachycardia through its actions on the SA node; thereby increasing the oxygen demand on the heart. Caution is advised when using glycopyrronium in patients with pre-existing cardiac disease such as tachycardia, hypertension, coronary artery disease, cardiac arrhythmias, or congestive heart failure.
Glycopyrronium may cause transient blurred vision. Instruct patients to use caution when driving or operating machinery until they know how glycopyrronium affects them. In addition, consider the benefits and risks of administering glycopyrronium with other anticholinergic medications, since additive effects may occur.
Heat illness (i.e., hyperpyrexia, heat stroke) due to decreased sweating may occur in patients being treated with glycopyrronium. This condition can occur when the drug is administered in the presence of high environmental temperature (ambient temperature increase). Instruct drug recipients to watch for generalized lack of sweating when in hot or very warm temperatures, and to avoid use if not sweating in these conditions.
Caution is advised when prescribing glycopyrronium to patients with prostatic hypertrophy or bladder-neck obstruction (urinary tract obstruction). Treatment with glycopyrronium has been associated with new or worsening signs and symptoms of urinary retention (e.g., difficulty passing urine, distended bladder) in patients with and without a documented history of urinary retention. Instruct patients to immediately discontinue use of glycopyrronium and consult a physician if any signs or symptoms of urinary retention develop.
There are no human data regarding use of glycopyrronium during pregnancy. In animal studies, intravenous doses administered to maternal rabbits during organogenesis did not result in any adverse effect on embryo-fetal development. In rats, daily oral doses of 200 and 400 mg/kg/day administered during organogenesis were associated a significant reduction in mean fetal weight and minor skeletal effects. In addition, fetal resorption was observed in 2 litters exposed to maternal doses of 400 mg/kg/day. When deciding to use this drug during pregnancy, consider the potential benefits to the mother against the potential risks to the fetus.
According to the manufacturer, it is not known if glycopyrronium or its metabolites are excreted into breast milk. Drugs with anticholinergic properties, such as glycopyrronium, may suppress lactation, particularly when lactation is starting to be established. Consider the benefits of breast-feeding, the risk of potential infant drug exposure, and the risk of an untreated or inadequately treated condition. If a breast-feeding infant experiences an adverse effect related to a maternally applied drug, health care providers are encouraged to report the adverse effect to the FDA.
Cases of accidental ocular exposure resulting in mydriasis, anisocoria, and blurred vision have been reported during postmarketing use of glycopyrronium. These exposures occurred when children accessed wipes discarded in the trash or when patients touched the periocular area after using glycopyrronium. In most cases, symptoms resolved within 1 week. Strictly adhere to the recommended handwashing and disposal instruction to prevent accidental exposure to glycopyrronium.
For the treatment of primary axillary hyperhidrosis:
Topical dosage:
Adults: Wipe 1 pre-moistened cloth topically across the entire underarm area once. Using the same cloth, wipe the other underarm once. Note, a single cloth will be used for both underarms. Apply no more frequently than once every 24 hours.
Children and Adolescents 9 years and older: Wipe 1 pre-moistened cloth topically across the entire underarm area once. Using the same cloth, wipe the other underarm once. Note, a single cloth will be used for both underarms. Apply no more frequently than once every 24 hours.
Maximum Dosage Limits:
-Adults
1 application every 24 hours.
-Geriatric
1 application every 24 hours.
-Adolescents
1 application every 24 hours.
-Children
9 to 12 years: 1 application every 24 hours.
1 to 8 years: Safety and efficacy have not been established.
-Infants
Safety and efficacy have not been established.
-Neonates
Safety and efficacy have not been established.
Patients with Hepatic Impairment Dosing
Specific guidelines for dosage adjustments in hepatic impairment are not available; it appears that no dosage adjustments are needed.
Patients with Renal Impairment Dosing
Specific guidelines for dosage adjustments in renal impairment are not available; it appears that no dosage adjustments are needed.
