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PubMed1992

Endometrial patterns during therapy with danazol or gestrinone for endometriosis: structural and ultrastructural study.

We treated 36 women with laparoscopically proven endometriosis with danazol 600 mg/d (n = 17) or gestrinone 5.0 mg/wk (n = 19) for 6 months. Endometrial samples were obtained before and at 3 and 6 months of treatment and were studied by light, scanning, and transmission electron microscopy. At 3 months of treatment, the endometria of the danazol-treated patients were more atrophic than those of the women who received gestrinone. Some cell organelle involution was evident in patients of both treatment groups. After 6 months of treatment, marked endometrial atrophy was observed in all the patients, including those in whom spotting had occurred. The ultrastructural investigation demonstrated complete involution of the cytoplasmic organelles with cytoplasmic collapse in glandular cells of patients treated with danazol, whereas in the gestrinone group degeneration phenomena were observed in both nucleus and cytoplasm. Irregular secretory transformation was seen in the endometria of patients in both groups. Long-term treatment with danazol caused endometrial atrophy similar to that induced by gestrinone, but it appeared earlier; thus, the former drug seems preferable in short-term treatment.

Adult↗

PubMed1990

A randomized double-blind prospective trial of two doses of gestrinone in the treatment of endometriosis.

The purpose of this randomized double blind prospective trial was to study the efficacy and safety of two doses of oral gestrinone in the treatment of endometriosis. Six patients received gestrinone 1.25 mg twice weekly (group I) and six patients received gestrinone 2.5 mg twice weekly (group II). Patients underwent pretreatment and post-treatment laparoscopies and their endometriosis scores were recorded. The mean total endometriosis scores declined significantly from 20.0 +/- 5.2 (mean +/- standard error of the mean) pretreatment to 9.5 +/- 3.9 post-treatment in group I and from 19.1 +/- 4.8 pretreatment to 7.1 +/- 2.1 post-treatment in group II. A total of 67% of patients reported side effects. This study suggests that oral gestrinone 1.25 mg or 2.5 mg twice weekly is efficacious and safe in the treatment of endometriosis.

Adult↗

PubMed1988

The inhibitory effects of danazol, danazol metabolites, gestrinone, and testosterone on the growth of human endometrial cells in vitro.

Danazol and gestrinone are effective drugs in the treatment of endometriosis. Their mechanism of action remains uncertain, but may be related to their androgenic activity. The authors examined the effect of danazol on human endometrial cells cultured in vitro, its two major metabolites, ethisterone and 2 hydroxymethyl ethisterone, gestrinone, and testosterone (T) at 1X and 10X expected plasma concentrations. Danazol and T suppressed growth by 20.8 and 25.0% (P less than 0.01), respectively, at the lower dose, and by 26.9 and 35.5% (P less than 0.01), respectively, at the 10-fold higher dose. No significant suppression of growth occurred with gestrinone, ethisterone, or 2 hydroxymethyl ethisterone. The results provide further evidence that danazol and T (but not gestrinone) may act by a direct effect on endometrial tissue.

Cell Division↗

PubMed1989

Studies on the mechanism of action of danazol and gestrinone (R2323) in the rat: evidence for a masked estrogen component.

The effects of androgen and estrogen receptor antagonists on the action of danazol and gestrinone (R2323) were investigated. The tropic effect of danazol and gestrinone on sex accessory tissues of castrated, immature male rats was inhibited by the antiandrogen flutamide, whereas the uterotropic action of these steroids in immature female and adult ovariectomized rats was not inhibited by flutamide. In contrast, the uterotropic effect of danazol was reduced by the antiestrogen, LY156758. The estrogen-sensitive endpoints, vaginal keratinization and uterine progesterone receptor concentration, were enhanced by treatment with a combination of flutamide and either danazol or gestrinone. These data indicate that danazol and gestrinone have estrogenic activity that is masked by the androgenic component of these drugs.

Animals↗

PubMed1993

Tissue and endocrine responses to gestrinone and danazol in the treatment of endometriosis.

