Loperamide/simethicone Loperamide/simethicone Loperamide/simethicone is combination medication marketed under the trade name Imodium Multi-Symptom Relief (formerly Imodium A-D Advanced) used to treat diarrhea and gas simultaneously. It is manufactured by the McNeil Consumer Healthcare Division of McNeil PPC, Inc. Loperamide is a μ-opioid receptor agonist that works in the intestines. Although it is an opioid, it has no effects on the central nervous system. It reduces diarrhea by slowing the transit time of contents through the intestinal tract thereby allowing more water to be reabsorbed from the intestinal lumen. Simethicone reduces gas by allowing smaller gas bubbles to coalesce into larger bubbles
Loperamide physical dependence during preclinical studies, specifically in mice, rats, and rhesus monkeys. Symptoms of mild opiate withdrawal were observed following abrupt discontinuation of long-term treatment of animals with loperamide. When originally approved for medical use in the United States, loperamide was considered a narcotic and was put into Schedule II of the Controlled Substances Act 1970. It was transferred to Schedule V on 17 July 1977 and then decontrolled as of 3 November 1982. Loperamide hydrochloride was first synthesized by Paul Janssen from Janssen Pharmaceutica in Beerse (Belgium), following previous discoveries of diphenoxylate hydrochloride (1956) and fentanyl citrate (1960). The