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一项长期研究中口服和肌肉注射醋酸甲羟孕酮(MPA)后的血浆水平

Medroxyprogesterone acetate (MPA) plasma levels after oral and intramuscular administration in a long-term study.

作者信息

Hesselius I, Johansson E D

出版信息

Acta Obstet Gynecol Scand Suppl. 1981;101:65-70. doi: 10.3109/00016348109157815.

Abstract

In a long-term study (1 year) the plasma concentration of medroxyprogesterone acetate (MPA, Depo-Provera, Provera, Upjohn) was measured in 30 patients with endometrial carcinoma treated with MPA in the following dosages: 1) MPA 1 000 mg i.m. weekly; 2) MPA 1 000 mg i.m. once every second week, and; 3) MPA 100 mg orally twice daily. In the orally treated group the blood samples were taken just before the next tablet. The plasma concentration in the orally treated group rapidly reached steady state, while the i.m. treated group showed gradually increasing levels that had a tendency to level off after 6 months. The mean concentration at the end of the year was about three times higher for MPA 1000 mg i.m. weekly than for MPA 100 mg orally twice daily. This does not take into consideration the peak MPA level that occurs 2-4 hours after each tablet. MPA i.m. has a very good depot effect, with release of MPA from the injection site for up to 9 months. The steady initial increase in MPA plasma concentration seen in the i.m. treated groups is probably due to the additions of new depots rather than accumulation in the body generally.

摘要

在一项为期1年的长期研究中,对30例接受醋酸甲羟孕酮(MPA,商品名:狄波 - 普维拉、安宫黄体酮、普维拉、优普琼)治疗的子宫内膜癌患者的血浆浓度进行了测量,给药剂量如下:1)MPA 1000 mg,每周肌肉注射一次;2)MPA 1000 mg,每两周肌肉注射一次;3)MPA 100 mg,每日口服两次。口服治疗组在下一次服药前采集血样。口服治疗组的血浆浓度迅速达到稳态,而肌肉注射治疗组的血浆浓度逐渐升高,6个月后有趋于平稳的趋势。年末时,每周肌肉注射1000 mg MPA组的平均浓度比每日口服两次100 mg MPA组高约3倍。这未考虑每次服药后2 - 4小时出现的MPA峰值水平。MPA肌肉注射有很好的长效作用,MPA从注射部位释放可持续长达9个月。肌肉注射治疗组中MPA血浆浓度最初的稳定升高可能是由于新的药物储存库的增加,而非总体上在体内的蓄积。

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