Tiotidine and cimetidine—kinetics and dynamics

Abstract
Tiotidine and cimetidine kinetics and dynamics were compared to assess mechanisms of the longer duration of effect of tiotidine in man. Both drugs had similar lag times for absorption. Tiotidine with a meal was more slowly absorbed than when fasting and was more slowly absorbed than cimetidine with a meal. The elimination rates for both drugs did not differ; they were both .apprx. 2-3 h. Oral doses of cimetidine achieved areas under the plasma concentration curve .apprx. 3 times that of tiotidine but these concentrations were only 1/10 as potent. The cimetidine concentration inducing 50% inhibition of food-stimulated gastric acid secretion was 0.41 .+-. 0.04 but it was 0.04 .+-. 0.003 .mu.g/ml for tiotidine. The effect of tiotidine lasted longer than that of cimetidine as the doses recommended for use in man caused higher concentrations in plasma relative to effective concentration than clinical doses of cimetidine.

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