H2-Receptor Antagonist

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R. P. Walt - One of the best experts on this subject based on the ideXlab platform.

  • The effects of roxatidine acetate (HOE-760) on 24-hour intragastric acidity in healthy volunteers: comparison with ranitidine and placebo.
    Alimentary pharmacology & therapeutics, 2007
    Co-Authors: H S Merki, L Witzel, D. Kaufmann, M. Kempf, V. Müssig, J. Neumann, E. Scheurle, J. Röhmel, R. P. Walt
    Abstract:

    SUMMARY In a series of double-blind randomized studies in normal volunteers using continuous intragastric pH monitoring, the effects of different dosage regimens of roxatidine, a new H2-Receptor Antagonist, were compared with placebo and ranitidine. Roxatidine acetate, 75 mg twice daily, decreased median 24 h gastric acidity from pH 1.6 to 3.2 and median nocturnal acidity from 1.5 to 3.0. Roxatidine acetate, 150 mg at bedtime, raised median 24 pH of the same 17 subjects to 2.4 and nocturnal pH to 5.9. In another series of experiments, 150 mg roxatidine acetate at bedtime was as effective as ranitidine 300 mg nocte raising median nocturnal pH (14 volunteers) from 1.4 to 6.65 compared to 6.7, respectively. However, when drugs were taken after the evening meal (post cenam nocte, pcn) roxatidine acetate 150 mg was less potent than ranitidine 300 mg with median night-time pH rising from 1.3 to 3.2 and 4.0, respectively, in 28 volunteers. Roxatidine acetate 300 mg pcn raised the pH to 4.9 suggesting that roxatidine is 1–2 times as potent as ranitidine, on a milligram-for-milligram basis.

Amir Haider - One of the best experts on this subject based on the ideXlab platform.

  • In vitro Interaction of Fexofenadine with H2 Receptor Antagonist
    Asian Journal of Research in Chemistry, 2012
    Co-Authors: Hina Shahnaz, M Saeed Arayne, Najma Sultana, Amir Haider
    Abstract:

    Fexofenadine is a second generation H1-receptor Antagonist, much widely used due to its non-sedative effects. The in vitro availability of fexofenadine in the presence of H2-Receptor Antagonist (cimetidine, ranitidine and famotidine) was studied on a BP 2005 dissolution test apparatus to observe the kinetics and energies of fexofenadine in the presence of H2-Receptor Antagonist (cimetidine, ranitidine and famotidine). These studies were carried out in buffers of pH 2, 4 (simulated gastric juice), 7.4 (blood pH) and 9 (simulated intestinal juice) at 37°C and at elevated temperatures. These studies showed that all H2-Receptor Antagonist (cimetidine, ranitidine and famotidine) interact to fexofenadine. Moreover, these interactions were not temperature dependent but pH dependent.

C C Lim - One of the best experts on this subject based on the ideXlab platform.

  • roxatidine versus ranitidine in the treatment of duodenal ulcers a randomized double blind controlled multicentre study in singapore
    Journal of Gastroenterology and Hepatology, 1995
    Co-Authors: K M Fock, J Y Kang, K A Gwee, C C Lim
    Abstract:

    Roxatidine acetate, a new H2 receptor Antagonist, was compared with ranitidine in the treatment of duodenal ulcers in a double-blind multicentre study. Eighty-four patients with endoscopically proven duodenal ulcer were randomized to receive 150 mg roxatidine acetate or 300 mg ranitidine at bedtime. Repeat endoscopy was performed after 4 weeks (25-33 days) and if the ulcer had not healed, another endoscopy was performed after a further 4 weeks of treatment. Using per protocol analysis 73.6% of ulcers treated with roxatidine healed at 4 weeks compared to 72.2% of ulcers treated with ranitidine (P = NS). The healing rates at 8 weeks were 92% with roxatidine and 83.3% with ranitidine (P = NS). Using equivalence tests, the healing rate of roxatidine was found to be equivalent to that of ranitidine within a 20% region. Roxatidine users took significantly less antacids than ranitidine users (P < 0.05). There were no significant adverse effects due to roxatidine or ranitidine. Roxatidine is a safe effective drug in the treatment of duodenal ulcers with a healing rate comparable to that of ranitidine.

H S Merki - One of the best experts on this subject based on the ideXlab platform.

  • The effects of roxatidine acetate (HOE-760) on 24-hour intragastric acidity in healthy volunteers: comparison with ranitidine and placebo.
    Alimentary pharmacology & therapeutics, 2007
    Co-Authors: H S Merki, L Witzel, D. Kaufmann, M. Kempf, V. Müssig, J. Neumann, E. Scheurle, J. Röhmel, R. P. Walt
    Abstract:

    SUMMARY In a series of double-blind randomized studies in normal volunteers using continuous intragastric pH monitoring, the effects of different dosage regimens of roxatidine, a new H2-Receptor Antagonist, were compared with placebo and ranitidine. Roxatidine acetate, 75 mg twice daily, decreased median 24 h gastric acidity from pH 1.6 to 3.2 and median nocturnal acidity from 1.5 to 3.0. Roxatidine acetate, 150 mg at bedtime, raised median 24 pH of the same 17 subjects to 2.4 and nocturnal pH to 5.9. In another series of experiments, 150 mg roxatidine acetate at bedtime was as effective as ranitidine 300 mg nocte raising median nocturnal pH (14 volunteers) from 1.4 to 6.65 compared to 6.7, respectively. However, when drugs were taken after the evening meal (post cenam nocte, pcn) roxatidine acetate 150 mg was less potent than ranitidine 300 mg with median night-time pH rising from 1.3 to 3.2 and 4.0, respectively, in 28 volunteers. Roxatidine acetate 300 mg pcn raised the pH to 4.9 suggesting that roxatidine is 1–2 times as potent as ranitidine, on a milligram-for-milligram basis.

Seymour M. Sabesin - One of the best experts on this subject based on the ideXlab platform.

  • Safety issues relating to long-term treatment with histamine H2-Receptor Antagonists
    Alimentary Pharmacology & Therapeutics, 2007
    Co-Authors: Seymour M. Sabesin
    Abstract:

    H2-Receptor Antagonist therapy is associated with a low incidence of adverse reactions. Adverse events reported in clinical trials of ranitidine in daily doses of up to 1200 mg include headache, tiredness and mild gastrointestinal disturbances, but the incidence is similar to or less than that for placebo. High doses of cimetidine (> 5 g/day) can cause reversible impotence or gynaecomastia. While ranitidine exhibits no clinically significant drug-drug interactions, cimetidine interacts with many drugs metabolized by cytochrome P450. In contrast to ranitidine and cimetidine, where safety data are available for up to 10 years of continuous therapy, experience with famotidine and nizatidine is limited. The safety of long-term H2-Receptor Antagonist therapy needs to be considered in relation to the potential consequences of prolonged acid suppression, including the risk of proliferation of gastric flora and the risk of developing enterochromaffin-like cell hyperplasia, which could in turn, theoretically, lead to gastric malignancy. Such problems have not been observed in patients during long-term therapy at low or full doses of H2-Receptor Antagonists. Standard doses of currently available H2-Receptor Antagonists permit acid secretion in response to food and other stimuli, and this daily acid tide prevents persistent bacterial colonization.