Ovulatlon Inhibitors Containing Cyproterone Acetate Or Desogestrel In The Treatment Of Hyperandrogenic Symptoms

Abstract

An open, randomized, multicenter study was carried out to compare two oral contraceptives as regards their therapeutic efficacy in androgenization symptoms such as acne, seborrhea and hirsutism in women. The preparations used were the combination of 2 mg cyproterone acetate (CPA) with 0.035 mg ethinyl estradiol (EE) (Diane 35, Schering AG, Berlin-West) and 0.150 mg desogestrel (DG) with 0.03 mg ethinyl estradiol (Marvelon, Organon, Oss, The Netherlands). The duration of therapy was 9 months. The combination of CPA-EE was used by 83 patients for 658 cycles and the combination of DG-EE by 79 women for 618 cycles. No pregnancy occurred under either therapy. Both preparations are well tolerated. However, some side-effects, such as reduced libido, nervousness and breast tenderness, were observed more frequently (p less than 0.05) in the DG-EE group than among the users of the CPA-EE combination. The therapeutic outcome was better in the CPA-EE group, especially in cases of facial acne (p less than 0.05). Seborrheic symptoms also responded better to the CPA-EE therapy. The results show that the CPA-EE combination is superior to the DG-EE combination in the treatment of acne and seborrhoea.

Oral Spironolactone for Acne Vulgaris in Adult Females: A Hybrid Systematic Review

“…Data from over 50 articles reporting effects on serum androgens are equivocal. One report showed inhibition of 5α-reductase type I in genital skin—relevance to acne at therapeutic doses unclearNACimetidineSuppression of sebum excretion at doses ≥1 g/day [82, 84, 93]AR antagonistInhibits 2-hydroxylation of estradiol, thereby reducing testosterone productionNACyproterone acetate/EE (Diane-35™)Suppression of sebum excretion [94–99]AR antagonist/partial agonistSteroidogenesis inhibitor (mainly 3β-hydroxysteroid dehydrogenase and 17, 20-lyase); suppresses gonadotrophin release; increases hepatic SHBG production but does not bind to itNoneDesogestrel/EE (Marvelon™)Suppression of sebum excretion [94, 99–103]Steroidogenesis inhibitorSuppresses gonadotrophin release, thereby decreasing ovarian androgen output; increases hepatic SHBG production (significantly more than levonorgestrel). Active metabolite binds to SHBGLow-affinity agonistLevonorgestrel/EE (Triphasil™)Suppression of sebum excretion (no in vivo evidence in humans)Steroidogenesis inhibitorSuppresses gonadotrophin release, thereby decreasing ovarian androgen output; increases hepatic SHBG production and binds to it with high affinityAgonist (more potent than desogestrel and much more potent than norgestimate)Norgestimate/EE (Ortho-Cyclen™)Suppression of sebum excretion [100, 104]Steroidogenesis inhibitorSuppresses gonadotrophin release, thereby decreasing ovarian androgen output; increases hepatic SHBG production; possible 5α-reductase inhibitor.…”

Isotretinoin and the Risk of Depression in Patients With Acne Vulgaris

“…Studies conducted on cyproterone acetate have been of poor quality. Only one study was a randomized trial, but used subjective dermatological measurements, such as "complete healing" and "definitive healing" to assess treatment efficacy (76). Other studies were not randomized trials (77,78) and only one used an objective dermatological measure such as lesion count to assess treatment efficacy (78).…”

“…Other studies were not randomized trials (77,78) and only one used an objective dermatological measure such as lesion count to assess treatment efficacy (78). In ail, these studies reported 60% to 73% in improvement compared to baseline (76)(77)(78).…”

The use of cyproterone acetate/ethinyl estradiol in hyperandrogenic skin symptoms – a review

“…In the study by Erkkola et al [52], CPA/EE normalised seborrhea in 59.2% of patients within nine months and also led to an improvement of facial acne in 80.7% and complete healing of acne in 59.7% of women. Golland and Elstein [51] also described improvements in coexisting acne and seborrhea with CPA/EE.…”

“…For example, when combined with antibiotics (tetracycline) in the treatment of acne, or with antiandrogens (finasteride or spironolactone) in the treatment of hirsutism, the potential for enhanced efficacy was suggested [31,36,37,55]. Studies where CPA/EE was added to gonadotropin releasing hormone agonist (GnRHa) to evaluate potential for amplification of treatment response in hyperandrogenic symptoms of PCOS described significant improvement in hirsutism symptoms overall (reductions in hirsutism score were between 24% and 47.4%) but no significant difference between the two groups [50,52,56]. Sequential use of CPA/EE with rosiglitazone did not generate any greater symptom improvement than use of CPA/EE alone in women with PCOS [49].…”