Formulary
Neostigmine: Indications, Dosing, Side Effects and Interactions
They prolong the action of acetylcholine by inhibiting the action of the enzyme acetylcholinesterase.
MedNext Academy | 4 min read
Neostigmine: Indications, Dosing, Side Effects and Interactions
They prolong the action of acetylcholine by inhibiting the action of the enzyme acetylcholinesterase.
Drug action
They prolong the action of acetylcholine by inhibiting the action of the enzyme acetylcholinesterase.
Indications and dose
**Treatment of myasthenia gravis**
- **Adult** (By Mouth): Initially 15-30 mg, dose repeated at suitable intervals throughout the day, total daily dose 75-300 mg, the maximum that most patients can tolerate is 180 mg daily.
- **Adult** (By Subcutaneous Injection, Or By Intramuscular Injection): 1-2.5 mg, dose repeated at suitable intervals throughout the day (usual total daily dose 5-20 mg).
**Reversal of non-depolarising (competitive) neuromuscular blockade**
- **Adult** (By Intravenous Injection): 2.5 mg (max. per dose 5 mg), repeated if necessary after or with glycopyrronium or atropine, to be given over 1 minute.
**Treatment of myasthenia gravis for neostigmine**
- **Neonate** (By mouth): Initially 1-2 mg, then 1-5 mg every 4 hours, given 30 minutes before feeds.
- **Child 1 month-5 years** (By mouth): Initially 7.5 mg, dose repeated at suitable intervals throughout the day, total daily dose 15-90 mg.
- **Child 6-11 years** (By mouth): Initially 15 mg, dose repeated at suitable intervals throughout the day, total daily dose 15-90 mg.
- **Child 12-17 years** (By mouth): Initially 15-30 mg, dose repeated at suitable intervals throughout the day, total daily dose 75-300 mg, the maximum that most patients can tolerate is 180 mg daily.
- **Neonate** (By subcutaneous injection, or by intramuscular injection): 150 micrograms/kg every 6-8 hours, to be given 30 minutes before feeds, then increased if necessary up to 300 micrograms/kg every 4 hours.
- **Child 1 month-11 years** (By subcutaneous injection, or by intramuscular injection): 200-500 micrograms, dose repeated at suitable intervals throughout the day.
- **Child 12-17 years** (By subcutaneous injection, or by intramuscular injection): 1-2.5 mg, dose repeated at suitable intervals throughout the day.
**Reversal of non-depolarising (competitive) neuromuscular blockade for neostigmine**
- **Neonate** (By intravenous injection): 50 micrograms/kg, to be given over 1 minute after or with glycopyrronium or atropine, followed by 25 micrograms/kg if required.
- **Child 1 month-11 years** (By intravenous injection): 50 micrograms/kg (max. per dose 2.5 mg), to be given over 1 minute after or with glycopyrronium or atropine, then 25 micrograms/kg if required.
- **Child 12-17 years** (By intravenous injection): 50 micrograms/kg (max. per dose 2.5 mg), to be given over 1 minute after or with glycopyrronium or atropine, then 25 micrograms/kg (max. per dose 2.5 mg) if required.
Cautions
Arrhythmias; asthma (extreme caution); atropine or other antidote to muscarinic effects may be necessary (particularly when neostigmine is given by injection) but not given routinely because it may mask signs of overdosage; bradycardia; epilepsy; hyperthyroidism; hypotension; parkinsonism; peptic ulceration; recent myocardial infarction; vagotonia Cautions, further information Elderly Screening Tool of Older Persons' potentially inappropriate Prescriptions (STOPP) criteria to aid medication reviews (see Prescribing in the elderly for information). Potentially inappropriate: in patients with a known history of persistent bradycardia (heart rate less than 60 beats per minute), heart block, or recurrent unexplained syncope, or concurrent treatment with drugs that reduce heart rate (risk of cardiac conduction failure, syncope, and injury). Cautions For neostigmine With intravenous use Glycopyrronium or atropine should also be given when reversing neuromuscular blockade
Contraindications
Intestinal obstruction; urinary obstruction
Side effects
Frequency not known Abdominal cramps; diarrhoea; excessive tearing; hypersalivation; nausea; vomiting Overdose Signs of overdosage include bronchoconstriction, increased bronchial secretions, lacrimation, excessive sweating, involuntary defaecation, involuntary micturition, miosis, nystagmus, bradycardia, heart block, arrhythmias, hypotension, agitation, excessive dreaming, and weakness eventually leading to fasciculation and paralysis. Side-effects For neostigmine Frequency not known With parenteral use Intestinal hypermotility; muscle spasms
Interactions
**Other interactions (7):**
- Administration of landiolol should be titrated with caution when concomitantly used with anaesthetics with heartrate lowering effect, esterase substrates (e.g., suxamethonium chloride) or...
- These include: potentiation of its direct blocking action at the neuromuscular junction by aminoglycoside antibiotics; inhibition of its metabolism by cimetidine which may increase plasma...
- Pharmacodynamic interactions Because of its mechanism of action, galantamine should not be given concomitantly with other cholinomimetics (such as ambenonium, donepezil, neostigmine, pyridostigmine,...
- Drugs lowering heart rate, causing automaticity or conduction disorders Combined therapy with the following active substances is not recommended: bradycardic active substances such as beta...
- Neostigmine has an effect on the non-depolarising relaxants, but has no effect on the relaxing action of isoflurane itself.
- These include: Antibacterials Enhanced effects of suxamethonium with Aminoglycosides Clindamycin, polymyxins and vancomycin Piperacillin Antimalarials Quinine and chloroquine - effects of...
Pregnancy
Manufacturer advises use only if potential benefit outweighs risk.
Breast feeding
Amount probably too small to be harmful.
Renal impairment
Dose adjustments May need dose reduction.
Medicinal forms
Solution
Clinical governance
**Author:** MedNext Clinical Team. **Clinical reviewer:** Dr Shameer Deen, MBBS, MS, MRCS. **Sources:** BNF, Indian Pharmacopoeia, CIMS India. **Correction:** Report errors at support@mednext.academy.
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