Brand Information

Strength	Rate	Packing Style
mg	0.00	unit

Indication:

Peptic ulcer

Summary-

In clinical studies, pirenzepine is equally effective as cimetidine in the treatment of

peptic ulcer disease. It low incidence of side effects and selective inhibition of

muscarinic gastric secretion will make it a valuable additon to existing agents used

to treat ulcers.

Pirenzepine is currently available in some European countries, expected date of availability

in the United States is unknown. A new drug application(NDA) is pending

Adverse Reaction:

Side effects-

Pienzepine is well tolerated with few reported adverse effects. Dry mouth is the most common

effect but nausea, vomiting , diarrhea, constipation , increased appetite , anorexia, tiredness,

and difficulty of accomodation have all occurred.

Daily doses of less than 150mg seem to significantly reduce the incidence of at least some

of these problems.

Pharmacology/ Pharmacokinetics:

Pharmacology-

Pirenzepine is a tricyclic benzodiazepine antiulcer agent comparable to standard antiulcer

agents such as cimetidine and ranitidine. However, its uniqueness and mechanism of action

hinge on the selectiv antimuscarinic activity for gastric acid secretory cells

Pirenzepine selectively suppress both basal and stimulated acid pepsin secretion with

lesser effects om other muscarainic sites (eg salivary secretion ) compared to atropine

and other classic antichlinergic agents.

Controlled trials show that 50mg 2 to 3 times a daily, inhibits acid secretion at least 4.5 hrs

after dosing. Higher doses inhibit esophageal and colonic motility and decrease lower

esophageal sphincter pressure

Pharmacokinetics-

Pirenzepine is a hydrophilic molecule which systemic bioavailability after oral dosing

of 20% to 30%. Approximately 10% of the drug is protein bound. Little drug is found in the

brain, brain to serum concentration is 1 to 10.

At least 80% is renally excreted unchanged. Most metabolites are of a desmethyl variety.

The parent molecule has a half life of about 10 hours

Clinical studies-

Numerous short term ( 1 to 6 weeks) studies have been conducted comparing pirenzepine

to placebo and other antiulcer drugs in ulcer patients. In small doses (50 to 75mg/day)

duodenal ulcer healing percentages with pirenzepine are not superior to placebo.

Doses of 100 to 150mg /day produce healing in 70% to 90% of patients.

Statistically significant improvement (decreased antiacid use and pain) occurs

with both dosage levels

Short-term double-blind studies comparing duodenal ulcer healing rates of pirenzepine

( 100mg to 150mg/day) and cimetidine (1g/day) produced similar results (60% to 79%

for pirenzipine and 53% to 83% for cimetidine)

A single study comparing pirenzipine (100mg/day) to cimetidine (1g/day) and ranitidine

(300mg/day) found similar ulcer healing. However, pirenzipine showed slower effect on

symptoms disappearance.

Fewer studies have been conducted in patients with gastric ulcer. Double-bind studies

comparing pirenzipine to placebo show a need to use adequate doses

(100mg to 150mg/day).

Pirenzepine and cimetidine have produced similar healing rates( 50% vs 48%) in patients

with gastric ulcer, but more studies are indicated.

Trials were also performed comparing maintenance doses of pirenzepine (30 to 50mg/day)

to placebo and cimetidine (400mg/day) in duodenal ulcer patients for 12 months.

Results indicate statistically significant reductions in ulcer recurrences for active treatment

groups vs placebo (24% recurrence in active treatment group vs 80% in placebo treated

patients). No difference was demonostrated in recurrence rates between pirenzepine and

cimetidine patients

Combined use of pirenzepine with ranitidine or cimetidine shows more effective inhibition

of gastric acid secretion than the use of a single agent.

Such combinations may be useful in peptic ulcer conditions resistent to single drug therapy

and in the Zollinger-Ellison syndrome

GASTROZEPINE*

Indication

Adverse Reaction

Pharmacology/ Pharmacokinetics

Indication:

Adverse Reaction:

Pharmacology/ Pharmacokinetics:

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