Abstract
Objective
The ideal medication for the treatment of acid-related diseases, e.g., peptic ulcers, stress-related gastric bleeding, functional dyspepsia, and gastroesophageal reflux disease, should have a rapid onset of action to promote hemostasis and relieve the symptoms. The aim of our study was to investigate the inhibitory effects on gastric acid secretion of a single oral administration of a proton pump inhibitor, omeprazole 20 mg, and an H2-receptor antagonist, roxatidine 75 mg.
Methods
Ten Helicobacter pylori-negative male subjects participated in this randomized, two-way crossover study. Intragastric pH was monitored continuously for 6 h after single oral administration of omeprazole 20 mg and roxatidine 75 mg. Each administration was separated by a 7-d washout period.
Results
During the 6-h study period, the average pH after administration of roxatidine was higher than that after administration of omeprazole (median: 4.45 vs. 2.65; P=0.0367). Also during the 6-h study period, a longer duration of maintenance at pH above 2, 5, and 6 was observed after administration of roxatidine 75 mg than after administration of omeprazole 20 mg (median: 90.6% vs. 55.2%, P=0.0284; 43.7% vs. 10.6%, P=0.0125; 40.3% vs. 3.3%, P=0.0125; respectively).
Conclusions
In Helicobacter pylori-negative healthy male subjects, oral administration of roxatidine 75 mg increased the intragastric pH more rapidly than that of omeprazole 20 mg.
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References
Abe, Y., Inamori, M., Togawa, J., Kikuchi, T., Muramatsu, K., Chiguchi, G., Kawamura, H., Kobayashi, N., Kirikoshi, H., Sakaguchi, T., et al., 2004. The comparative effects of single intravenous doses of omeprazole and famotidine on intragastric pH. J. Gastroenterol., 39(1):21–25. [doi:10.1007/s00535-003-1240-6]
Andersson, T., 1996. Pharmacokinetics, metabolism and interactions of acid pump inhibitors. Focus on omeprazole, lansoprazole and pantoprazole. Clin. Pharmacokinet., 31(1):9–28. [doi:10.2165/00003088-199631010-00002]
Arnestad, J.S., Kleveland, P.M., Waldum, H.L., 1997. In single doses ranitidine effervescent is more effective than lansoprazole in decreasing gastric acidity. Aliment. Pharmacol. Ther., 11(2):355–358. [doi:10.1046/j.1365-2036.1997.300000.x]
Burget, D.W., Chiverton, S.G., Hunt, R.H., 1990. Is there an optimal degree of acid suppression for healing of duodenal ulcers? A model of the relation-ship between ulcer healing and acid suppression. Gastroenterology, 99(2): 345–351.
Chassany, O., Bergmann, J.F., Simoneau, G., Elouaer-Blanc, L., Segrestaa, J.M., Caulin, C., 1996. The comparative effects of single intravenous doses of cimetidine, ranitidine, famotidine, and omeprazole on intragastric pH. Curr. Ther. Res., 57(3):159–169. [doi:10.1016/S0011-393X(96)80121-4]
Green, F.W.Jr., Kaplan, M.M., Curtis, L.E., Levine, P.H., 1978. Effect of acid and pepsin on blood coagulation and platelet aggregation. A possible contributor pro-longed gastroduodenal mucosal hemorrhage. Gastroenterology, 74(1):38–43.
de Morais, S.M., Wilkinson, G.R., Blaisdell, J., Meyer, U.A., Nakamura, K., Goldstein, J.A., 1994a. Identification of a new genetic defect responsible for the polymorphism of (S)-mephenytoin metabolism in Japanese. Mol. Pharmacol., 46(4):594–598.
de Morais, S.M., Wilkinson, G.R., Blaisdell, J., Nakamura, K., Meyer, U.A., Goldstein, J.A., 1994b. The major genetic defect responsible for the polymorphism of S-mephenytoin metabolism in humans. J. Biol. Chem., 269(22):15419–15422.
Ducrotté, P., Guillemot, F., Elouaer-Blanc, L., Hirschauer, C., Thorel, J.M., Petit, A., Hochain, P., Michel, P., Cortot, A., Colin, R., et al., 1994. Comparison of omeprazole and famotidine on esophageal pH in patients with moderate to severe esophagitis: a cross-over study. Am. J. Gastroenterol., 89(5):717–721.
