Version May 2024
Note: Orally disintegrating tablet 1.7 mg = Regular tablet 2 mg.
Reduction of secretions (preoperative): IM: 4 mcg/kg 30 to 60 minutes before anesthesia or when the preanesthetic opioid and/or sedative are administered
Reversal of bradycardia, vagal reflexes (intraoperative): IV: 0.1 mg as a single dose; repeat as needed at 2- to 3-minute intervals
Reversal of muscarinic effects of cholinergic agents: IV: 0.2 mg for each 1 mg of neostigmine or 5 mg of pyridostigmine administered
Dosage adjustment for concomitant therapy: Significant drug interactions exist, requiring dose/frequency adjustment or avoidance. Consult drug interactions database for more information.
There are no specific dosage adjustments provided in the manufacturer's labeling; elimination is severely impaired in renal failure; use with caution; dosage adjustment may be necessary.
There are no specific dosage adjustments provided in the manufacturer's labeling; use with caution; consider dose reduction.
Refer to adult dosing. Use with caution; consider dose reduction.
(For additional information see "Glycopyrrolate (glycopyrronium) (systemic): Pediatric drug information")
Dosage guidance:
Safety: Dosing may be presented as mcg/kg or mg/dose; use extra caution.
Chronic drooling: Children ≥3 years and Adolescents ≤16 years: Oral solution (Cuvposa): 20 mcg/kg/dose 3 times daily; titrate in increments of 20 mcg/kg/dose every 5 to 7 days as tolerated to response up to a maximum dose of 100 mcg/kg/dose 3 times daily, not to exceed 1,500 to 3,000 mcg/dose.
Primary focal hyperhidrosis: Limited data available; optimal dose not established:
Children ≥8 years and Adolescents: Oral: Usual dose: 1 to 2 mg once or twice daily; titrate per response and tolerability; reported range: 0.5 to 6 mg per day in divided doses one to three times daily (Ref).
Reduction of respiratory secretions, palliative care: Limited data available: Children: Oral: 40 to 100 mcg/kg/dose every 4 to 8 hours (Ref).
Reduction of secretions, preoperative:
Infants and Children ≤2 years: IM: 4 to 9 mcg/kg as a single dose 30 to 60 minutes before procedure.
Children >2 years and Adolescents: IM: 4 mcg/kg as a single dose 30 to 60 minutes before procedure.
Reversal of bradycardia, vagal reflexes (intraoperative): Infants, Children, and Adolescents: IV: 4 mcg/kg/dose (maximum dose: 100 mcg/dose) at 2- to 3-minute intervals.
Reversal of muscarinic effects of cholinergic agents: Infants, Children, and Adolescents: IV: 0.2 mg for each 1 mg of neostigmine or 5 mg of pyridostigmine administered.
Dosage adjustment for concomitant therapy: Significant drug interactions exist, requiring dose/frequency adjustment or avoidance. Consult drug interactions database for more information.
There are no specific dosage adjustments provided in the manufacturer's labeling; elimination is severely impaired in renal failure; use with caution; dosage adjustment may be necessary.
There are no specific dosage adjustments provided in the manufacturer's labeling (has not been studied); use with caution.
Anticholinergic agents, including systemic glycopyrrolate, may cause reversible, dose-dependent anticholinergic effects, including, but not limited to, CNS effects (eg, behavioral changes [eg, irritability, agitation, dizziness, headache]); genitourinary effects (eg, urinary retention); GI effects (eg, xerostomia, constipation, gastrointestinal pseudo-obstruction); ophthalmic effects (eg, blurred vision, mydriasis); cardiovascular effects (eg, palpitations); and dermatologic effects (eg, hypohidrosis) in adult and pediatric patients (Ref). Xerostomia is the most frequent adverse reaction resulting in discontinuation (Ref).
Mechanism: Dose-related; an extension of antimuscarinic pharmacological properties (Ref).
Risk factors:
• Higher doses (Ref)
• Concurrent use of other anticholinergic medications
• Older age
Various GI effects may occur with systemic glycopyrrolate, including xerostomia, constipation, and gastrointestinal pseudo-obstruction in adult and pediatric patients (Ref). Diarrhea may be an early sign of incomplete intestinal obstruction, especially in patients with an ileostomy or colostomy.
Mechanism: Dose-related; an extension of antimuscarinic pharmacological properties (Ref).
