Estrogen Induction of Liver Proteins and High-Density Lipoprotein Cholesterol: Comparison between Estradiol Valerate and Ethinyl Estradiol

Abstract

The effects of ethinyl estradiol and estradiol valerate were compared in 135 postmenopausal women during estrogen replacement therapy. Subfractions of high-density lipoprotein (HDL) cholesterol and its apolipoproteins and the serum levels of 2 estrogen-sensitive liver proteins were followed during 3 cycles of unopposed treatment with either ethinyl estradiol 10 or 30 µg or estradiol valerate 2 mg daily. Estrogen therapy induced significant and dose-dependent changes in all serum factors except HDL₃ cholesterol. The effects of 10 µg of ethinyl estradiol upon the lipoproteins were 1.5–2.5 times greater than those of 2 mg of estradiol valerate. Sex-hormone-binding globulin and the pregnancy zone protein were the most sensitive markers for the estrogenic effect and these 2 liver-derived plasma proteins were also much more sensitive to ethinyl estradiol than to estradiol valerate. Although satisfactory therapeutic effects were achieved with both estrogens, the marked influence of ethinyl estradiol on liver protein synthesis should make estradiol valerate the first choice in clinical replacement therapy.

Cardiovascular Risk Factors During Estrogen-Norethindrone and Cholecalciferol Treatment

“…Blood pressure and body mass index did not change throughout the study. We demonstrated a decrease (11%) in serum cholesterol level after 1 year of treatment with estrogen-norethindrone. When this treatment was combined with cholecalciferol, a similar decrease (13%) was observed.…”

“…Women in group 4 had one cholecalciferol and one estrogen-norethindrone combination tablet. Treatment went on for 1 year. All participants were encouraged to maintain their usual diet, but no diet records were made.…”

“…The hypocholesterolemic effect was correlated to body mass index in a way that indicated the most pronounced decrease in lean women. The high-density lipoprotein cholesterol/total cholesterol fraction increased by 45% after 1 year of estrogen-norethindrone treatment, while an increase of 25% after 1 year was seen when cholecalciferol was added to the treatment. The latter increase was not different from a similar increase in the placebo group.…”

Estrogen therapy and liver function—metabolic effects of oral and parenteral administration

“…The distinct differences between the two estrogens as regards their effect on the pituitary (inhibition of follicle-stimulating hormone [FSH]) and on the liver (liver-derived plasma protein concentrations) have been revealed in studies on postmenopausal women receiving estrogen replacement therapy. Comparative data on mean FSH suppression and liver protein induction from 135 women treated for a period of 3 months are illustrated in Figure 1 [42]. Although a satisfactory therapeutic effect was achieved with both estrogens, the influence on liver metabolism was much more pronounced for the alkylated estrogen.…”

Contraception orale estro-progestative : quelle différence entre éthinylestradiol et estradiol ?

“…Aux posologies é valué es, la synthè se de ces proté ines, é tait selon leur type augmenté d'un facteur 100 à 1000 avec l'EE en comparaison au 17b-estradiol. Même à la posologie de 10 mg/j, l'EE augmente d'un facteur 1,5 à 2,5 fois, les sous-fractions du HDL-cholesté rol [18], ainsi que celle des triglycé rides [19] par rapport à la prise de 2 mg/j de valé rate d'estradiol chez la femme mé nopausé e. Cet effet sur le mé tabolisme des lipoproté ines est retrouvé avec l'EE même avec des doses aussi faibles que 1 mg/j pour l'augmentation des triglycé rides et de 2,5 mg/j pour la baisse du LDL-cholesté rol ou l'augmentation du HDL-cholesté rol [20]. L'EE à la posologie de 50 mg/j ou de 20 mg/j entraîne é galement une augmentation nettement plus marqué e que le valé rate d'estradiol (2 mg/j) de certains facteurs impliqué s dans l'hé mostase, comme le fragment 1 + 2 de la prothrombine [21].…”