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Figure 1. Rebamipide.
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Figure 2. Tissue distribution of the radioactivity after single oral administration of 14 C-rebamipide to the rat. 14 C-rebamipide (10 mg/kg) suspended in 0.5% carboxymethylcellulose sodium salt solution was orally administered to the male Sprague-Dawley rat and tissue concentrations of rebamipide were measured by radioactivity. Data represents the mean value of three rats per point. The brain, heart, spleen and pancreas concentrations of rebamipide at 8 h were not detectable. Data from [23].
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Rebamipide is a gastroprotective agent and has been prescribed for the treatment of gastric ulcer and gastritis. The trade name 'Mucosta® ' is derived from gastric mucosal stabilizer and gastric mucosal prostaglandin inducer. One Mucosta tablet contains 100 mg of rebamipide and the prescribed dosage is 100 mg three-times daily. Rebamipide was approved in Japan in September 1990 for the treatment of gastric ulcer and has been on the Japanese market since December 1990. The additional indication for gastritis was approved in June 1994. Mucosta 20% granules have been on the market since 2003 and Mucosta tablets have also been on the Korean market since 1993. Rebamipide is currently marketed in Japan, Korea, China, the Philippines, Thailand, Indonesia, Cambodia, Vietnam, Malaysia and Egypt.
Rebamipide was screened by the acceleration of the healing of a rat acetic acid-induced gastric ulcer model [1-3]. It has no effect on gastric acid secretion in the rat [4] and human [5]. The precise mechanisms are still unknown; however, it has a beneficial effect on gastric mucosa through several mechanisms: increased gastric mucosal prostaglandin production [6-9], increased gastric mucus production [5,10], scavenging of hydroxyl radicals [11-13], inhibition of neutrophil activation [11,14-16], suppression of gastric mucosal inflammation [17,18], regulation of apoptosis-related genes [19], inhibition of tyrosine nitration [20] and promotion of Sonic hedgehog (Shh) restoration [21]. Based on these pleiotropic pharmacological actions of rebamipide, in the last 5 years clinical studies have been performed in patients with functional dyspepsia, chronic gastritis, NSAID-induced gastrointestinal injuries, gastric ulcer following eradication therapy for Helicobacter pylori , gastric ulcer after endoscopic surgery and ulcerative colitis. In this article, we present the basic pharmacological information of rebamipide and review recent studies using this agent.
Chemistry
Rebamipide (developmental code number,...