Loperamide Hydrochloride

Loperamide Hydrochloride is indicated in-

• Acute diarrhea
• Chronic diarrhea
• Abdominal cramps associated with diarrhea
• Crohn's disease
• Postgastric surgery
• Ulcerative colitis.

Loperamide Hydrochloride inhibits the peristaltic activity of the longitudinal and circular smooth muscle in the intestine by interacting with cholinergic and noncholinergic neuronal mechanisms responsible for producing the peristaltic reflex. Loperamide Hydrochloride binds to the opiate receptor in the gut wall, reducing propulsive peristalsis and increasing intestinal transit time. Loperamide Hydrochloride increases the tone of the anal sphincter. This also inhibits electrolyte and fluid secretion in the intestine.

Loperamide Hydrochloride is an orally administered capsule. After administration absorption is more than 65% which occurs at a modest rate, with peak serum levels of 2-3 µgm/litre occurring at about 4 hours later after oral administration. The rest 35% is excreted unchanged in the faeces. Loperamide Hydrochloride undergoes an extensive presystemic first-pass metabolism in the gut wall and in the liver. Loperamide does not act centrally due to its high affinity for the gut wall and its presystemic metabolism. This is why it reaches the systemic circulation in a very minute amount. The route of elimination is 0.63-1.4% in urine as an unchanged drug, 58% is excreted in the bile and 15-23% appears in the faeces.

Acute diarrhea-

• Adults: 2 capsules initially followed by 1 capsule after every loose stool.
• Usual dosage: 3-4 capsules/day. The maximum daily dose should not exceed 8 capsules.
• Children (9-12 years): 1 capsule after each loose stool until diarrhea is controlled. But not more than 6 capsules daily.
• Children (5-9 years): 1 capsule 4 times daily until diarrhea is controlled. But not more than 4 capsules daily.

Chronic diarrhea-

• Adults: 2-4 capsules daily in divided doses, depending on severity.
• Children: 1-2 capsules daily, depending on severity. Or directed by physician.

There are no data available.

Hypersensitivity to the drug and in patients who must avoid constipation. Loperamide Hydrochloride should not be used alone in acute dysentery, which is characterized by blood in the stool and elevated body temperature.

Abdominal pain and other gastrointestinal disturbances including dry mouth, dizziness, fatigue and skin rashes etc. have been reported.

Safety in human pregnancy has not been established. As with other drugs, it is not advisable to administer Loperamide in pregnancy. Although the fraction of Loperamide Hydrochloride secreted in human breast milk is extremely low, caution is advised if Loperamide Hydrochloride is to be administered to a nursing mother.

Loperamide Hydrochloride must be used with caution in cases of severe hepatic disturbance.

Overdosage of Loperamide may result in constipation, CNS depression, and nausea.

Anti-diarrhoeal, Anti-motility drugs.

Keep all medicines out of reach of children. Store in a cool and dry place protected from light.