Lafutidine

Lafutidine is a histamine H₂ receptor antagonist with gastroprotective activity.¹ It inhibits histamine-induced cAMP production in CHO cells expressing human histamine H₂ receptors when used at a concentration of 10 nM. Intragastric administration of lafutidine (3, 10, and 30 mg/kg) reduces hemorrhagic esophageal lesion size and gastric acid secretion in a rat model of pyloric ligation-induced reflux esophagitis.² It prevents 5-fluorouracil-induced intestinal mucositis, diarrhea, and body weight loss in wild-type, but not Trpv1^-/- or sensory deafferented, mice when administered at doses ranging from 3 to 30 mg/kg.³ Lafutidine (10 mg/kg) also reduces indomethacin-induced antral ulcer size in wild-type, but not chemically-deafferented, rats.⁴

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1. Fukushima, Y., Otsuka, H., Ishikawa, M., et al. Potent and long-lasting action of lafutidine on the human histamine H2 receptor. Digestion 64(3), 155-160 (2001).

2. Nagahama, K., Yamato, M., Kato, S., et al. Protective effect of lafutidine, a novel H2-receptor antagonist, on reflux esophagitis in rats through capsaicin-sensitive afferent neurons. J. Pharmacol. Sci. 93(1), 55-61 (2003).

3. Sano, T., Utsumi, D., Amagase, K., et al. Lafutidine, a histamine H2 receptor antagonist with mucosal protective properties, attenuates 5-fluorouracil-induced intestinal mucositis in mice through activation of extrinsic primary afferent neurons. J. Physiol. Pharmacol. 68(1), 79-90 (2017).

4. Onodera, S., Shibata, M., Tanaka, M., et al. Gastroprotective mechanism of lafutidine, a novel anti-ulcer drug with histamine H2-receptor antagonistic activity. Arzneimittelforschung 49(6), 519-526 (1999).