Cimetidine-a clinical and pharmacokinetic study

1 The effect of six months therapy with cimetidine (800 mg or 1600 mg/day) and subsequent withdrawal was studied in 19 patients with duodenal ulceration. 2 The overall rates of healing were 63% and 79% of patients after 3 and after 6 months of treatment respectively. The longer course (6 months) or the higher dose (1600 mg) did not result in significantly increased rates of ulcer healing. 3 Abrupt withdrawal of cimetidine resulted in the recurrence of severe symptoms in 15 patients (79%). 4 Pharmacokinetic studies showed the mean elimination half-life of cimetidine to be 100 +/- 25 min, the total body cimetidine clearance 652 +/- 223 ml/min, the mean volume of distribution at steady state 65 +/- 181 and the overall bioavailability 78%. 5 Long term cimetidine treatment does not result in drug accumulation or changes in its pharmacokinetic profile. 6 Inter-individual differences in clinical and endoscopic response to cimetidine cannot be explained by pharmacokinetic differences.