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Endocrine Therapies
Published in David E. Thurston, Ilona Pysz, Chemistry and Pharmacology of Anticancer Drugs, 2021
There are many other approved progesterone-like drugs including dienogest (used for endometriosis), desogestrel, etonogestrel, and levonorgestrel (used as components of contraceptive pills) and progesterone itself (used for infertility treatments, premenstrual syndrome, postnatal depression, and HRT). These agents are not discussed any further here.
Recurrence of endometriosis
Published in Seema Chopra, Endometriosis, 2020
Recurrence of endometriosis can be managed either surgically or medically. According to ACOG updated guidelines [1], NSAIDs or combined OCPs can be used for pain management in women who wish to preserve fertility. Depot or oral medroxyprogesterone is also effective. A levonorgestrel-releasing intrauterine device (LNG-IUD) can also be used for pain relief. If the patient fails to respond to the above therapies, GnRH agonists or androgens can be tried. If GnRH agonist therapy is used, add-back therapy with progestogens is recommended to reduce bone loss. The most commonly recommended progestogen by the FDA is norethindrone 5 mg daily. For those who can't tolerate norethindrone, a daily combination of oral medroxyprogesterone acetate 2.5 mg and transdermal estradiol 25 ug can be used. Supplementation with 1000 mg calcium is also recommended. Dienogest [69,70] 2 mg per day can be used and is well-tolerated for recurrent endometrioma. It reduces the size of the cyst as well as the pain-free interval within 3 months of usage.
Chronic pelvic pain and endometriosis
Published in Joseph S. Sanfilippo, Eduardo Lara-Torre, Veronica Gomez-Lobo, Sanfilippo's Textbook of Pediatric and Adolescent GynecologySecond Edition, 2019
Joseph S. Sanfilippo, Jessica Papillon Smith, M. Jonathon Solnik
Dienogest is an oral progestin now used as a monotherapy at a dose of 2 mg daily in patients with endometriosis. This medication is highly selective for the progesterone receptor, leading to strong progestational effects, moderate antigonadotrophic effects, and minimal androgenic, glucocorticoid, or mineralocorticoid effects.61 Multiple studies have shown dienogest to be both safe and effective in the treatment of adults with endometriosis.62–64 However, studies in the pediatric adolescent population were lacking until recently. In 2017, Ebert et al. published the results of the VISanne Study to Assess Safety in ADOlescents (VISADO study). This prospective observational study evaluated the safety and efficacy of dienogest 2 mg daily in adolescents aged 12–18 with clinically suspected or laparoscopically confirmed endometriosis. Results demonstrated that endometriosis-associated pain was substantially reduced and that the drug was very well tolerated during the 52-week trial. However, there was an associated decrease in lumbar bone mineral density with only a partial recovery after 6 months of treatment discontinuation.65 In light of these findings, it is necessary to adopt an individualized approach when prescribing dienogest, as with DMPA. One must balance the benefits of decreased pain with the potential risks to bone health in each patient, and provide counseling in this regard. Patients should also be informed that dienogest has not been tested or approved as a contraceptive, so the concomitant use of barrier contraception is necessary in sexually active teenagers.
Primary choice of estrogen and progestogen as components for HRT: a clinical pharmacological view
Published in Climacteric, 2022
Even larger differences can be seen, for example, with dienogest. The transformation dose listed as 6 mg/cycle (Table 5) is much lower compared to the results of endometrial biopsy studies performed in postmenopausal women: we were involved in the first dose-finding study needed for the registration of E2/dienogest preparation for continuous-combined therapy testing 1 mg, 2 mg, 3 mg and 5 mg oral dienogest/day in postmenopausal women treated with 2 mg oral E2/day [36]. Based on the endometrial histology and bleeding pattern, the result was best for 3 mg dienogest/day. Because efficacy was better using 2 mg/day, E2/dienogest (2/2 mg/day) was launched, also considering follow-up studies and studies investigating endometrial efficacy for the indication of endometriosis, where efficacy was demonstrated for a 2 mg dienogest-only preparation [30,31,37–39]. Derived from these clinical studies, it must be concluded that the transformation dose for dienogest is about 60–90 mg/cycle, which is in very large contrast to the index presented in Table 5 (6 mg). This is also in contrast to the Kaufmann Index, which is assessed to be only about 0.5 mg/day for dienogest [30].
Successful treatment of peritoneal inclusion cysts with dienogest: two case reports
Published in Journal of Obstetrics and Gynaecology, 2022
Hiroki Shinmura, Takashi Matsushima, Takehiko Fukami, Toshiyuki Takeshita
Dienogest, which is a synthetic progestin that is typically used for the treatment of endometriosis, reduces serum progesterone levels to anovulatory levels and inhibits folliculogenesis. One reason for peritoneal inclusion cysts is adhesion, which causes a decline in the ability of the peritoneum to absorb ovarian stroma-derived serous fluid (Fu and Su 2018). It is believed that dienogest can reduce the production of serous fluid derived from the ovarian stroma, which causes peritoneal inclusion cysts (Ruan et al. 2012; Maeda et al. 2014). It is thought that the presence of focal oestrogen and progesterone receptors on peritoneal inclusion cyst walls play a supportive role in hormonal management until menopause (Vallerie et al. 2009). Thrombus is a critical potential side effect of hormonal therapy, but dienogest does not exert the same effects as oestrogen, and therefore, its use is not associated with an increased risk of thrombus (Ruan et al. 2012). Irregular bleeding is a frequently encountered side effect of dienogest, but the two cases presented here experienced no adverse events because they had already undergone hysterectomy.
Dienogest vs GnRH agonists as postoperative therapy after laparoscopic eradication of deep infiltrating endometriosis with bowel and parametrial surgery: a randomized controlled trial
Published in Gynecological Endocrinology, 2021
Marcello Ceccaroni, Roberto Clarizia, Stefano Liverani, Agnese Donati, Matteo Ceccarello, Maria Manzone, Giovanni Roviglione, Simone Ferrero
Dienogest has a strong atrophying effect on endometriotic implants, associating anti-inflammatory and anti-angiogenic properties [12–14]. At a dosage of 2 mg/day, estrogen levels are basic but not abolished: such a low estradiol level is not able to reactivate the outbreaks of endometriosis, but it is sufficient to avoid estrogen deprivation symptoms [14–16]. Dienogest has excellent tolerability, possible adverse effects are spotting, mood disorders, headache, acne, nausea, and weight gain [13,14]. In four RCT, Dienogest was well tolerated with a good safety profile [17,18]. Adverse effects were headache, breast discomfort, acne, and mood disorders, each occurring in less than 10%, all of the mild-to-moderate intensity, and associated with a low discontinuation rate. Spotting was well tolerated, and 0.6% only reported that as the reason for premature discontinuation of therapy [17,18]. Previously published data [19–26] encouraged the employ of Dienogest as an effective medical treatment for DIE showing comparable results in terms of symptoms relief to the gold-standard treatments and good compliance profile. No RCT in literature was today designed to confirm the long-term efficaciousness of Dienogest to maintain the patient’s well-being and contemporarily preventing DIE relapses after radical surgical excision of the disease.