Neostigmine is a synthetic quaternary ammonium agent, the commonly used indirect reversible acetylcholinestrase  inhibitor of insignificant absorption, since their permanent charge renders them relatively insoluble in lipids.

Neostigmin has the ability of producing its primary effects temporarily through inhibiting the actions of acetylcholinestrase through the mechanism of action via blocking the enzymatic hydrolysis of acetylcholine through binding process which hinders it's effects, consequently, protecting the action of acetylcholine in the body from degradation, thereby increasing the concentration of endogenous acetylcholine in the synaptic clefts, and neuroeffector junction, the access of acetylcholine in turn stimulates cholinergic receptors of the involuntary muscles to evoke increased receptors, which has demonstrated to provide marked muscarinic effects on the gastro-intestinal tract and the urinary bladder.

 

INTESTIGMIN is indicated in the treatment of the following conditions :

- Diagnosis and management of myasthenia gravis pseudoparalytica.

- Curare antagonist.

- Post-operative intestinal atony and urinary retention.

- Treatment of atropine overdosage.

 

- Concomitant administration of Neostigmine in conjunction with the following drugs should be avoided include Methylprednisolone, due to decrease in muscle strength.

- Caution is used with concomitant use antiarrhythmic drugs, aminoglycosides and beta-blockers.

 

- The side effects of Neostigmine are chiefly due to excessive cholinergic stimulation and most commonly include increased salivation, nausea, vomiting, abdominal cramps, diarrhea and allergic reactions.

- C.N.S. adverse effects : Confusion, ataxia, and rarely convulsions.

- Paradoxical increase in blood pressure and heart rate has been reported.

 

Neostigmine should be used with caution in:

-Patients with arrhythmias, bradycardia, and hypotension.

- Patients with epilepsy, hyperthyroidism, parkinsonism, bronchial asthma, or peptic ulcer.

- In patients with myasthenia gravis, in whom other symptoms of over dosage may be mild or absent.

- Pregnancy and lactation: Should be used only if clearly needed.

 

Administration of the drug is not recommended in the following conditions:

- In patients with mechanical intestinal or urinary-tract obstruction.

- Peritonitis.

- The drug should not be used during halothane or cyclopropane anaesthesia.

- It should be avoided in patients known to be hypersensitive.

 

Adults: (5 – 20) mg/day by IM or subcutaneous injection at intervals, usually in the average of 2.5 mg repeated when necessary, INTESTIGMIN may be given by slow intravenous injection taking into consideration that the usual dosage is 0.5 mg which is approximately equivalent in effect to 1 to 1.5 mg of INTESTIGMIN by intramuscular or subcutaneous injection.

Children: (200 – 500) µg 4  hourly.

Neonates: (50 – 200) µg 4 hourly. 

 

- INTESTIGMIN 0.5 – Injection: A Pack of  5 ampoules of 2 mL. Each 2 mL ampoule  contains Neostigmin Methylsulfate equivalent to Neostigmin base 0.5 mg.

- INTESTIGMIN 2.5 – Injection: A Pack of  5 or 100 ampoules of 5 mL. Each 5 mL ampoule  contains Neostigmin Methylsulfate equivalent to Neostigmin base 2.5 mg.

 

Store INTESTIGMIN – Injection at temperature below 25°C. Protect from light and moisture.