Koetsawang S, Nukulkarn P, Fotherby K, Shrimanker K, Mangalam M, Towobola K
Contraception. 1982 Apr;25(4):321-31. doi: 10.1016/0010-7824(82)90090-7.
Levels of norethisterone and medroxyprogesterone acetate were measured in serum and milk of women receiving the injectable contraceptive formulations Norigest and DepoProvera, respectively, throughout complete injection intervals. In 5 of 10 women receiving Norigest, serum norethisterone levels were undetectable by 8 weeks after injection and only 2 women had detectable levels of norethisterone in milk at this time. In contrast, 8 of 10 women receiving DepoProvera had detectable levels of medroxyprogesterone acetate in both serum and milk 12 weeks after injection. The ratio of the milk:serum concentrations of norethisterone varied from 0.12 to 0.92 (mean 0.34) and for medroxyprogesterone acetate from 0.12 to 2.60 (mean 0.88). It is unlikely that these differences between the two formulations are due entirely to differences between the binding of norethisterone and medroxyprogesterone acetate to serum proteins. The area under the curve of serum steroid concentrations plotted against time was only 50% higher for women injected with DepoPovera than for those injected with Norigest but the area under the curve for milk values was 400 times higher. Assuming the infant ingests 600 ml daily, the daily intake of steroids in the first week after injection would be 0.5 to 2.4 micrograms for norethisterone and 1 to 13 micrograms for medroxyprogesterone acetate. By 8 weeks after injection, the amount of norethisterone ingested would be small but that of medroxyprogesterone acetate would still be significant.
在整个完整的注射间隔期内,分别测定了接受注射用避孕药诺瑞酯(Norigest)和醋酸甲羟孕酮避孕针(DepoProvera)的女性血清和乳汁中炔诺酮和醋酸甲羟孕酮的水平。在接受诺瑞酯的10名女性中,有5名在注射后8周血清炔诺酮水平检测不到,此时只有2名女性乳汁中炔诺酮水平可检测到。相比之下,接受醋酸甲羟孕酮避孕针的10名女性中有8名在注射后12周血清和乳汁中醋酸甲羟孕酮水平均可检测到。炔诺酮乳汁与血清浓度之比在0.12至0.92之间(平均0.34),醋酸甲羟孕酮则在0.12至2.60之间(平均0.88)。这两种制剂之间的这些差异不太可能完全归因于炔诺酮和醋酸甲羟孕酮与血清蛋白结合的差异。注射醋酸甲羟孕酮避孕针的女性血清类固醇浓度随时间变化曲线下的面积仅比注射诺瑞酯的女性高50%,但乳汁值曲线下的面积却高400倍。假设婴儿每天摄入600毫升乳汁,注射后第一周类固醇的每日摄入量炔诺酮为0.5至2.4微克,醋酸甲羟孕酮为1至13微克。注射后8周,摄入的炔诺酮量会很少,但醋酸甲羟孕酮的量仍然可观。