Glycopyrrolate

DEA Class;  Rx

Common Brand Names; Cuvposa, Dartisla ODT, glycopyrronium, Robinul, Robinul Forte, Seebri Neohaler, Lonhala Magnair

  • Anesthetic Premedication Agents; 
  • Anticholinergic Agents
  •  Respiratory; COPD Agents
 

Parenteral, oral, and inhalational antimuscarinic anticholinergic; less CNS penetration than atropine or scopolamine
Used parenterally to reduce GI secretions perioperatively; commonly used orally to reduce severe drooling in patients with certain neurologic conditions
Long-acting muscarinic antagonist (LAMA) when used by inhalation and used in adults for the maintenance treatment of COPD

Indicated for use as a preoperative antimuscarinic to reduce salivary, tracheobronchial, and pharyngeal secretions; reduce gastric acid production and acidity (aspiration prophylaxis); and to block vagal inhibitory reflexes during intubation and induction of anesthesia.

For the treatment of sialorrhea.

For the treatment of cardiac arrhythmias (e.g., bradycardia) that occur intraoperatively and are drug-induced or are associated with visceral traction stimulation of vagal reflexes.

For cholinesterase inhibitor-induced muscarinic effects prophylaxis when anticholinesterase agents (i.e., neostigmine, physostigmine, pyridostigmine) are used to reverse neuromuscular blockade produced by curariform agents.

For use as adjunctive therapy in the treatment of peptic ulcer disease.

Chronic Obstructive Pulmonary Disease (COPD)

Hypersensitivity to drug or components

Glaucoma

Obstructive uropathies, including prostatic hypertrophyMechanical obstructive diseases of gastrointestinal tract (eg, pyloroduodenalstenosis, strictures)

Gastrointestinal motility disorders (eg, achalasia, paralytic ileus, intestinal atony)Bleeding gastrointestinal ulcer

Active inflammatory or infectious colitis which can lead to toxic megacolon

History of or current toxic megacolon

Myasthenia gravis

  • Anticholinergic symptoms (mydriasis, hyperthermia, tachycardia, cardiac arrhythmia)
  • Dry mouth
  • Dry skin
  • Anhidrosis
  • Flushing
  • Blurred vision
  • Cycloplegia
  • Photophobia
  • Palpitation
  • Xerophthalmia
  • Constipation
  • Urinary retention
  • Angioedema
  • Paradoxical bronchospasm
  • Dysphonia

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

May cause increased intraocular pressure in patients with glaucoma and reduce effects of antiglaucoma agents; instruct patients to discontinue therapy and promptly seek medical care if they experience symptoms of acute angle-closure glaucoma (pain and reddening of the eyes accompanied by dilated pupils)

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

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

Should not be initiated in patients with acutely deteriorating or potentially life-threatening episodes of COPD; also do not use for the relief of acute symptoms (ie, as rescue therapy) for treating acute episodes of bronchospasm

Over decades of use, there is absence of published data on orally administered glycopyrrolate in pregnant women, including an absence of any reports of drug-associated risk of major birth defects, miscarriage, or other adverse maternal or fetal outcomes

There are no data on the presence of glycopyrrolate in either human or animal milk, effects on breastfed infants, or milk production; as with other anticholinergic drugs, glycopyrrolate may cause suppression of lactation; the developmental and health benefits of breastfeeding should be considered along with mother’s clinical need for therapy and any potential adverse effects on the breastfed infant from therapy

Adults

0.004 mg/kg IM preanesthesia; 0.2 mg/dose IV; 8 mg/day PO for oral tablets and 6.8 mg/day PO for orally disintegrating tablets; 2 capsules/day (total of 31.2 mcg) via oral inhalation (Seebri Neohaler) or 2 vials/day (total of 50 mcg) via oral inhalation (Longhala Magnair).

Geriatric

0.004 mg/kg IM preanesthesia; 0.2 mg/dose IV; 8 mg/day PO for oral tablets and 6.8 mg/day PO for orally disintegrating tablets; 2 capsules/day (total of 31.2 mcg) via oral inhalation (Seebri Neohaler) or 2 vials/day (total of 50 mcg) via oral inhalation (Longhala Magnair).

Adolescents

17 years and older: Safety and efficacy of inhaled glycopyrrolate not established; maximum dosage is dependent on indication for parenteral therapy; 8 mg/day PO for oral tablets.
16 years: Safety and efficacy of inhaled glycopyrrolate not established; maximum dosage is dependent on indication for parenteral therapy; 0.1 mg/kg/dose PO 3 times daily, not to exceed 1.5 to 3 mg/dose PO (depending on weight) for oral solution or 8 mg/day PO for oral tablets.
13 to 15 years: Safety and efficacy of parenteral and inhaled glycopyrrolate have not been established; 0.1 mg/kg/dose PO 3 times daily, not to exceed 1.5 to 3 mg/dose PO (depending on weight) for oral solution or 8 mg/day PO for oral tablets.

Children

12 years: Safety and efficacy of parenteral and inhaled glycopyrrolate have not been established; 0.1 mg/kg/dose PO 3 times daily, not to exceed 1.5 to 3 mg/dose PO (depending on weight) for oral solution or 8 mg/day PO for oral tablets.
3 to 11 years: Safety and efficacy of parenteral and inhaled glycopyrrolate have not been established; 0.1 mg/kg/dose PO 3 times daily, not to exceed 1.5 to 3 mg/dose PO (depending on weight) for oral solution.
Less than 3 years: Safety and efficacy have not been established.

Infants

Safety and efficacy have not been established.

Neonates

Safety and efficacy have not been established.

Glycopyrrolate

tablets

  • 1mg (generic, Robinul)

  • 1.5mg (generic)

  • 2mg (generic, Robinul Forte)

tablet, oral disintegrating

  • 1.7mg (Dartisla ODT)

oral solution

  • 1mg/5mL (Cuvposa)

injectable solution

  • 0.2mg/mL

encapsulated powder for oral inhalation

  • 15.6mcg/capsule (Seebri Neohaler)

solution for oral inhalation via nebulizer

  • 25mcg/mL vial (Lonhala Magnair)

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