COMPOSITION:
Each 5ml ampoule contains: Neostigmine Methylsulphate BP 2.5 mg.

PHARMACOLOGY:
Neostigmine belongs to "Reversible" Carbamate inhibitors group. These drugs inhibit or inactivate acetyl cholinesterase. They cause acetylcholine to accumulate at cholinergic receptors throughout the body, and therefore are capable of producing effects equivalent to excessive stimulation of cholinergic receptors throughout the central and peripheral nervous system.

The following pharmacological effects are observed.

a) CARDIOVASCULAR SYSTEM:
Peripheral accumulation of acetyloholine may cause profound bradycardia due to vagal stimulation. In addition, vasodilation and hypotension occur.

b) RESPIRATORY SYSTEM:
Bronchoconstriction may occur due to contraction of bronchial smooth muscles, and there may be increased oropharyngeal and bronchial gland secretions.

c) NEUROMUSCULAR JUNCTION:
Neostigmine is routinely used during anaesthesia to reverse the action of the non-depolarizing neuromuscular blocking agents. A small dose of Neostigmine, increases skeletal muscle contractility and reverse a competitive neuromuscular block.

After I.V. Injection Neostigmine is absorbed quickly. The distribution half life varies between 1 to 3.5 minutes and elimination half life has been reported as ranging from 15 to 80 minutes. Approximately 80% of the drug is eliminated in the urine within 24 hours; 50% as unchanged drug, 15% as 3-hydroxyphenyl trimethyl ammonium; and 15% as other metabolites.

INDICATION:
Although anti-cholinesterases have been recommended for the treatment of a wide variety of conditions. Their wide spread acceptability has been established in four areas.

• Reversal of the effects of non-depolarizing neuromuscular blocking drugs.
  
• Paralytic ileus and post-operative constipation (due to atony of the smooth muscles of the intestinal tract).
  
• Retention of urine (due to paralysis of smooth muscles of urinary bladder).
  
• Glaucoma.
  
• Symptomatic control of Myasthenia gravis.
  

DOSAGE AND ADMINISTRATION:
Reversal of non-depolarizing effects of neuro-muscular blocking drugs

ADULTS/CHILDREN:
Neostigmine, 40-50 µg/kg body weight in combination with Glycopyrrolate 10-15 µg/kg body weight is recommended. A dose of 2.5 to 3.0 mg (5ml to 6ml) of Neostigmine accompanied by 0.5mg of Glycopyrrolate may therefore be safely administered at the termination of anaesthesia.

In atonic constipation and meteorism (Before radiological examination).

ADULTS:
0.5 mg to 1 mg (1 ml to 2 ml ) I.M.

CHILDREN:
0.25 mg to 0.5 mg (0.5 ml to 1 ml ) I.M.

Post-operative intestinal atony and urinary retention.

PROPHYLAXIS:
0.25mg (0.5 ml) I.M. immediately after surgery. The dose can be repeated every 4 to 6 hours if required.

TREATMENT
ADULTS:
0.5 mg (1 ml) I.M. every 4-6 hours.

CHILDREN:
Half of the adult dose i.e. 0.25mg (0.5ml)

SYMPTOMATIC CONTROL OF MYASTHENIA GRAVIS
0.5mg (1ml) subcutaneously or I.M based on individual patient.
Dose is adjusted according to the degree of disability.

CONTRA-INDICATION:
Known hypersensitivity to Neostigmine.
Mechanical obstruction of intestinal tract or urinary tract.

SIDE-EFFECT:
Generally the drug is very well tolerated, side-effects include: nausea, vomiting, abdominal cramps, increased salivations, lacrimation, increased bronchial secretions, bradycardia, hypotension and miosis.

PRECAUTION:
Neo-Choline (Neostigmine) should be used with caution in patients with bradycardia,
bronchial asthma, diabetes mellitus, and after gastrointestinal surgery.
Pregnant and nursing mothers should take this medicine only under medical supervision.

PRESENTATION:
Pack of 5 x 5 ml ampoules.