H2 Receptor Antagonists

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

  • Trends in prescribing H2Receptor Antagonists and proton pump inhibitors in primary care
    Alimentary pharmacology & therapeutics, 1998
    Co-Authors: Martin, Lim, Kerry, Hilton
    Abstract:

    Background: H2-Receptor Antagonists and proton pump inhibitors account for approximately 15% of primary care prescribing costs in the UK. Aim: To examine the use of antisecretory drugs in primary care between October 1991 and September 1996. Method: Analysis of prescribing data from an ongoing postal survey performed every 3 months on a rolling quota of 250 UK general practitioners (GPs), identified from a representative sampling frame of 1000 GPs. Results: There were 8811 new courses of proton pump inhibitors and 11 948 new courses of H2-Receptor Antagonists during this study. The number of new prescriptions for proton pump inhibitors increased by 174.5%, but decreased for H2-Receptor Antagonists by 12.5%. Proton pump inhibitors were mostly prescribed for reflux disease (52.7%) and H2-Receptor Antagonists for non-specific dyspepsia (43.6%). Proton pump inhibitors (14.1%) were less likely to be stopped than H2-Receptor Antagonists (35.3%) overall, and they were less likely to be stopped because of perceived ineffectiveness (5.3%) than H2-Receptor Antagonists (23.8%). The rate of stopping treatment because of side-effects was about 3% for both classes of drug. Conclusions: Prescribing of proton pump inhibitors has increased sharply each year since 1991. One reason may be that GPs perceive proton pump inhibitors to be more effective than H2-Receptor Antagonists.

E. C. Klinkenberg-knol - One of the best experts on this subject based on the ideXlab platform.

  • Treatment of reflux oesophagitis with H2-Receptor Antagonists.
    Scandinavian Journal of Gastroenterology, 2009
    Co-Authors: S. G. M. Meuwissen, E. C. Klinkenberg-knol
    Abstract:

    The important therapeutic value of H2-Receptor Antagonists for the treatment of patients with reflux oesophagitis has been demonstrated beyond doubt. A large number of patients have been treated with cimetidine or ranitidine in controlled as well as open short-term studies. Mild to moderately severe reflux oesophagitis heals effectively when H2-Receptor Antagonists are prescribed for a sufficient time period, preferentially 12 weeks. The more severe forms of oesophagitis, however, need more profound acid suppression, with potent H2-Receptor Antagonists, addition of prokinetic agents, or treatment with H+/K + ATP-ase Antagonists. Omeprazole has proven to be of high efficacy, particularly in the management of severe reflux oesophagitis. Data on long-term treatment with H2-Receptor Antagonists, to prevent recurrences after healing, are not reassuring: long-term low-dose H2-Receptor antagonist therapy is not effective, and trials should be undertaken with higher doses of H2-Receptor Antagonists, more potent a...

J. R. Wood - One of the best experts on this subject based on the ideXlab platform.

  • H2-Receptor Antagonists in the Treatment of Reflux Oesophagitis
    Scandinavian Journal of Gastroenterology, 2009
    Co-Authors: E. J. S. Boyd, J. R. Wood
    Abstract:

    H2-Receptor Antagonists are useful for relief of symptoms and in the healing of reflux oesophagitis. The therapeutic response is related to the initial degree of severity of oesophagitis, and standard doses of H2-Receptor Antagonists are only reliably effective in the treatment of mild disease. Pharmacodynamic studies indicate that in patients with more severe grades of oesophagitis standard doses of H2-Receptor Antagonists may be less effective at inhibiting gastric secretion and reducing total reflux time. This is associated with a suboptimal response to therapy. In non-responders to standard dose therapy, 24-h intra-oesophageal pH profiles can be normalized by increasing the dose of H2-Receptor antagonist. A high-dose ranitidine regimen (300 mg four times daily) markedly improves healing of oesophagitis and symptom relief compared with standard therapy. Reflux oesophagitis relapses rapidly after cessation of medical therapy. It appears that continuous treatment with doses similar to those required to a...