*non-FDA-approved indication
Anticholinergics: (Moderate) Although glycopyrronium is minimally absorbed into the systemic circulation after topical application, there is the potential for glycopyrronium to have additive anticholinergic effects when administered with other antimuscarinics. Per the manufaturer, avoid concomitant administration of glycopyrronium with other anticholinergic medications.
Atropine: (Moderate) Although glycopyrronium is minimally absorbed into the systemic circulation after topical application, there is the potential for glycopyrronium to have additive anticholinergic effects when administered with other antimuscarinics. Per the manufaturer, avoid concomitant administration of glycopyrronium with other anticholinergic medications.
Atropine; Difenoxin: (Moderate) Although glycopyrronium is minimally absorbed into the systemic circulation after topical application, there is the potential for glycopyrronium to have additive anticholinergic effects when administered with other antimuscarinics. Per the manufaturer, avoid concomitant administration of glycopyrronium with other anticholinergic medications.
Belladonna; Opium: (Moderate) Although glycopyrronium is minimally absorbed into the systemic circulation after topical application, there is the potential for glycopyrronium to have additive anticholinergic effects when administered with other antimuscarinics. Per the manufaturer, avoid concomitant administration of glycopyrronium with other anticholinergic medications.
Benzoic Acid; Hyoscyamine; Methenamine; Methylene Blue; Phenyl Salicylate: (Moderate) Although glycopyrronium is minimally absorbed into the systemic circulation after topical application, there is the potential for glycopyrronium to have additive anticholinergic effects when administered with other antimuscarinics. Per the manufaturer, avoid concomitant administration of glycopyrronium with other anticholinergic medications.
Benztropine: (Moderate) Although glycopyrronium is minimally absorbed into the systemic circulation after topical application, there is the potential for glycopyrronium to have additive anticholinergic effects when administered with other antimuscarinics. Per the manufaturer, avoid concomitant administration of glycopyrronium with other anticholinergic medications.
Budesonide; Glycopyrrolate; Formoterol: (Moderate) Although glycopyrronium is minimally absorbed into the systemic circulation after topical application, there is the potential for glycopyrronium to have additive anticholinergic effects when administered with other antimuscarinics. Per the manufaturer, avoid concomitant administration of glycopyrronium with other anticholinergic medications.
Chlordiazepoxide; Clidinium: (Moderate) Although glycopyrronium is minimally absorbed into the systemic circulation after topical application, there is the potential for glycopyrronium to have additive anticholinergic effects when administered with other antimuscarinics. Per the manufaturer, avoid concomitant administration of glycopyrronium with other anticholinergic medications.
Dicyclomine: (Moderate) Although glycopyrronium is minimally absorbed into the systemic circulation after topical application, there is the potential for glycopyrronium to have additive anticholinergic effects when administered with other antimuscarinics. Per the manufaturer, avoid concomitant administration of glycopyrronium with other anticholinergic medications.
Diphenoxylate; Atropine: (Moderate) Although glycopyrronium is minimally absorbed into the systemic circulation after topical application, there is the potential for glycopyrronium to have additive anticholinergic effects when administered with other antimuscarinics. Per the manufaturer, avoid concomitant administration of glycopyrronium with other anticholinergic medications.
Flavoxate: (Moderate) Although glycopyrronium is minimally absorbed into the systemic circulation after topical application, there is the potential for glycopyrronium to have additive anticholinergic effects when administered with other antimuscarinics. Per the manufaturer, avoid concomitant administration of glycopyrronium with other anticholinergic medications.
Glycopyrrolate: (Moderate) Although glycopyrronium is minimally absorbed into the systemic circulation after topical application, there is the potential for glycopyrronium to have additive anticholinergic effects when administered with other antimuscarinics. Per the manufaturer, avoid concomitant administration of glycopyrronium with other anticholinergic medications.
Glycopyrrolate; Formoterol: (Moderate) Although glycopyrronium is minimally absorbed into the systemic circulation after topical application, there is the potential for glycopyrronium to have additive anticholinergic effects when administered with other antimuscarinics. Per the manufaturer, avoid concomitant administration of glycopyrronium with other anticholinergic medications.
