Glycopyrrolate and Neostigmine

Other CNS Drugs · Anticholinergic/Anticholinesterase

Indications

Reversal of residual non-depolarising (competitive) neuromuscular block.

Dosage

Adults: 1-2 mL IV over a period of 10-30 sec. Alternatively 0.02 mL/kg intravenously over a period of 10-30 sec. Children: 0.02 mL/kg IV over a period of 10-30 sec. Alternatively dilute to 10 mL with water for injection or 0.9% sodium chloride injection and administer 1 mL/5 kg body weight. These doses may be repeated if adequate reversal of neuromuscular blockade is not achieved, max dose 2 mL.

Adverse Effects

Nausea, vomiting, increased salivation, diarrhoea and abdominal cramp.

Risk Factor (Pregnancy/Lactation)

Pregnancy: Risk cannot be ruled out. Lactation: Contraindicated or not recommended. Contraindications: Intestinal or urinary obstruction. Precautions: Bronchial asthma, cardiac disease, vagotonia, epilepsy, Parkinsonism.

Interactions

Cyclopropane or halothane anaesthesia. Depolarising muscle relaxants.

Pharmacokinetics

GLYCOPYRROLATE: 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%). NEOSTIGMINE: Onset: Oral: 45-75 mins. IV: 4-8 mins. IM/SC: 20-30 mins. Duration: 2-4 hrs. Absorption: Oral: Poorly absorbed. Metabolism: Hepatic. Also via…

Compiled by Healify Pharmacy from published drug references. How we compile it →

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