Glycopyrrolate (Systemic)

Excipient information presented when available (limited, particularly for generics); consult specific product labeling. [DSC] = Discontinued product

Solution, Injection:

Robinul: 0.2 mg/mL (1 mL); 0.4 mg/2 mL (2 mL); 1 mg/5 mL (5 mL); 4 mg/20 mL (20 mL) [contains benzyl alcohol]

Generic: 0.2 mg/mL (1 mL); 0.4 mg/2 mL (2 mL); 1 mg/5 mL (5 mL); 4 mg/20 mL (20 mL)

Solution, Oral:

Cuvposa: 1 mg/5 mL (473 mL) [contains methylparaben, propylene glycol, propylparaben, saccharin sodium; cherry flavor]

Solution Prefilled Syringe, Intravenous:

Generic: 0.4 mg/2 mL (2 mL [DSC])

Tablet, Oral:

Glycate: 1.5 mg [DSC] [dye free]

Robinul: 1 mg [scored]

Robinul-Forte: 2 mg [scored]

Generic: 1 mg, 2 mg

• Cuvposa
• Glycate [DSC]
• Robinul
• Robinul-Forte

AUC of IV is 10.6 mcg•h/L in renally impaired patients. Elimination is severely impaired in patients with renal failure with plasma clearance of IV lowering to 0.43 L/h/kg.

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 (Robinul injection only): To reduce salivary, tracheobronchial, and pharyngeal secretions preoperatively; to reduce the volume and free acidity of gastric secretions

Reversal of bradycardia, vagal reflexes (Robinul 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 (Robinul injection only): Protects against the peripheral muscarinic effects (eg, bradycardia and excessive secretions) of cholinergic agents such as neostigmine and pyridostigmine given to reverse the neuromuscular blockade due to non-depolarizing muscle relaxants

Chronic drooling: Children and Adolescents 3 to 16 years: Oral solution (Cuvposa): Initial: 0.02 mg/kg 3 times daily; titrate in increments of 0.02 mg/kg every 5 to 7 days as tolerated, up to a maximum dose of 0.1 mg/kg 3 times daily, not to exceed 3 mg/dose

Reduction of secretions (preoperative):

Infants and Children ≤2 years: IM: 4 to 9 mcg/kg 30 to 60 minutes before anesthesia or when the preanesthetic opioid and/or sedative are administered

Children >2 years and Adolescents: Refer to adult dosing

Reversal of bradycardia, vagal reflexes (intraoperative): Infants, Children, and Adolescents: IV: 4 mcg/kg/dose (maximum dose: 0.1 mg); repeat at 2- to 3-minute intervals as needed

Reversal of muscarinic effects of cholinergic agents: Infants, Children, and Adolescents: IV: Refer to adult dosing.

Control of secretions (chronic) (off-label use): Limited data available (Nelson 1996): Children:

Oral: 40 to 100 mcg/kg/dose 3 to 4 times daily

IM, IV: 4 to 10 mcg/kg/dose every 3 to 4 hours

There are no dosage adjustments provided in the manufacturer’s labeling; use with caution.

A 0.5 mg/mL oral suspension may be made with 1 mg tablets and a 1:1 mixture of Ora-Plus and either Ora-Sweet or Ora-Sweet SF. Crush thirty 1 mg tablets in a mortar and reduce to a fine powder. Prepare diluent by mixing 30 mL of Ora-Plus with 30 mL of either Ora-Sweet or Ora-Sweet SF and stir vigorously. Add 30 mL of diluent (via geometric dilution) to powder until smooth suspension is obtained. Transfer suspension to 60 mL amber bottle. Rinse contents of mortar into bottle with sufficient quantity of remaining diluent to obtain 60 mL (final volume). Label “shake well”. Stable at room temperature for 90 days. Due to bitter aftertaste, chocolate syrup may be administered prior to or mixed (1:1 v/v) with suspension immediately before administration (Cober 2011).

A 0.5 mg/mL oral solution can be made from tablets. Crush fifty 1 mg tablets in a mortar and reduce to a fine powder. Add enough distilled water to make about 90 mL, mix well. Transfer to a bottle, rinse mortar with water, and add a quantity of water sufficient to make 100 mL. Label “shake well” and “protect from light”. Stable at room temperature for 25 days (Gupta 2001).

A 0.1 mg/mL oral solution may be made using glycopyrrolate 0.2 mg/mL injection without preservatives. Withdraw 50 mL from vials with a needle and syringe, add to 50 mL of a 1:1 mixture of Ora-Sweet and Ora-Plus in a bottle. Label “shake well”, “protect from light,” and “refrigerate”. Stable refrigerated for 35 days (Landry 2005).