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

  • tolerance during dosing with H2 Receptor Antagonists an overview
    Scandinavian Journal of Gastroenterology, 1992
    Co-Authors: Clive H Wildersmith, H. S. Merki
    Abstract:

    Diminution of antisecretory effect of H2-Receptor Antagonists with repeated oral dosing, termed tolerance, has been established in healthy volunteers. Anecdotal evidence indicates the development of tolerance with intravenous dosing. These findings demonstrate that tolerance may be clinically relevant in diseases where tight control of acidity is required. Patients with duodenal ulcer disease, however, do not develop significant tolerance, according to the sparse investigations available. Tolerance will, at most, only be of minor clinical significance in failures of DU to heal. The mechanisms implicated in the development of tolerance remain unclear.

  • tolerance to oral H2 Receptor Antagonists
    Digestive Diseases and Sciences, 1990
    Co-Authors: Clive H Wildersmith, T. Ernst, M. Gennoni, B. Zeyen, F. Halter, H. S. Merki
    Abstract:

    The acid-inhibitory action of H2-Receptor Antagonists was shown to decrease after one to two weeks of dosing in healthy volunteers. This tolerance was evaluated in three randomized, placebo-controlled trials with the H2-Receptor Antagonists famotidine, 40 mg given after the evening meal for 28 days; ranitidine, 300 mg four times a day for seven days followed by 300 mg at night until day 28; and ranitidine, 300 mg three times a day vs 300 mg at night for 14 days. Continuous 24-hr pH monitoring with glass electrodes was performed under fed conditions. The median 24-hr pH decreased from 3.2 on day 1 with famotidine 40 mg to 1.9 on day 28 (P<0.0012). After seven days of dosing with ranitidine 300 mg four times a day the median 24-hr pH dropped from 5.0 on day 1 to 3.0 on day 7 (P<0.001) and then to 2.2 with ranitidine 300 mg at night on day 28. With ranitidine 300 mg three times a day the median 24-hr pH fell from 4.3 on day 1 to 2.4 on day 14 (P< 0.0005). With ranitidine 300 mg at night the respective pH values were 2.5 and 1.8 (P< 0.003). Tolerance to H2-Receptor Antagonists given in a single evening dose was only evident during the night, whereas tolerance occurred throughout the day and night with the three- and four-times-a-day regimens. A large increase in the interindividual variability of pH response was seen during the nighttime.

  • Tolerance to oral H2-Receptor Antagonists.
    Digestive diseases and sciences, 1990
    Co-Authors: Clive H. Wilder-smith, T. Ernst, M. Gennoni, B. Zeyen, F. Halter, H. S. Merki
    Abstract:

    The acid-inhibitory action of H2-Receptor Antagonists was shown to decrease after one to two weeks of dosing in healthy volunteers. This tolerance was evaluated in three randomized, placebo-controlled trials with the H2-Receptor Antagonists famotidine, 40 mg given after the evening meal for 28 days; ranitidine, 300 mg four times a day for seven days followed by 300 mg at night until day 28; and ranitidine, 300 mg three times a day vs 300 mg at night for 14 days. Continuous 24-hr pH monitoring with glass electrodes was performed under fed conditions. The median 24-hr pH decreased from 3.2 on day 1 with famotidine 40 mg to 1.9 on day 28 (P

  • loss of acid suppression during dosing with H2 Receptor Antagonists
    Alimentary Pharmacology & Therapeutics, 1990
    Co-Authors: Clive H Wildersmith, T. Ernst, M. Gennoni, B. Zeyen, F. Halter, L. Varga, J J Roehmel, H. S. Merki
    Abstract:

    The suppression of intragastric acidity with H2-Receptor Antagonists may diminish with repeated administration. To assess the degree and dose-dependence of this tolerance after short-term dosing, two doses of the H2-Receptor Antagonists, ranitidine (300 mg nocte or q.d.s.) and sufotidine (300 mg or 600 mg b.d.), were given to healthy volunteers for 1 and 2 weeks, respectively. After 1 and 7 days of dosing with ranitidine 300 mg q.d.s. the median 24-h and night-time pH, measured by continuous 24-h pH-metry, dropped from 3.7 to 2.2 and 5.8 to 3.2, respectively (P less than 0.0001 for both). The decline in median pH with ranitidine 300 mg nocte was only significant during the night (from 4.1 to 2.9) (P less than 0.04). There was little change in plasma gastrin concentrations between days 1 and 7 with either dosage. With sufotidine 300 mg b.d. and 600 mg b.d. for 1 and 14 days, the median 24-h pH fell from 3.7 to 2.1 and from 4.6 to 2.6, respectively (P less than 0.0001). The equivalent medians for the night decreased from 6.3 to 2.3 and from 6.6 to 3.1 (P less than 0.0001). Gastrin concentrations did not change after 14 days of dosing with sufotidine 300 mg b.d., but increased significantly during dosing with sufotidine 600 mg b.d. (P less than 0.001). Significant tolerance developed in 7-14 days and it seemed to show some dose relationship. The mechanisms behind tolerance and the role of gastrin are discussed, but remain unclear.

