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Metiamide is a small molecule histamine H2 receptor antagonist developed by Smith Kline & French Laboratories as part of the search for effective anti-ulcer therapies[1][4][5]. It was derived from burimamide and served as an intermediate in the development of cimetidine. Metiamide competitively inhibits the histamine H2 receptor on gastric parietal cells, leading to reduced basal and stimulated gastric acid secretion[1][2][3]. It demonstrated significant efficacy in increasing peptic ulcer healing rates and reducing symptoms of acid-related disorders such as gastroesophageal reflux disease (GERD) and peptic ulcer disease[2][5]. However, its clinical use was discontinued due to unacceptable rates of agranulocytosis observed during trials. The drug also inhibits several hepatic CYP450 isoenzymes and can increase gastric bacterial flora. Its development directly led to safer alternatives like cimetidine.
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