Loperamide 2mg tablets -Loperium

LOPERIUM inhibits the peristaltic activity of longitudinal and circular smooth muscle in the intestine by interacting with cholinergic and noncholinergic neuronal mechanisms responsible for producing the peristaltic reflex. LOPERIUM binds to the opiate receptor in the gut wall, reducing propulsive peristalsis, and increase intestinal transit time.LOPERIUM is 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. LOPERIUM undergoes an extensive presystemic first pass metabolism in the gut wall and in the liver. LOPERIUM 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 very minute amount. The route of elimination is 0.63-1.4% in urine as unchanged drug, 58% is excreted in the bile and 15-23% appears in the faeces.