“May all be happy, may all be healed, may all be at peace and may no one ever suffer."
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.
Loperamide Hydrochloride is indicated in-
Acute diarrhea-
Chronic diarrhea-
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.
Overdose Effects
Overdosage of Loperamide may result in constipation, CNS depression, and nausea.
Loperamide Hydrochloride must be used with caution in cases of severe hepatic disturbance.
Pregnancy & Lactation
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.