Risk factors:
• Mechanical GI obstructive diseases (contraindicated)
• GI motility disorders (contraindicated)
• Concurrent use of medications that affect GI peristalsis
Anticholinergic agents, including systemic glycopyrrolate, may cause hypohidrosis, which may result in life-threatening hyperthermia or heatstroke (Ref).
Mechanism: Dose-related; related to the pharmacologic action. Antagonism of central and peripheral muscarinic receptors results in increased heat production due to increased muscle activity and impaired sweat gland function (Ref).
Risk factors:
• Physical exertion in high ambient temperature and humidity (Ref)
• Concurrent use of other anticholinergic medications (Ref)
• Children and older adults
The following adverse drug reactions and incidences are derived from product labeling unless otherwise specified. Incidences reported with oral use of glycopyrrolate in children and adolescents.
>10%:
Cardiovascular: Flushing (30%)
Gastrointestinal: Constipation (35%) (table 1), vomiting (40%), xerostomia (40%) (table 2)
|
Drug (Glycopyrrolate) |
Placebo |
Population |
Dose |
Dosage Form |
Indication |
Number of Patients (Glycopyrrolate) |
Number of Patients (Placebo) |
|---|---|---|---|---|---|---|---|
|
35% |
22% |
Pediatric patients 3 to 16 years |
20 mcg/kg/dose 3 times daily, titrate in increments of 20 mcg/kg/dose every 5 to 7 days up to a maximum dose of 100 mcg/kg/dose 3 times daily |
Oral solution |
Chronic drooling |
20 |
18 |
|
Drug (Glycopyrrolate) |
Placebo |
Population |
Dose |
Dosage Form |
Indication |
Number of Patients (Glycopyrrolate) |
Number of Patients (Placebo) |
|---|---|---|---|---|---|---|---|
|
40% |
11% |
Pediatric patients 3 to 16 years |
20 mcg/kg/dose 3 times daily, titrate in increments of 20 mcg/kg/dose every 5 to 7 days up to a maximum dose of 100 mcg/kg/dose 3 times daily |
Oral solution |
Chronic drooling |
20 |
18 |
Genitourinary: Urinary retention (15%) (table 3)
|
Drug (Glycopyrrolate) |
Placebo |
Population |
Dose |
Dosage Form |
Indication |
Number of Patients (Glycopyrrolate) |
Number of Patients (Placebo) |
|---|---|---|---|---|---|---|---|
|
15% |
0% |
Pediatric patients 3 to 16 years |
20 mcg/kg/dose 3 times daily, titrate in increments of 20 mcg/kg/dose every 5 to 7 days up to a maximum dose of 100 mcg/kg/dose 3 times daily |
Oral solution |
Chronic drooling |
20 |
18 |
Nervous system: Headache (15%) (table 4)
|
Drug (Glycopyrrolate) |
Placebo |
Population |
Dose |
Dosage Form |
Indication |
Number of Patients (Glycopyrrolate) |
Number of Patients (Placebo) |
|---|---|---|---|---|---|---|---|
|
15% |
6% |
Pediatric patients 3 to 16 years |
20 mcg/kg/dose 3 times daily, titrate in increments of 20 mcg/kg/dose every 5 to 7 days up to a maximum dose of 100 mcg/kg/dose 3 times daily |
Oral solution |
Chronic drooling |
20 |
18 |
Respiratory: Nasal congestion (30%), sinusitis (15%), upper respiratory tract infection (15%)
Postmarketing (all routes of administration and ages):
Cardiovascular: Cardiac arrhythmia (including bradycardia, ventricular fibrillation, ventricular tachycardia), hypertension, hypotension, palpitations (Cruddas 2017)
Dermatologic: Cheilosis (Eiland 2012)
Gastrointestinal: Ageusia, diarrhea (Eiland 2012), gastrointestinal pseudo-obstruction (Eiland 2012), halitosis (Eiland 2012)
Genitourinary: Lactation insufficiency (suppression)
Hypersensitivity: Facial swelling (Cruddas 2017)
Local: Injection-site reaction (including erythema at injection site, injection-site pruritus, localized edema, pain at injection site)
Nervous system: Agitation (Eiland 2012), behavioral changes (Eiland 2012), dizziness (Cruddas 2017), irritability (Eiland 2012), personality changes (Eiland 2012), seizure
Ophthalmic: Blurred vision (Cruddas 2017), mydriasis (Eiland 2012)
Respiratory: Epistaxis (Eiland 2012)
Miscellaneous: Fever (Chabicovsky 2019), malignant hyperthermia
Hypersensitivity to glycopyrrolate or any component of the formulation; medical conditions that preclude use of anticholinergic medication (eg, severe ulcerative colitis, toxic megacolon complicating ulcerative colitis, paralytic ileus, obstructive disease of GI tract [eg, achalasia, pyloroduodenal stenosis, strictures], bleeding GI ulcer, intestinal atony in older adult or debilitated patients, unstable cardiovascular status in acute hemorrhage, glaucoma, obstructive uropathy [eg, bladder neck obstruction due to prostatic hypertrophy], myasthenia gravis)
Oral solution: Additional contraindication: Concomitant use of potassium chloride in a solid oral dosage form.
