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Micronutrients in Prevention and Improvement of the Standard Therapy in Hearing Disorders
Published in Kedar N. Prasad, Micronutrients in Health and Disease, 2019
The role for oxidative stress in MD is supported by the fact that free radical scavengers such as rebamipide, vitamin C, and glutathione, when administered orally for 8 weeks to patients with poorly controlled MD, improved tinnitus, hearing loss, and disability.74
Development of rebamipide-loaded spray-dried microsphere using distilled water and meglumine: physicochemical characterization and pharmacokinetics in rats
Published in Pharmaceutical Development and Technology, 2021
Dae Woong Ko, Jung Hyun Cho, Han-Gon Choi
Rebamipide [2-(4-chlorobenzoylamino)-3-[2(1H)-quinolinon-4-yl] propionic acid], an amino acid derivative of 2-(1H)-quinolinone, has been used as a potent antiulcer agent, because it increases endogenous prostaglandin synthesis and scavenges oxygen-derived free radicals in damaged gastric mucosal cells (Holland et al. 2019; Jaafar et al. 2018; Simsek et al. 2019). It is a BCS (Biopharmaceutics Classification System) class IV drug, because of its low solubility and permeability (Ha et al. 2017; Takeuchi et al. 2018). In particular, rebamipide has been reported to provide absolute oral bioavailability of 4.8% in rats (Shi et al. 2013). Therefore, the solubility and permeability of oral rebamipide in the gastrointestinal tract are two factors in its enhanced oral bioavailability. Much research has been focused on its enhanced bioavailability resulting from increased permeability with penetration enhancers (Huang et al. 2008; Mustapha, Din, et al. 2016; Narala et al. 2019; Tanaka et al. 2019). However, the use of specific penetration enhancers has not been approved by the US FDA since these materials might induce severe irritation to biological membranes. Many solubility-enhancing techniques, such as solid dispersion (Pradhan et al. 2015; Xiong et al. 2017; Takeuchi et al. 2018; Tanaka et al. 2019), nanosuspension (Shi et al. 2013), orally disintegrating tablets (Takano et al. 2019) and nano/microemulsion (Kim et al. 2017; Narala et al. 2019), have been studied.
Intra-articular injection of rebamipide prevents articular cartilage degeneration in murine post-traumatic osteoarthritis models
Published in Modern Rheumatology, 2020
Yoshiaki Suzuki, Masahiro Hasegawa, Yuriyo Matsui, Hironori Unno, Takahiro Iino, Toshimichi Yoshida, Akihiro Sudo
Rebamipide is a mucosa-protective drug used to treat gastric mucosal injuries such as gastric ulcers and gastritis. Furthermore, rebamipide protects against NSAID-induced gastrointestinal events [5]. Rebamipide up-regulates mucus glycoprotein synthesis and protects against oxygen radical-induced damage in gastric mucosa by inhibiting the production of oxygen radicals [6–8]. Recent studies showed that rebamipide also exerts protective effects for a variety of other tissues and cell types, including small intestine [9], umbilical vein endothelium [10], hepatocytes [11], mesangial cells [12], and corneal epithelial cells [13]. In recent studies, rebamipide inhibited production of pro-inflammatory cytokines, including TNF-α [10] and IL-8 [14], by suppressing activation of NF-κB transcription factor; down-regulated matrix metalloproteases (MMPs), which act as catabolic regulators of cartilage destruction [9,15]; and up-regulated the anabolic regulators, bFGF [16] and TGF-β [15]. So, given these potentially chondroprotective effects, we expected that rebamipide would have a protective effect on articular cartilage in the setting of OA.
Letter to the editor: are proton pump inhibitors suitable for prevention of non-steroidal anti-inflammatory drug/COX-2 selective non-steroidal anti-inflammatory drug-associated gastric ulcers?
Published in Expert Review of Clinical Pharmacology, 2019
Dr. Savarino et al. reported that prevention of non-steroidal anti-inflammatory drug (NSAID)/COX-2 selective NSAID (COXIB)-associated gastric ulcers was one of the evidence-based indications for proton pump inhibitors (PPIs) acknowledged by many scientific societies [1]. PPIs are not safe medicines. PPIs cause many serious adverse effects including lower gastrointestinal complications [2]. When NSAIDs are prescribed in combination with PPIs, upper gastrointestinal complications are decreased, however, lower gastrointestinal complications are increased. When NSAIDs are prescribed in combination with PPIs, adverse effects of PPIs are added to adverse effects of NSAIDs. Rebamipide protects NSAIDs-induced upper and lower gastrointestinal complications [2]. Rebamipide is available only in some Asian countries (Philippines, Thailand, Vietnam, the Republic of Korea, China, Cambodia, Indonesia, and Japan) and Egypt. I believe that PPIs should not be administered to prevent NSAID/COXIB-associated gastric ulcers at least in those countries. I believe that PPIs should not be administered as much as possible if other medicines are effective in other indications.