Presentation and Status in Health Basket
10 X 2.5 mg/ml
Neostigmine Methylsulphate should be given very slowly by the IV route.
A syringe of Atropine Sulphate should always be available to counteract severe cholinergic reactions should they occur.
Myasthenia Gravis: 1 – 2.5 mg by IM or SC injection at intervals throughout the day, when maximum strength is needed. The usual duration of action of a dose is two to four hours. The total daily dose is usually 5 – 20 mg by injection but higher doses may be needed by some patients.
Neonatal Myasthenia Gravis may be treated with 0.1 mg Neostigmine intramuscularly initially. Thereafter, the dose must be titrated individually.
But is usually 0.05 – 0.25 mg IM or 0.03 mg/kg IM, every two – four hours. Because of the self-limiting nature of the disease in neonates, the daily dosage should be reduced until the drug can be withdrawn.
Older Children: (Under 12 years of age) May be given 0.2 – 0.5 mg by injection as required. Dosage requirements should be adjusted according to the response of the patient.
Antagonist to Non-depolarizing Neuromuscular Blockade: Reversal of
Neuromuscular blockade with Neostigmine should not be attempted unless there is spontaneous recovery from paralysis.
Adults and Children: A single dose of Neostigmine 0.05 – 0.07 mg/kg body-weight and Atropine 0.02 – 0.03 mg/kg body weight, by slow IV injection over one minute is usually adequate for complete reversal of Non-depolarizing Muscle Relaxants within 5 – 15 minutes. The maximum recommended dose of Neostigmine in adults is 5 mg and in children 2.5 mg.
Atropine and Neostigmine may be given simultaneously, but in patients with Bradycardia, the pulse rate should be increased to 80 per minute with Atropine before administering Neostigmine.
Adults: 0.5 – 2.5 mg Neostigmine Methylsulphate by SC or IM injection.
Children: 0.125 – 1 mg by injection. Doses may be varied according to
the individual needs of the patient.
Elderly: There are no specific dosage recommendations for Neostigmine
Methylsulphate in the elderly.
Myasthenia Gravis, antagonist to non-depolarizing neuromuscular blockade, Paralytic Ileus.
Use of neostigmine is contraindicated in patients with hypersensitivity to
neostigmine or to any of the excipients in this injection.
Neostigmine should not be administered to patients with mechanical obstruction of gastrointestinal or urinary tracts, peritonitis or doubtful
Neostigmine should not be used in conjunction with depolarising muscle relaxants such as suxamethonium as neuromuscular blockade may be potentiated.
Neostigmine should be used with extreme caution in patients with asthma as the parasympathomimetic action of neostigmine may cause bronchoconstriction.
Bradycardia, with the potential for progression to asystole, may occur in patients receiving neostigmine by intravenous injection unless atropine is given simultaneously. Extreme caution should be employed when treating patients with pre-existing bradycardia, cardiac arrhythmia or recent coronary occlusion.
Patients who are hyperreactive to neostigmine experience a severe cholinergic reaction to the drug. Atropine sulphate should always be available as an antagonist for the muscarinic effects of neostigmine.
Neostigmine should be used with caution in patients with epilepsy, vagotonia, hyperthyroidism, peptic ulceration or parkinsonism.
Administration of anticholinesterase agents to patients with intestinal anastomoses may produce rupture of the anastomosis or leakage of intestinal contents.
Elderly: Although there are no specific dosage requirements in the elderly, these patients may be more susceptible to dysrhythmias than younger patients.
Inhaled anaesthetics: Neostigmine Methylsulphate should not be given during cyclopropane or halothane anaesthesia; although it may be used after withdrawal of these agents.
Excipients: This medicinal product contains approximately 3.54 mg sodium per ml. This should be taken into consideration by patients on a controlled sodium diet.
The label shall state the following: Protect from light and store at less than 25°C. If only part used discard the remaining solution.
Adverse effects of Neostigmine are chiefly those of exaggerated response to parasympathetic stimulation.
Nervous system disorders: Cholinergic syndrome, especially at high doses. In patients with myasthenia gravis, cholinergic crisis may be difficult to distinguish from myasthenia crisis.
Eye disorders: Miosis, lacrimation increased.
Cardiac disorders: Bradycardia, decreased cardiac conduction, in severe cases possibly leading to heart block or cardiac arrest.
Vascular disorders: Hypotension.
Respiratory, thoracic or mediastinal disorders: Increased bronchial secretion, bronchospasm.
Gastrointestinal disorders: Nausea, vomiting, diarrhoea, abdominal cramps, salivary hypersecretion.
Increased intestinal motility may result in involuntary defecation.
Skin and subcutaneous tissue disorders: Hyperhidrosis.
Musculoskeletal, connective tissue and bone disorders: Muscle spasms.
Renal and urinary disorders: Urinary incontinence.
Neuromuscular Blocking Agents: Neostigmine effectively antagonises the effect of Non-depolarizing muscle relaxants (e.g. Tubocurarine, Gallamine or Pancuronium) and this interaction is used to therapeutic advantage to reverse muscle relaxation after surgery. Neostigmine does not antagonise, and it may in fact prolong, the phase I block of depolarizing muscle relaxants such as Succinylcholine.
Other Drugs: Atropine antagonises the muscarinic effects of Neostigmine, the interaction is utilised to counteract the muscarinic symptoms of the Neostigmine toxicity.
Anticholinesterase agents are sometimes effective in reversing Neuromuscular Block induced by Aminoglycoside Antibiotics. However,
Aminoglycoside Antibiotics and other drugs that interfere with Neuromuscular transmission should be used cautiously, if at all, in patients with Myasthenia Gravis and the dose of Neostigmine may have to be adjusted accordingly.
Pregnancy and Lactation
The use of Neostigmine Methylsulphate during pregnancy or lactation
has not been established. Although the possible hazards to mother and
child must be weighed against the potential benefits in every case.
Experience with Myasthenia Gravis has revealed no untoward effect of
the drug on the course of pregnancy. As the severity of Myasthenia
Gravis often fluctuates considerably, particular care is required to avoid
cholinergic crisis due to overdosage of Neostigmine.
Only negligible amounts of Neostigmine Methylsulphate are excreted in
breast milk. Nevertheless, attention should be paid to possible effects on
the breast-feeding infant.
Neostigmine Methylsulphate overdosage may include Cholinergic Crisis, which is characterised by nausea, vomiting, diarrhoea, excessive salivation and sweating, increased bronchial secretions, miosis, bradycardia or tachycardia, cardiospasm, bronchospasm, incoordination, muscle cramps, fasciculation and paralysis. Extremely high doses may produce CNS symptoms of agitation, fear or restlessness. Death may result from cardiac arrest or respiratory paralysis and pulmonary oedema. In patients with Myasthenia Gravis, in whom overdosage is most likely to occur, fasciculation and adverse parasympathomimetic effects may be mild or absent making cholinergic crisis difficult to distinguish from Myasthenia crisis.
Treatment: Maintenance of adequate respiration is of primary importance. Tracheostomy, Bronchial aspiration and postural drainage may be required; Respiration can be assisted mechanically or with oxygen, if necessary.
Neostigmine Methylsulphate should be discontinued immediately and 1–4 mg of Atropine Sulphate administered IV. Additional doses of Atropine may be given every 5 – 30 minutes as needed to control muscarinic symptoms. Atropine overdosage should be avoided as tenacious secretions and bronchial plugs may result.