Homatropine; Hydrocodone: (Moderate) Although glycopyrronium is minimally absorbed into the systemic circulation after topical application, there is the potential for glycopyrronium to have additive anticholinergic effects when administered with other antimuscarinics. Per the manufaturer, avoid concomitant administration of glycopyrronium with other anticholinergic medications.
Hyoscyamine: (Moderate) Although glycopyrronium is minimally absorbed into the systemic circulation after topical application, there is the potential for glycopyrronium to have additive anticholinergic effects when administered with other antimuscarinics. Per the manufaturer, avoid concomitant administration of glycopyrronium with other anticholinergic medications.
Hyoscyamine; Methenamine; Methylene Blue; Phenyl Salicylate; Sodium Biphosphate: (Moderate) Although glycopyrronium is minimally absorbed into the systemic circulation after topical application, there is the potential for glycopyrronium to have additive anticholinergic effects when administered with other antimuscarinics. Per the manufaturer, avoid concomitant administration of glycopyrronium with other anticholinergic medications.
Indacaterol; Glycopyrrolate: (Moderate) Although glycopyrronium is minimally absorbed into the systemic circulation after topical application, there is the potential for glycopyrronium to have additive anticholinergic effects when administered with other antimuscarinics. Per the manufaturer, avoid concomitant administration of glycopyrronium with other anticholinergic medications.
Ipratropium: (Moderate) Although ipratropium and glycopyrronium are minimally absorbed into the systemic circulation, there is the potential for additive anticholinergic effects if these drugs are administered together. Per the manufaturer, avoid concomitant administration of glycopyrronium with other anticholinergic medications.
Ipratropium; Albuterol: (Moderate) Although ipratropium and glycopyrronium are minimally absorbed into the systemic circulation, there is the potential for additive anticholinergic effects if these drugs are administered together. Per the manufaturer, avoid concomitant administration of glycopyrronium with other anticholinergic medications.
Methenamine; Sodium Acid Phosphate; Methylene Blue; Hyoscyamine: (Moderate) Although glycopyrronium is minimally absorbed into the systemic circulation after topical application, there is the potential for glycopyrronium to have additive anticholinergic effects when administered with other antimuscarinics. Per the manufaturer, avoid concomitant administration of glycopyrronium with other anticholinergic medications.
Methscopolamine: (Moderate) Although glycopyrronium is minimally absorbed into the systemic circulation after topical application, there is the potential for glycopyrronium to have additive anticholinergic effects when administered with other antimuscarinics. Per the manufaturer, avoid concomitant administration of glycopyrronium with other anticholinergic medications.
Neostigmine; Glycopyrrolate: (Moderate) Although glycopyrronium is minimally absorbed into the systemic circulation after topical application, there is the potential for glycopyrronium to have additive anticholinergic effects when administered with other antimuscarinics. Per the manufaturer, avoid concomitant administration of glycopyrronium with other anticholinergic medications.
Oxybutynin: (Moderate) Although glycopyrronium is minimally absorbed into the systemic circulation after topical application, there is the potential for glycopyrronium to have additive anticholinergic effects when administered with other antimuscarinics. Per the manufaturer, avoid concomitant administration of glycopyrronium with other anticholinergic medications.
Phenobarbital; Hyoscyamine; Atropine; Scopolamine: (Moderate) Although glycopyrronium is minimally absorbed into the systemic circulation after topical application, there is the potential for glycopyrronium to have additive anticholinergic effects when administered with other antimuscarinics. Per the manufaturer, avoid concomitant administration of glycopyrronium with other anticholinergic medications.
Propantheline: (Moderate) Although glycopyrronium is minimally absorbed into the systemic circulation after topical application, there is the potential for glycopyrronium to have additive anticholinergic effects when administered with other antimuscarinics. Per the manufaturer, avoid concomitant administration of glycopyrronium with other anticholinergic medications.
