Comparison of pharmacodynamic properties of various estrogen formulations

Am J Obstet Gynecol. 1982 Nov 1;144(5):511-8. doi: 10.1016/0002-9378(82)90218-6.

Abstract

A group of 23 healthy postmenopausal women received one or more 2-week courses of daily administration of the following estrogen preparations: piperazine estrone sulfate (Ogen), 0.3, 0.625, 1.25, 2.5, and 5.0 mg; micronized estradiol (Estrace), 1, 2, and 10 mg; conjugated estrogens (Premarin), 0.3, 0.625, 1.25, and 2.5 mg; ethinyl estradiol (Estinyl), 10 and 20 micrograms; and diethylstilbestrol, 0.1 and 0.5 mg. Each dosage of each formulation was ingested by three women. In those women who received more than one dosage, each course was separated by a drug-free interval of at least 4 weeks. Pretreatment and posttreatment levels of follicle-stimulating hormone (FSH), luteinizing hormone (LH), corticosteroid-binding globulin-binding capacity, sex hormone-binding globulin-binding capacity, angiotensinogen, estrone, and estradiol were determined. The relative potency of these five estrogen formulations was determined by parallel line analysis for each of these responses, except LH. On a weight basis, piperazine estrone sulfate and micronized estradiol were equipotent for all responses. Conjugated estrogens suppressed FSH in a fashion equipotent to that of the other nonsynthetic estrogens; however, for all three hepatic parameters, the response was exaggerated twofold to threefold. The synthetic estrogens, diethylstilbestrol and ethinyl estradiol, were relatively more potent on a weight basis for every response and produced the most marked response (fourfold to eighteenfold in excess of their FSH suppression) for the hepatic parameters.

Publication types

  • Comparative Study
  • Research Support, Non-U.S. Gov't
  • Research Support, U.S. Gov't, Non-P.H.S.

MeSH terms

  • Angiotensinogen / blood
  • Diethylstilbestrol / pharmacology
  • Estradiol / blood
  • Estradiol / pharmacology
  • Estrogens / pharmacology*
  • Estrogens, Conjugated (USP) / pharmacology
  • Estrone / blood
  • Estrone / pharmacology
  • Ethinyl Estradiol / pharmacology
  • Female
  • Follicle Stimulating Hormone / blood
  • Humans
  • Luteinizing Hormone / blood
  • Menopause
  • Sex Hormone-Binding Globulin / metabolism
  • Transcortin / metabolism

Substances

  • Estrogens
  • Estrogens, Conjugated (USP)
  • Sex Hormone-Binding Globulin
  • Angiotensinogen
  • Estrone
  • Ethinyl Estradiol
  • Estradiol
  • Diethylstilbestrol
  • Luteinizing Hormone
  • Follicle Stimulating Hormone
  • Transcortin