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Medical treatment of endometriosis
Published in Caroline Overton, Colin Davis, Lindsay McMillan, Robert W Shaw, Charles Koh, An Atlas of ENDOMETRIOSIS, 2020
Caroline Overton, Colin Davis, Lindsay McMillan, Robert W Shaw, Charles Koh
Gestrinone is derived from 19-nortestosterone and causes endometrial and endometriosis atrophy. Similar to danazol, it reduces serum progesterone and has marked androgenic side-effects including acne and hirsuitism, as well as a negative effect on the lipid profile. At a dose of 2.5 mg weekly it has been shown to be effective in reducing pelvic pain. However, its side-effect profile limits its use.
Therapeutics in obstetrics and gynaecology
Published in Marwan Habiba, Andrea Akkad, Justin Konje, MRCOG Part 2, 2017
Marwan Habiba, Andrea Akkad, Justin Konje
D. COCP is suitable treatment for endometriosis, but is contraindicated in this patient because of a history of hypertension. Gestrinone 2.5 mg twice weekly can be used to treat endometriosis. Depot preparations may be considered as an alternative.
Endometriosis
Published in David M. Luesley, Mark D. Kilby, Obstetrics & Gynaecology, 2016
Gestrinone is a 19-nortestosterone derivative that also has progestogenic and antiprogestogenic actions. It has been compared with danazol and with a GnRH analogue in randomised trials.15,20 Reduction of pain scores was not significantly different [A], but both androgenic and hypo-oestrogenic side effects were less frequent with gestrinone. Side effects of gestrinone were reduced by lowering the dose from 2.5 mg twice weekly to 1.25 mg twice weekly without a reduction in efficacy [A].15 The reported incidence of breakthrough bleeding is much lower with gestrinone than with progestogens, making it a potentially useful alternative to other therapies [A]. However, there is a lack of information relating to its long-term safety.
Current and emerging treatment options for endometriosis
Published in Expert Opinion on Pharmacotherapy, 2018
Simone Ferrero, Giulio Evangelisti, Fabio Barra
Recently a double blind RCT including 360 women with laparoscopic diagnosis of endometriosis investigated the effectiveness and safety of oral mifepristone (daily tablet of 2.5, 5 and 10 mg) in comparison with a placebo [102]. Mifepristone at higher doses (5 and 10 mg daily) significantly improved the symptoms compared to mifepristone at a lower dose (2.5 mg) and to placebo. Moreover, 3.4% of the patients treated with mifepristone had a significant increase in the transaminases. The authors concluded that mifepristone at 5 mg was safer and more effective than the other mifepristone doses and placebo. Another recent RCT including 150 patients with endometriosis compared oral gestrinone (2.5 mg twice weekly) and a combined treatment with oral gestrinone (2.5 mg twice weekly) and oral mifepristone (12.5 mg/time once daily). The combined treatment was more efficacious than gestrinone alone in improving dysmenorrhea, dyspareunia and pelvic pain [103].
Effects of progestin-only contraceptives on the endometrium
Published in Expert Review of Clinical Pharmacology, 2020
Carlo Bastianelli, Manuela Farris, Vincenzina Bruni, Elena Rosato, Ivo Brosens, Giuseppe Benagiano
Several decades ago, a steroid known as ethyl-gestrinone (R2323) was tested at the dose of 5 mg administered as a once a week POP, with good results in terms of pregnancy prevention. An interesting feature of this method was that in approximately one third of the subjects studied, endometrial biopsies showed the presence of a secretory endometrium [50]. Development of a once-a-week contraceptive was not pursued, although its application to the treatment of endometriosis and as an emergency contraceptive are still being evaluated.
Comparison of the effect of isotretionin and alitretionin on endometriotic implants and serum vascular endothelial growth factor level: an experimental study
Published in Gynecological Endocrinology, 2019
Deniz Kulaksiz, Cavit Kart, Suleyman Guven, Kubra Akbulut, Umit Cobanoglu, Orhan Deger
The aim of conventional medical treatment for endometriosis is to relieve the symptoms associated with pain, by reducing the production of endogenous steroids. Danazol, medroxyprogesterone acetate, gestrinone, oral contraceptives and GnRH analogues are used to treat endometriosis; however, these treatments do not exhibit a positive development on infertility. Additionally, long-term usage of these agents is limited due to side effects [10].