Open AccessFAT‐SOLUBLE 17β‐ESTRADIOL: A WAY OF REDUCING DOSAGE IN STEROID HORMONAL SUBSTITUTION?
Author(s) -
Schubert Werner,
Cullberg Göran
Publication year - 1988
Publication title -
acta obstetricia et gynecologica scandinavica
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 1.401
H-Index - 102
eISSN - 1600-0412
pISSN - 0001-6349
DOI - 10.3109/00016348809004218
Subject(s) - desogestrel , endocrinology , medicine , sex hormone binding globulin , estrone , climacteric , ingestion , globulin , ovariectomized rat , resorption , hormone , meal , menopause , androgen , population , research methodology , environmental health , family planning
. Eight ovariectomized women were given 0.5 mg 17β‐estradiol cyclo‐octyl acetate (E 2 COA) dissolved in arachis oil+0.15 mg desogestrel, and 2 mg micronized 17β‐estradiol (mE 2 ) + 0.15 mg desogestrel orally in a crossover fashion for 20 days each. The preparations were taken on 10 days together with a meal, on 10 days 3 hours after a meal. Blood samplings were performed 3 h after capsule ingestion for analysis of serum estradiol (S‐E 2 ), estrone (S‐E 1 ) and sex hormone binding globulin (SHBG). Before treatment, all women had climacteric complaints. During treatment these symtoms were alleviated and no discomfort was reported. No differences in serum levels of estrogens were found in either of the preparations when capsules were taken with or without food. However, serum levels of E 2 were found to be 100% higher per mg substance given after E 2 COA vis‐à‐vis mE 2 . This indicates either a delayed breakdown and/or a better resorption. The E 1 /E 2 ratio after E 2 COA was only half that after mE 2 intake. This hints at another route of resorption. SHBG concentrations were somewhat elevated following mE 2 administration, whereas a slight decrease was found after E 2 COA. The resulting post‐treatment difference was significant, suggesting a less estrogenic liver effect by E 2 COA. No accumulation of E 2 or E 1 was seen after either of the preparations. Our findings support the hypothesis that E 2 COA. being fat soluble, is resorbed via the lymphatic system. By avoiding the first liver pass the dosage of estrogen can be halved.