J G Moore - One of the best experts on this subject based on the ideXlab platform.

  • Stress ulceration in the intensive care unit: use of H2-Receptor Antagonists.
    Alimentary Pharmacology & Therapeutics, 2007
    Co-Authors: J G Moore
    Abstract:

    SUMMARY H2-Receptor antagonist drug therapy is the mainstay of peptic ulcer treatment in the USA. About 75 % of patients in intensive care units receive parenteral H2-Antagonists. The rationale for their use is that parenteral H2-Antagonists offer about a four-fold protective effect compared with placebo against significant upper gastrointestinal haemorrhage. Parenteral administration of H2-Receptor Antagonists appears to be preferred to oral antacid or sucralfate regimens because of ease of administration and, perhaps, lower treatment costs. Recommended dosage schedules for intravenously administered H2-Receptor Antagonists are at fixed intervals, 6- to 8-h intervals for cimetidine and ranitidine and 12-h intervals for famotidine. These dosage schedules assume a fixed dose-response relationship (i.e. a given dose of H2-antagonist results in equivalent acid suppression throughout the circadian, or 24-h, period). However, human basal gastric acid secretion exhibits circadian variation, with peak rates occurring during the evening hours. Recent evidence from 24-h continuous intragastric pH studies in fasting patients with healed duodenal ulcer suggests that larger doses of intravenous H2-Antagonists are required in the evening than in the morning to achieve equivalent acid suppression. These findings are consistent with a changing H2-antagonist dose/acid-inhibiting response over the circadian period. Continuous infusion has the advantage of providing consistent and sustained suppression of gastric acid secretion in patients at risk for stress ulceration. Results of a double-blind, randomized, crossover study indicated that equally effective suppression of acidity and time-to-onset of pharmacological effect can be achieved with and without priming bolus doses of ranitidine, and presumably other H2-Receptor Antagonists as well. Furthermore, continuous intravenous H2-antagonist therapy, compared with intravenous bolus administration, appears to offer more effective control of 24-h pH at a reduced cost. These cost savings may be augmented by administration of the H2-antagonist with the patient's total parenteral nutrition.

  • Stress ulceration in the intensive care unit: use of H2-Receptor Antagonists.
    Alimentary pharmacology & therapeutics, 1991
    Co-Authors: J G Moore
    Abstract:

    H2-Receptor antagonist drug therapy is the mainstay of peptic ulcer treatment in the USA. About 75% of patients in intensive care units receive parenteral H2-Antagonists. The rationale for their use is that parenteral H2-Antagonists offer about a four-fold protective effect compared with placebo against significant upper gastrointestinal haemorrhage. Parenteral administration of H2-Receptor Antagonists appears to be preferred to oral antacid or sucralfate regimens because of ease of administration and, perhaps, lower treatment costs. Recommended dosage schedules for intravenously administered H2-Receptor Antagonists are at fixed intervals, 6- to 8-h intervals for cimetidine and ranitidine and 12-h intervals for famotidine. These dosage schedules assume a fixed dose-response relationship (i.e. a given dose of H2-antagonist results in equivalent acid suppression throughout the circadian, or 24-h, period). However, human basal gastric acid secretion exhibits circadian variation, with peak rates occurring during the evening hours. Recent evidence from 24-h continuous intragastric pH studies in fasting patients with healed duodenal ulcer suggests that larger doses of intravenous H2-Antagonists are required in the evening than in the morning to achieve equivalent acid suppression. These findings are consistent with a changing H2-antagonist dose/acid-inhibiting response over the circadian period. Continuous infusion has the advantage of providing consistent and sustained suppression of gastric acid secretion in patients at risk for stress ulceration. Results of a double-blind, randomized, crossover study indicated that equally effective suppression of acidity and time-to-onset of pharmacological effect can be achieved with and without priming bolus doses of ranitidine, and presumably other H2-Receptor Antagonists as well.(ABSTRACT TRUNCATED AT 250 WORDS)