Anticholinergic agent work on the

parasympathetic nervous system. In the lung,

agent given by inhaled aerosol can block
cholinergic-induce airway constriction.
Anticholinergic are classified according the
receptor involved; antimuscarinic and
antinicotinic.
Pirenzepine
Pharmacology and use:
Pirenzepine belongs to a group of medications
called antispasmodics/anticholinergics. These medications are used to relieve cramps or spasms of the
stomach, intestines, and bladder. Pirenzepine is used to treat duodenal or stomach ulcers or intestine
problems. It can be used together with antacids or other medicine in the treatment of peptic ulcer. It may
also be used to prevent nausea, vomiting, and motion sickness. For the treatment of peptic ulcer; Gastric
ulcer; Duodenal ulcer
Mechanism Of Action:
Pirenzepine is a muscarinic receptor antagonist and binds to the muscarinic acetylcholine receptor. The
muscarinic acetylcholine receptor mediates various cellular responses, including inhibition of adenylate
cyclase, breakdown of phosphoinositides and modulation of potassium channels through the action of G
proteins.

Pirenzepine is a 'selective' antimuscarinic agent which, unlike classic anticholinergic

agents, inhibits gastric acid secretion at lower doses than are required to affect
gastrointestinal motility, salivary, central nervous system, cardiovascular, ocular
and urinary functions. On a weight basis, pirenzepine has one-tenth to one-eighth
the potency of atropine in inhibiting stimulated gastric acid secretion in humans.
Extensive controlled trials utilising endoscopy in outpatients with duodenal ulcers
indicate that patient response to pirenzepine is dose related. Doses of 100 to 150
mg/day are superior to placebo in promoting duodenal ulcer healing and in
diminishing day and night pain and supplementary antacid consumption. At such
doses, the efficacy of pirenzepine appears to be superior to that of gefarnate 300

mg/day and generally not significantly different from that of cimetidine 1 g/day in
treating duodenal ulcers. A beneficial effect of pirenzepine in the prevention of
duodenal ulcer recurrence was apparent in preliminary studies in small numbers of
patients, but its efficacy in this regard needs further confirmation and the optimum
dosage determined. Less extensive data on the treatment of benign gastric ulcers
suggest that pirenzepine 100 to 150 mg/day is superior to placebo and gefarnate
300 mg/day and does not differ significantly from cimetidine 1 g/day promoting
gastric ulcer healing. Pirenzepine is well tolerated by most patients, with a low
incidence of typical antimuscarinic effects on the gastrointestinal tract,
genitourinary system or heart being reported in clinical studies. However, dry
mouth and blurred vision are the more common side effects with clinically effective
doses. Thus, pirenzepine appears to have relatively selective antimuscarinic
activity, although controlled studies comparing pirenzepine and conventional
antimuscarinics in patients with peptic ulcer disease have not been reported.