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Safety issues relating to long‐term treatment with histamine H 2 ‐receptor antagonists
Author(s) -
SABESIN S. M.
Publication year - 1993
Publication title -
alimentary pharmacology and therapeutics
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 3.308
H-Index - 177
eISSN - 1365-2036
pISSN - 0269-2813
DOI - 10.1111/j.1365-2036.1993.tb00597.x
Subject(s) - cimetidine , ranitidine , medicine , famotidine , histamine h2 receptor , gastric acid , adverse effect , pharmacology , placebo , histamine , receptor antagonist , gastroenterology , antagonist , stomach , receptor , pathology , alternative medicine
SUMMARY H 2 ‐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 H 2 ‐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 H 2 ‐receptor antagonists. Standard doses of currently available H 2 ‐receptor antagonists permit acid secretion in response to food and other stimuli, and this daily acid tide prevents persistent bacterial colonization.

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