AbobotulinumtoxinA: Anticholinergic Agents may enhance the anticholinergic effect of AbobotulinumtoxinA. Monitor therapy

Acetylcholinesterase Inhibitors: Anticholinergic Agents may diminish the therapeutic effect of Acetylcholinesterase Inhibitors. Acetylcholinesterase Inhibitors may diminish the therapeutic effect of Anticholinergic Agents. Monitor therapy

Aclidinium: May enhance the anticholinergic effect of Anticholinergic Agents. Avoid combination

Amantadine: May enhance the anticholinergic effect of Glycopyrrolate (Systemic). Monitor therapy

Amifampridine: May diminish the anticholinergic effect of Anticholinergic Agents. Anticholinergic Agents may diminish the therapeutic effect of Amifampridine. Monitor therapy

Analgesics (Opioid): Anticholinergic Agents may enhance the adverse/toxic effect of Analgesics (Opioid). Specifically, the risk for constipation and urinary retention may be increased with this combination. Monitor therapy

Anticholinergic Agents: May enhance the adverse/toxic effect of other Anticholinergic Agents. Monitor therapy

Atenolol: Glycopyrrolate (Systemic) may increase the serum concentration of Atenolol. Monitor therapy

Cannabinoid-Containing Products: Anticholinergic Agents may enhance the tachycardic effect of Cannabinoid-Containing Products. Exceptions: Cannabidiol. Monitor therapy

Chloral Betaine: May enhance the adverse/toxic effect of Anticholinergic Agents. Monitor therapy

Cimetropium: Anticholinergic Agents may enhance the anticholinergic effect of Cimetropium. Avoid combination

Digoxin: Glycopyrrolate (Systemic) may increase the serum concentration of Digoxin. Monitor therapy

Eluxadoline: Anticholinergic Agents may enhance the constipating effect of Eluxadoline. Avoid combination

Gastrointestinal Agents (Prokinetic): Anticholinergic Agents may diminish the therapeutic effect of Gastrointestinal Agents (Prokinetic). Monitor therapy

Glucagon: Anticholinergic Agents may enhance the adverse/toxic effect of Glucagon. Specifically, the risk of gastrointestinal adverse effects may be increased. Avoid combination

Glycopyrrolate (Oral Inhalation): Anticholinergic Agents may enhance the anticholinergic effect of Glycopyrrolate (Oral Inhalation). Avoid combination

Haloperidol: Glycopyrrolate (Systemic) may decrease the serum concentration of Haloperidol. Management: Monitor patients closely for signs/symptoms of reduced clinical response to haloperidol if concurrent use with glycopyrrolate is required. When possible, consider avoiding concurrent use. Consider therapy modification

Ipratropium (Oral Inhalation): May enhance the anticholinergic effect of Anticholinergic Agents. Avoid combination

Itopride: Anticholinergic Agents may diminish the therapeutic effect of Itopride. Monitor therapy

Levodopa: Glycopyrrolate (Systemic) may decrease the serum concentration of Levodopa. Monitor therapy

Levosulpiride: Anticholinergic Agents may diminish the therapeutic effect of Levosulpiride. Avoid combination

MetFORMIN: Glycopyrrolate (Systemic) may increase the serum concentration of MetFORMIN. Monitor therapy

Mianserin: May enhance the anticholinergic effect of Anticholinergic Agents. Monitor therapy

Mirabegron: Anticholinergic Agents may enhance the adverse/toxic effect of Mirabegron. 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. Monitor therapy

OnabotulinumtoxinA: Anticholinergic Agents may enhance the anticholinergic effect of OnabotulinumtoxinA. Monitor therapy

Oxatomide: May enhance the anticholinergic effect of Anticholinergic Agents. Avoid combination

Potassium Chloride: Glycopyrrolate (Systemic) may enhance the adverse/toxic effect of Potassium Chloride. This is specific to solid oral dosage forms of potassium chloride. Avoid combination

Potassium Citrate: Anticholinergic Agents may enhance the ulcerogenic effect of Potassium Citrate. Avoid combination

Pramlintide: May enhance the anticholinergic effect of Anticholinergic Agents. These effects are specific to the GI tract. Consider therapy modification

Ramosetron: Anticholinergic Agents may enhance the constipating effect of Ramosetron. Monitor therapy

RimabotulinumtoxinB: Anticholinergic Agents may enhance the anticholinergic effect of RimabotulinumtoxinB. Monitor therapy

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. Consider therapy modification

Thiazide and Thiazide-Like Diuretics: Anticholinergic Agents may increase the serum concentration of Thiazide and Thiazide-Like Diuretics. Monitor therapy

Tiotropium: Anticholinergic Agents may enhance the anticholinergic effect of Tiotropium. Avoid combination

Topiramate: Anticholinergic Agents may enhance the adverse/toxic effect of Topiramate. Monitor therapy

Umeclidinium: May enhance the anticholinergic effect of Anticholinergic Agents. Avoid combination