Significant drug interactions exist, requiring dose/frequency adjustment or avoidance. Consult drug interactions database for more information.
Canadian labeling: Additional contraindications (not in US labeling): Injection: Use in newborns; chronic lung disease in older adult or debilitated patients.
Concerns related to adverse effects:
• CNS effects: May cause drowsiness and/or blurred vision, which may impair physical or mental abilities; patients must be cautioned about performing tasks which require mental alertness (eg, operating machinery or driving).
• GI transit: Slowing of GI muscular action can occur resulting in constipation or intestinal pseudo-obstruction. Constipation is a common dose-limiting adverse event. Intestinal pseudo-obstruction can result in abdominal distention, pain, nausea, or vomiting; discontinue if these symptoms develop or worsen during treatment.
• Heat prostration: May occur in the presence of fever, increased environmental temperature, and/or during physical exercise, particularly in children and the elderly; use caution in hot weather and/or exercise. Avoid exertion and high environmental temperature after administration.
• Mechanical obstruction (incomplete): Diarrhea may be an early sign of incomplete intestinal obstruction, especially in patients with an ileostomy or colostomy; avoid use in these patients. Discontinue treatment if incomplete mechanical intestinal obstruction is suspected or if diarrhea occurs.
Disease-related concerns:
• Cardiovascular disease: Use with caution in patients with coronary artery disease, arrhythmias, heart failure, hypertension, or tachycardia; evaluate tachycardia prior to administration.
• Hepatic impairment: Use with caution in patients with hepatic impairment; consider dosage reduction.
• Hiatal hernia: Use with caution in patients with hiatal hernia with reflux esophagitis; consider dosage reduction.
• Hyperthyroidism: Use with caution in patients with hyperthyroidism.
• Neuropathy: Use with caution in patients with autonomic neuropathy; consider dosage reduction.
• Prostatic hyperplasia/bladder neck obstruction: May worsen the symptoms (eg, urinary retention) of prostatic hyperplasia and/or bladder neck obstruction; use with caution; consider dosage reduction in patients with prostatic hypertrophy.
• Renal impairment: Use with caution in patients with renal impairment; elimination is severely impaired in renal failure; dosage adjustment may be necessary.
• Ulcerative colitis: Use with caution in patients with ulcerative colitis; large doses may suppress intestinal motility; consider dosage reduction; may precipitate/exacerbate an ileus or toxic megacolon. Use is contraindicated in patients with severe ulcerative colitis.
Special populations:
• Older adult: Use with caution in the elderly; increased risk for anticholinergic effects, confusion, and hallucinations; consider dosage reduction.
• Pediatric: Infants, patients with Down syndrome, and pediatric patients with spastic paralysis or brain damage may experience an increased response to anticholinergics, increasing the potential for adverse events. A paradoxical reaction characterized by hyperexcitability may occur in pediatric patients taking large doses. Infants and young children are especially susceptible to the toxic effects of anticholinergics.
Dosage form specific issues:
• Benzyl alcohol and derivatives: Some dosage forms may contain benzyl alcohol; large amounts of benzyl alcohol (≥99 mg/kg/day) have been associated with a potentially fatal toxicity (“gasping syndrome”) in neonates; the “gasping syndrome” consists of metabolic acidosis, respiratory distress, gasping respirations, CNS dysfunction (including convulsions, intracranial hemorrhage), hypotension and cardiovascular collapse (AAP ["Inactive" 1997]; CDC 1982); some data suggests that benzoate displaces bilirubin from protein binding sites (Ahlfors 2001); avoid or use dosage forms containing benzyl alcohol with caution in neonates. See manufacturer's labeling.
