title: Markedly elevated levels of estrone sulfate after long-term oral, but not transdermal, administration of estradiol in postmenopausal women.
abstract: OBJECTIVE
  To compare serum estrone sulfate (E1S) levels in postmenopausal women during long-term treatment with commonly prescribed doses of oral and transdermal estradiol (E2).
  
  
  METHODS
  A retrospective study performed in a University setting in the United States involving 33 healthy postmenopausal women. Two groups of postmenopausal women were studied: group 1 (n = 10) received 1 mg oral micronized E2 daily for 16 months; blood was drawn at 0, 7, and 15 months. Group 2 (n = 23) was randomized into three subgroups. Two of the subgroups (n = 8; n = 7) received E2 delivered at a rate of 0.05 mg/day and 0.1 mg/day, respectively, by transdermal patch, changed twice weekly; the third subgroup received a placebo (without E2) patch for 9 continuous months. Blood samples were drawn at 0, 6, and 9 months. Serum E1S and E2 were quantified by specific radioimmunoassays. Statistical analysis was performed by analysis of variance.
  
  
  RESULTS
  After oral E2 treatment, E1S levels increased significantly (p < 0.01) from baseline, reaching an average level of 38.8 ng/mL at 15 months. After transdermal E2 treatment, E1S levels increased significantly, yet to a much lesser extent, reaching levels of 1.8 ng/mL and 3.2 ng/mL after 9 months of treatment with the 0.05 mg/day and 0.1 mg/day patches, respectively.
  
  
  CONCLUSIONS
  Markedly elevated levels of E1S were found after long-term oral estrogen treatment. In comparison to the increase in E1S levels after long-term oral estrogen treatment, there was only a small increase in E1S levels after transdermal E2 therapy. This difference may be attributed to the higher dosage of oral E2 that is required because of the low bioavailability compared with the transdermal dosages.
authors.affiliation: Department of Obstetrics and Gynecology, Keck School of Medicine of the University of Southern California, Los Angeles, USA.
authors.forename: C C
authors.initials: CC
authors.lastname: Slater
authors.forename: H N
authors.initials: HN
authors.lastname: Hodis
authors.forename: W J
authors.initials: WJ
authors.lastname: Mack
authors.forename: D
authors.initials: D
authors.lastname: Shoupe
authors.forename: R J
authors.initials: RJ
authors.lastname: Paulson
authors.forename: F Z
authors.initials: FZ
authors.lastname: Stanczyk
mesh_terms: D000279:Administration, Cutaneous; D000284:Administration, Oral; D000368:Aged; D004958:Estradiol / Q000008:administration & dosage* / Q000097:blood; D004970:Estrone / Q000031:analogs & derivatives* / Q000097:blood*; D005260:Female; D020249:Hormone Replacement Therapy; D006801:Humans; D008137:Longitudinal Studies; D008875:Middle Aged; D017698:Postmenopause; D012189:Retrospective Studies
chemical_list: D004970:Estrone; D004958:Estradiol; C017296:estrone sulfate