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Differential Effects of Oral Estrone Versus 170-Estradiol on Lipoproteins in Postmenopausal Women^*

Departments of Internal Medicine and Comparative Medicine, Bowman Gray School of Medicine, Wake Forest University Winston-Salem, North Carolina 27103

Address all correspondence and requests for reprints to: Perry L. Colvin, Jr., M.D. Department of Internal Medicine, Bowman Gray School of Medicine, 300 South Hawthorne Road, Winston-Salem, North Carolina 27103.

Toward the definition of optimal postmenopausal estrogen replacement we compared the effects of three graduated doses of two oral estrogens, estrone sulfate and 17/3-estradiol, on the lipid profiles of two groups of six postmenopausal women. Because of metabolic interconversions equivalent serum concentrations of estrone and estradiol were produced with these regimens. However, differential effects were noted in lipoproteins. 17/3-Estradiol caused an increase in total plasma cholesterol (from 5.71 ± 0.36 to 5.99 ± 0.57 mmol/L, baseline to high dose; P < 0.02), high density lipoprotein (HDL) cholesterol (from 1.45 ± 0.15 to 1.78 ± 0.36 mmol/L; P < 0.02), HDL₂ cholesterol concentration (from 0.41 ± 0.08 to 0.62 ± 0.26 mmol/ L; P < 0.01), and triglyceride concentration (from 1.09 ± 0.29 to 1.24 ± 0.30 mmol/L; P < 0.01) without affecting low density lipoprotein (LDL) cholesterol concentration. By contrast, estrone sulfate caused a decrease in total plasma cholesterol (from 6.51 ± 0.85 to 5.87 ± 0.41 mmol/L; P < 0.05) and LDL cholesterol concentration (from 4.34 ± 0.57 to 3.67 ± 0.44 mmol/L; P < 0.01) and an increase in HDL cholesterol (from 1.37 ± 0.20 to 1.50 ± 0.26 mmol/L; P < 0.05) and HDL2 cholesterol concentration (from 0.34 ± 0.18 to 0.49 ± 0.18 mmol/L; P < 0.01), but no change in total triglyceride concentration. We deduce that the differential effect of orally administered estrogens on lipoprotein metabolism in postmenopausal women may be attributed to a first pass effect on hepatic metabolism.

^* This work was supported in part by NIH Grants HL-38624 and HL-38222.

Received March 13, 1989.

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