Glycopyrrolate

Brand Name: Cuvposa, glycopyrronium, Robinul

Generic Name: Glycopyrrolate

Drug Class: Anesthetic Premedication Agents; Anticholinergic Agents

Glycopyrrolate is an anticholinergic that helps to control conditions such as peptic ulcers that involve excessive stomach acid production. The injectable form of glycopyrrolate is also used to reduce saliva, nasal, lung, and stomach secretions and to help control heart rate during surgery.

Glycopyrrolate is available under the following different brand names: Cuvposa, glycopyrronium, and Robinul.

Dosage Forms and Strengths

Tablets

• 1mg
• 1.5mg
• 2mg

Oral solution

• 1mg/5mL

Injectable solution

• 0.2mg/mL

Dosage Considerations – Should be Given as Follows:

Surgery

Preoperative reduction of saliva or intraoperative reduction of cholinergic effects

Adult

• Preoperative: 4mcg/kg intravenously/intramuscularly (IV/IM) 30-60 min before surgery 
• Intraoperative: 0.1 mg IV/IM; may repeat every 2-3 minutes

Pediatric

• Children 1 month to 2 years (preoperative): 4 mcg/kg intramuscularly (IM); may increase to 8 mcg/kg 
• Children older than 2 years: 4 mcg/kg IM

Administration

Preoperative: 30-60 min before surgery Intraoperative: May repeat every 2-3 minutes; not to exceed 0.1 mg

Neuromuscular Blockade Reversal

Prevention of muscarinic AEs:

• Adult: 0.2 mg intravenously (IV) per 1 mg of neostigmine or 5 mg of pyridostigmine administered
• Pediatric: 0.2 mg IV per 1 mg of neostigmine or 5 mg of pyridostigmine administered

Administration

Concurrently in same syringe or a few minutes before cholinergic agent

Drooling (Off-label)

• Adult: 0.1 mg/kg orally every 8-12 hours; not to exceed 8 mg/day
• FDA-approved for children with chronic, severe drooling associated with neurologic conditions (e.g., cerebral palsy)
• Children under 3 years: Safety and efficacy not established
• Children 3-16 years: 0.02 mg/kg orally every 8 hours initially; may increase by 0.02 mg/kg every 5-7 days if warranted, up to 0.1 mg/kg every 8 hours 
• Not to exceed 1.5-3 mg/dose (based on weight; see manufacturer's info)

Administration

Administer 1 hour before meals or 2 hours after meals High fat food reduces orally bioavailability

Control of Secretions, Pediatric (Off-label)

• 0.004-0.01 mg/kg intravenously/intramuscularly (IV/IM) every 6 hours
• 0.04-0.1 mg/kg orally every 6 hours

Side effects of glycopyrrolate include:

Abdominal bloating

• Anticholinergic symptoms (dilated pupils, increased body temperature, fast or irregular heart rate)
• Blurred vision
• Constipation

Dizziness Drowsiness

• Dry eyes
• Dry mouth
• Dry skin

Flushing (warmth, redness, or tingly feeling)

• Loss of visual focus
• Palpitations
• Sensitivity of eyes to light

Sinus pain Stuffy nose Vomiting Weakness

Serious side effects of glycopyrrolate include:

Decreased sweating Fast/irregular heartbeat Mental/mood changes (such as confusion, hallucinations, agitation, nervousness, unusual excitement) Difficulty urinating Decreased sexual ability

Postmarketing side effects of glycopyrrolate reported include:

• Skin swelling
• Paradoxical bronchospasm
• Difficulty speaking

This document does not contain all possible side effects and others may occur. Check with your physician for additional information about side effects.

If your doctor has directed you to use this medication, your doctor or pharmacist may already be aware of any possible drug interactions and may be monitoring you for them. Do not start, stop, or change the dosage of any medicine before checking with your doctor, health care provider or pharmacist first.

Glycopyrrolate has no known severe interactions with other drugs.

Serious Interactions of glycopyrrolate include:

• pramlintide

Glycopyrrolate has moderate interactions with at least 104 different drugs. Mild Interactions of glycopyrrolate include:

• desipramine/li>
• dimenhydrinate
• donepezil
• dosulepin
• galantamine
• lofepramine
• mianserin
• prochlorperazine
• promazine
• promethazine
• rimantadine
• tacrine
• thioridazine
• trazodone
• trifluoperazine

 This document does not contain all possible interactions. Therefore, before using this product, tell your doctor or pharmacist of all the products you use. Keep a list of all your medications with you, and share the list with your doctor and pharmacist. Check with your physician if you have health questions or concerns.

Warnings

This medication contains glycopyrrolate. Do not take Cuvposa, glycopyrronium, or Robinul if you are allergic to glycopyrrolate or any ingredients contained in this drug.

Keep out of reach of children. In case of overdose, get medical help or contact a Poison Control Center immediately.

Contraindications

Hypersensitivity to glycopyrrolate or other ingredients.

Medical conditions that preclude anticholinergic therapy (e.g., angle-closure glaucoma, obstructive uropathy, gastrointestinal (GI) obstruction, paralytic ileus, intestinal atony of elderly or debilitated patient; unstable cardiovascular status in acute hemorrhage; severe ulcerative colitis, toxic megacolon, myasthenia gravis, reflux esophagitis, hiatal hernia, mitral stenosis).

Concomitant use of solid oral dosage forms of potassium chloride

Effects of Drug Abuse

• No information available

Short-Term Effects

• See "What Are Side Effects Associated with Using Glycopyrrolate?"

Long-Term Effects

• See "What Are Side Effects Associated with Using Glycopyrrolate?"

Cautions

Use caution in patients with hepatic impairment.

May cause urinary retention and further complicate existing renal impairment; dose adjustment may be necessary.

Use caution in patients with hiatal hernia with reflux esophagitis.

May worsen symptoms of prostatic hyperplasia and/or bladder neck destruction (may increase urinary retention); use with caution.

Use caution in patients with autonomic neuropathy.

Use caution in patients with hyperthyroidism.

In ulcerative colitis, large doses may suppress intestinal motility and exacerbate an ileus or toxic magacolon; use is contraindicated in patients with ulcerative colitis.

May decrease gastrointestinal (GI) motility, which can result in constipation or intestinal pseudo-obstruction; intestinal pseudo-obstruction can result in abdominal distention, pain, nausea, or vomiting; if obstruction suspected, discontinue and evaluate.

Incomplete mechanical intestinal obstruction may present as diarrhea, especially in patients with an ileostomy or colostomy; discontinue treatment if incomplete mechanical intestinal obstruction is suspected or if diarrhea occurs.

May cause heat prostration in the presence of fever, high ambient temperature, physical exercise; to avoid heat prostration; use caution in hot weather and/or exercise.

May impair mental abilities to perform tasks that require mental alertness, including operating heavy machinery.

Parenteral product contains benzyl alcohol; generally avoid in neonates.

Pediatric patients with spastic paralysis may experience increased response to anticholinergics, increasing the potential for adverse effects; a paradoxical reaction characterized by hyperexcitability may occur in pediatric patients taking large doses; use caution.

May increase risk for anticholinergic effects, confusion, and hallucinations; use caution.

Pregnancy and Lactation

• Glycopyrrolate may be acceptable for use during pregnancy. Either animal studies show no risk but human studies are not available or animal studies showed minor risks and human studies were done and showed no risk.
• Glycopyrrolate's excretion in milk is unknown; use with caution if breastfeeding.