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 first clinical reports on loperamide were published in 1973 in the" Journal of Medicinal Chemistry" with the inventor being one of the authors. The trial name for it was "R-18553". Loperamide oxide has a different research code: R-58425. The trial against placebo was conducted from December 1972 to February 1974, its results being published in 1977 in "Gut", an edition of British Society of Gastroenterology. In 1973, Janssen started to promote loperamide under the brand name Imodium. In December 1976, Imodium got US FDA approval. During the 1980s, Imodium became the best-selling prescription antidiarrheal in the United States. In March