晚期乳腺癌患者在负荷剂量后及稳态水平时他莫昔芬及其代谢物的血清和尿液水平。
Serum and urine levels of tamoxifen and its metabolites in patients with advanced breast cancer after a loading dose and at steady-state levels.
作者信息
de Vos D, Slee P H, Briggs R J, Stevenson D
机构信息
Medical Department Pharmachemie BV, Haarlem, The Netherlands.
出版信息
Cancer Chemother Pharmacol. 1998;42(6):512-4. doi: 10.1007/s002800050854.
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.
目的
比较负荷剂量及稳态时他莫昔芬及其代谢产物的血清和尿液水平。
方法
对14例晚期乳腺癌患者给予160mg他莫昔芬的负荷剂量。此后，每日给予常规剂量30mg他莫昔芬。采用高效液相色谱法测定他莫昔芬及其代谢产物的血清和尿液水平，并与31例每日剂量30mg他莫昔芬达到稳态的晚期乳腺癌患者所测定的水平进行比较。
结果
负荷剂量后他莫昔芬及其代谢产物的血清和尿液水平（24小时值）低于稳态时（P<0.05）。代谢产物的差异最为明显，而他莫昔芬负荷剂量水平接近稳态。
结论
给予2天160mg他莫昔芬的负荷剂量可在1-2天内达到他莫昔芬稳态。在应用负荷剂量4周或更长时间后，他莫昔芬代谢产物可定期达到稳态水平。极少有他莫昔芬或其代谢产物排泄到尿液中。
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