Scopolamine: (Moderate) Although glycopyrronium is minimally absorbed into the systemic circulation after topical application, there is the potential for glycopyrronium to have additive anticholinergic effects when administered with other antimuscarinics. Per the manufaturer, avoid concomitant administration of glycopyrronium with other anticholinergic medications.
Solifenacin: (Moderate) Although glycopyrronium is minimally absorbed into the systemic circulation after topical application, there is the potential for glycopyrronium to have additive anticholinergic effects when administered with other solfenacin. Per the manufaturer, avoid concomitant administration of glycopyrronium with other anticholinergic medications.
Tolterodine: (Moderate) Although glycopyrronium is minimally absorbed into the systemic circulation after topical application, there is the potential for glycopyrronium to have additive anticholinergic effects when administered with tolterodine. Per the manufaturer, avoid concomitant administration of glycopyrronium with other anticholinergic medications.
Trihexyphenidyl: (Moderate) Although glycopyrronium is minimally absorbed into the systemic circulation after topical application, there is the potential for glycopyrronium to have additive anticholinergic effects when administered with other antimuscarinics. Per the manufaturer, avoid concomitant administration of glycopyrronium with other anticholinergic medications.
Trospium: (Moderate) Although glycopyrronium is minimally absorbed into the systemic circulation after topical application, there is the potential for glycopyrronium to have additive anticholinergic effects when administered with trospium. Per the manufaturer, avoid concomitant administration of glycopyrronium with other anticholinergic medications.
Glycopyrronium is an anticholinergic agent that blocks acetylcholine receptors located on certain peripheral tissues, including sweat glands. Once apply topically, glycopyrronium competitively inhibits the action of acetylcholine on sweat glands, thereby reducing sweating. Glycopyrronium has a polar quaternary ammonium group that reduces its ability to cross membranes such as the blood-brain barrier. This group differentiates the drug from other anticholinergic agents, such as scopolamine hydrobromide and atropine sulfate, which are nonpolar amines and readily cross the blood-brain barrier.
Glycopyrronium is applied topically. Once in systemic circulation, glycopyrronium has a mean volume of distribution in children aged 1 to 14 years of approximately 1.3 to 1.8 L/kg, with a range from 0.7 to 3.9 L/kg. In adults aged 60 to 75 years, the volume of distribution is lower at 0.42 +/- 0.22 L/kg. Although a small portion of the drug appears to be metabolized, the metabolic pathway has not been established. Elimination occurs primarily through the kidneys, with 85% of the dose being excreted in the urine and less than 5% in bile drainage.
Affected Cytochrome P450 (CYP450) isoenzymes and drug transporters: None
-Route-Specific Pharmacokinetics
Topical Route
Following topical application of glycopyrronium to the axillae, maximum plasma concentration (0.08 +/- 0.04 ng/mL) was achieved within 1 hour (range, 0 to 10 hours). Systemic drugs exposures at 6 and 24 hours post dose were 0.2 +/- 0.14 ng x hour/L and 0.88 +/- 0.57 ng x hour/L, respectively. No evidence of drug accumulation was identified following daily doses to the axillae for 5 days.
-Special Populations
Renal Impairment
Pharmacokinetics of topically applied glycopyrronium in patients with renal dysfunction have not been studied; however, data are available from an intravenous glycopyrronium formulation. Following a 4 mcg/kg IV dose, the mean glycopyrronium exposure (10.5 mcg x hour/L), clearance (0.43 L/kg/hour), and 3-hour urinary excretion (0.7%) were significantly different in uremic subjects undergoing renal transplant surgery than in those of healthy subjects (3.73 mcg x hour/L, 1.14 L/kg/hour, and 50%, respectively).
Pediatrics
The pharmacokinetics of glycopyrronium in pediatric patients (aged 10 to 17 years) were similar to those observed in adults. Following topical application to the axillae, maximum plasma concentration (0.07 +/- 0.06 ng/mL) was achieved within 1.5 hour (range, 0 to 6 hours). Systemic drug exposure at 6 hours was 0.18 +/- 0.13 ng x hour/L. No evidence of drug accumulation was identified following daily doses to the axillae for 5 days.