Frank, W.O., Peace, K.E., Watson, M., Seaman, J.J., Szego, P.L., Braverman, A., Mico, B., Dickson, B., 1986. The effect of single intravenous doses of cimetidine or ranitidine on gastric secretion. Clin. Pharmacol. Ther., 40(6): 665–672. [doi:10.1038/clpt.1986.242]
Fullarton, G.M., Macdonald, A.M., Mann, S.G., McColl, K.E., 1991. Controlled study of the effects of intravenous famotidine on intragastric pH in bleeding peptic ulcers. Aliment. Pharmacol. Ther., 5(1):77–84. [doi:10.1111/j.1365-2036.1991.tb00008.x]
Furuta, T., Ohashi, K., Kosuge, K., Zhao, X.J., Takashima, M., Kimura, M., Nishimoto, M., Hanai, H., Kaneko, E., Ishizaki, T., 1999. CYP2C19 genotype status and effect of omeprazole on intragastric pH in humans. Clin. Pharmacol. Ther., 65(5):552–561. [doi:10.1016/S0009-9236(99)70075-5]
Hedenstrom, H., Alm, C., Kraft, M., Grahnen, A., 1997. Intragastric pH after oral administration of single doses of ranitidine effervescent tablets, omeprazole capsules and famotidine fast-dissolving tablets to fasting healthy volunteers. Aliment. Pharmacol. Ther., 11(6):1137–1141. [doi:10.1046/j.1365-2036.1997.00264.x]
Howden, C.W., Forrest, J.A., Reid, J.L., 1984. Effects of single and repeated doses of omeprazole on gastric acid and pepsin secretion in man. Gut, 25(7):707–710. [doi:10.1136/gut.25.7.707]
Hurlimann, S., Abbuhl, B., Inauen, W., Halter, F., 1994. Comparison of acid inhibition by either oral high-dose ranitidine or omeprazole. Aliment. Pharmacol. Ther., 8(2):193–201. [doi:10.1111/j.1365-2036.1994.tb00278.x]
Ichikawa, T., Ishihara, K., Kusakabe, T., Kawakami, T., Hotta, K., 1999. Stimulant effects of nitric oxide generator and roxatidine on mucin biosynthesis of rat gastric oxyntic mucosa. Life Sci., 65(4):PL41–PL46. [doi:10.1016/S0024-3205(99)00266-0]
Iida, H., Inamori, M., Akimoto, K., Mawatari, H., Endo, H., Nozaki, Y., Akiyama, T., Ikeda, T., Sakamoto, Y., Fujita, K., et al., 2009. Early effects of intravenous administrations of lansoprazole and famotidine on intragastric pH. Hepatogastroenterology, 56(90):551–554.
Inamori, M., Togawa, J., Iwasaki, T., Ozawa, Y., Kikuchi, T., Muramatsu, K., Chiguchi, G., Matsumoto, S., Kawamura, H., Abe, Y., et al., 2005. Early effects of lafutidine or rabeprazole on intragastric acidity: which drug is more suitable for on-demand use? J. Gastroenterol., 40(5): 453–458. [doi:10.1007/s00535-005-1569-0]
Ishizaki, T., Horai, Y., 1999. Cytochrome P450 and the metabolism of proton pump inhibitors: emphasis on rabeprazole. Aliment. Pharmacol. Ther., 13(s3):27–36. [doi:10.1046/j.1365-2036.1999.00022.x]
Jansen, J.B., Lundborg, P., Baak, L.C., Greve, J., Ohman, M., Stöver, C., Röhss, K., Lamers, C.B., 1988. Effect of single and repeated intravenous doses of omeprazole on pentagastrin stimulated gastric acid secretion and pharmacokinetics in man. Gut, 29(1):75–80. [doi:10.1136/gut.29.1.75]
Khoury, R.M., Katz, P.O., Castell, D.O., 1999. Post-prandial ranitidine is superior to post-prandial omeprazole in control of gastric acidity in healthy volunteers. Aliment. Pharmacol. Ther., 13(9):1211–1214. [doi:10.1046/j.1365-2036.1999.00587.x]
Kubota, T., Chiba, K., Ishizaki, T., 1996. Genotyping of S-mephenytoin 4′-hydroxylation in an extended Japanese population. Clin. Pharmacol. Ther., 60(6):661–666. [doi:10.1016/S0009-9236(96)90214-3]
Moore, J.G., 1991. Stress ulceration in the intensive care unit: use of H2-receptor antagonists. Aliment. Pharmacol. Ther., 5(s1):111–119.