• Injection: Sensitivity of the eyes to light may occur. Protect eyes from light after administration.
• Propylene glycol: Some dosage forms may contain propylene glycol; large amounts are potentially toxic and have been associated hyperosmolality, lactic acidosis, seizures, and respiratory depression; use caution (AAP 1997; Zar 2007).
Some dosage forms may contain propylene glycol; in neonates large amounts of propylene glycol delivered orally, intravenously (eg, >3,000 mg/day), or topically have been associated with potentially fatal toxicities which can include metabolic acidosis, seizures, renal failure, and CNS depression; toxicities have also been reported in children and adults including hyperosmolality, lactic acidosis, seizures, and respiratory depression; use caution (AAP 1997; Shehab 2009).
Excipient information presented when available (limited, particularly for generics); consult specific product labeling. [DSC] = Discontinued product
Solution, Injection:
Glyrx-PF: 0.2 mg/mL (1 mL); 0.4 mg/2 mL (2 mL)
Generic: 0.2 mg/mL (1 mL, 2 mL); 0.4 mg/2 mL (2 mL); 1 mg/5 mL (5 mL); 4 mg/20 mL (20 mL)
Solution, Injection [preservative free]:
Generic: 0.2 mg/mL (1 mL); 0.4 mg/2 mL (2 mL)
Solution, Oral:
Cuvposa: 1 mg/5 mL (473 mL) [contains methylparaben, propylene glycol, propylparaben, saccharin sodium; cherry flavor]
Generic: 1 mg/5 mL (473 mL)
Solution Prefilled Syringe, Injection [preservative free]:
Glyrx-PF: 0.6 mg/3 mL (3 mL); 1 mg/5 mL (5 mL)
Generic: 0.2 mg/mL (1 mL); 0.4 mg/2 mL (2 mL); 0.6 mg/3 mL (3 mL)
Tablet, Oral:
Glycate: 1.5 mg [DSC]
Glycate: 1.5 mg [dye free]
Robinul: 1 mg [scored; dye free]
Robinul-Forte: 2 mg [scored; dye free]
Generic: 1 mg, 1.5 mg, 2 mg
Tablet Disintegrating, Oral:
Dartisla ODT: 1.7 mg [DSC] [contains gelatin (fish)]
May be product dependent
Solution (Cuvposa Oral)
1 mg/5 mL (per mL): $1.27
Solution (Glycopyrrolate Injection)
0.2 mg/mL (per mL): $0.84 - $16.25
0.4 mg/2 mL (per mL): $2.40 - $14.38
1 mg/5 mL (per mL): $0.66 - $11.00
4 mg/20 mL (per mL): $1.44 - $8.93
Solution (Glycopyrrolate Oral)
1 mg/5 mL (per mL): $0.96 - $1.14
Solution (Glyrx-PF Injection)
0.2 mg/mL (per mL): $4.56
0.4 mg/2 mL (per mL): $3.96
Solution Prefilled Syringe (Glycopyrrolate PF Injection)
0.2 mg/mL (per mL): $8.38 - $8.50
0.4 mg/2 mL (per mL): $8.33
0.6 mg/3 mL (per mL): $6.11
Solution Prefilled Syringe (Glyrx-PF Injection)
0.6 mg/3 mL (per mL): $4.00
1 mg/5 mL (per mL): $3.84
Tablets (Glycate Oral)
1.5 mg (per each): $19.90
Tablets (Glycopyrrolate Oral)
1 mg (per each): $1.06 - $1.31
1.5 mg (per each): $39.80
2 mg (per each): $1.76 - $2.20
Tablets (Robinul Oral)
1 mg (per each): $11.80
Tablets (Robinul-Forte Oral)
2 mg (per each): $18.01
Disclaimer: A representative AWP (Average Wholesale Price) price or price range is provided as reference price only. A range is provided when more than one manufacturer's AWP price is available and uses the low and high price reported by the manufacturers to determine the range. The pricing data should be used for benchmarking purposes only, and as such should not be used alone to set or adjudicate any prices for reimbursement or purchasing functions or considered to be an exact price for a single product and/or manufacturer. Medi-Span expressly disclaims all warranties of any kind or nature, whether express or implied, and assumes no liability with respect to accuracy of price or price range data published in its solutions. In no event shall Medi-Span be liable for special, indirect, incidental, or consequential damages arising from use of price or price range data. Pricing data is updated monthly.
