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. 1988 Jan;29(1):75–80. doi: 10.1136/gut.29.1.75

Effect of single and repeated intravenous doses of omeprazole on pentagastrin stimulated gastric acid secretion and pharmacokinetics in man.

J B Jansen 1, P Lundborg 1, L C Baak 1, J Greve 1, M Ohman 1, C Stöver 1, K Röhss 1, C B Lamers 1
PMCID: PMC1433269  PMID: 3343017

Abstract

Single intravenous doses of 10, 20, 40, and 80 mg and repeated once daily intravenous doses of 10 and 20 mg omeprazole induced a powerful and long lasting inhibition of pentagastrin stimulated gastric acid secretion (PAO) in healthy male volunteers. Single intravenous doses of 10, 20, 40, and 80 mg omeprazole inhibited PAO by 30% (p less than 0.01), 45% (p less than 0.01), 61% (p less than 0.01), and 80% (p less than 0.01), respectively when measured 1.5 h after dose, and by 20% (NS), 27% (NS), 36% (p less than 0.01) and 59% (p less than 0.01), respectively when measured 24 h after dose. Six days after repeated once daily intravenous doses of 10 and 20 mg omeprazole, PAO was inhibited by 63% (p less than 0.01) and 82% (p less than 0.01), respectively when measured 1.5 h after dose, and by 32% (p less than 0.01) and 43% (p less than 0.01), respectively when measured 24 h after dose. The inhibition of PAO by 10 mg administered intravenously as a single bolus injection was comparable with the inhibition by 20 mg as a single oral dose. Repeated once daily administration of 10 mg intravenously and 20 mg orally also resulted in comparable reductions in PAO. The reduction in PAO after repeated once daily oral administration of 20 mg was comparable with the effect of a single intravenous dose of 40 mg. Terminal half lives were short, but significantly (p less than 0.05) prolonged after a single intravenous injection of 80 mg. Repeated once daily intravenous administration of 10 and 20 mg did not result in prolongation of terminal half lives. It is concluded that intravenous administration of omeprazole causes a potent and long acting inhibition of pentagastrin stimulated gastric acid secretion in man. Its potency is augmented after repeated once daily administration.

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Selected References

These references are in PubMed. This may not be the complete list of references from this article.

  1. Dammann H. G., Müller P., Seitz H. K., Simon B. Säuresekretionsverhalten unter einer mehrtägigen Omeprazol-Gabe. Schweiz Med Wochenschr. 1983 Jun 18;113(24):895–898. [PubMed] [Google Scholar]
  2. Fellenius E., Berglindh T., Sachs G., Olbe L., Elander B., Sjöstrand S. E., Wallmark B. Substituted benzimidazoles inhibit gastric acid secretion by blocking (H+ + K+)ATPase. Nature. 1981 Mar 12;290(5802):159–161. doi: 10.1038/290159a0. [DOI] [PubMed] [Google Scholar]
  3. Gustavsson S., Adami H. O., Löf L., Nyberg A., Nyrén O. Rapid healing of duodenal ulcers with omeprazole: double-blind dose-comparative trial. Lancet. 1983 Jul 16;2(8342):124–125. doi: 10.1016/s0140-6736(83)90114-9. [DOI] [PubMed] [Google Scholar]
  4. Howden C. W., Forrest J. A., Reid J. L. Effects of single and repeated doses of omeprazole on gastric acid and pepsin secretion in man. Gut. 1984 Jul;25(7):707–710. doi: 10.1136/gut.25.7.707. [DOI] [PMC free article] [PubMed] [Google Scholar]
  5. Jensen J. C., Gugler R. Inhibition of human liver cytochrome P-450 by omeprazole. Br J Clin Pharmacol. 1986 Mar;21(3):328–330. doi: 10.1111/j.1365-2125.1986.tb05199.x. [DOI] [PMC free article] [PubMed] [Google Scholar]
  6. Klinkenberg-Knol E. C., Jansen J. M., Festen H. P., Meuwissen S. G., Lamers C. B. Double-blind multicentre comparison of omeprazole and ranitidine in the treatment of reflux oesophagitis. Lancet. 1987 Feb 14;1(8529):349–351. doi: 10.1016/s0140-6736(87)91726-0. [DOI] [PubMed] [Google Scholar]
  7. Lagerström P. O., Persson B. A. Determination of omeprazole and metabolites in plasma and urine by liquid chromatography. J Chromatogr. 1984 Aug 10;309(2):347–356. doi: 10.1016/0378-4347(84)80042-0. [DOI] [PubMed] [Google Scholar]
  8. Lambers C. B., Lind T., Moberg S., Jansen J. B., Olbe L. Omeprazole in Zollinger-Ellison syndrome. Effects of a single dose and of long-term treatment in patients resistant to histamine H2-receptor antagonists. N Engl J Med. 1984 Mar 22;310(12):758–761. doi: 10.1056/NEJM198403223101205. [DOI] [PubMed] [Google Scholar]
  9. Lauritsen K., Rune S. J., Bytzer P., Kelbaek H., Jensen K. G., Rask-Madsen J., Bendtsen F., Linde J., Højlund M., Andersen H. H. Effect of omeprazole and cimetidine on duodenal ulcer. A double-blind comparative trial. N Engl J Med. 1985 Apr 11;312(15):958–961. doi: 10.1056/NEJM198504113121505. [DOI] [PubMed] [Google Scholar]
  10. Lind T., Cederberg C., Ekenved G., Haglund U., Olbe L. Effect of omeprazole--a gastric proton pump inhibitor--on pentagastrin stimulated acid secretion in man. Gut. 1983 Apr;24(4):270–276. doi: 10.1136/gut.24.4.270. [DOI] [PMC free article] [PubMed] [Google Scholar]
  11. McArthur K. E., Collen M. J., Maton P. N., Cherner J. A., Howard J. M., Ciarleglio C. A., Cornelius M. J., Jensen R. T., Gardner J. D. Omeprazole: effective, convenient therapy for Zollinger-Ellison syndrome. Gastroenterology. 1985 Apr;88(4):939–944. doi: 10.1016/s0016-5085(85)80011-1. [DOI] [PubMed] [Google Scholar]
  12. Walt R. P., Reynolds J. R., Langman M. J., Smart H. L., Kitchingman G., Somerville K. W., Hawkey C. J. Intravenous omeprazole rapidly raises intragastric pH. Gut. 1985 Sep;26(9):902–906. doi: 10.1136/gut.26.9.902. [DOI] [PMC free article] [PubMed] [Google Scholar]
  13. Wilson J. A., Boyd E. J., Wormsley K. G. Omeprazole inhibits nocturnal and pentagastrin-stimulated gastric secretion in man. Dig Dis Sci. 1984 Sep;29(9):797–801. doi: 10.1007/BF01318421. [DOI] [PubMed] [Google Scholar]

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