Effect of lafutidine, a novel antiulcer agent, on healing and relapse of acetic acid-induced gastric ulcer in rats.

Onodera, Sadayoshi; Tanaka, Masato; Aoyama, Misao; Arai, Yoko; Shibata, Masahiro; Yamaura, Tetsuaki; Ohnishi, Haruo

doi:10.1254/fpj.111.167

Cited by 3 publications

(1 citation statement)

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“…Like the effects of capsaicin, the gastroprotective action of lafutidine was depressed or abolished by treatment with tetrodotoxin or CGRP 8 – 37 , or chemical defunctionalization of afferent nerves (Onodera et al ., 1995; 1999a), indicating that capsaicin sensitive nerves contribute significantly to the mechanisms underlying the actions of lafutidine. Additionally, lafutidine accelerated repair of chronic gastric or duodenal ulcer in rats and the recurrence rate of chronic gastric ulcer, induced by acetic acid or treatment of the serosa‐searing with a hot metal bar, was low (Ajioka et al ., 2000; Onodera et al ., 1998; 1999b). These observations suggest that the effects of lafutidine are due mostly to the activation of capsaicin sensitive afferent nerves.…”

Section: Introductionmentioning

confidence: 99%

Sensitizing effects of lafutidine on CGRP‐containing afferent nerves in the rat stomach

Nishihara

Nozawa

Nakano

et al. 2002

British J Pharmacology

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1 Capsaicin sensitive a erent nerves play an important role in gastric mucosal defensive mechanisms. Capsaicin stimulates a erent nerves and enhances the release of calcitonin gene-related peptide (CGRP), which seems to be the predominant neurotransmitter of spinal a erents in the rat stomach, exerting many pharmacological e ects by a direct mechanism or indirectly through second messengers such as nitric oxide (NO). 2 Lafutidine is a new type of anti-ulcer drug, possessing both an antisecretory e ect, exerted via histamine H 2 receptor blockade, and gastroprotective activities. Studies with certain antagonists or chemical dea erentation techniques suggest the gastroprotective actions of lafutidine to be mediated by capsaicin sensitive a erent nerves, but this is an assumption based on indirect techniques. In order to explain the direct relation of lafutidine to a erent nerves, we conducted the following studies.3 We determined CGRP and NO release from rat stomach and speci®c [ 3 H]-resiniferatoxin (RTX) binding to gastric vanilloid receptor subtype 1 (VR1), which binds capsaicin, using EIA, a microdialysis system and a radioreceptor assay, respectively. 4 Lafutidine enhanced both CGRP and NO release from the rat stomach induced by a submaximal dose of capsaicin, but had no e ect on speci®c [ 3 H]-RTX and capsaicin binding to VR1. 5 In conclusion, our ®ndings demonstrate that lafutidine modulates the activity of capsaicin sensitive a erent nerves in the rat stomach, which may be a key mechanism involved in its gastroprotective action.

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Section: Introductionmentioning

confidence: 99%

Sensitizing effects of lafutidine on CGRP‐containing afferent nerves in the rat stomach

Nishihara

Nozawa

Nakano

et al. 2002

British J Pharmacology

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Simultaneous improvement in dissolution profile and content uniformity of lafutidine through co-inclusion in urea

Dhall

Мадан

2015

J Incl Phenom Macrocycl Chem

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Pharmacological and therapeutic properties of lafutidine (stogar and protecadin), a novel histamine H2 receptor antagonist with gastroprotective activity.

Tanaka¹,

Banba²,

Joko³

et al. 2001

Folia Pharmacol. Jpn.

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Potent antisecretory agents, such as histamine H2-receptor antagonists and proton pump inhibitors, have achieved great improvement in peptic ulcer therapy. It has, however, been reported that incidence of ulcer relapse is high after discontinuation of these drugs. Insufficient efficacy against NSAID-induced ulcers is also critical. Lafutidine is a novel histamine H2 antagonist with gastroprotective activity. Lafutidine exhibited potent and long-lasting H2 antagonism and prolonged antisecretion. In addition, lafutidine showed a gastroprotective effect against noxious agents-induced gastric mucosal damage through capsaicin-sensitive afferent nerves. Lafutidine showed antiulcer activities against acute ulcer models, prevented gastric ulcer relapse of acetic ulcer, and accelerated the healing of indomethacin-induced antral ulcers in rats. These results suggest the advantage of the combined antisecretory and gastroprotective activities. In clinical studies, lafutidine showed prolonged antisecretion, healing effect against gastric and duodenal ulcers and gastritis, and its potency was equal or superior to that of conventional H2 antagonists. Additionally, lafutidine induced a high transition rate to the E0 stage determined by endoscopical ultrasonography, suggesting the high quality of ulcer healing. Furthermore, effectiveness of lafutidine against NSAIDs-induced ulcer was high. From these results, lafutidine is equal or superior to conventional H2 antagonists in antiulcer potency, and it may be useful for the prevention of ulcer relapse and or treatment of NSAIDs-induced gastroduodenal damage.

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Effect of lafutidine, a novel antiulcer agent, on healing and relapse of acetic acid-induced gastric ulcer in rats.

Cited by 3 publications

References 0 publications

Sensitizing effects of lafutidine on CGRP‐containing afferent nerves in the rat stomach

Sensitizing effects of lafutidine on CGRP‐containing afferent nerves in the rat stomach

Simultaneous improvement in dissolution profile and content uniformity of lafutidine through co-inclusion in urea

Pharmacological and therapeutic properties of lafutidine (stogar and protecadin), a novel histamine H2 receptor antagonist with gastroprotective activity.

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