Excipient information presented when available (limited, particularly for generics); consult specific product labeling.
Solution, Injection:
Generic: 0.2 mg/mL (1 mL, 2 mL, 20 mL); 0.4 mg/2 mL (2 mL); 4 mg/20 mL (20 mL)
Solution, Oral:
Cuvposa: 1 mg/5 mL (473 mL) [contains methylparaben, propylene glycol, propylparaben, saccharin sodium, sorbitol]
IM: May administer undiluted.
IV: May be administered IV without dilution or may dilute in a compatible solution. In perioperative setting, usually administered over 1 to 2 minutes (eg, in adults: 0.2 mg over 1 to 2 minutes). May also be administered via the tubing of a running IV infusion of a NS. May be administered IV in the same syringe with neostigmine or pyridostigmine for reversal of neuromuscular blockade.
Oral:
Orally disintegrating tablet: Administer at least 1 hour before or 2 hours after food. Remove tablet from blister packaging immediately prior to administration; do not push tablet through foil. Place tablet on tongue and allow to disintegrate then swallow without water. Tablets should not be broken or cut.
Oral solution: Administer 1 hour before or 2 hours after meals. Measure oral solution with an accurate measuring device (eg, dosing cup, oral syringe).
SUBQ (off-label route): May administer SUBQ (Ref).
Oral:
Tablets: Administer without regard to meals.
Oral solution: Administer on an empty stomach, 1 hour before or 2 hours after meals; measure with an accurate measuring device (eg, dosing cup, oral syringe).
Parenteral: May be administered IM (undiluted) or by slow IV injection (with or without dilution in a compatible fluid); in perioperative setting, usually administered over 1 to 2 minutes (eg, in adults: 0.2 mg over 1 to 2 minutes). May also be administered via the tubing of a running IV infusion of NS. May be administered IV in the same syringe with neostigmine or pyridostigmine for reversal of neuromuscular blockade.
Chronic drooling (Cuvposa only): To reduce chronic, severe drooling in pediatric patients 3 to 16 years with neurologic conditions (eg, cerebral palsy) associated with problem drooling
Reduction of secretions (injection only): To reduce salivary, tracheobronchial, and pharyngeal secretions and to reduce the volume and acidity of gastric secretions during induction of anesthesia and intubation
Reversal of bradycardia, vagal reflexes (injection only): To block cardiac vagal inhibitory reflexes during induction of anesthesia and intubation; intraoperatively to counteract surgically or drug-induced or vagal reflexes associated arrhythmias
Reversal of muscarinic effects of cholinergic agents (injection only): Protects against the peripheral muscarinic effects (eg, bradycardia, excessive secretions) of cholinergic agents (eg, neostigmine, pyridostigmine) given to reverse the neuromuscular blockade due to non-depolarizing muscle relaxants
Reduction of secretions at end of life (death rattle); Primary focal hyperhidrosis
Robinul [US and multiple international markets] may be confused with Reminyl brand name for galantamine [Canada and multiple international markets]
None known.
Note: Interacting drugs may not be individually listed below if they are part of a group interaction (eg, individual drugs within “CYP3A4 Inducers [Strong]” are NOT listed). For a complete list of drug interactions by individual drug name and detailed management recommendations, use the Lexicomp drug interactions program by clicking on the “Launch drug interactions program” link above.
