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Ranitidine, 75 mg, over‐the‐counter dose: pharmacokinetic and pharmacodynamic effects in children with symptoms of gastro‐oesophageal reflux
Author(s) -
Orenstein S. R.,
Blumer J. L.,
Faessel H. M.,
McGuire J. A.,
Fung K.,
Li B. U. K.,
Lavine J. E.,
Grunow J. E.,
Treem W. R.,
Ciociola A. A.
Publication year - 2002
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 - 10.1046/j.1365-2036.2002.01243.x
Subject(s) - ranitidine , medicine , pharmacokinetics , pharmacodynamics , placebo , cmax , heartburn , histamine , gastroenterology , population , pharmacology , dosing , reflux , histamine h2 receptor , antagonist , disease , receptor , pathology , alternative medicine , environmental health
Background: The use of over‐the‐counter antacids has increased in children under the age of 12 years, and has been followed by an apparent increase in the use of over‐the‐counter histamine‐2 receptor antagonists. However, the pharmacokinetic and pharmacodynamic effects of over‐the‐counter histamine‐2 receptor antagonists in the paediatric population are largely unknown. Aim: To evaluate the pharmacokinetics and pharmacodynamics of a single dose of the over‐the‐counter histamine‐2 receptor antagonist, ranitidine, 75 mg, in children with symptoms of gastro‐oesophageal reflux disease. Methods: Children aged between 4 and 11 years with symptoms of heartburn suspected to be due to gastro‐oesophageal reflux disease were recruited at six clinical centres. Following a single dose of either oral ranitidine, 75 mg ( n =19), or placebo ( n =10), recording of intragastric pH and serial blood sampling were carried out for 6 h. Results: The estimated pharmacokinetic parameters of ranitidine, 75 mg, were as follows: the median C max value of 477 ng/mL occurred within a median of 2.5 h after dosing, and the median half‐life was 2.0 h. The intragastric pH began to rise approximately 30 min after dosing with ranitidine to a peak of pH ˜ 4. The pH in the ranitidine group remained higher than that in the placebo group throughout the 6‐h evaluation period. Adverse events were generally mild. Conclusions: Ranitidine, 75 mg, significantly increased the intragastric pH in children aged 4–11 years. The pharmacokinetic and pharmacodynamic profiles were similar to those in adults. Ranitidine, 75 mg, appears to be effective for the control of intragastric acidity for 5–6 h in children aged 4–11 years.