Glycopyrrolate
Other CNS Drugs · Antimuscarinic
Indications
Inhibit salivation and excessive secretions of the respiratory tract pre-operatively; reversal of neuromuscular blockade; control of upper airway secretions; adjunct in treatment of peptic ulcer.
Dosage
Adults: INJECTION: Control of secretions: Intra-operative: IV: 0.1 mg repeated as needed at 2-3 mins intervals. Preoperative: IM: 4.4 mcg/kg 30-60 min before procedure. Reverse neuromuscular blockade: IV: 0.2 mg for each 1 mg of neostigmine or 5 mg of pyridostigmine administered or 5-15 mcg/kg glycopyrrolate with 25-70 mcg/kg of neostigmine or 0.1-0.3 mg/kg of pyridostigmine (agents usually administered simultaneously, but glycopyrrolate may be administered first if bradycardia is present). Peptic ulcer: IM/IV: 0.1-0.2 mg 3-4 times/day. Adults: ORAL: Peptic ulcer: 1-2 mg 2-3 times daily. Children: INJECTION: Premedication at induction: IV or IM injection: Neonate, 5 mcg/kg; 1 mth-12 yr, 4-8 mcg/kg, max 200 mcg; 12-18 yr, 200-400 mcg or 4-5 mcg/kg, max 400 mcg. Intra-operative bradycardia: IV injection: Neonate, 10 mcg/kg, repeated if necessary; 1 mth-18 yr, 4-8 mcg/kg, max 200 mcg,…
Administration
Administer IV at a rate of 0.2 mg over 1-2 min. May be administered IV or IM without dilution. May also be administered via the tubing of a running IV infusion of a compatible solution. May be administered IV in the same syringe with neostigmine or pyridostigmine. Stability: Store at 20°C-25°C. Compatibility: Do not mix glycopyrrolate with alkaline drugs or solutions that have a pH over 6.0 because drug stability may be affected. A pH over 6.0 may occur if glycopyrrolate is mixed with dexamethasone sodium phosphate or LR solution. Gas or precipitate may form if glycopyrrolate is mixed in same syringe as chloramphenicol, diazepam, dimenhydrinate, methohexital sodium, pentobarbital sodium, secobarbital sodium, sodium bicarbonate, or thiopental sodium.
Adverse Effects
Dry skin. Constipation, dry throat, dry mouth. Irritation at injection site. Dry nose. Diaphoresis (decreased).
Risk Factor (Pregnancy/Lactation)
Pregnancy: No evidence of risk in humans. Lactation: Caution advised or effect undetermined. Contraindications: Hypersensitivity to glycopyrrolate or any component of the formulation; ulcerative colitis; narrow-angle glaucoma; acute haemorrhage; tachycardia; obstructive uropathy; paralytic ileus, obstructive disease of GI tract; Myasthaenia gravis. Precautions: Not recommended in children <12 years of age for the management of peptic ulcer; infants, patients with Down syndrome and children with spastic paralysis or brain damage may be hypersensitive to antimuscarinic effects. Use caution in elderly, patients with autonomic neuropathy, hepatic or renal disease, ulcerative colitis may predispose megacolon, hyperthyroidism, CAD, CHF, arrhythmias, tachycardia, BPH, hiatus hernia with reflux.
Interactions
Amantadine, cyclopropane, anticholinergic agents, levodopa.
Advice to Patient
Take 30-60 minutes before meals. Contact prescriber if there is headache, blurred vision, eye pain, dizziness, severe constipation, nervousness, flushing, difficulty in breathing, irregular heartbeat, confusion, mental excitation, lack of sleep, taste disturbance, dry mouth, loss of appetite, difficulty in urination, urinary retention, palpitations, decreased sweating, impotency. Empty bladder before taking medication. Take sufficient amount of fluids (2-3 litres per day) to maintain hydration, unless restricted by the prescriber. Sucking on lozenges may help to prevent dry mouth. Avoid direct sunlight. Use sunscreen, wear proper clothing and eyewear to prevent photosensitivity. Avoid exercising in hot weather.
Pharmacokinetics
Onset of action: IM: 15 to 30 minutes; IV: Within 1 minute. Peak effect: IM: Within approx. 30 to 45 minutes. Duration: Vagal effect: 2 to 3 hours; Inhibition of salivation: up to 7 hours; Parenteral: 7 hours. Absorption: Oral tablet: Poor (approx.3 %); variable and erratic; Oral solution: 23% lower compared to tablet; high-fat meal markedly reduces the oral bioavailability. Bioavailability: Tablet: 3%. Half-life elimination: Infants: 21.6 to 130 minutes; Children: 19.2 to 99.2 minutes; IM: Adults: 0.55 to 1.25 hours; IV: 0.83 ± 0.13 hour; Oral solution: Adults: 3 hours. Time to peak, plasma: 3.1 hours. Excretion: Urine (as unchanged drug, IM: 65% to >80%, IV: 85%); bile (as unchanged drug, <5%).
Brands with this active ingredient
Compiled by Healify Pharmacy from published drug references. How we compile it →
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