gestodene and Acne-Vulgaris

Acne and seborrhea (or facial oiliness) are related androgenic skin disorders which affect a high proportion of women after menarche. They can have a negative effect on psychological well-being and social life. Androgens play an important role in the pathogenesis of acne through the stimulation of sebum secretion, increasing sebaceous gland size and possibly through follicular hyperkeratinization. Conversely, estrogens decrease sebum production by suppressing gonadotropin release and androgen production and increasing sex hormone binding globulin production. One of the treatment options for these conditions is hormonal therapy, especially for women who require contraception. The effect of combined oral contraceptives in androgenic skin disorders depends on their estrogen:progestogen balance and on the antiestrogenic activity of the progestogen component. Improved understanding of what women value about oral contraceptives suggests that the choice of product should be tailored as much as possible to the individual. Several combined oral contraceptives containing new-generation progestogens (e.g. desogestrel, gestodene) or progestational antiandrogens (e.g. cyproterone acetate, chlormadinone acetate) have demonstrated efficacy in the treatment of women with acne, although comparisons between trials are difficult because of differing endpoints. Seborrhea has been less well studied, but the few studies that are available show an improvement in women with this condition using combined oral contraceptives.

Topics: Acne Vulgaris; Contraceptives, Oral; Contraceptives, Oral, Combined; Dermatitis, Seborrheic; Desogestrel; Ethinyl Estradiol; Female; Humans; Norgestrel; Norpregnenes; Safety; Treatment Outcome

To investigate the effect of a triphasic low-dose oral contraceptive pill containing gestodene on acne severity and hormone levels in young women over 13 menstrual cycles.. A total of 33 subjects aged 16-25 years with moderate facial acne were enrolled in the study. The primary efficacy end-points used in the clinical assessment of acne were the overall severity and number of lesions, sebum secretion and superficial follicular biopsy. Both physicians and patients evaluated acne status. Blood levels of sex hormone binding globulin (SHBG), estradiol, progesterone and androgens were monitored.. By cycle 13, the total lesion count had been reduced by 80%. Physicians and patients assessed acne status in 90% and 95% of cases, respectively, as better or much better (p < 0.001). At the end of the study, SHBG levels had increased by 229% and total and free testosterone levels had decreased by 41% and 70%, respectively.. An oral contraceptive containing triphasic gestodene has a beneficial effect on the severity ofacne, decreases major circulating androgen levels and is well tolerated.

Topics: Acne Vulgaris; Adolescent; Adult; Androgens; Contraceptives, Oral, Synthetic; Estradiol; Female; Hormones; Humans; Norpregnenes; Progesterone; Progesterone Congeners; Severity of Illness Index; Sex Hormone-Binding Globulin; Treatment Outcome

To assess the contraceptive efficacy, cycle control and acceptability of two monophasic oral contraceptives containing either 30 micrograms ethinylestradiol plus 150 micrograms desogestrel or 30 micrograms ethinylestradiol plus 75 micrograms gestodene.. In a randomized, open-label, six-cycle, group-comparative, multicenter study performed in Brazil, pregnancies, cycle-control parameters, incidence of side-effects and the presence and severity of acne vulgaris were assessed, and blood pressure and body weight were measured at pretreatment and after one, three and six cycles of oral contraceptive use.. Of the 595 women enrolled, 274 (86.7%) in the desogestrel/ethinylestradiol group and 227 (81.4%) in the gestodene/ethinylestradiol group completed the six cycles, providing data for 1753 and 1487 treatment cycles, respectively. Two pregnancies occurred, one of which (in the desogestrel/ethinylestradiol group) was attributed to user failure, whilst the other (in the gestodene/ethinylestradiol group) was thought to result from method failure. Cycle control was observed to be excellent; the incidences of irregular bleeding and minor side-effects were low in both groups and decreased after an initial increase in the first cycle. Pre-existing acne improved in both groups, whereas blood pressure and body weight remained essentially unchanged.. Both desogestrel/ethinylestradiol and gestodene/ethinylestradiol provide effective oral contraception with comparable cycle control and acceptability.

Topics: Acne Vulgaris; Adult; Blood Pressure; Body Weight; Brazil; Contraceptives, Oral, Combined; Contraceptives, Oral, Synthetic; Desogestrel; Estradiol Congeners; Ethinyl Estradiol; Female; Humans; Menstrual Cycle; Norpregnenes; Progesterone Congeners; Severity of Illness Index; Uterine Hemorrhage