An open comparative study of gestrinone and danazol in the treatment of endometriosis demonstrated a similar decrease in the extent of active endometriotic deposits, assessed visually following therapy. Biochemical endocrinological changes during therapy with gestrinone showed that basal concentrations of gonadotrophin remained unchanged, oestradiol concentrations varied and the free fraction of testosterone increased. A similar range of side effects was reported in both treatment groups, consisting predominantly of 'androgenic' effects in 10 of 15 women treated with gestrinone and 5 of 12 treated with danazol. The results suggest that gestrinone is an effective alternative agent for the treatment of endometriosis.

Amenorrhea↗

PubMed1989

Gestrinone in the treatment of myomas.

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.

Adolescent↗

PubMed1995

[Gestrinone in pelvic endometriosis. A one-year evaluation].

The therapeutical effectiveness of gestrinone in endometriosis treatment, as well as its long term side effects, were evaluated. Prospective, clinical trial. At "Dr. Alejandro Castanedo Kimball" Hospital (PEMEX). Salamanca, Guanajuato. México. Thirty women with laparoscopically confirmed endometriosis, were studied. Subjects received 2.5 mg. of gestrinone two times per week for 6 months. Laparoscopy was performed before treatment, and clinical response was determined by second laparoscopy after 6 months. The pregnancy rate, frequency of side effects and recurrence of symptoms were determined. Median total endometriosis scores and symptoms decreased significantly after treatment. Four pregnancies were observed after treatment. The principal side effects were: ponderal increase, changes in the voice and hirsutism. However, the side effects disappeared after one year of clinical survey. The results indicate that gestrinone is effective in the treatment of pelvic endometriosis. In despite of a clear benefic effect on stage of the disease and symptoms; the use of gestrinone should weigh the risk-benefit (cost versus metabolic side effects) of treatment.

Adolescent↗

PubMed1996

Long-term follow-up of endometriosis after two different therapies (Gestrinone and Buserelin).

OBJECTIVE: To compare the efficacy, tolerance and recurrence rate of endometriosis after 5-year follow-up of treatment with Gestrinone and Buserelin, respectively. STUDY DESIGN: A prospective study with randomized follow-up of 5 years duration (minimum) for each patient was done. We included 43 cases of endometriosis diagnosed by laparoscopy or laparotomy and treated them with Gestrinone (Group G, n = 25 cases) or Buserelin intranasal spray (Group B, n = 18) for 6 months. RESULTS: General data: Age, height, weight of patients and AFS score of endometriosis were without significant differences in either group. Specific data: A) Global clinical efficacy was good or excellent in 74% (16/25) of group G and in 78% (14/18) of group B without significant differences. B) Global clinical tolerance was good in 50% of the patients in group G and in 0% in group B (p < 0.001). C) Global evaluation after 5-year follow-up showed "success" only for 36% of patients in group G and in 33% in group B (no significant differences), with "failure" in 40% and 33%, respectively (no significant differences). CONCLUSIONS: 1) Gestrinone and Buserelin intranasal spray are valid treatments for the remission of endometriosis, with "success", "failure" and "clinical recurrence" rates similar after a follow-up of 5 years of initial treatment. 2) The most significant androgenic effect of Gestrinone was the presence of acne. Vascular effects were also considered as very undesirable effects according to the comments of patients. On the contrary, the effects of analogs are generally better tolerated.

