Dose and duration effects of estradiol valerate on serum and lipoprotein lipids

Non-alkylated estrogens, like estradiol valerate (F2V), are widely used in the treatment of the postmenopausal hormonal deficiency syndrome. Their effects on serum and lipoprotein lipids are characterized by an increase in the lipid constituents of high density lipoproteins (HDL) and, usually, a decrease in low density lipoproteins (LDL). These effects are considered beneficial as regards atherogenesis and the risk for cardiovascular diseases. Unlike the effects of alkylated estrogens, no concomitant increase in triglycerides (TG) in serum and very low density lipoproteins (VLDL) - adverse effects - are seen in doses of up to 2 mg E2V. In order to compare the effects of 2 and 4 mg of E2V on serum and lipoprotein lipids, 19 bilaterally oophorectomized women participated in a cross-over study after a 4 week long wash-out period. To evaluate the influence of the time factor, 10 of the women continued taking 2 mg and 9 taking 4 mg of E2V respectively for an additional period of 12 weeks, resulting in a total treatment period of 24 weeks per group. The serum lipoproteins were separated by preparative ultracentrifugation, the serum and lipoprotein lipids being assessed using commercially available kits. In the cross-over part of the study, total (TC) and free cholesterol (FC) and phospholipids (PL) increased in HDL and decreased in LDL. Neither dose increased TG in serum or VLDL. These changes in the lipoprotein pattern persisted at the end of the entire study. Consequently, within the range of commonly used doses (2 and 4 mg) E2V seems to have a constant and, in terms of cardiovascular disease, favourable influence on lipoprotein metabolism irrespective of doses and periods studied.