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Rebamipide ophthalmic suspension for the treatment of dry eye syndrome: a critical appraisal

Authors Kashima T, Itakura H, Akiyama H, Kishi S

Received 3 January 2014

Accepted for publication 8 March 2014

Published 30 May 2014 Volume 2014:8 Pages 1003—1010

DOI https://doi.org/10.2147/OPTH.S40798

Checked for plagiarism Yes

Review by Single-blind

Peer reviewer comments 4


Tomoyuki Kashima,1 Hirotaka Itakura,1,2 Hideo Akiyama,1 Shoji Kishi1

1Department of Ophthalmology, Gunma University, School of Medicine, Maebashi, Gunma, Japan; 2Department of Ophthalmology, Maebashi Red Cross Hospital, Maebashi, Gunma, Japan

Abstract: Rebamipide was initially developed and approved for use in treating gastric ulcers and lesions associated with gastritis. Discovery of its ability to increase gastric mucin led to investigations of its effect on ocular surface mucin and the subsequent development for use in dry eye patients. Investigations have confirmed that rebamipide increases corneal and conjunctival mucin-like substances along with improving corneal and conjunctival injury. Clinically, rebamipide ophthalmic suspensions can effectively treat tear deficiency and mucin-caused corneal epithelial damage, and can restore the microstructure responsible for tear stability. Topical rebamipide has also been shown to be effective in treating other ocular surface disorders such as lagophthalmos, lid wiper epitheliopathy, and persistent corneal erosion. Rebamipide’s ability to modify epithelial cell function, improve tear stability, and suppress inflammation in the absence of any known major side effects suggest that it may be a beneficial first drug of choice for severe dry eye treatment and other ocular surface disorders. This review summarizes the history and development of this innovative dry eye treatment from its initial use as an effective stomach medication to its current use in the treatment of dry eye in Japan.

Keywords: quinolinone derivative, tear deficiency, ocular surface disorder, mucin secretion, Mucosta

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