Effect of ranitidine on the pharmacokinetics of orally administered eprosartan, an angiotensin II antagonist, in healthy male volunteers.

OBJECTIVE

To assess the effect of ranitidine on the pharmacokinetics of eprosartan in healthy male volunteers.

DESIGN

Single-center, randomized, open-label, two-period, period-balanced, crossover study.

PATIENTS

Seventeen healthy men aged 19 to 43 years.

INTERVENTION

In each period (separated by a > or = 7 d washout), subjects received a single 400-mg oral dose of eprosartan alone, or a single oral dose of eprosartan 400 mg and ranitidine 150 mg on day 4 after 3 days of ranitidine 150 mg twice daily. Serial pharmacokinetic samples were obtained for up to 24 hours following eprosartan dosing.

MAIN OUTCOME MEASURES

Plasma and urine eprosartan concentrations during each treatment session.

RESULTS

Eprosartan maximum concentration (Cmax), the AUC from time-zero to the last quantifiable concentration (AUC0-t), and renal clearance (Cl(r)) values were approximately 7%, 11%, and 4% lower, respectively, when administered with ranitidine compared with eprosartan alone. The 95% CIs for the ratio of eprosartan plus ranitidine compared with eprosartan alone were 0.81 to 1.07, 0.77 to 1.03, and 0.64 to 1.43, for Cmax, AUC0-t, and Cl(r), respectively, indicating no statistically significant difference between regimens.

CONCLUSIONS

Repeated doses of ranitidine did not have a marked effect on the single-dose pharmacokinetics of eprosartan.