glycopyrrolate (Cuvposa, glycopyrronium, Robinul)
Classes: Anesthetic Premedication Agents; Anticholinergic Agents
Dosing and uses of Cuvposa, glycopyrronium (glycopyrrolate)
Adult dosage forms and strengths
tablets
- 1mg
- 1.5mg
- 2mg
oral solution
- 1mg/5mL
injectable solution
- 0.2mg/mL
Surgery
Preoperative reduction of saliva or intraoperative reduction of cholinergic effects
Preoperative: 4mcg/kg IV/IM 30-60 min before surgery
Intraoperative: 0.1 mg IV/IM; may repeat q2-3min
Neuromuscular Blockade Reversal
Prevention of muscarinic AEs
0.2 mg IV per1 mg of neostigmine or 5 mg of pyridostigmine administered
Administration
- Concurrently in same syringe or a few minutes before cholinergic agent
Drooling (Off-label)
0.1 mg/kg PO q8-12hr; not to exceed 8 mg/day
Frey Syndrome (Orphan)
Orphan indication sponsor
- Wellesley Therapeutics, Inc; 200 Gerrard St., East Toronto, Ontario M5A 2E6; Canada
Pediatric dosage forms and strengths
tablets
- 1mg
- 2mg
injectable solution
- 0.2mg/mL
oral solution
- 1mg/5mL
Surgery
Preoperative reduction of saliva or intraoperative reduction of cholinergic effects
1 month to 2 years (preoperative): 4 mcg/kg IM; may increase to 8 mcg/kg
>2 years: 4 mcg/kg Im
Administration
- Preoperative: 30-60 min before surgery
- Intraoperative: May repeat q2-3min; not to exceed 0.1 mg
Drooling
FDA-approved for children with chronic, severe drooling associated with neurologic conditions (eg, cerebral palsy)
<3 years: Safety and efficacy not established
3-16 years: 0.02 mg/kg PO q8hr initially; may increase by 0.02 mg/kg q5-7days if warranted, up to 0.1 mg/kg q8hr
Not to exceed 1.5-3 mg/dose (based on weight; see Mfr info)
Administration
- Administer 1 hr ac or 2 hr pc
- High fat food reduces PO bioavailability
Control of Secretions (Off-label)
0.004-0.01 mg/kg IV/IM q6hr
0.04-0.1 mg/kg PO q6hr
Neuromuscular Blockade Reversal
0.2 mg IV per 1 mg of neostigmine or 5 mg of pyridostigmine administered
Cuvposa, glycopyrronium (glycopyrrolate) adverse (side) effects
Frequency not defined
Anticholinergic symptoms (mydriasis, hyperthermia, tachycardia, cardiac arrhythmia)
Dry mouth
Dry skin
Anhidrosis
Flushing
Blurred vision
Cycloplegia
Photophobia
Palpitation
Xerophthalmia
Constipation
Urinary retention
Warnings
Contraindications
Hypersensitivity to glycopyrrolate or other ingredients
Medical conditions that preclude anticholinergic therapy (eg, angle-closure glaucoma, obstructive uropathy, 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
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 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 postration; 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
Pregnancy category: B
Lactation: Excretion in milk unknown; use with caution
Pregnancy categories
A: Generally acceptable. Controlled studies in pregnant women show no evidence of fetal risk.
B: May be acceptable. Either animal studies show no risk but human studies not available or animal studies showed minor risks and human studies done and showed no risk.
C: Use with caution if benefits outweigh risks. Animal studies show risk and human studies not available or neither animal nor human studies done.
D: Use in LIFE-THREATENING emergencies when no safer drug available. Positive evidence of human fetal risk.
X: Do not use in pregnancy. Risks involved outweigh potential benefits. Safer alternatives exist.
NA: Information not available.
Pharmacology of Cuvposa, glycopyrronium (glycopyrrolate)
Mechanism of action
Competitively inhibits action of ACh on autonomic effectors innervated by postganglionic nerves
Inhibits salivation, tracheobronchial secretions, bradycardia, and hypotension
Absorption
Onset: 1 min (IV); 15-30 min (IM, SC)
Duration: 2-3 hr (parenteral, vagal block); 7 hr (parenteral, inhibition of salivation); 8-12 hr (PO; anticholinergic effects)
Peak plasma time: 30-45 min
Incompletely absorbed from GI tract since completely ionized
Distribution
Vd: 1.3-1.8 L/kg (children); 0.2-0.62 L/kg (adults)
Metabolism
Several metabolites
Elimination
Excretion: Mainly as unchanged drug in feces via biliary elimination and in urine
Administration
IV Incompatibilities
Additive: Methylprednisolone sodium succinate
Syringe: Chloramphenicol, dexamethasone sodium phosphate, diazepam, dimenhydrinate, methohexital, pentazocine, pentobarbital, secobarbital, sodium bicarbonate, thiopentaL
IV Compatibilities
Syringe: Atropine, hydroxyzine, lidocaine, meperidine, morphine
IV Administration
Inspect product visually to ensure there is no particulate matter
Administer at a rate of 0.2 mg over 1-2 min
For IV administration, glycopyrrolate may be administered by IM or IV without dilution
May also be administered via tubing of a running IV infusion of a compatible solution
Storage
Unstable at pH >6
