COMPOSITION
Each film coated tablet
contains
Itopride 50 mg
DESCRIPTION
A novel gastroprokinetic agent, itopride
hydrochloride (itopride), simulates gastrointestinal motor activity through
synergistic effects of dopamine D2-receptor blockade and acetylcholinesterase
inhibitors.
PHARMACOLOGY
Pharmacodynamics:
Itopride inhibits
the dopamine D2 receptor at the parasympathetic nerve ends and thereby
increases the release of acetylcholine and drecreases the metabolism of
acetylcholine by inhibiting the enzyme acetylcholinesterase (AChE). By
maintaining higher acetylcholine levels, itopride increases the lower
esophageal and gastrointestinal peristalsis, increases the lower esophageal
sphincter pressure stimulates gastric motility, accelerates gastric emptying
and improves gastro duodenal coordination. Because of its dopamine D2 rececptor
antagonist action, it also exerts anti emetic action.
Pharmacokinetics:
On oral administration,
Itopride is rapidly and extensively absorbed and peak serum concentrations are
achieved within 35 minutes after oral dosing1. Thus it has a rapid onset of
action, unlike cisapride and mosapride, which take around 60 minutes to reach
peak plasma concentrations. Food does not affect its abosorption. Itopride is
metabolized in the liver by N-oxidation to inactive metabolites by the enzyme
flavin-containing monooxygenase (FMO).The half life of Itopride is about 6
hours. It is excreted mainly by the kidneys as metabolites and unchanged drug.
INDICATIONS
Treatment of gastrointestinal
symptoms caused by reduced gastrointestinal motility, like feeling of gastric
fullness, upper abdominal pain, anorexia, heartburn, nausea and vomiting,
non-ulcer dyspepsia or chronic gastritis.
DOSAGE
The usual daily
dosage is 150 mg of itopride hydrochloride orally in three divided doses before
meals.
The dose may be
reduced, if required, depending on the patient’s age and symptoms at discretion
of
physician. This
drug should be discontinued if no improvement of gastrointestinal symptoms is
observed.
CONTRAINDICATIONS
GI hemorrhage, mechanical
obstruction or perforation, hypersensitivity
ADVERSE REACTIONS
Hypersensitivity,
diarrhea, constipation, abdominal pain, increased salivation. Neurologic,
endocrinologic and hematologic adverse effects have been reported infrequently,
therapy should be discontinued if hypersensitivity is seen.
DRUG INTERACTIONS
Anticholinergic
drugs may reduce the action of itopride. No interactions detected with
warfarin, diazepam, diclofenac, nifedipine and nicardipine. Metabolic
interactions are not to be expected because itopride is mainly metabolized by
flavin monooxygenase.
WARNINGS AND PRECAUTIONS
To be used with
caution as it enhances the action of acetylcholine. Safety in children less
than 12 years, pregnancy and lactation has not been established. Hence,
treatment should be avoided in these conditions.