Acetylcholinesterase Inhibitors: May diminish the therapeutic effect of Anticholinergic Agents. Anticholinergic Agents may diminish the therapeutic effect of Acetylcholinesterase Inhibitors. Risk C: Monitor therapy
Aclidinium: May enhance the anticholinergic effect of Anticholinergic Agents. Risk X: Avoid combination
Amantadine: May enhance the anticholinergic effect of Glycopyrrolate (Systemic). Risk C: Monitor therapy
Anticholinergic Agents: May enhance the adverse/toxic effect of other Anticholinergic Agents. Risk C: Monitor therapy
Atenolol: Glycopyrrolate (Systemic) may increase the serum concentration of Atenolol. Risk C: Monitor therapy
Botulinum Toxin-Containing Products: May enhance the anticholinergic effect of Anticholinergic Agents. Risk C: Monitor therapy
Cannabinoid-Containing Products: Anticholinergic Agents may enhance the tachycardic effect of Cannabinoid-Containing Products. Risk C: Monitor therapy
Chloral Betaine: May enhance the adverse/toxic effect of Anticholinergic Agents. Risk C: Monitor therapy
Chlorprothixene: Anticholinergic Agents may enhance the anticholinergic effect of Chlorprothixene. Risk C: Monitor therapy
Cimetropium: Anticholinergic Agents may enhance the anticholinergic effect of Cimetropium. Risk X: Avoid combination
CloZAPine: Anticholinergic Agents may enhance the constipating effect of CloZAPine. Management: Consider alternatives to this combination whenever possible. If combined, monitor closely for signs and symptoms of gastrointestinal hypomotility and consider prophylactic laxative treatment. Risk D: Consider therapy modification
Digoxin: Glycopyrrolate (Systemic) may increase the serum concentration of Digoxin. Risk C: Monitor therapy
Eluxadoline: Anticholinergic Agents may enhance the constipating effect of Eluxadoline. Risk X: Avoid combination
Gastrointestinal Agents (Prokinetic): Anticholinergic Agents may diminish the therapeutic effect of Gastrointestinal Agents (Prokinetic). Risk C: Monitor therapy
Glucagon: Anticholinergic Agents may enhance the adverse/toxic effect of Glucagon. Specifically, the risk of gastrointestinal adverse effects may be increased. Risk C: Monitor therapy
Glycopyrrolate (Oral Inhalation): Anticholinergic Agents may enhance the anticholinergic effect of Glycopyrrolate (Oral Inhalation). Risk X: Avoid combination
Glycopyrronium (Topical): May enhance the anticholinergic effect of Anticholinergic Agents. Risk X: Avoid combination
Haloperidol: Glycopyrrolate (Systemic) may decrease the serum concentration of Haloperidol. Management: Consider avoiding concurrent use of glycopyrrolate and haloperidol.Monitor patients closely for signs/symptoms of reduced clinical response to haloperidol if concurrent use with glycopyrrolate is required. Risk D: Consider therapy modification
Ipratropium (Oral Inhalation): May enhance the anticholinergic effect of Anticholinergic Agents. Risk X: Avoid combination
Itopride: Anticholinergic Agents may diminish the therapeutic effect of Itopride. Risk C: Monitor therapy
Levodopa-Foslevodopa: Glycopyrrolate (Systemic) may decrease the serum concentration of Levodopa-Foslevodopa. Risk C: Monitor therapy
Levosulpiride: Anticholinergic Agents may diminish the therapeutic effect of Levosulpiride. Risk X: Avoid combination
MetFORMIN: Glycopyrrolate (Systemic) may increase the serum concentration of MetFORMIN. Risk C: Monitor therapy
Mianserin: May enhance the anticholinergic effect of Anticholinergic Agents. Risk C: Monitor therapy
Mirabegron: Anticholinergic Agents may enhance the adverse/toxic effect of Mirabegron. Risk C: Monitor therapy
Nitroglycerin: Anticholinergic Agents may decrease the absorption of Nitroglycerin. Specifically, anticholinergic agents may decrease the dissolution of sublingual nitroglycerin tablets, possibly impairing or slowing nitroglycerin absorption. Risk C: Monitor therapy
Opioid Agonists: Anticholinergic Agents may enhance the adverse/toxic effect of Opioid Agonists. Specifically, the risk for constipation and urinary retention may be increased with this combination. Risk C: Monitor therapy
Oxatomide: May enhance the anticholinergic effect of Anticholinergic Agents. Risk X: Avoid combination
Potassium Chloride: Anticholinergic Agents may enhance the ulcerogenic effect of Potassium Chloride. Management: Patients on drugs with substantial anticholinergic effects should avoid using any solid oral dosage form of potassium chloride. Risk X: Avoid combination