Adult↗

PubMed1986

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

Ninety-seven women, aged 18 to 53 years, with uterine leiomyomas diagnosed by bimanual palpation and ultrasonography, were treated for 4 to 13 months with gestrinone, a potent steroidal, antiestrogen, antiprogesterone. Thirteen women were less than 30 years old and six 50 years old or older. Forty-six women were 30 to 40 years old and 32 others were 40 to 50 years old. Sixty-one women were nulliparous. Patients were divided in a random fashion into three groups according to treatment schedule. In group A, 34 patients received capsules containing 5 mg of gestrinone twice weekly. In group B, 36 patients received 2.5 mg capsules three times weekly. In group C, 27 patients were instructed to insert 2.5 mg tablets in the vagina three times weekly. Uterine volume was measured by ultrasonography before and at the end of treatment. At the end of 4 months, uterine volume fell from 303 to 251 cm3 in group A, from 361 to 266 cm3 in group B, but increased from 371 to 387 cm3 in group C. For those patients treated for 10 (+/- 1) months, mean uterine volume fell from 368 to 282 cm3 in group A and from 384 to 327 cm3 in group B, but increased from 262 to 290 cm3 in group C. Mean uterine volume of patients who were treated for 13 (+/- 1) months also fell from 325 to 259 cm3 in group A, from 416 to 268 cm3 in group B, and from 406 to 399 cm3 in group C. Changes in uterine volume measured at the time of discontinuation for the various groups revealed volume decrease in 71 and increase or no change in 26. Differences between groups A, B, and C were statistically significant when comparisons were made at 4 and 13 months. Uterine bleeding ceased by the second month of treatment in half the patients initially complaining of menometrorrhagias. After 4 months of treatment, 95% of the women were amenorrheic. Hemoglobin increased in 85 of 90 patients for whom values were available before treatment began. Both dyspareunia and chronic pain were significantly reduced by the gestrinone treatment. Androgenic side effects such as seborrhea, acne, and hirsutism, whenever they occurred, were benign and reverted soon after discontinuing the medication.

Adolescent↗

PubMed1993

A randomized comparative study of the metabolic effects of two regimens of gestrinone in the treatment of endometriosis.

OBJECTIVE: To study some of the metabolic effects of oral gestrinone on plasma lipoprotein risk markers for cardiovascular disease and on bone density, a risk marker for osteoporosis. DESIGN: Randomized double-blind study. SETTING: All patients were referred to Gynaecology Clinic of Royal Free Hospital Medical School. PATIENTS: Twenty premenopausal women with laparoscopically confirmed endometriosis. INTERVENTIONS: Subjects were randomized in a double-blind fashion to receive either 1.25 mg or 2.5 mg gestrinone two times per week for 6 months. MAIN OUTCOME MEASURE: Laparoscopy was performed before treatment, and clinical responses were determined by second laparoscopy after 6 months. Plasma lipid and bone density measurements during and after therapy were compared with baseline. RESULT: Median total endometriosis scores decreased from 7.5 to 1.0 in the 1.25-mg group and from 7.0 to 0 in the 2.5-mg group. There were no significant between-group differences in endometriosis scores. At both doses, bone density in the spine and the proximal femur was conserved, but plasma concentrations of low-density lipoproteins rose by 13% and those of high-density lipoproteins fell by 40%. CONCLUSIONS: Reducing the dose of gestrinone to 1.25 mg appeared to maintain the therapeutic effectiveness of this treatment but was still associated with potentially unfavorable effects on lipids and lipoproteins.

Adult↗

PubMed1989

Long-term treatment of leiomyomas with gestrinone.

A prospective randomized study was conducted in 100 women with leiomyomas in order to evaluate the effect of gestrinone, a synthetic derivative of ethynil-nor-testosterone. Patients in group A received capsules containing 2.5 mg of gestrinone three times weekly orally. Those in group B received capsules containing 5.0 mg twice weekly, also orally. In group C, patients used by vaginal route tablets containing 5 mg of gestrinone three times weekly. Reduction in uterine volume occurred in all three groups of patients. Of patients who discontinued treatment at 6 months, uterine volume remained lower than pretreatment values in 89%, 18 months after discontinuation. Of those patients who discontinued at 1 year, uterine volume remained below pretreatment levels in 76% 1 year after discontinuation. In patients treated continuously for 24 months, mean uterine volume decreased from a mean 339 cm3 to 273 cm3, a statistically significant difference. The vaginal route showed statistically more significant volume decreases than the oral route for all treatment intervals.

Administration, Intravaginal↗

PubMed1989

Endocrine, metabolic, and clinical effects of gestrinone in women with endometriosis.

