Estradiol sulfate
As the sodium salt, sodium estradiol sulfate, E2S is present as a minor constituent (0.9%) of conjugated equine estrogens (CEEs), or Premarin. It effectively functions as a prodrug to estradiol in this preparation, similarly to E1S. E2S is also formed as a metabolite of estradiol, as well as of estrone and E1S. Aside from its presence in CEEs, E2S is not available as a commercial pharmaceutical drug.
Pharmacokinetics of estradiol
Lauritzen (1986) reported that 3 hours after a single rectal dose of 1 mg micronized estradiol, estradiol levels increased by 620 pg/mL and estrone levels increased by 120 pg/mL. Subsequently, Lauritzen (1987, 1990) reported that 0.5 mg/day and 1 mg/day rectal estradiol resulted in respective estradiol levels of 363 pg/mL and 515 pg/mL 6 hours following the last dose. These estradiol levels are fairly similar to those achieved by vaginal estradiol. The estradiol-to-estrone ratio of rectal estradiol is about 5:1, which likewise is the same as that of vaginal estradiol. Absorption of rectal estradiol occurs rapidly within 30 to 60 minutes, maximal estradiol levels occur at 3 hours post-dose, and circulating estradiol levels are reportedly maintained for 4 to 10 hours. The duration of rectal estradiol is said to necessitate repeated administration 1 to 2 times per day.