The effect of gestodene 75 micrograms (GTD) versus desogestrel 150 micrograms (DSG) combined with 30 micrograms of ethinylestradiol (EE) on acne lesions and plasma androstenedione (A), total testosterone (T), sex hormone binding globulin (SHBG) and "free androgen index" (FAI) was evaluated in an open study on 19 patients aged 18-35 years affected with postpubertal or persistent non-severe acne vulgaris. The patients were randomly allocated into two groups receiving EE-GTD (n = 8) and EE-DSG (n = 11), 21 tablets per cycle for 9 consecutive cycles. Clinical and hormonal evaluations were made between days 17-21 in the cycle before treatment and between days 17-21 of the cycle 3, 6 and 9 of treatment. During treatment, acne improved in most patients, reaching at cycle 9 a low score (absent or minimal) in 62% of the cases in the GTD group (mean acne score = 1.25) and in 90% of the cases in the DSG group (mean acne score = 0.90). Before treatment, about 75% of the patients showed one or more signs of biochemical hyperandrogenism, including elevated FAI (57%), elevated A (15%), elevated total T (15%) and decreased SHBG (21%), and there was evidence of inverse correlation between SHBG and acne scores (p < 0.05). The echogenic texture of the ovaries was multifollicular in 55% of the cases. By the end of the third cycle of treatment, the hormonal changes observed in both groups included significant decreases, with normalization of individual elevated levels of T, and a 3-fold rise of the initial values of plasma SHBG, which showed a further gradual increase at cycle 9 of EE-DSG administration. At cycle 9, normalization of the echogenic ovarian texture was observed. Acne improvement under treatments with estrogen and progestin (EP) could be significantly correlated with the normalization of biochemical hyperandrogenism. In conclusion, the biochemical and clinical efficacy of EE-GTD and EE-DSG indicate that both these preparations can be a good choice in the therapy of acne vulgaris, with a non-significant better clinical result with EE-DSG.. At the Sacred Heart Catholic University in Rome, Italy, health researchers randomly allocated 19 nulligravidae aged 18-35 with either postpubertal or persistent non-severe acne vulgaris to receive either the combined oral contraceptive (OC) containing 30 mcg ethinyl estradiol (EE) and 75 mcg gestodene (GTD) (Minulet) or 30 mcg EE and 150 mcg desogestrel (DSG) (Marvelon). They aimed to evaluate the effect of GTD and DSG combined with low doses of EE on acne lesions and on hormone levels. The women used the OCs (21 tablets/cycle) for nine consecutive cycles. At baseline, about 75% of all patients had at least one sign of biochemical hyperandrogenism (57% for elevated free androgen index, 15% for elevated androstenedione, 15% for elevated total testosterone, and 21% for reduced sex hormone binding globulin [SHBG]). At baseline, the higher the acne score was, the lower the SHBG level was (p 0.05). The ovaries of 55% of the women had multiple follicles. Acne improved significantly in both groups (mean acne score, 2.9-0.9 for EE/DSG and 2.87-1.25 for EE/GTD; p 0.05). In fact, 62% of cases in the EE/GTD group and 90% of those in the EE/DSG group had either minimal or no acne lesions. Acne improvement during treatment was significantly associated with normalization of biochemical hyperandrogenism. At completion of the third cycle of treatment, both groups experienced significant decreases in hormones. Individual elevated levels of testosterone normalized. The initial values of plasma SHBG had increased 3-fold. SHBG increased gradually to cycle 9 of EE-DSG OC use. At completion of cycle 9, the echogenic ovarian texture returned to normal. These findings suggest that, since both OCs are biochemically and clinically effective, these OCs may be a good treatment for acne vulgaris.

Topics: Acne Vulgaris; Adolescent; Adult; Androgens; Androstenedione; Desogestrel; Ethinyl Estradiol; Female; Humans; Norpregnenes; Ovary; Sex Hormone-Binding Globulin; Testosterone

Two triphasic oral contraceptives containing either gestodene or norethindrone as the progestogenic compound combined with ethinyl estradiol were compared in a randomized clinical trial to assess their contraceptive reliability, clinical tolerance and cycle control. Both preparations were effective in preventing pregnancy. The gestodene preparation proved significantly superior regarding cycle control and general tolerance.. In Germany, researchers randomly placed 126 women into a group taking a triphasic oral contraceptive (OC) with gestodene and 128 women into another group taking triphasic norethindrone to do a 1-year controlled, multicenter open trial examining contraceptive efficacy, cycle control, and general tolerance. No one became pregnant during the study, despite mistakes in pill intake in 32 (2.5%) and 44 (3.7%) pill cycles of the gestodene group and norethindrone group, respectively. Women in the gestodene group experienced spotting at a higher rate than those in the norethindrone group (27% vs. 15.8%; p .05). The difference remained significant even when the researchers examined only 1st-time OC users (10.2% vs. 5%; p .05). On the other hand, breakthrough bleeding occurred less often in women in the gestodene group (19.3% vs. 29.6%). Over time, women in the norethindrone group were more likely to gain more than 2 kg than those in the gestodene group. Neither group experienced changes in blood pressure. Neither OC caused any serious adverse events, e.g., thromboembolism. The most common subjective adverse events were painful menstrual periods, breast tension, and headache. The incidence of acne increased in the norethindrone group. Adverse events were responsible for 3.5% of women in the gestodene group and 11.3% in the norethindrone group dropping out, sometimes citing more than 1 adverse event. Women in the norethindrone group were more likely to drop out because of adverse events than were those in the gestodene group (50% of all dropouts vs. 25%; p .05). Triphasic gestodene had better cycle control and was better tolerated than triphasic norethindrone. Weight gain and acne were less common in the gestodene group than the norethindrone group. In conclusion, triphasic gestodene is superior to that of triphasic norethindrone.

