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

Tanaka, Masato; Banba, Masaru; Joko, Akihiro; Moriyama, Yasutoshi

doi:10.1254/fpj.117.377

Cited by 9 publications

(4 citation statements)

References 9 publications

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“…The gastrointestinal-protective action of lafutidine has been widely reported. Lafutidine has a powerful effect in suppressing the secretion of gastric acid via its H2-receptor antagonistic action (18), and acts to increase gastric mucus via capsaicin-sensitive sensory nerves (19). In basic experiments using rats with sodium dextran sulphate-induced ulcerative colitis, a comparison of lafutidine and famotidine to treat 5-fluorouracil-induced intestinal mucositis showed that rates of diarrhoea and weight loss were significantly lower in the lafutidine group (8).…”

Section: Discussionmentioning

confidence: 99%

Effect of Concomitant Lafutidine on Adjuvant S-1 for Head and Neck Cancer: A Comparative Study

et al. 2021

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Background/Aim: This study evaluated the utility of the histamine H2-receptor antagonist lafutidine in patients taking oral fluorouracil (S-1) for head and neck squamous cell carcinoma (HNSCC), by comparing patients with and without concomitant lafutidine. Patients and Methods: Study subjects comprised 63 patients who received adjuvant S-1 following curative resection of HNSCC at our institutions between August 1, 2013 and December 31, 2019. The primary endpoint was the completion rate of S-1 therapy. Results: For the lafutidine-treated group, the median completion rate was significantly greater (94.4% vs. 24.6%, p=0.01), and progression-free and overall survival were both significantly prolonged compared to the non-lafutidine group. In terms of adverse events, the incidence of diarrhoea was significantly reduced (p<0.00189) in the lafutidinetreated group. Conclusion: Taking lafutidine during S-1 treatment appeared to reduce gastrointestinal disturbance and increased the S-1 completion rate, improving both progression-free and overall survival as a result.Curative treatment for locally advanced head and neck cancer has conventionally involved a combination of surgery and radiotherapy (1). Because the head and neck region not only carries out functions that play crucial roles in daily life, but is also an important site cosmetically, recent years have seen attempts to use concurrent chemoradiotherapy as curative treatment, with the goal of sparing organs and their functions.In cases of advanced cancer, however, the prognosis cannot be considered satisfactory, even for patients who have undergone curative therapy, and adjuvant chemotherapy following curative treatment is reportedly useful (1, 2).Two large-scale Japanese studies of adjuvant chemotherapy for advanced head and neck cancer have been reported. The first, a comparative trial conducted by Tsukada et al., administered tegafur and uracil (UFT) to patients for 1 year following curative therapy for head and neck cancer (3). The study incIuded patients with I-IV primary squamous cell carcinoma of the head and neck with no distant metastasis. Although both the 3-year overall survival (OS) rate (UFT group, 77.9%; untreated group, 72.9%) and 3-year relapse-free survival rate (UFT group, 73.4%; untreated group, 66.2%) tended to be better in the UFT-treated group, the difference was not significant. The distant recurrence rate, however, was significantly lower in the UFT group (7.9% vs. 14.6%, respectively; p=0.034), suggesting that UFT is useful as adjuvant chemotherapy.The second large-scale study was the ACTS-HNC study by Tsukahara et al., as a comparative trial of S-1 and UFT (4). Both 3-year disease-free survival and 3-year relapse-free survival tended to be better in the S-1-treated group, and OS was significantly better (p=0.022). However, the incidence of mucositis/stomatitis as an adverse event was significantly higher in the S-1 group than in the UFT group. The 1-year completion rate for S-1 was low, at 43%, and control of adverse events was conjectured ...

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Section: Discussionmentioning

confidence: 99%

Effect of Concomitant Lafutidine on Adjuvant S-1 for Head and Neck Cancer: A Comparative Study

et al. 2021

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“…It induces a high transition rate to the EO stage, an indication of efficient ulcer healing as determined by endoscopical ultrasonography, the healing of IM induced antral ulcers and proved highly effective against NSAID induced ulcer and gastritis. 312 Lansoprazole, a proton pump inhibitor having inhibitory action on acid secretion in pylorus ligated rats, is not dependent on c.s nerves, NO, or PGs. 248 When administered directly into the gastric chamber its increase of both gmbf and NO is reversed by L-NAME.…”

