Neostigmine


Concise Prescribing Info
Indications/Uses
Listed in Dosage.
Dosage/Direction for Use
Adult : PO Myasthenia gravis As neostigmine bromide: 15-30 mg in divided doses, up to a total dose of 75-300 mg/day. Paralytic ileus and post-op urinary retention As neostigmine bromide: 15-30 mg. IM/SC Myasthenia gravis As neostigmine metilsulfate: 0.5-2.5 mg in divided doses, up to a total dose of 5-20 mg/day. Paralytic ileus and post-op urinary retention As neostigmine metilsulfate: 0.5-2.5 mg as required. IV Reversal of neuromuscular blockade As neostigmine metilsulfate: 0.05-0.07 mg/kg by inj as required.
Dosage Details
Intramuscular
Neonatal myasthenia gravis
Child: As neostigmine metilsulfate: Initially, 0.1 mg, followed by 0.05-0.25 mg or 0.03 mg/kg 2-4 hrly.

Intravenous
Reversal of neuromuscular blockade
Adult: As neostigmine metilsulfate: 0.05-0.07 mg/kg by inj over 60 sec, as required.
Child: Same as adult dose.

Oral
Myasthenia gravis
Adult: As neostigmine bromide: 15-30 mg. Doses are given at intervals according to response up to a usual total daily dose of 75-300 mg.
Child: <6 yr Initially, 7.5 mg; 6-12 yr Initially, 15 mg. Doses are adjusted according to response up to a usual total daily dose of 15-90 mg.

Oral
Paralytic ileus and postoperative urinary retention
Adult: As neostigmine bromide: 15-30 mg. Frequency of doses may vary according to response.
Child: 2.5-15 mg. Frequency of doses may vary according to response.

Parenteral
Paralytic ileus and postoperative urinary retention
Adult: As neostigmine metilsulfate: 0.5-2.5 mg by SC or IM inj, as required.
Child: 0.125-1 mg by SC or IM inj.

Parenteral
Myasthenia gravis
Adult: As neostigmine metilsulfate: 0.5-2.5 mg by IM or SC inj, doses are given at intervals according to response up to a total daily dose of 5-20 mg.
Child: <12 yr 0.2-0.5 mg, repeated at suitable intervals throughout the day.
Renal Impairment
Oral:
Continuous renal replacement therapy (CRRT): 50% of normal dose.
CrCl (mL/min)
Dosage
<10 25% of normal dose.
10-50 50% of normal dose.
IM/IV:
Dose adjustment may be required.
Contraindications
Peritonitis, mechanical GI or urinary obstruction.
Special Precautions
Patient w/ bronchial asthma, CV disorders (e.g. bradycardia, recent MI, hypotension), peptic ulcer disease, vagotonia, epilepsy, parkinsonism, hyperthyroidism. Patient who underwent recent intestinal or bladder surgery. Renal impairment. Childn. Pregnancy and lactation.
Adverse Reactions
Nausea and vomiting, increased salivation, diarrhoea and abdominal cramps; hypersensitivity reactions (e.g. anaphylaxis, urticaria, angioedema); neuromuscular dysfunction in high doses of IV preparation.
Potentially Fatal: Resp failure, due to a combination of muscarinic, nicotinic and central effects or cardiac arrest.
IM/IV/Parenteral/PO/SC: C
MonitoringParameters
Monitor ECG, BP and heart rate esp w/ IV use.
Overdosage
Symptoms: Muscarinic effects e.g. abdominal cramps, increased peristalsis, diarrhoea, nausea and vomiting, increased bronchial secretions, salivation, diaphoresis, miosis and nicotinic effects e.g. muscular cramps, fasciculations, general weakness. Bradycardia and hypotension may also occur. Management: Empty the stomach by gastric lavage. May give activated charcoal to decrease absorption. Artificial respiration should be instituted for severe resp depression. Give atropine sulfate 1-2 mg IV to control muscarinic effects.
Drug Interactions
May potentiate neuromuscular blockade w/ depolarising muscle relaxants (e.g. suxamethonium) resulting to prolonged apnoea. Drugs w/ neuromuscular blocking activity (e.g. aminoglycosides, clindamycin, colistin, cyclopropane, halogenated inhalational anaesth) may antagonise the effects of neostigmine. Reduced effects w/ quinine, chloroquine, hydroxychloroquine, quinidine, procainamide, propafenone, lithium. Prolonged bradycardia w/ β-blockers.
Action
Description: Neostigmine inhibits the hydrolysis of acetylcholine by competing w/ acetylcholine for its binding site on acetylcholinesterase. It facilitates impulse transmission across neuromuscular junctions thus, enhancing cholinergic action. It also has a direct cholinomimetic effect on skeletal muscle and possibly on autonomic ganglion cells and neurons of the CNS.
Onset: 1-2 hr (oral); 20-30 min (IM).
Duration: 2-4 hr (oral); 2.5-4 hr (IM).
Pharmacokinetics:
Absorption: Poorly absorbed from the GI tract. Bioavailability: Approx 1-2%. Time to peak plasma concentration: 1-2 hr.
Distribution: Crosses the placenta and enters breast milk (small amounts). Volume of distribution: 0.12-1.4 L/kg (IV). Plasma protein binding: 15-25%.
Metabolism: Undergoes hepatic metabolism and hydrolysis by cholinesterases.
Excretion: Via urine, as unchanged drug and metabolites. Half-life: 42-60 min (oral); 51-90 min (IM); 24-113 min (IV).
Chemical Structure

Chemical Structure Image
Neostigmine

Source: National Center for Biotechnology Information. PubChem Database. Neostigmine, CID=4456, https://pubchem.ncbi.nlm.nih.gov/compound/Neostigmine (accessed on Jan. 22, 2020)

Storage
Store between 20-25°C. Protect from light.
ATC Classification
N07AA01 - neostigmine ; Belongs to the class of anticholinesterase. Used as parasympathomimetics.
References
Anon. Neostigmine. Lexicomp Online. Hudson, Ohio. Wolters Kluwer Clinical Drug Information, Inc. https://online.lexi.com. Accessed 30/07/2015.

Buckingham R (ed). Neostigmine. Martindale: The Complete Drug Reference [online]. London. Pharmaceutical Press. https://www.medicinescomplete.com. Accessed 30/07/2015.

Neostigmine Methylsulfate Injection, Solution (Fresenius Kabi USA, LLC). DailyMed. Source: U.S. National Library of Medicine. https://dailymed.nlm.nih.gov/dailymed/. Accessed 03/07/2015.

Disclaimer: This information is independently developed by MIMS based on Neostigmine from various references and is provided for your reference only. Therapeutic uses, prescribing information and product availability may vary between countries. Please refer to MIMS Product Monographs for specific and locally approved prescribing information. Although great effort has been made to ensure content accuracy, MIMS shall not be held responsible or liable for any claims or damages arising from the use or misuse of the information contained herein, its contents or omissions, or otherwise. Copyright © 2020 MIMS. All rights reserved. Powered by MIMS.com
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