COMPOSITION:
Each 1ml ampoule contains Glycopyrrolate USP 0.2 mg.

PHARMACOLOGY:
Glycopyrrolate is an anti-cholinergic drug which has been used in the treatment of peptic ulcer for a number of years and has recently been introduced into anaesthetic practice. It is a synthetic quaternary ammonium compound.
The following pharmacological effects are oberved.

Glycopyrrolate inhibits the muscarinic actions of acetyl choline.

Depending on the dose, glycopyrrolate may reduce the motility and secretory activity of the gastrointestinal system, the tone of the ureter and urinary bladder. It also has a slight relaxant action on the bile duct and gall bladder.

In general, smaller doses of anti-cholinergics inhibit salivary and bronchial secretions, sweating and can cause dilatation of the pupil and increase in heart rate. Large doses are required to decrease motility of the gastrointestinal and urinary tracts and to inhibit the gastric acid secretion.

Anti-spasmodic effect on gastrointestinal tract is due to the direct action on smooth muscle.
Anti -dysmenorrhoeal effect is due to spasmolytic action on the uterine muscles.
The highly polar quaternary ammonium group of glycopyrrolate limits its passage acrose lipid membranes, such as the blood brain barrier, in contrast to atropine sulphate and scopolamine hydrobromide, which are non-polar tertiary amines and can cross blod-brain barrier.
Peak effects occur approximately 30-45 minutes after intramuscular administration. The vagal blocking effect persists for 2-3 hours and the
anti-sialogogue effect persist for 7 hours (period longer than that for atropine).

With intravenous injection, the onset of action is generally evident within one minute.

INDICATION:

A) ANTI-MUSCARINIC
Pyrolate (glycopyrrolate) is indicated for use as a pre-operative, anti-muscarinic drug to reduce salivary, tracheo-bronchial, and pharyngeal secretions.
To reduce the volume of free gastric acid and to raise pH of gastric contents above 2.5.
It also blocks cardiac vagal inhibitory reflexes during induction and intubation.

B) ANTI -ARRHYTHMIC
Pyrolate may be used intra-operatively to counteract drug induced or vagal traction reflexes with associated arrhythmias.

C) REVERSAL OF NEUROMUSCULAR BLOCKADE
Pyrolate is indicated to reverse the neuromuscular block produced by non-depolarizing neuromuscular blocking agents such as Neo-choline (Neostigmine) and pyridostigmine.

DOSAGE AND ADMINISTRATION:
Pyrolate (glycopyrrolate) may be administered intramuscularly on intravenously without dilution for the following:

A) PRE-ANAESTHETIC MEDICATION
Prophylaxis of excessive salivation and respiratory tract secretions.

ADULTS:
4.4µg (0.0044 mg) per kg of body weight, one-half to one hour before induction of anaesthesia or at the time the pre-anaesthetic narcotic or sedative are administered.

CHILDREN:
Intramuscular 4.4 to 8.8µg (0.0044 to 0.0088mg) per kg of body weight, one-half to one hour before induction of anaesthesia.

B) INTRAOPERATIVE MEDICATION:
Counteract arrhythmias during surgery.

ADULTS:
Intravenous 100µg (0.1 mg), the dosage being repeated, if necessary at two to three minutes interval.

CHILDREN:
Intravenous 4.4µg (0.0044mg) per kg of body weight upto a maximum of 100µg (0.1mg), the dosage being repeated, if necessary, at two to three minutes intervals.

C) REVERSAL OF NEUROMUSCULAR
BLOCK (NON-DEPOLARIZING TYPE)

ADULTS:
Intravenous 200µg (0.2 mg), for each 1mg of neostigmine or 5 mg of pyridostigmine given simultaneously.

Note: In old age patients, the dose to be adjusted accordingly.

CHILDREN:
( 1 month to 12 years)
Intravenous 200µg (0.2 mg) 1 mg of neostigmine or 5mg pyridostigmine given simultaneously.

CONTRAINDICATION:
Known hypersensitivity to glycopyrrolate.
Due to its benzyl alcohol content, Pyrolate should not be used in newborn or children less than 1 month of age.
Concurrent glaucoma.
Obstructive uropathy (for example, bladder neck obstruction due to prostatic hypertrophy).
Obstructive diseases of the gastrointestinal tract (as in achalasia, pyloroduodenal stenosis)
Paralytic ileus, intestinal atony.
Un-stable cardiovascular status in acute haemorrhage.
Severe ulecerative colitis.
Myasthenia gravis.

SIDE-EFFECT:
Anti-cholinergic produce certain side effects most of which are extension of their pharmacological actions; they include: dry mouth, urinary retention, blurred vision, tachycardia, decrease sweating, loss of taste, headache, drowsiness, weakness, nausea, vomiting, suppression of lactation, constipation, allergic reactions and some degree of mental confusion or excitement.

PRECAUTION:
Investigate any tachycardia since an increase in heart rate may occur.
Use with caution in patients with coronary artery disease, congestive heart failure, hypertension and hyperthyroidism.

PRESENTATION:
Pack of 10 x 1 ml ampoules.