Loperamide 1980s, prior to the expiration of US patent on 30 January 1990, McNeil company started to develop Imodium Advanced containing loperamide and simethicone for treating both diarrhea and gas. In March 1997, the company patented such combination. The drug was approved in June 1997 by the FDA as Imodium Multi-Symptom Relief in the form of a chewable tablet. In November 1993, loperamide was launched as an orally disintegrating tablet based on Zydis technology. Imodium Instant Melts from Johnson & Johnson is currently the only loperamide available in the form of orally disintegrating tablets. In 2013, loperamide in the form of
Loperamide on the μ-opioid receptors in the myenteric plexus of the large intestine. Loperamide works like morphine, decreasing the activity of the myenteric plexus, which decreases the tone of the longitudinal and circular smooth muscles of the intestinal wall. This increases the time material stays in the intestine, allowing more water to be absorbed from the fecal matter. Loperamide also decreases colonic mass movements and suppresses the gastrocolic reflex. Loperamide's circulation in the bloodstream is limited in two ways. Efflux by P-glycoprotein in the intestinal wall reduces passage of loperamide, and the fraction of drug crossing is then further reduced through