Authors: Teyssen S.¹; Singer M.V.¹; Pfützer R.¹; Heinze H.²; Fischer R.²

Source: Clinical Drug Investigation, Volume 21, Number 4, 1 April 2001 , pp. 273-279(7)

Publisher: Adis International

Abstract:

Objectives: Development of tolerance (tachyphylaxis) has been observed during treatment with H receptor antagonists, but not with proton pump inhibitors. In the present study, the time-course of acid inhibition during repeated administration of pantoprazole was compared with that of ranitidine.

Methods and Study Participants: 20 healthy individuals were included in an open, randomised, two-period, crossover study. Each participant received pantoprazole 40mg or ranitidine 300mg for 28 days and vice versa, separated by a 28-day washout period. Intragastric 24-hour pH-metry as well as determination of serum gastrin levels were performed on days 1, 7 and 28 of each treatment period.

Results: Administration of pantoprazole led to an increase in median 24-hour pH from 1.6 (baseline) to 2.5 on day 1. In the case of ranitidine, median 24-hour pH increased from 1.6 (baseline) to 2.4. However, on day 7 of ranitidine administration, development of tolerance was evident; the median 24-hour pH decreased to 2.0 and remained at 1.9 until the end of the study. In contrast, pantoprazole effectively inhibited acid secretion and achieved a constant pH-elevation until day 28 (pH 3.6 and 3.7 on days 7 and 28, respectively). On days 7 and 28, the median 24-hour pH was significantly higher with pantoprazole than with ranitidine (p < 0.001). Pharmacodynamic tolerance was shown by a crossover analysis for ranitidine but not for pantoprazole (p < 0.01). Following administration of either ranitidine or pantoprazole, serum gastrin levels were moderately elevated.

Conclusion: Pantoprazole achieved a long-lasting inhibition of acid secretion, while tolerance was observed with ranitidine within 7 days of administration.

Keywords: Histamine H2 receptor antagonists, pharmacodynamic; Pantoprazole, pharmacodynamics; Proton pump inhibitors, pharmacodynamics; Ranitidine, pharmacodynamics

Document Type: Original article

Affiliations: 1: University Hospital of Heidelberg in Mannheim, Mannheim, Germany 2: Byk Gulden, Konstanz, Germany

Publication date: 2001-04-01

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