title: Absence of systemic hormonal effects in an oestradiol diether topically active on the vaginal mucosa.
abstract: The women in this study were either post-menopausal or ovariectomised for at least 1 yr prior to the study. They had also been treated for cancer of the cervix (27 women), endometrium (5), ovaries (5) or breast (1). All women presented with sexual troubles, mainly genital discomfort (dyspareunia or vaginism). In a double-blind fashion, gynaecological capsules containing either an oestradiol diether (ICD: promestriene) or only the excipient were administered for 40 consecutive days. At the end of the treatment, the FSH, LH, oestrone (E1) and oestradiol (E2) plasma levels were not found to be significantly different from the pre-therapeutic values. These results suggest that promestriene acts on the vaginal mucosa, therefore not being converted back into the hormone from which it was derived. Also, in its dietheroxide form, promestriene is incapable of crossing the malpighian (vaginal or epidermal) epithelium and of reaching the general blood circulation. This discrepancy between the local anti-atrophic effects and the inability to exert systemic oestrogen activities singles out promestriene and justifies its therapeutic use when hormonally active oestrogens are contra-indicated, as in patients who have an oestrogen-sensitive cancer in their medical history.
mesh_terms: D000287:Administration, Topical; D000328:Adult; D004958:Estradiol / Q000008:administration & dosage / Q000009:adverse effects / Q000031:analogs & derivatives* / Q000494:pharmacology; D045166:Estradiol Congeners / Q000494:pharmacology*; D004967:Estrogens / Q000097:blood*; D005260:Female; D006062:Gonadotropins / Q000097:blood*; D006801:Humans; D008875:Middle Aged; D014621:Vagina / Q000187:drug effects*
chemical_list: D045166:Estradiol Congeners; D004967:Estrogens; D006062:Gonadotropins; D004958:Estradiol; C013657:promestriene