Clinical Pharmacology Details


NEOSTIGMINE METHYLSULPHATE


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Indications & Dose:

Reversal of non-depolarising neuromuscular blockade. Myasthenia gravis.


Adults


Reversal of non depolarising neuromuscular blockade, by intramuscular injection; over 1 minute, 50-70 microgram/kg (max; 5mg) after or with atropine sulphate or glycopyrolate


Adult


by intravenous injection, 200microgram per 1mg of neostigmine or 10-15 microgram/kg with neostigmine 50 microgram/kg


Children


10 microgram/kg with neostigmine 50 micrograms/ kg

Contraindications:

Side Effects:

Nausea, vomiting, increased salivation, diarrhoea, abdominal cramps (more marked with higher doses). Signs of overdosage are increased gastrointestinal discomfort, bronchial secretions, sweating, involuntary defecation and micturition,miosis, nystagmus, bradycardia, hypotension, agitation, excessive dreaming, and weakness eventually leading to fascicula-tion and paralysis. arrrythmia, AV block, cardiac arrest, syncope. Convulsions, dizziness, headache, dysaesthesia, dystonia, G.I. Disturbances,  increased secretions. Skin rash, thrombophlebitis, muscle cramps, spasm,  laryngospasm,  respiratory  depression, urinary frequency and incontinence


 

Cautions:

Asthma (extreme caution), bradycardia, recent myocardial infractions, epilepsy, hypotension, parkinsonism, vagotonia, peptic ulceration, renal impairment, pregnancy and breast-feeding. Atropine or glycopyrrnoium antidote to muscarinic effects may be necessary (particularly when neostigmine is given by injection), but it should be  given routinely as it may signs of overdosage.

Precautions:

Epilepsy, bronchial asthma, bradycardia, recent coronary occlusion, hyperthyroidism, cardiac disorders, urinary retention, peptic ulcer. Anticholinesterase insensitivity may develop.


PREGNANCY: Safety not established. Use only when clearly indicated.


BREAST-FEEDING: May be used.


OLD AGE: May be used in reduced dose.

Interaction:

 


Drug


Aminoglycoside  anti-biotics: Neuromuscular blockade potentiated.


Anticholinesterase drugs: In myasthenic patients receiving anticholinesterase muscle stimulants exercise caution since symptoms of anticholinesterase overdose (cholinergic crisis) may mimic under dosage (myasthenic weakness).


Corticosteroids: Anticholinesterase effect of neostigmine blunted.


Depolarising muscle relaxants: Neostigmine prolongs phase I block of these drugs.


Magnesium: May antagonise the effects of neostigmine.


Succinylcholine: Neuromuscular blocking effects enhanced – prolonged respiratory depression with extended periods of apnoea.


 

Warnings:

Adverse Effects:

Lactations:

Special Precautions:

Counselling:

Side Effects Or Adverse Reactions:

CNS: Dizziness, drowsiness, headache, seizures, syncope, weakness


CV: Arrhythmias (AV block, bradycardia, nodal rhythm, tachycardia), cardiac arrest, EGG changes, hypotension


EENT: Increased salivation, lacrimation, miosis, vision changes


GI: Abdominal cramps, diarrhea, flatulence, increased peristalsis, nausea, vomiting


GU: Urinary frequency


MS: Arthralgia, dysarthria, muscle spasms


RESP: Bronchospasm, dyspnea, increased bronchial secretions, respiratory arrest or depression


SKIN: Flushing, diaphoresis, rash, urticari 

Patient And Carer Advice: