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Endocrine Therapies
Published in David E. Thurston, Ilona Pysz, Chemistry and Pharmacology of Anticancer Drugs, 2021
MPA is well absorbed orally, with blood levels peaking after 2–4 hours and a half-life of 12–17 hours. It can also be administered in a depot form (i.e., Depo-ProveraTM) by deep intramuscular injection (normally into the gluteal muscle) which provides a half-life of 40–50 days. As with most progestogens, side effects include GI disturbances (e.g., nausea), cardiovascular abnormalities (e.g., hypertension, palpitation, congestive heart failure), depression, fluid retention, breast and menstrual cycle irregularities in women, alopecia, sexual dysfunction, skin reactions, and weight changes. In addition to these general adverse effects, the glucocorticoid effects associated with MPA can lead to Cushingoid syndrome at higher doses. Also, rarely, vision disorders such as retinal thrombosis can occur, in which case treatment should be immediately discontinued. Medroxyprogesterone acetate should be avoided during conception or pregnancy, as genital malformations in the fetus may occur.
Unresolved issues in endometrial cancer and postmenopausal hormone therapy
Published in Barry G. Wren, Progress in the Management of the Menopause, 2020
N. S. Weiss, S. A. A. Beresford, L. F. Voigt, P. K. Green, J. A. Shapiro
Using data from 45-64-year-old cases and controls in the early part of this study (1985-87), we previously observed that women who took cyclic combined therapy in which the progestogen was used for less than 10 days per cycle were at an increased risk of endometrial cancer3. Table 3 presents data that address the same hypothesis, excluding the women who had comprised our prior analysis. The same pattern of results was obtained. Compared to women who had never used hormones (or had done so for fewer than 6 months), those who used estrogen combined with progestogen for less than 10 days per month had a 3.1-fold increase in their risk of developing endometrial cancer (95% CI 1.7-5.7). In contrast, the relative risk associated with use of a progestogen for 10-21 days per month was only 1.3 (95% CI 0.8-2.2). The large majority of cases and controls had used medroxyprogesterone acetate as their progestational agent.
Clinical Aspects on the Role of Prolactin in Human Breast Cancer
Published in Nagasawa Hiroshi, Prolactin and Lesions in Breast, Uterus, and Prostate, 2020
In spite of the poor prognosis of patients with hyperprolactinemia, remissions were achieved with chemotherapy or hormonal therapy. It remains to be established under which conditions and in which patients PRL inhibitors are of therapeutic value. Clinical trials have so far failed to demonstrate a significant therapeutic effect of PRL inhibitors, e.g., bromocriptine in advanced breast cancer.60,61 PRL probably modulates the effect of other hormones on tumor growth or vice versa. Ward62 noted that 14 of 36 patients with advanced breast cancer, whose disease had progressed on treatment with tamoxifen alone, subsequently responded to continued treatment with bromocriptine and tamoxifen. In another report, the combination of medroxyprogesterone acetate with bromocriptine resulted in longer remission duration than when medroxyprogesterone acetate was given alone.64
Oculo-auriculo-vertebral spectrum and maternal drug ingestion: cause or coincidence?
Published in Hearing, Balance and Communication, 2023
Joana Raquel Costa, Miguel Bebiano Coutinho, Teresa Soares, Luís Meireles
Fluoxetine intake during pregnancy was observed in 3 cases. One case throughout the first trimester of pregnancy and the second case during the first and second trimester. In two cases, a history of Gestational Diabetes requiring insulin in the third trimester was found. The use of Hormonal Contraceptives with oestrogen and progesterone components during the first trimester of pregnancy has been reported in 4 cases: Perlutan® – algestone acetophenide + oestradiol enanthade; Provera® – medroxyprogesterone acetate; and Harmonet® – ethinylestradiol + gestodene (2 cases). In two cases, a history of Hypothyroidism requiring Levothyroxine intake was reported. Also in two cases, history of intake of Isotretinoin during the first trimester of pregnancy for the treatment of acne has been described. Other drugs reported were: Domperidone (until the fifth week of gestation); Enalapril; Acyclovir (in the seventh week for herpes zoster) and Pseudoephedrine/Triprolidine.
Progestin or anti-estrogen treatment for endometrial cancer: choosing the best option for selected patients
Published in Gynecological Endocrinology, 2021
Marta Caretto, Tommaso Simoncini
Fertility-sparing treatments should be restricted to women with atypical hyperplasia/endometrioid intra-epithelial neoplasia (AH/EIN) or grade 1 endometrioid carcinoma without myometrial invasion. Hysteroscopic resection followed by the progestin therapy achieve the highest complete remission rate according to recent literature. The progestin therapy includes oral progestin as well as intrauterine progestin application. Medroxyprogesterone acetate (400–600 mg/day) or megestrol acetate (160–320 mg/day) are the recommended oral treatments [3]. Only patients undergoing oral treatment should be informed of major risks or the presentation of systemic adverse effects. Instead, in case of the intrauterine progestin therapy such as levonorgestrel-releasing intrauterine system combined with gonadotropin-releasing hormone receptor agonist or progestin a satisfactory pregnancy rate and a low recurrence rate have been reported. The combination of levonorgestrel intrauterine device with oral progestins with or without gonadotropin-releasing hormone analogs can also be considered. There is a lack of evidence for anti-estrogenic treatment in women who wish to preserve fertility [4].
A rare complication of combined oral contraceptives (COCs): optic neuritis
Published in Journal of Obstetrics and Gynaecology, 2021
Oestrogens seem to ameliorate the symptoms of keratoconjunctivitis sicca and exhibit protective effect against glaucoma, cataractogenesis and degradation of corneal collagen. Moreover, the antioxidant and neuroprotective action of oestrogens indicates their possible therapeutic use in neurodegenerative eye diseases, including AMD and diabetic retinopathy (Moschos and Nitoda 2017). The intraocular effects of COCs have been shown to vary depending on the type of progesterone. De Souza et al. (2013), used colour doppler imaging to show that progesterone can increase the resistance of retinal arteries. Progesterone receptors are present in the arterial smooth-muscle walls, and progesterone counteracts oestrogen by reducing endothelial nitric oxide production. Progestin-derived levonorgestrel antagonises ethinyl oestradiol-induced vasodilatation via the α1 and α2 receptors (Torgrimson et al. 2007). Medroxyprogesterone acetate also plays a role in endothelial dysfunction by altering the effects of oestrogen (Sorensen et al. 2002).