Glycopyrrolate

Table of contents

  • Brand Names
  • Drug Combinations
  • Chemistry
  • Pharmacologic Category
  • Mechanism of Action
  • Therapeutic Use
  • Pregnancy and Lactation Implications
  • Contraindications
  • Warnings and Precautions
  • Adverse Reactions
  • Genes that may be involved
  • Drug Interactions
  • Dosage
  • Pharmacokinetics and Pharmacodynamics
  • Special Considerations

Brand Names

Europe

Austria: Robinul; Belgium: Robinul; Denmark: Robinul; Finland: Robinul; Germany: Robinul; Greece: Robinul; Ireland: Robinul; Sweden: Robinul; UK: Glycopyrrolate, Robinul.

North America

Canada: Glycopyrrolate; USA: Cuvposa, Glycopyrrolate, Robinul.

Asia

Japan: Robinul.

Drug combinations

Glycopyrrolate and Neostigmine

Chemistry

Glycopyrrolate: C~19~H~28~BrNO~3~. Mw: 398.33. (1) Pyrrolidinium, 3-[(cyclopentylhydroxyphenylacetyl)oxy]-1,1-dimethyl-, bromide; (2) 3-Hydroxy-1,1-dimethylpyrrolidinium bromide α-cyclopentylmandelate. CAS-596-51-0 (1963).

Pharmacologic Category

Anticholinergic Agents; Antimuscarinics/Antispasmodics. (ATC-Code: A03AB02).

Mechanism of action

Blocks action of acetylcholine at parasympathetic sites in smooth muscle, secretory glands, and CNS.

Therapeutic use

Preoperative inhibitor of salivation and excessive secretions of respiratory tract. Reversal of neuromuscular blockade. Control of upper airway secretions. Adjunct in treatment of peptic ulcer.

Pregnancy and lactiation implications

Teratogenic effects not observed in animal studies. Small amounts of glycopyrrolate cross human placenta. Use caution during lactation (might suppress lactation).

Unlabeled use

Contraindications

Hypersensitivity to glycopyrrolate or any component of the formulation. Severe ulcerative colitis. Toxic megacolon complicating ulcerative colitis. Paralytic ileus. Obstructive disease of GI tract. Intestinal atony in elderly or debilitated patients. Unstable cardiovascular status in acute hemorrhage. Narrow-angle glaucoma. Acute hemorrhage. Tachycardia. Obstructive uropathy. Myasthenia gravis.

Warnings and precautions

May cause CNS effects (drowsiness and/or blurred vision). Diarrhea may be a sign of incomplete intestinal obstruction (extreme caution). Heat prostration might occur in presence of fever, exposure to high environmental temperatures, and/or exercise. Use with caution in decreased pigmentation (skin and iris coloration, dark vs light). Use with caution in coronary artery disease, tachyarrhythmias, heart failure, or hypertension. Use of anticholinergics in gastric ulcer treatment may cause delay in gastric emptying due to antral statis. Use with caution in hepatic impairment, hiatal hernia with reflux, hyperthyroidism, autonomic neuropathy, prostatic hyperplasia, renal impairment, ulcerative colitis (may precipitate/aggravate toxic megacolon), and in the elderly (increased risk for anticholinergic effects, confusion, and hallucinations). Infants, patients with Down’s syndrome, and children with spastic paralysis or brain damage may be hypersensitive to antimuscarine effects. Not recommended for use in children <12 years of age for management of peptic ulcer or <16 years for preanesthetic use. Injection contains benzyl alcohol, associated with «gasping syndrome» in neonates. Potential risk of curariform neuromuscular blockade resulting in muscle weakness or paralysis with overdosage (avoid overdosage). Caution in esophageal reflux and hiatal hernia. Extreme caution in partial obstructive uropathy. Caution in autonomic neuropathy. Caution in hyperthyroidism.

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