Potassium Citrate: Anticholinergic Agents may enhance the ulcerogenic effect of Potassium Citrate. Management: Patients on drugs with substantial anticholinergic effects should avoid using any solid oral dosage form of potassium citrate. Risk X: Avoid combination
Pramlintide: May enhance the anticholinergic effect of Anticholinergic Agents. These effects are specific to the GI tract. Risk X: Avoid combination
Ramosetron: Anticholinergic Agents may enhance the constipating effect of Ramosetron. Risk C: Monitor therapy
Revefenacin: Anticholinergic Agents may enhance the anticholinergic effect of Revefenacin. Risk X: Avoid combination
Rivastigmine: Anticholinergic Agents may diminish the therapeutic effect of Rivastigmine. Rivastigmine may diminish the therapeutic effect of Anticholinergic Agents. Management: Use of rivastigmine with an anticholinergic agent is not recommended unless clinically necessary. If the combination is necessary, monitor for reduced anticholinergic effects. Risk D: Consider therapy modification
Secretin: Anticholinergic Agents may diminish the therapeutic effect of Secretin. Management: Avoid concomitant use of anticholinergic agents and secretin. Discontinue anticholinergic agents at least 5 half-lives prior to administration of secretin. Risk D: Consider therapy modification
Thiazide and Thiazide-Like Diuretics: Anticholinergic Agents may increase the serum concentration of Thiazide and Thiazide-Like Diuretics. Risk C: Monitor therapy
Tiotropium: Anticholinergic Agents may enhance the anticholinergic effect of Tiotropium. Risk X: Avoid combination
Topiramate: Anticholinergic Agents may enhance the adverse/toxic effect of Topiramate. Risk C: Monitor therapy
Umeclidinium: May enhance the anticholinergic effect of Anticholinergic Agents. Risk X: Avoid combination
Administration with a high-fat meal significantly reduced absorption. Management: Administer at least 1 hour before or 2 hours after meals.
When given as a single maternal injection prior to delivery, glycopyrrolate was not found to cross the placenta in significant amounts. In addition, fetal heart rate, fetal heart rate variability, and Apgar scores were not significantly affected (Abboud 1981; Abboud 1983; Ali-Melkkilä 1990; Ure 1999).
Use of topical glycopyrrolate for the treatment of hyperhidrosis in a pregnant patient diagnosed with herpetic neuralgia has been described in a case report (Ladjevic 2009).
It is not known if glycopyrrolate is present in breast milk.
According to the manufacturer, the decision to breastfeed during therapy should consider the risk of infant exposure, the benefits of breastfeeding to the infant, and benefits of treatment to the mother. Glycopyrrolate is an anticholinergic and may suppress lactation.
Heart rate; anticholinergic effects; bowel sounds; bowel movements; effects on drooling
Blocks the action of acetylcholine at parasympathetic sites in smooth muscle, secretory glands, and the CNS; indirectly reduces the rate of salivation by preventing the stimulation of acetylcholine receptors
Onset of action: IM: 15 to 30 minutes; IV: Within 1 minute.
Peak effect: IM: Within ~30 to 45 minutes.
Duration: Vagal effect: 2 to 3 hours; Inhibition of salivation: Up to 7 hours; Parenteral: 7 hours.
Absorption: Oral tablet: Poor (~3%); variable and erratic; Oral solution: 23% lower compared to tablet; high-fat meal markedly reduces the oral bioavailability.
Distribution: Vd: IV: Children and Adolescents ≤14 years: 1.3 to 1.8 L/kg (range: 0.7 to 3.9 L/kg); Adults: 0.42 ± 0.22 L/kg.
Bioavailability: Tablet: 3%.
Half-life elimination: IV: Infants: 21.6 to 130 minutes; Children: 19.2 to 99.2 minutes; IM: Adults: 0.55 to 1.25 hours; IV: 0.83 ± 0.27 hour; Oral solution: Adults: 3 hours; Orally disintegrating tablet: Adults: 2.8 hours.
Time to peak, plasma: IM: ~30 minutes; Oral solution: 3.1 hours; Orally disintegrating tablet: Median: 3 hours.
Excretion: Urine (as unchanged drug, IM: >80%, IV: 85%); bile (as unchanged drug, <5%).
Clearance: Children and Adolescents ≤14 years: Mean range: 1.01 to 1.41 L/kg/hour (range: 0.32 to 2.22 L/kg/hour); Adults: 0.54 ± 0.14 L/kg/hour.
Altered kidney function: Elimination is severely impaired in patients with renal failure.
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