The effect of oral gestrinone, 2.5 mg twice weekly for 6 months, was studied in 11 women with mild or moderate endometriosis laparoscopically confirmed. The mean laparoscopic score decreased from 17.18 to 9.09 (P greater than 0.005). Painful symptoms were relieved in all patients within 2 months from start of therapy. Gonadotropins, prolactin (PRL) 17 beta-estradiol (17 beta-E2), estrone (E1), progesterone (P), androstenedione (A), and dehydroepiandrosterone sulfate (DHEA-S) remained in the follicular phase range. Total testosterone (TT) and sex hormone-binding globulin (SHBG) decreased, whereas free testosterone (FT) slightly increased. Metabolic studies showed a decrease of total triglycerides, very low-density lipoprotein (VLDL) triglycerides, and high-density lipoprotein (HDL) and VLDL cholesterol, parallel to the decrease of associated apoproteins. Low-density lipoprotein cholesterol and apoprotein B increased during therapy. The results suggest that gestrinone possesses antiestrogenic, androgenic, and progestigenic effects at therapeutic dosages both by acting on central and peripheral steroid receptors. For its efficacy and good tolerance, gestrinone may be considered an option for treating endometriosis.

Adult↗

PubMed2005

Discovery, biosynthesis, and structure elucidation of metabolites of a doping agent and a direct analogue, tetrahydrogestrinone and gestrinone, using human hepatocytes.

Tetrahydrogestrinone (18a-homo-pregna-4,9,11-trien-17beta-ol-3-one, THG) is an anabolic androgenic steroid sold to athletes as an undetectable performance enhancer. Being an unapproved substance, no legitimate in vivo human excretion studies could be performed to identify urinary markers of this doping agent. In vitro systems were used as an alternative approach to study the human metabolism of THG and the gestrinone analogue, which is a marketed drug. Incubations of both compounds in the presence of human hepatocytes led to formation of oxidative and glucuroconjugated metabolites. Microgram quantities of the major in vitro metabolites were biosynthesized using human hepatocytes, characterized by HPLC/MS/MS, and their structures elucidated by NMR. Due to high structure similarity, both THG and gestrinone had an analogous in vitro metabolic pathway leading to successive addition of a hydroxyl and a beta-glucuronic acid at C-18. This in vitro metabolite of gestrinone was consistent with a previously reported major but unknown human urinary metabolite. The structure of another metabolite of THG was proposed to be a glucuroconjugate of an oxidative product with a hydroxyl group most likely at C-16epsilon. In vitro information reported therein could significantly impact the identification of new urinary markers of THG for doping control purposes.

Anabolic Agents↗

PubMed1986

A comparison of the effects of danazol and gestrinone on testosterone binding to sex hormone binding globulin in vitro and in vivo.

Danazol and gestrinone are both effective agents in the treatment of endometriosis. Their mechanism of action is unknown but may be related to their androgenic activity, which is at least partly dependent on increases in the proportion of testosterone which circulates unbound to plasma protein. We have quantified these increases in patients on treatment, and by experimentation in vitro have demonstrated the relative importance of the reduction of sex hormone binding globulin (SHBG) binding capacity and competition with testosterone for SHBG binding sites by the drugs and some of their metabolites. The mean SHBG binding capacity in patients treated with danazol (400 mg/d, n = 7) and gestrinone (5 mg/week, n = 7) fell from 66.9 and 56.4 nmol/l to 36.1 and 28.1 nmol/l, after 1 week's treatment and to 11.1 and 7.1 nmol/l after 4 weeks respectively. Despite the similarity between the falls in SHBG binding capacity there was a significantly greater increase in % free testosterone in plasma samples from patients treated with danazol than in those from patients treated with gestrinone at 1 week. Experiments in vitro suggest that this was largely due to ethisterone (a major metabolite of danazol) competing with testosterone for SHBG binding sites. After 4 weeks on treatment there was a similar, near maximal reduction in SHBG binding of testosterone in both treatment groups. At the low levels of SHBG binding capacity reached by this time the extra effect of any competition for binding sites was much reduced.

