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The menopause
Published in Michael J. O’Dowd, The History of Medications for Women, 2020
Allen and Doisy (1923) isolated an ovarian hormone, later called estrogen. Dodds and Robertson (1930) described the use of ‘estrin’, a substance derived from human placental sources, in the treatment of women with menopausal complaints. Oral estrogen therapy became widely available after the development of the semi-synthetic estrogen, stilboestrol, by Dodds and associates (1938). The semi-synthetic estrogens, ethinyl estradiol and mestranol were produced for oral contraception but also used for menopausal therapy. Natural estrogens were mainly used thereafter.
Estrogen treatment for senile dementia-Alzheimer’s type
Published in Barry G. Wren, Progress in the Management of the Menopause, 2020
H. Honjo, M. Urabe, K. Iwasa, T. Okubo, H. Tsuchiya, N. Kikuchi, T. Yamamoto, S. Fushiki, T. Mizuno, K. Nakajima, M. Hayashi, K. Hayashi
In the next study, CE (0.625 mg/day) was given for 7 weeks to another nine women with AD, and 1 mg/day of norethisterone and 50 µg/day of mestranol were added during the 4th to the 7th week. The scores on HDS-R, NSD and MMS were increased (improved, p <0.05, p <0.01 and p <0.05, respectively) in the 3rd week, but again decreased in the 6th week compared with scores in the 3rd week. Breakthrough bleeding was reduced to 22% (two of nine patients), butwithdrawal bleeding was not reduced (56%, five of nine). Uterine bleeding still occurred in 78% (seven of nine). Other kinds of progestogen and various ways of administering them should be further examined, but at present, estrogen only without progestogen might be used to improve the quality of life for women with AD.
Effects of Environmental Factors on the Endocrine System
Published in George H. Gass, Harold M. Kaplan, Handbook of Endocrinology, 2020
Hormonal contraceptives are steroid analogs that alter gonadotropin release. The risk of voluntarily taking oral contraceptives has frequently been discussed.48 The dosage used for contraception is maintained at a low daily level (e.g., 50 μg). However, occupational exposure to these preparations for female workers is hazardous to their reproductive health. Impaired ovarian function is often observed in women exposed to dust containing mestranol or ethinylestradiol, leading to reduced fertility.49 Occupational exposure to androgens is also a concern for women. Exposed individuals may develop an enlarged clitoris, increased hair growth, and masculinization.
Drospirenone 4 mg-only pill (DOP) in 24+4 regimen: a new option for oral contraception
Published in Expert Review of Clinical Pharmacology, 2020
Maria Chiara Del Savio, Riccardo De Fata, Fabio Facchinetti, Giovanni Grandi
The dilemma of the presence or absence of estrogens in hormonal contraception has been present since the 60 s, when the contraceptive pill was first introduced. The first pills that Gregory Pincus and John Rock tested were based only on a progestin (norethynodrel), representing the first POP. However, the pharmaceutical company G. D. Searle & Company (Chicago, US) sent the researchers a batch of failed drugs that seemed to better control the patients’ menstrual cycle. The researchers realized that these pills contained residues of an estrogenic component (mestranol), and they decided by chance that the combination of estrogen and progestin was a solution to explore in subsequent experiments. However, the contraceptive efficacy of contraceptive pills is primarily due to the progestin component, and POPs have remained an important option in hormonal contraception ever since [42].
Pharmacodynamics of combined estrogen–progestin oral contraceptives: 4. Effects on uterine and cervical epithelia
Published in Expert Review of Clinical Pharmacology, 2020
Carlo Bastianelli, Manuela Farris, V. Bruni, Ivo Brosens, Giuseppe Benagiano
In 1966 Roland et al. [16] tried to determine which morphological alterations produced by a COC were due to the estrogen component. To this end, they administered daily 0.1 mg mestranol (MSN) to normally ovulating women and after 5 and 10 days observed straight, tubular glands with minimal tortuosity. After 15 and 20 days the glands remained tubular, but the tall columnar epithelium displayed accentuated stratification, but no secretion. Overall, the picture is indistinguishable from that observed in an anovulatory cycle. They then administered 50 μg of EE to normally ovulating women over three cycles. Biopsies taken after 5 and 10 days of medication showed a picture similar to that observed with MSN. However, a biopsy taken after 15 days showed in some glands the presence of subnuclear secretory vacuoles and the presence of products of secretion. After 20 days glands appeared tubular, with no mitoses, no secretion, and a cellular stroma without vascular development. Again, a picture identical to that seen in an anovulatory cycle.
Hormonal and natural contraceptives: a review on efficacy and risks of different methods for an informed choice
Published in Gynecological Endocrinology, 2023
Andrea R. Genazzani, Tiziana Fidecicchi, Domenico Arduini, Andrea Giannini, Tommaso Simoncini
The estrogenic component of combined hormonal contraceptives (CHCs) enhances contraceptive effectiveness by suppressing gonadotropins and provides better endometrial control. Moreover, it compensates the estrogenic deficiency induced by the inhibition of gonadotropin secretion. The first estrogen used for a pill was mestranol, the 3-methyl ether of ethinylestradiol (EE). Pharmacokinetally, 50 µg of oral mestranol is bioequivalent to 35 µg of EE; thus, considering that Enovid® contained 150 µg of mestranol, it is easy to see that the estrogen doses used initially were much higher than now. The dose of mestranol was then reduced to 75 µg, until EE definitely replaced mestranol [34].