Estrogen replacement in postmenopausal women: Are we currently overdosing our patients?

Ron Tepper, Shmuel Goldberger, Ilan Cohen, Jehoshua Segal, Shai Yarkoni, Moshe Fejgin, Yoram Beyth

Research output: Contribution to journalArticlepeer-review


As there are no proven optimal serum estradiol levels, we sought to evaluate the pharmacokinetic profiles of serum estradiol levels following a single oral dose of 2 mg estradiol and 1 mg of estriol (Trisequens) among 26 surgically induced, postmenopausal patients. Their serum estradiol levels were periodically measured over 24 h following oral administration of the drug. They were divided into two groups according to the computed hourly mean estradiol values: group A, <250 pg/ml/h (<918 pmol/l/h) and group B, >250 pg/ml/h (>918 pmol/l/h). The mean peak estradiol concentrations were noted 2 h after drug administration and amounted to 595 ± 190 pg/ml (2, 184 ± 697 pmol/1) in theentire cohort; 435 ±117 pg/ml (1, 597 ± 430 pmol/1) in group A and 712 ±142 pg/ml (2, 614 ± 521 pmol/1) in group B (p< 0.001). The mean total area under the curve in group A was 4, 887 pg/ml (17, 940 pmol/1), which was significantly lower than that of 7, 995 ± 652 pg/ml/24 h (29, 350 ± 2, 393 pmol/1/24 h) found for group B (p < 0.001). The mean body mass index showed a significant difference (p < 0.003) between group A and group B (29.4 ± 0.56 vs. 24.3 ± 0.24). We found that 57% of our patients were exposed to excessively high levels of estradiol during the 24-hour period following drug ingestion. We advise monitoring estradiol levels and individualizing estrogen relacement therapy, to avoid the long-term exposure of postmenopausal patients to superphysiological estradiol levels.

Original languageEnglish
Pages (from-to)113-116
Number of pages4
JournalGynecologic and Obstetric Investigation
Issue number2
StatePublished - 1994
Externally publishedYes


  • Body mass index
  • Estrogen replacement therapy
  • Estrogens
  • Monitoring
  • Pharmacokinetics
  • Postmenopause


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