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Endocrine Therapies
Published in David E. Thurston, Ilona Pysz, Chemistry and Pharmacology of Anticancer Drugs, 2021
Norethisterone, also known as norethindrone or 19-nor-17α-ethynyltestosterone, was the first potent orally administered progestin, and was synthesized by Carl Djerassi and colleagues at Syntex in Mexico City (USA) in 1951 (Figure 8.50). It was reported in the chemical and patent literature between 1954 and 1958, and was first introduced for medical use as a standalone agent in 1957 and in combination with an estrogen for use as a birth control pill in 1963. Sometimes referred to as a first-generation progestin, it was the first agent of its type to be used in the first three oral contraceptives approved for clinical use. The two best-known brands of norethisterone, Primolut NTM and UtovlanTM, are now distributed by Bayer and Pfizeer, respectively, although many generic versions are available. The related ester (norethisterone acetate) was also developed for similar indications.The structure of norethisterone (Primolut NTM, UtovlanTM).
Monographs of Topical Drugs that Have Caused Contact Allergy/Allergic Contact Dermatitis
Published in Anton C. de Groot, Monographs in Contact Allergy, 2021
A 50-year-old postmenopausal woman, using 2x weekly transdermal patches containing 5 mg estradiol and 15 mg norethisterone, developed itchy discoid indurated erythema under the 3rd patch applied, followed by a bullous reaction. Because of this, treatment was switched to the estradiol-containing gel, but acute eczema also developed on sites of application of this gel. Patch tests yielded strongly positive reactions to norethisterone acetate 0.1% and 1% alcohol and to 17β-estradiol 1% and 0.1% alc. Twenty controls were negative. (2).
Hormone replacement therapy, insulin-like growth factor I and breast cancer
Published in A. R. Genazzani, Hormone Replacement Therapy and Cancer, 2020
P. Sismondi, N. Biglia, R. Ponzone, S. Ambroggio
Progestins can be divided into four groups with different metabolic activities: Progesterone derivatives (dydrogesterone and medrogestone), devoid of androgenic, estrogenic or glucocorticoid action;19-Nortestosterone derivatives (norethisterone and norethisterone acetate (NETA)), characterized by a residual androgenic action and, at high doses, also by a certain estrogenic action;17-Hydroxyprogesterone derivatives (medroxyprogesterone acetate (MPA) and cyproterone acetate), both devoid of estrogenic action, but characterized by a weak androgenic action (MPA) and by a strong antiandrogenic action (cyproterone acetate);19-Norprogesterone (nomegestrol acetate), devoid of estrogenic or glucocorticoid activity and characterized by a certain antiandrogenic activity56–59.
Efficacy and safety of ultra-low-dose estradiol and norethisterone in postmenopausal Brazilian women
Published in Climacteric, 2023
R. Bonassi Machado, L. de Melo Pompei, E. A. P. Nahas, J. Nahas-Neto, L. da Costa-Paiva, S. Y. O. Del Debbio, M. Badalotti, M. C. O. Wender, A. M. Cruz
HT in combination with an ultra-low dose of 0.5 mg 17β-E2 and 0.1 mg norethisterone acetate (NETA) as a first-line oral option has shown to be effective, with high tolerability and safety [12]. A study assessing 577 postmenopausal women has shown a significant reduction of moderate to severe vasomotor symptoms with an ultra-low dose of 0.5 mg 17β-E2/0.1 mg NETA or 0.5 mg 17β-E2/0.25 mg NETA from 3 weeks of treatment when compared to placebo [14]. The rate of amenorrhea was approximately 90% after 6 months of treatment, and there were no significant changes in the mean endometrial thickness [15]. The bleeding pattern with an ultra-low dose of 0.5 mg 17β-E2/0.1 mg NETA was assessed in a prospective study involving 169 postmenopausal women with a 52-week follow-up. The cumulative rates of amenorrhea were 67% in the first 3 months and 84% in the last months of follow-up. This low occurrence of bleeding-related adverse events, together with the beneficial effects on vasomotor symptoms, may promote treatment adherence [16].
Current approaches to overcome the side effects of GnRH analogs in the treatment of patients with uterine fibroids
Published in Expert Opinion on Drug Safety, 2022
Mohamed Ali, Mohamed Raslan, Michał Ciebiera, Kornelia Zaręba, Ayman Al-Hendy
A scientific working group advocated for the use of suitable add-back therapy in conjunction with GnRH agonist treatment to ameliorate hypoestrogenic symptoms, prevent precancerous endometrial changes and perhaps prolong the duration of medication beyond 6 months while maintaining therapeutic efficacy [58,59]. Earlier and following the results of randomized controlled trials in women with endometriosis, the FDA approved progestin NETA, also known as norethisterone acetate, at a daily dose of 5 mg in combination with a synthetic GnRH agonist (leuprolide acetate), as an add-back therapy in women with endometriosis. NETA has profound tissue-specific progestogenic, estrogenic or antiestrogenic, and androgenic actions, where the average conversion ratio of NETA to ethynyl estradiol (E2) by aromatization is 0.7% to 1% at 5 mg NETA dosages. It is believed that the estrogenic action of NETA may explain its beneficial effect on BMD. Low dosages of E2 1 mg coupled with NETA 0.5 mg have been shown to prevent bone loss in endometriosis patients receiving GnRH agonist treatment [60]. Consequently, this combination is being used for women with UFs who are on long-term GnRH antagonist therapy.
Effects of progestogens used in menopause hormone therapy on the normal breast and benign breast disease in postmenopausal women
Published in Climacteric, 2021
C. Rueda Beltz, A. Rojas Figueroa, S. Hinestroza Antolinez, A. Bastidas
Three randomized CCTs evaluating mastodynia as an outcome in a total population of 27,463 women using two different progestogens (medroxyprogesterone acetate [MPA] and micronized progesterone [MP]) were included. The second outcome evaluated was histological changes due to epithelial proliferation in four randomized CCTs with a total of 16,868 women using mainly four progestogens (dienogest, norethisterone, MP, and MPA). Another evaluated outcome was breast density, with six randomized CCTs with 17,921 women using MPA, dienogest, levonorgestrel, norethindrone, trimegestone, norethisterone, and MP. Additionally, three cohort studies were reviewed: one evaluating the induced histological changes of proliferation by expression of biomarkers in 86 women using MPA; and two studies evaluating breast density in 206 women using MPA, norethisterone, and levonorgestrel. Last, only one quasi-experimental study was identified that analyzed breast density in 202 women using norethisterone acetate. The progestogen used in the majority of the population was MPA since it was used in the Women’s Health Initiative (WHI) study, a base sample for four included studies. In total, 17 articles were reviewed, and the characteristics of each of these studies are described in Appendix 1.