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Androgens and bone function
Published in Barry G. Wren, Progress in the Management of the Menopause, 2020
Watts and associates19 studied surgically menopausal women who were treated with either oral esterified estrogen (1.25 mg) or esterified estrogen (1.25 mg) and methyl- testosterone (2.5 mg) daily for 2 years. Bone loss at the spine and hip was prevented by both treatment regimens; however, combined estrogen/androgen therapy was associated with an increase in spinal BMD compared with baseline19. The effects of estrogen alone, and estrogen plus androgen, on biochemical markers of bone formation and resorption in postmenopausal women have also been investigated. Postmenopausal women were treated for 9 weeks with either a combination of 1.25 mg esterified estrogen and 2.5 mg methyltestosterone orally, or 1.25 mg conjugated equine estrogen (CEE) given alone. A similar decrease in the urinary excretion of the bone absorption markers deoxy- pyridinoline, pyridinoline and hydroxyproline occurred in both groups. However, women treated with CEE had a reduction in the serum markers of bone formation, bone-specific alkaline phosphatase, osteocalcin and C- terminal procollagen peptide, whereas the women treated with estrogen plus androgen had increases in all of these markers of bone formation.
Transdermal estrogen therapy and the risk of breast cancer: a clinical appraisal
Published in A. R. Genazzani, Hormone Replacement Therapy and Cancer, 2020
There are no data to support monitoring of the breast tissue response to ET with serum estradiol assays. However, in selective circumstances, plasma estradiol monitoring may be needed for other reasons. Plasma estradiol levels in women taking either oral or transdermal estradiol, as opposed to the more complex estrogens such as CEE and esterified estrogen, will be more reflective of the actual amount of estrogen prescribed and absorbed. It will also allow for comparison with studies of endogenous plasma estradiol levels and breast cancer risk in untreated postmenopausal women.
Alternate Pathways of Steroid Biosynthesis and the Origin, Metabolism, and Biological Effects of Ring B Unsaturated Estrogens
Published in Ronald Hobkirk, Steroid Biochemistry, 1979
B. R. Bhavnani, C. A. Woolever
Specific ring B unsaturated estrogens, like other estrogenic hormones, are known to stimulate the tissues of the reproductive system. In addition, they have been shown to modify the frequency and the severity of the flushes and sweats associated with estrogen withdrawal in the human female and to lower the concentration of gonadotropins in the serum and urine. However, their effect on other systems in the human is less clear and the available data primarily are derived from clinical studies using conjugated equine estrogen preparations, usually Premarin®. Obtained from the unhydrolyzed urine of pregnant mares, this product is a mixture of the classical estrogens (represented by the sodium sulfate ester of estrone (approximately 45%)) and the ring B unsaturated estrogens (represented by the sodium sulfate ester of equilin (approximately 25%)), plus lesser amounts of other estrogens of both classes (Table 13).129,130 A similar product, known as “esterified estrogens,” contains somewhat different proportions of the same compounds.131 Highly soluble in water, the conjugated equine estrogens are easily absorbed from the gut in effective concentrations and have been used extensively as replacement therapy for estrogen-deficient women. Since the biological responses these compounds elicit are the sum of the effects of the various constituents, it is not possible to arrive at a reliable estimate of the potency of any specific ring B unsaturated compound from data derived from studies using these mixtures.
International Society for the Study of Women's Sexual Health Clinical Practice Guideline for the Use of Systemic Testosterone for Hypoactive Sexual Desire Disorder in Women
Published in Climacteric, 2021
Sharon J. Parish, James A. Simon, Susan R. Davis, Annamaria Giraldi, Irwin Goldstein, Sue W. Goldstein, Noel N. Kim, Sheryl A. Kingsberg, Abraham Morgentaler, Rossella E. Nappi, Kwangsung Park, Cynthia A. Stuenkel, Abdulmaged M. Traish, Linda Vignozzi
Historically, there have been some formulations approved for women. Testosterone implants (Testosterone Implant, Organon) were previously approved for use in Australia but are no longer available. Oral methyltestosterone, combined with conjugated equine estrogens or esterified estrogens, were never formally approved for treatment of sexual dysfunction in postmenopausal women in the United States. These formulations were not specifically evaluated for HSDD, and the conjugated equine estrogens with methyltestosterone product is no longer available. The transdermal testosterone patch (Intrinsa), developed for treatment of HSDD, was approved in Europe but only for the treatment of surgically menopausal women with HSDD with adequate concomitant estrogen therapy. As the European Medicines Agency refused to broaden the treatment indication to naturally menopausal women, the product was withdrawn from the market. A transdermal 1% testosterone cream (AndroFeme, Lawley Pharmaceuticals, Perth, Australia) is available by prescription in Australia, approved in 2020 by the Australian Register of Therapeutics Goods for treatment of HSDD in postmenopausal women.
Hormone replacement therapy – where are we now?
Published in Climacteric, 2021
R. D. Langer, H. N. Hodis, R. A. Lobo, M. A. Allison
However, pharmaceutical-grade, FDA-approved, ‘bioidentical’ transdermal estradiol is available as a patch or gel. It is important to note that transdermal estrogens are exclusively estradiol, while there are a variety of oral preparations available, with the most data available for CEE (a mix of estrogens, dominated by estrone sulfate and equilin sulfate, with minimal estradiol content). Other commonly available oral estrogen preparations for use in menopause include estradiol, esterified estrogens, and estropipate. In contrast to estradiol, and to some degree other oral estrogen preparations, the metabolic conversion of the mixed estrogens in CEE results in the circulation of estrogens with a variety of receptor affinities, and estrogen receptor agonism and antagonism, or selective estrogen receptor modulator-like activity.
Sexual Function in Postmenopausal Women and Serum Androgens: A Review Article
Published in International Journal of Sexual Health, 2019
Soheila Nazarpour, Masoumeh Simbar, Fahimeh Ramezani Tehrani
Some studies have shown that addition of testosterone to estrogen significantly improves sexual function. A clinical trial was conducted on postmenopausal women who were experiencing hypoactive sexual desire. In this study, sexual interest and desire was assessed using the Sexual Interest Questionnaire. The results showed that treatment with the combination of esterified estrogens (0.625 mg) and methyltestosterone (1.25 mg) significantly increased the concentration of bioavailable testosterone and suppressed SHBG resulting an improvement sexual function (sexual interest or desire; Lobo et al., 2003).