glycopyrrolate (Robinul, Cuvposa, Qbrexza)

Introduction

Tradenames: Robinul, Cuvposa, Qbrexza. (glycopyrronium bromide)

Indications

• used preoperatively to reduce salivary, tracheobronchial & pharyngeal secretions
• used to prevent cholinergic effects during surgery, i.e. cardiac arrhythmias, hypotension, bradycardia
• adjunct agent in management of peptic ulcer disease
• reversal of neuromuscular blockade
• drooling
• irritable bowel syndrome, diarrhea
• axillary hyperhidrosis (topical)

Contraindications

• myasthenia gravis
• unstable cardiovascular status
• acute hemorrhage
• glaucoma
• paralytic ileus
• severe ulcerative colitis
• Sjogren syndrome
• when anticholinergic agents (parasympatholytics) are contraindicated

pregnancy category = b

safety in lactation = -

Dosage

• induction (intraoperative)
  • 0.1-0.2 mg IV/IM
  • 4 ug/kg up to 0.1 mg
  • may repeat at 2-3 min intervals PRN
• control of secretions
  • 4-10 ug/kg every 3-4 hours
  • maximum: 0.2 mg/dose or 0.8 mg/day
• 1-2 mg PO BID/TID

Tabs: 1 & 2 mg.

Injection: 0/2 mg/mL (1 mL, 5 mL, 20 mL)

Solution: Cuvposa is a flavored oral solution for children

Topical: Qbrexza (anticholinergic cloth)

Pharmacokinetics

• following IV administration, onset of action is 1 minute
• after IM or SC administration, onset of action is 15-30 min
• inhibition of salivation persists for up to 7 hours
• does NOT reach significant levels in CSF
• excreted largely unchanged in the bile & feces
• also eliminated in the urine

elimination via kidney

Adverse effects

• common (> 10%)
  • constipation
  • decreased sweating
  • dry mouth, nose, throat or dry skin
  • urinary retention
  • irritation at site of injection
• less common (1-10%)
  • decreased flow of breast milk
  • difficulty swallowing
  • photosensitivity
• uncommon (< 1%)
  • rash, confusion, increased intraocular pain, orthostatic hypotension, bloating, difficult urination, blurred vision, drowsiness, headache, loss of memory, nausea/vomiting, weakness, tiredness, ventricular fibrillation, tachycardia, palpitations, ataxia

• drug adverse effects of parasympatholytics

Mechanism of action

• quaternary ammonium muscarinic antagonist
• less CNS anticholinergic effects than scopalamine

More general terms

• parasympatholytic (anticholinergic, antimuscarinic agent)
• dissociative anesthetic
• topical agent

Component of

• budesonide/formoterol/glycopyrrolate (Breztri Aerosphere)
• formoterol/glycopyrrolate (Bevespi Aerosphere)
• glycopyrrolate/indacaterol

Database

• PubChem: http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?cid=11693
• PubChem: http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?cid=3494
• PubChem: http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?cid=521843
• PubChem: http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?cid=5284564