Topics: Acne Vulgaris; Adult; Contraceptives, Oral, Combined; Female; Headache; Humans; Menstrual Cycle; Middle Aged; Norethindrone; Norpregnenes; Patient Dropouts; Progesterone Congeners; Weight Gain

Hyperandrogenism is a condition affecting 5-10% of adolescents. The aim of this study was to evaluate the efficacy of very low dose of flutamide in the treatment of hyperandrogenism in adolescence. One hundred and fifty-eight patients, presenting severe acne and/or hirsutism, received 62.5 mg/day of flutamide + ethinylestradiol + gestodene for 18 months. The patients were subjected to assessments of hepatic enzymes levels. Thirty subjects treated with drospirenone + ethinylestradiol represented the control group. After 18 months of treatment, it was obtained a decrease of hirsutism (-39.9%), an almost recovery of acne (98% of patients) with better results of those obtained in control group. Only one case of light hypertransaminasemia was recorded, regressed spontaneously. Very low dose of flutamide was successful and safe and in the treatment of hyperandrogenism in adolescence.

Topics: Acne Vulgaris; Adolescent; Androgen Antagonists; Androstenes; Dose-Response Relationship, Drug; Drug Therapy, Combination; Ethinyl Estradiol; Female; Flutamide; Hirsutism; Humans; Hyperandrogenism; Norpregnenes; Treatment Outcome; Young Adult

A case of unusual combination of polycystic ovaries (PCO), adrenal non-functioning adenoma and severe hirsutism in a young woman from Southern Italy is reported here. A 18-yr-old woman was referred to our Department because of oligomenhorrea, acne and severe hirsutism. During evaluation of the cause of her symptoms, PCO and small left adrenal adenoma were revealed. Although adrenal androgen excess has been shown to dysregulate the hypothalamic-pituitary-gonadal axis, causing PCO-like syndrome, normal circulating androgen values were found. Androgens and cortisol levels were completely suppressed by low-dose dexamethasone test, excluding autonomous steroid secretion by the adrenal mass. Normal response of cortisol and adrenal androgens to corticotropin stimulation test permitted the exclusion of functional adrenal hyperandrogenism. Despite normal LH/FSH ratio, anovulatory cycles were revealed by persistently low progesterone values. Glucose and insulin response to oral glucose tolerance test did not differ from those of normal population. The patient showed an improvement of acne and hirsutism on therapy with estro-progestins (EP). In conclusion, despite normal pattern of serum androgens and LH/FSH ratio, this patient had anovulatory cycles and good response to the EP treatment. These findings suggest that ultrasonography evidence of PCO together with anovulatory cycles contributed to her clinical picture whereas adrenal adenoma seemed to have no relevant role. This case report underlines the need of cautious interpretation of imaging results and clinical signs of severe hirsutism, reminding one that the true cause of a medical problem may not be the most evident.

Topics: Acne Vulgaris; Adenoma; Adolescent; Adrenal Gland Neoplasms; Androgens; Estrogens; Ethinyl Estradiol; Female; Hirsutism; Humans; Norpregnenes; Oligomenorrhea; Ovary; Polycystic Ovary Syndrome; Progestins; Treatment Outcome; Ultrasonography

Four new precise accurate and selective methods have been developed for the determination of gestodene (I) and cyproterone acetate (II). The first method (A) depends on reaction of (I) and (II) with isoniazide in an acid medium and the colored products were measured at 378 and 400 nm, respectively. The second method (B) depends on the reaction of (I) and (II) with tetrazolium blue in an alkaline medium and the colored products were measured quantitatively at 515 and 520 nm, respectively. The optimum conditions for the analysis were studied. Both methods determined gestodene (I) in concentration range from 4 to 24 microg ml(-1) with mean percentage recoveries 99.54%+/-1.20 and 99.63%+/-1.89 for method A and B, respectively. For cyproterone acetate, the concentration ranges were 4-36 and 8-40 microg ml(-1) with mean percentage recoveries 99.94%+/-1.19 and 99.23%+/-2.00 for methods A and B, respectively. The third method (C) depends on the quantitative evaluation of (I) and (II) densitometrically using dichloroethane:methanol:water (95:5:0.2) as mobile phase and the chromatogram were scanned at 247 and 281 nm, respectively. Method (C) determines (I) and (II) in concentration ranges from 0.2 to 1.6 and 0.1-0.7 microg microl(-1) using Hamilton syringe 10 microl, with mean percentage recoveries 99.94%+/-1.19, and 99.82%+/-1.75, respectively. The fourth method (D) is a first derivative one depends on measuring the D(1) value at 303 nm for (II) only in concentration range 10-20 microg ml(-1) with mean percentage recoveries 99.95%+/-1.49.

Topics: Acne Vulgaris; Contraceptives, Oral, Synthetic; Cyproterone Acetate; Dosage Forms; Norpregnenes; Tablets