glycopyrrolate (Rx)

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

Postmarketing Reports

Angioedema

Paradoxical bronchospasm

Dysphonia

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 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.

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

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