Danazol↗

PubMed1997

Evaluation of gestrinone after surgery in treatment of endometriosis.

OBJECTIVE: The clinical and histological efficacy of gestrinone in the treatment of endometriosis was evaluated. METHODS: A prospective study was performed with longitudinal follow-up of 4 years duration (minimum) for each patient. Twenty-five cases of endometriosis were treated with gestrinone (as a drug of choice or associated with other local surgical treatment) during 6 months. RESULTS: The total or partial response to pain was induced with treatment in 19 of the 20 cases (95%), and posttreatment pregnancies were induced in 3 of the 9 cases of infertility (33.3%). The global clinical efficacy was as follows: none (n = 5, 20%), poor (n = 2, 8%), moderate (n = 2, 8%), good (n = 3, 12%) and excellent (n = 13, 52%). The pretreatment American Fertility Society score was 23.1 +/- 3.8 points (2-58) and that after treatment (re-examination) 7.8 +/- 3.7 points (0-52), p < 0.01. Global histological efficacy (n = 17) results were as follows: none (23.6%), poor (0%), moderate (5.8%), good (35.3%) and excellent (35.3%). CONCLUSIONS: Gestrinone is presented as a drug with an efficacy comparable to other pharmacological agents currently available in the medical treatment of endometriosis. Adequate posology and acceptable effectiveness were also observed.

Abdominal Pain↗

PubMedDate not supplied

Endometriosis-associated infertility: evaluation of preoperative use of danazol, gestrinone, and buserelin.

In order to assess adequately the effectiveness of danazol, Gestrinone, and Buserelin, a prospective nonrandomized study was initiated in 126 patients with laparoscopically confirmed ovarian endometriosis. After hormonal therapy, laparotomy with microsurgical resection of endometriotic cysts was carried out. Regression (greater than 25%) of ovarian endometriosis was noted in 30%, 34%, and 73% of cases after danazol, Gestrinone, and Buserelin, respectively. The pregnancy rate in moderate endometriosis (53%) differed significantly from the rate obtained in severe endometriosis (45%). The highest percentages were found after Buserelin therapy. In conclusion, Buserelin emerged superior to danazol or Gestrinone treatment. Nevertheless, hormonal treatment leads to an incomplete suppression of ovarian endometriotic implants and this suggests the necessity of surgically removing invasive ovarian endometriosis.

Adult↗

PubMed1987

Oral gestrinone: a novel antiprogestin with no antitumor activity in endocrine-sensitive breast cancer.

We have treated 15 patients with locally advanced or metastatic breast cancer using the synthetic 19-norsteroid gestrinone (2.5 mg orally every 3 days). All patients had assessable disease and endocrine-sensitive tumors, as defined by a previous positive response to endocrine therapy. There were no objective responses. Six patients had disease stabilization and nine had progressive disease on treatment. Seven patients were given endocrine therapy after gestrinone and three have responded. Gestrinone has no significant antitumor activity in hormone-sensitive breast cancer. This, however, does not preclude its use in benign breast disease, particularly since other agents used for benign breast disease can mask occult primary carcinoma.

Administration, Oral↗

PubMedDate not supplied

Comparative efficacy of gestrinone and danazol in infertile women with endometriosis.

The relationship between endometriosis and infertility is observed frequently. Patients with both conditions require a conservative approach to their management. Since hormonal therapy is one of those approaches, we sought to compare the efficacy of Danazol and Gestrinone in 80 infertile patients (48 and 32, respectively). Therapy lasted 6 months in both treatment groups, and all patients studied had laboratory tests performed and were clinically evaluated and classified through laparoscopy before and after therapy. The improvement of symptoms and favorable follow-up were similar with both treatments. The reestablishment of menstrual patterns and fertility were also nearly alike in both groups. However, Gestrinone was associated with fewer secondary effects and is easier to administer than Danazol. We conclude that Gestrinone is a useful medication in the management of the infertile patient with endometriosis.

Adult↗