Effect of raloxifene on salivary sex steroid concentrations in premenopausal women

Abstract

Raloxifene is a selective oestrogen receptor modulator used clinically for the treatment and the prevention of osteoporosis in postmenopausal women. The drug has been evaluated in the Study of Tamoxifen and Raloxifene as an agent to reduce breast cancer incidence in postmenopausal women at high risk. However, about 30% of women who develop breast cancer do so in their premenopausal years. In this pilot study, salivary oestradiol and progesterone were determined throughout the menstrual cycle for a total of 22 subjects, 14 of whom completed pre-and postraloxifene (60 mg daily) salivary collections. The mean concentration of oestradiol during the menstrual cycle when subjects were taking raloxifene was significantly greater (P!0 . 001) than during baseline cycles. Neither salivary progesterone and cortisol nor menstrual cycle length were affected by raloxifene treatment. These data demonstrate that raloxifene administered to premenopausal women increases the concentration of oestradiol that diffuses into the salivary glands, and which presumably represents the concentration available to other organs as well. The results reflect increases in serum oestradiol reported earlier.

Effect of Raloxifene on Mammographic Density and Breast Magnetic Resonance Imaging in Premenopausal Women at Increased Risk for Breast Cancer

“…Participants enrolled in a phase II trial of raloxifene in premenopausal women at high risk for developing invasive breast cancer. Details of the study have been reported previously (23)(24)(25)(26). In brief, all participants provided written informed consent.…”

Sex-Specific Associations of Androgen Receptor CAG Trinucleotide Repeat Length and of Raloxifene Treatment with Testosterone Levels and Perceived Stress in Schizophrenia

“…Overall, most studies confirm a relatively beneficial effect of raloxifene in patients with schizophrenia, despite inconsistencies as to which clinical aspects (symptoms or cognition) are ameliorated by the drug [32, 35, 36]. Raloxifene increased sex steroid levels in healthy samples, including estrogen in women [37-39] and testosterone in men [40-43], although several studies found no change in testosterone levels in either sex with raloxifene treatment [39, 44-46]. Modification of circulating testosterone levels may be a mechanism by which raloxifene elicits beneficial effects in patients with schizophrenia.…”

A Pilot and Feasibility Study on the Effects of Naturopathic Botanical and Dietary Interventions on Sex Steroid Hormone Metabolism in Premenopausal Women

“…However, the Study of Tamoxifen and Raloxifene trial was limited to postmenopausal women. Pilot studies of raloxifene have been conducted in premenopausal women but have shown increases in estradiol concentrations and decreases in bone mineral density (9,10). Surgical breast cancer prevention options include mastectomy and oophorectomy (11)(12)(13), yet these options are undesirable for many women given their side effects (e.g., loss of ovarian estrogen production and increased risk of endometrial cancer) and implications (e.g., disfigurement and inability to conceive).…”