Regression of uterine leiomyomas after treatment with gestrinone, an antiestrogen, antiprogesterone

Coutinho, Elsimar Metzker; Boulanger, G.; Gonçalves, Maria Tereza

doi:10.1016/s0002-9378(86)80016-3

Cited by 48 publications

(21 citation statements)

References 10 publications

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“…Gestrinone is used in clinical medicine on a small scale, especially for the treatment of endometriosis (Dawood et al 1997), uterine myoma (De Leo et al 2002) and mastalgia (Peters 1992). The side effects observed with gestrinone include hirsutism, acne, voice changes, weight gain and increased hemoglobin (Coutinho et al 1986, Coutinho 1989. It is expected that THG will also decrease gonadotropin secretion by the anterior pituitary gland as observed in our animal studies with the parent compound gestrinone (Kelly et al 1979), thus leading to inhibition of testicular and ovarian activity in men and women taking THG.…”

Section: Discussionmentioning

confidence: 99%

Tetrahydrogestrinone induces a genomic signature typical of a potent anabolic steroid

Labrie¹,

Luu‐The²,

Calvo³

et al. 2005

Journal of Endocrinology

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Tetrahydrogestrinone (THG) is a recently identified compound having the greatest impact in the world of sports. In order to obtain a highly accurate and sensitive assessment of the potential anabolic/androgenic activity of THG, we have used microarrays to identify its effect on the expression of practically all the 30 000 genes in the mouse genome and compared it with the effect of dihydrotestosterone (DHT), the most potent natural androgen. Quite remarkably, we found that 671 of the genes modulated by THG in the mouse muscle levator ani are modulated in a similar fashion by DHT, while in the gastrocnemius muscle and prostate, 95 and 939 genes respectively, are modulated in common by the two steroids. On the other hand, THG is more potent than DHT in binding to the androgen receptor, while, under in vivo conditions, THG possesses 20% of the potency of DHT in stimulating prostate, seminal vesicle and levator ani muscle weight in the mouse. The present microarray data provide an extremely precise and unquestionable signature of the androgenic/anabolic activity of THG, an approach which should apply to the analysis of the activity of any anabolic steroid.

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Section: Discussionmentioning

confidence: 99%

Tetrahydrogestrinone induces a genomic signature typical of a potent anabolic steroid

Labrie¹,

Luu‐The²,

Calvo³

et al. 2005

Journal of Endocrinology

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“…Until recently, the treatment of uterine fibroids has been primarily surgical, since prior attempts at medical treatment with progesterone [1], danazol [2], or gestrinone [3] produced disappointing results. Myomectomy may not be an easy surgical procedure because leiomyomas are often multiple and those most associated with symptoms lie deep in the myometrium.…”

Section: Introductionmentioning

confidence: 99%

Mechanism of LHRH Analogue Action in Uterine Fibroids

Shaw

1989

Horm Res

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“…Clinical trials with gestri none, involving over 100 patients with myomas, have shown the effectiveness of the drug not only with regard to the reduction in uterine volume, but also in suppress ing excessive uterine bleeding and pain associated with the tumors [7]. In another study we have shown that the drug was effective irrespective of tumor size, but the large or very large uteri required prolonged treatment of 1 or 2 years in order to restore normal uterine function [8].…”

Section: Introductionmentioning

confidence: 93%

“…Administered by either the oral or vaginal route and given at the same dose used to treat endometriosis or benign breast dis ease, the drug effectively induces uterine hypothrophy and shrinkage of myomata [7,9). Large myomatous uteri require prolonged treatment of 2 years or longer.…”

Section: Commentsmentioning

confidence: 99%

Treatment of Large Fibroids with High Doses of Gestrinone

Coutinho

1990

Gynecol Obstet Invest

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Twenty-four women with large, myomatous uteri, measuring between 218.7 and 2,920 cm³ were treated with gestrinone, a tri-enic steroid with antiestrogen and antiprogesterone properties. In order to saturate the receptors of the large myomata, the doses used to treat these women were twice the recommended dosage of 2.5 mg, 3 times weekly, used to treat smaller tumors. The treatment lasted 6 months to 1 year. In all cases there was a reduction in uterine volume. In the 24 patients, the mean uterine volume of 724.9 cm³ on admission decreased to 450.73 cm³ at 6 months. For 14 patients treated for a full year, the mean uterine volume of 689.73 cm³ decreased to 329.22 cm³. Menstruation was suppressed in all patients by the end of the 2nd month of treatment. Episodic bleeding occurred in 6 patients but in only 1 did this last longer than 1 week. Other symptoms such as pelvic discomfort and dysuria disappeared or were significantly alleviated by the 2nd month of treatment. Side effects included seborrhea, acne, nervousness, myalgia and arthraglia, hoarseness and mild hirsutism but all these symptoms were promptly reversed following discontinuation. The mean increase in weight was 3.4 kg in 6 months. No menopausal symptoms such as hot flushes and depression developed during this trial. Six patients complained of excessive sweating. Blood glucose creatinine, blood urea nitrogen, alkaline phosphatase, pyruvic and glutamic transaminases remained within the normal range.

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Regression of uterine leiomyomas after treatment with gestrinone, an antiestrogen, antiprogesterone

Cited by 48 publications

References 10 publications

Tetrahydrogestrinone induces a genomic signature typical of a potent anabolic steroid

Tetrahydrogestrinone induces a genomic signature typical of a potent anabolic steroid

Mechanism of LHRH Analogue Action in Uterine Fibroids

Treatment of Large Fibroids with High Doses of Gestrinone

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