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Monday 01 September 2003

The effect of ketoconazole and diltiazem on oestrogen metabolism in postmenopausal women after single dose oestradiol treatment.

By: Annas A, Carlstrom K, Alvan G, AL-Shurbaji A.

Br J Clin Pharmacol 2003 Sep;56(3):334-6

AIMS: The effect of the CYP3A4 inhibitors ketoconazole and diltiazem on the pharmacokinetics of oestrone was studied in six healthy postmenopausal women after treatment with a single oral dose of oestradiol. METHODS: Plasma oestrone concentrations were measured following the administration of 1) oestradiol, 2) oestradiol and ketoconazole and 3) oestradiol and diltiazem. RESULTS: Treatment with ketoconazole increased the AUC of oestrone (+ 4029 nmol l-1 h; 95% CI on the difference: 1588, 6471) and its Cmax (+ 306 nmol l-1; 95% CI on the difference: 117, 496). The AUC and Cmax of oestrone tended to increase on treatment with diltiazem although this did not reach the level of statistical significance. CONCLUSIONS: The small increase in the plasma concentrations of oestrone formed from 17beta-oestradiol during co-administration with ketoconazole is unlikely to be clinically significant.

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