RESUMO

Gestrinone (R-2323), or ethylnorgestrienone, is a synthetic steroid of the 19-nortestosterone group more commonly used as an oral, intravaginal, or subcutaneous implant for the treatment of endometriosis, contraception, and estrogen-dependent conditions such as hypermenorrhea, premenstrual dysphoria, and intense menstrual cramps. This review aims to reevaluate the routes, doses, and applicability proposed for using gestrinone, including its use in new conditions such as menopause, lipedema, and sarcopenia. Here, we present the possible application of gestrinone as a long-acting therapeutic possibility through hormonal implants and the benefits and potential risks. Available evidence on the safety of doses and routes is limited. Gestrinone appears to be effective compared to other progestins and may have some advantages in the treatment of estrogen-dependent pathologies. Future research must evaluate gestrinone's long-term safety and potential therapeutic indications.

RESUMO

PURPOSE: Endometriosis is a common chronic gynecological disease defined as the presence of endometrial glands and stroma tissue outside the uterus. Gestrinone is an effective antiestrogen that induces endometrial atrophy and/or amenorrhea. The purpose of this systematic review is to provide an evaluation of safety and effectiveness of gestrinone for the treatment of endometriosis. METHODS: We performed a search in six electronic databases: PubMed, MEDLINE (ovid), Embase, Cochrane CENTRAL (clinical trials), Web of Science and Scopus. Our selected primary outcomes were the changes in dysmenorrhea, pain relief including pelvic pain and dyspareunia. The secondary outcomes embrace hormones parameters, pregnancy rate and adverse events. RESULTS: Of 3269 references screened, 16 studies were included involving 1286 women. All studies compared gestrinone with other drugs treatments (placebo, Danazol, Mifepristone tablets, Leuprolide acetate, Quyu Jiedu Recipe) during 6 months. When compared with other drugs treatments, gestrinone relieved dysmenorrhea, pelvic pain, and morphologic response in the ovary. There was an increase on the pregnancy rate. Regarding the side effects observed, gestrinone showed the same adverse events and increased the risk of acne and seborrhea when compared to other treatments. Even if there was any difference in efficacy between gestrinone, danazol, leuprolide acetate, or Quyu Jiedu Recipe Chinese Medicine, it remains unclear due to insufficient data. CONCLUSION: Based limited evidence available suggests that gestrinone appeared to be safe and may have some efficacy advantages over danazol, as well as other therapeutic interventions for treating endometriosis. However, this conclusion should be interpreted with caution, due the quality of the evidence provided is generally very low or unclear. TRIAL REGISTRATION: CRD42021284148.

Assuntos

Endometriose , Gravidez , Feminino , Humanos , Endometriose/tratamento farmacológico , Endometriose/complicações , Gestrinone/efeitos adversos , Danazol/uso terapêutico , Leuprolida/efeitos adversos , Dismenorreia/tratamento farmacológico , Dismenorreia/complicações , Dor Pélvica/tratamento farmacológico , Dor Pélvica/etiologia

RESUMO

OBJECTIVE: To evaluate the effects of estrogen treatment in combination with gestrinone on an experimental rat model of endometriosis. METHODS: Uterine transplants were attached to the peritoneum of female Wistar rats via a surgical autotransplantation technique. The implanted area was measured during the proestrus phase and after hormonal treatment. We performed morphometric analysis and examined the macroscopic and morphometric alterations of endometrial implants after hormonal treatment in ovariectomized rats. RESULTS: The high dose of estrogen caused macroscopic increases in the endometrial implant group compared with other groups, which were similar to increases in the proestrus phase. The low dose showed morphometric development of implants, such as an increase in number of endometrial glands, leukocyte infiltration and mitosis. Gestrinone antagonized both doses of estrogen. CONCLUSION: Our findings suggest that gestrinone antagonizes estrogen's effects on rat peritoneal endometrial implants.

Assuntos

Animais , Feminino , Ratos , Endometriose/tratamento farmacológico , Antagonistas de Estrogênios/uso terapêutico , Estrogênios/uso terapêutico , Gestrinone/uso terapêutico , Progestinas/uso terapêutico , Modelos Animais de Doenças , Avaliação Pré-Clínica de Medicamentos , Endometriose/patologia , Ovariectomia , Ratos Wistar

RESUMO

In a study involving over 300 women, gestrinone has been found to induce regression of uterine myomas. Gestrinone was given in doses of 2.5-5 mg (orally or by vaginal pessary), two or three times weekly. The treatment regimen depended upon tumor size and tumor age. Patients with small tumors, i.e. uterine volumes of less than 200 cm3 , were treated for 6 months, whereas those with uterine volumes of 200-300 cm3 were treated for 1 year. In severe cases where uterine volumes were greater than 400 cm3 , the patients were treated for 2 years. Large myomas of 300 cm3 or more required higher doses of steroid. During the first 6 months of treatment there was a marked reduction in uterine volume, but subsequently the rate of tumor regression was slower. Following discontinuation of treatment, reactivation of tumor growth was slow in most patients. Gestrinone caused amenorrhea in all patients and in most women it lasted throughout therapy. The abdominal discomfort, dyspareunia and dysuria which resulted from the myoma were progressively alleviated during treatment. Most patients experienced at least some side-effects associated with the mild androgenicity of gestrinone. These included weight gain, seborrhea and acne (which developed in most patients). Hirsutism, hoarseness and increase in libido were less common, affecting 10-20% of patients, depending on the dose and duration of treatment. All side effects were reversible.