Section: Downloaded By [Florida Atlantic University] At 11:00 18 Novementioning

confidence: 99%

Capsaicin and Gastric Ulcers

2006

Critical Reviews in Food Science and Nutrition

108

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In recent years, infection of the stomach with the organism Helicobacter Pylori has been found to be the main cause of gastric ulcers, one of the common ailments afflicting humans. Excessive acid secretion in the stomach, reduction in gastric mucosal blood flow, constant intake of non-steroid anti-inflammatory drugs (NSAIDS), ethanol, smoking, stress etc. are also considered responsible for ulcer formation. The prevalent notion among sections of population in this country and perhaps in others is that "red pepper" popularly known as "Chilli," a common spice consumed in excessive amounts leads to "gastric ulcers" in view of its irritant and likely acid secreting nature. Persons with ulcers are advised either to limit or avoid its use. However, investigations carried out in recent years have revealed that chilli or its active principle "capsaicin" is not the cause for ulcer formation but a "benefactor." Capsaicin does not stimulate but inhibits acid secretion, stimulates alkali, mucus secretions and particularly gastric mucosal blood flow which help in prevention and healing of ulcers. Capsaicin acts by stimulating afferent neurons in the stomach and signals for protection against injury causing agents. Epidemiologic surveys in Singapore have shown that gastric ulcers are three times more common in the "Chinese" than among Malaysians and Indians who are in the habit of consuming more chillis. Ulcers are common among people who are in the habit of taking NSAIDS and are infected with the organism "Helicobacter Pylori," responsible for excessive acid secretion and erosion of the mucosal layer. Eradication of the bacteria by antibiotic treatment and avoiding the NSAIDS eliminates ulcers and restores normal acid secretion.

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“…1 Insufficient efficacy against NSAID-induced ulcers is also critical. 2 Lafutidine, (š)-2-(furfurylsulfinyl)-N-(4-[4-(piperidinomethyl)-2-pyridyl] oxy-(Z)-2-butenyl) acetamide, a newly synthesized antiulcer drug, was developed as a second-generation H 2 -receptor antagonist with an increased action on the gastric mucosal-defensive capacity. It has been shown to exhibit potent gastroprotective activity in addition to gastric acid antisecretory effect.…”

Section: Introductionmentioning

confidence: 99%

“…It may be useful for the prevention of ulcer relapse and treatment of NSAID-induced gastroduodenal damage. 2 The therapeutic dose of lafutidine given orally every day is only 10 or 20 mg, so the concentration of lafutidine in human plasma is relatively low, and a sensitive analytical method is needed for its determination in plasma. A high-performance liquid chromatographic method using UV detection has previously been established for the determination of lafutidine in human plasma.…”

Section: Introductionmentioning

confidence: 99%

Determination of lafutidine in human plasma by high‐performance liquid chromatography‐electrospray ionization mass spectrometry: application to a bioequivalence study

et al. 2005

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A rapid, sensitive and specific high-performance liquid chromatography-electrospray ionization mass spectrometry (LC/ESI-MS) method was developed and validated for the first time to determine the concentration of lafutidine in human plasma. After the addition of diazepam (the internal standard, IS) and 1 M sodium hydroxide solution to 0.5-ml plasma sample, lafutidine was extracted from plasma with n-hexane : isopropanol (95 : 5, v/v). The organic layer was evaporated and the residue was redissolved in 200-microl mobile phase. The analyte was chromatographically separated on a prepacked Shimadzu Shim-pack VP-ODS C(18) column (250 x 2.0 mm i.d.) using a mixture of methanol-water (20 mM CH(3)COONH(4)) = 80 : 20 (v/v) as mobile phase. Detection was performed on a single quadrupole mass spectrometer using an electrospray ionization interface and the selected-ion monitoring (SIM) mode. The method showed excellent linearity (r = 0.9993) over the concentration range of 5-400 ng/ml and had good accuracy and precision. The within- and between-batch precisions were within 10% relative standard deviation. The limit of detection was 1 ng/ml. The validated LC/ESI-MS method has been successfully applied to the bioequivalence study of lafutidine in 24 healthy male Chinese volunteers.

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

Cited by 9 publications

References 9 publications

Effect of Concomitant Lafutidine on Adjuvant S-1 for Head and Neck Cancer: A Comparative Study

Effect of Concomitant Lafutidine on Adjuvant S-1 for Head and Neck Cancer: A Comparative Study

Capsaicin and Gastric Ulcers

Determination of lafutidine in human plasma by high‐performance liquid chromatography‐electrospray ionization mass spectrometry: application to a bioequivalence study

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