Serum and urine levels of tamoxifen and its metabolites in patients with advanced breast cancer after a loading dose and at steady-state levels

被引:10
作者
de Vos, D
Slee, PHTJ
Briggs, RJ
Stevenson, D
机构
[1] Med Dept Pharmachem BV, NL-2003 RN Haarlem, Netherlands
[2] St Antonius Hosp, NL-3435 CM Nieuwegein, Netherlands
[3] Univ Surrey, Sch Biol Sci, Robens Analyt Ctr, Guildford GU2 5XH, Surrey, England
关键词
tamoxifen; serum levels; urinary excretion; loading dose; steady state;
D O I
10.1007/s002800050854
中图分类号
R73 [肿瘤学];
学科分类号
100214 ;
摘要
Purpose: To compare serum and urine levels of tamoxifen and metabolites after a loading dose and at the steady state. Methods: A loading dose of 160 mg of tamoxifen was given to 14 patients with advanced breast cancer. Thereafter a regular daily dose of 30 mg of tamoxifen was given. Serum and urine levels of tamoxifen and metabolites were measured by high-performance liquid chromatography and compared with levels determined in 31 patients with advanced breast cancer at the steady state at a daily dose of 30 mg of tamoxifen. Results: Serum and urine levels (24-h values) of tamoxifen and metabolites were lower (P < 0.05) after a loading dose than at the steady state. The difference was most pronounced for the metabolites, whereas the tamoxifen loading-dose level was near the steady state. Conclusion: Tamoxifen steady state can be reached in 1-2 days by the administration of a loading dose of 160 mg of tamoxifen for 2 days. Tamoxifen metabolite steady-state levels are reached regularly after 4 or more weeks during application of a loading dose. Very little tamoxifen or metabolites are excreted into the urine.
引用
收藏
页码:512 / 514
页数:3
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