Post-menopausal concentrations of plasma oestradiol, oestrone, FSH and LH and of total urinary oestradiol and oestrone after a single sublingual dose of oestradiol-17β

Abstract

We report the effects of sublingual absorption of a single dose (0.5 mg) of oestradiol-17\g=b\(E2) in 8 post-menopausal women, on plasma E2 and oestrone (E1), urine elimination of total E2 + E1 and on plasma FSH and LH.The results show that sublingual absorption of E2 occurs and that plasma concentrations of E2 obtained (between 133.2 to 320 pmol/1) in this way were higher than those obtained after percutaneous absorption of a single dose (3 mg)of E2. The ratio E1/E2 in plasma is close to that of pre-menopausal women.Although synthetic forms of oestrogen are effec¬ tive in treating menopausal symptoms, they are now less commonly used because of side-effects in the liver (Kern et al. 1978) and cardiovascular system (Irey & Norris 1973; Gammal 1976), and the natural oestrogen oestradiol-I7ß (E2) is con¬ sidered preferable. Nevertheless, its concentration in the patients plasma after administration, as well as that of its chief metabolite oestrone (Ei) should both remain as close as possible to pre-menopausal physiological levels. Many absorption routes have been studied for E2, including the percutaneous (Basdevant & De Lignieres 1980), oral (Yen et al. 1975, vaginal (Rigg et al. 1978), intramuscular (Sommerville 1975) and implantation pathways (Greenblatt et al. 1977). Apart from one very recent paper (Burnier et al. 1981), however, no description exists of absorption by the sublingual route.Our aim was to determine whether E2 can be absorbed sublingually. 'Glossettes1' of E2 were administered in single doses to 8 post-menopausal women and plasma concentration of E2, E^F SH and LH were measured, in addition to the sum of the Et and E2 excreted in the urine.Finally, for purposes of comparison, 6 of the 8 women were given a percutaneous application of E2 one week after the sublingual dose and the same parameters were measured. Materials and Methods PatientsOur series was of 9 post-menopausal women, but we excluded one 70-year-old patient with very high levels of basal E2. Investigation revealed that she was using beauty creams containing oestrogen.The ages of the 8 patients studied ranged from 47 to 69 years and their mean weight was 55 kg. Six patients had experienced a natural menopause and 2 had under¬ gone hysterectomy with bilateral ovariectomy. The time elapsing between the onset of menopause and the in¬ vestigation ranged from 4 to 24 years. No patient had received oestrogen treatment during that time. None was suffering from kidney, liver or thyroid complaints or disturbed salivation. All medication was stopped during the trial. »Laboratoire Fournier, BP 130, 21004 DIJON cédex,

Effect of estradiol on fibroblasts from postmenopausal idiopathic carpal tunnel syndrome patients

“…However, there were no correlations between the percentages of ERα‐positive and ERβ‐positive cells and collagen type I or III expression. The concentration of estradiol in the blood of postmenopausal women drops severely to less than 10 pg/ml from 15 to 350 pg/ml before menopause (Elmlinger, Kuhnel, & Ranke, ; Fiet et al, ). Although ER expression is present in the SSCT of postmenopausal women, the low concentration of estradiol in the blood suggests that it is unable to act on these ERs, and thereby is incapable of regulating collagen expression.…”