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EPISTIGMIN

Composition
Ampoule Vial
(1 ml) (5 ml)
Neostigmine methylsulfate 0.5 mg 12.5 mg

Properties and Mode of Action

EPISTIGMIN is a cholineesterase inhibitor (anticholineesterase)which inhibits destruction of acetylcholine and thus
prolongs and intensifies the physiological actions of acetylcholine. EPISTIGMIN thus facilitates transmission of impulses
across the myoneural junction.
The clinical effects of EPISTIGMIN usually begin within 20 - 30 minutes after I.M. injection and last from 2.5 - 4 hours.
The anticholineesterase actions of EPISTIGMIN are reversible.

Indications
Diagnosis and treatment of Myasthenia Gravis.
Prevention and treatment of postoperative gastrointestinal ileus.
Prevention of postoperative urinary retention.
Treatment of postoperative non-obstructive urinary retention.
Curtailment of the muscular relaxation produced by non-depolarising muscle relaxants such as: tubocurarine or gallamine.

Dosage and Administration

Diagnosis and Treatment of Myasthenia Gravis:
For Diagnosis:
Adults:
1.5 mg by I.M. or S.C. injection concurrently with atropine 600 mcg (0.6 mg).
Significant improvement of muscle weakness occurring within several minutes to one hour indicates Myasthenia.
Pediatrics:
40 mcg (0.04 mg)/Kg body weight I.M..
For Treatment:
Adults:
0.5 mg I.M. or S.C. injection.
Subsequent doses should be based on the patient's response.
(Total daily dose range is 5 - 20 mg).
Pediatrics:
10 - 40 mcg (0.01 - 0.04 mg)/Kg body weight I.M. or S.C. every 2 - 3 hours concurrently with atropine 10 mcg (0.01
mg)/Kg body weight I.M. or S.C.. (Treatment is rarely needed beyond 8 weeks of age).

Prevention of Postoperative Distension or Urinary Retention in Adults:

0.25 mg I.M. or S.C. injection immediately following the surgery, repeated every 4 - 6 hours for 2 or 3 days.

Treatment of Postoperative Distension in Adults:

0.5 mg I.M. or S.C. injection as needed.

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Treatment of Urinary Retention in Adults:

0.5 mg by I.M. or S.C. injection, to be repeated every 3 hours for at least 5 doses after the patient has voided or the
bladder has been emptied. If urination does not occur within one hour following the initial 0.5 mg dose, the patient should
be catheterized.

Curtailment of Muscular Relaxation Produced by Non-depolarising Muscle Relaxants e.g. Tubocurarine or

Gallamine:
50 - 70 mcg (0.05 - 0.07 mg)/kg body weight given by slow I.V. injection over a period of 60 seconds concomitantly with
0.6 - 1.2 mg of atropine sulphate.
Additional EPISTIGMIN may be given until the muscle power is normal but a total dose of 5 mg for adults and 2.5 mg for
children should not be exceeded.

Precautions
EPISTIGMIN should be used with extreme caution in patients who have undergone recent intestinal or bladder surgery.
Also it should be used with caution in patients with cardiovascular disorders including arrhythmias, bradycardia and
hypotension as well as in patients with vagotonia, epilepsy, hyperthyroidism, parkinsonism, bronchial asthma and peptic
ulcer.
Pregnancy and Lactation:
Safety for use of EPISTIGMIN during pregnancy has not been established. It may cause uterine irritability and induce
premature labour when given I.V. to pregnant women near term.
It is not known whether EPISTIGMIN is excreted in breast milk, but problems in humans have not been documented.
Overdosage:
Overdosage may lead to cholinergic crisis characterised by:
severe diarrhoea, excessive bronchial secretions or salivation, severe vomiting, bradycardia, increasing muscle weakness,
nervousness and irritability.
Treatment of Overdosage: Atropine sulphate should be given in a dose of 1 - 2 mg I.V. or I.M. and repeated as
necessary (up to 4 mg).
Assisted respiration and further supportive treatment should be given.

Drug Interactions
The action of EPISTIGMIN may be antagonised by:
Aminoglycoside antibiotics and some anti-arrhythmic agents such as quinidine.

Contra_indications
Hypersensitivity to anticholineesterase.
Mechanical intestinal or urinary tract obstruction.
Peritonitis.
With depolarising muscle relaxants such as suxamethonium.
With other cholineesterase inhibitors including demecarium, echothiophate and isoflurophate.
During anaesthesia with cyclopropane or halothane.

Side effects
As with other cholineesterase inhibitors, side effects are chiefly due to excessive cholinergic stimulation and most
commonly include increased salivation, nausea, vomiting, abdominaal cramps and diarrhoea.
Allergic reactions may occur in some hypersensitive cases.

Presentation
EPISTIGMIN Ampoules : Box of 5 ampoules of 1 ml each.
EPISTIGMIN Vials : Vials of 5 ml each.

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