Nakamura, M., Oda, M., Akiba, Y., 1995. Autoradiographic demonstration of lansoprazole uptake sites in rat antrum and colon. J. Clin. Gastroenterol., 20(s2):S8–S13. [doi:10.1097/00004836-199506002-00004]
Ohara, S., Hongo, M., Asaki, S., Sato, A., Shibuya, D., Sato, H., Motojima, T., Yamaguchi, N., Ohara, T., Tamura, T., et al., 1988. The effects of famotidine and omeprazole on 24-hour intragastric pH of normal subjects. Nippon Shokakibyo Gakkai Zasshi, 85(7):1353–1359 (in Japanese).
Saito, H., Sugiyama, A., Sato, T., 2000. An influence on the human gastric surface mucous gel layer of roxatidine acetate hydrochloride. Ulcer Res., 27(1):132–134 (in Japanese).
Saitoh, T., Fukushima, Y., Otsuka, H., Hirakawa, J., Mori, H., Asano, T., Ishikawa, T., Katsube, T., Ogawa, K., Ohkawa, S., 2002. Effects of rabeprazole, lansoprazole and omeprazole on intragastric pH in CYP2C19 extensive metabolizers. Aliment. Pharmacol. Ther., 16(10):1811–1817. [doi:10.1046/j.1365-2036.2002.01348.x]
Shirai, N., Furuta, T., Moriyama, Y., Okochi, H., Kobayashi, K., Takashima, M., Xiao, F., Kosuge, K., Nakagawa, K., Hanai, H., et al., 2001. Effects of CYP2C19 genotypic differences in the metabolism of omeprazole and rabeprazole on intragastric pH. Aliment. Pharmacol. Ther., 15(12):1929–1937. [doi:10.1046/j.1365-2036.2001.01108.x]
Smythe, M.A., Zarowitz, B.J., 1994. Changing perspectives of stress gastritis prophylaxis. Ann. Pharmacother., 28(9): 1073–1085.
Stothert, J.C.Jr., Dellinger, E.P., Simonowitz, D.A., Schilling, J.A., 1980. Gastric pH monitoring as a prognostic indicator for the prophylaxis of stress ulceration in the critically III. Am. J. Surg., 140(6):761–763. [doi:10.1016/0002-9610(80)90112-9]
Tarutani, M., Sakuma, H., Shiratsuchi, K., Mieda, M., 1985. Histamine H2-receptor antagonistic action of N-(3-[3-(1-piperidinylmethyl)phenoxy]propyl)acetoxyacetamide hydrochloride (TZU-0460). Arzneimittelforschung, 35(4): 703–706.
Watanabe, Y., Tsumura, H., Sasaki, H., Morimoto, T., 1990. The effects of intermittent and continuous intravenous infusion of famotidine on gastric acidity in patients with peptic ulcers. Clin. Ther., 12(6):534–546.
Wedlund, P.J., Aslanian, W.S., McAllister, C.B., Wilkinson, G.R., Branch, R.A., 1984. Mephenytoin hydroxylation deficiency in Caucasians: frequency of a new oxidative drug metabolism polymorphism. Clin. Pharmacol. Ther., 36(6):773–780. [doi:10.1038/clpt.1984.256]
Williams, M.P., Sercombe, J., Hamilton, M.I., Pounder, R.E., 1998. A placebo-controlled trial to assess the effects of 8 days of dosing with rabeprazole versus omeprazole on 24-h intragastric acidity and plasma gastrin concentrations in young healthy male subjects. Aliment. Pharmacol. Ther., 12(11):1079–1089. [doi:10.1046/j.1365-2036.1998.00418.x]
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Iida, H., Kato, S., Sekino, Y. et al. Early effects of oral administration of omeprazole and roxatidine on intragastric pH. J. Zhejiang Univ. Sci. B 13, 29–34 (2012). https://doi.org/10.1631/jzus.B1100078
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DOI: https://doi.org/10.1631/jzus.B1100078