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Ethinylestradiol/Dienogest in Oral Contraception

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Abstract

The low-dose combined oral contraceptive of ethinylestradiol 30 μg and dienogest 2 mg was launched in Germany in 1995, and is now the most commonly prescribed oral contraceptive in this country. Dienogest is a novel 19-nortestosterone-derived progestin with a unique pharmacokinetic and pharmacological profile, including antiandrogenic properties. Clinical studies have demonstrated that ethinylestradiol/dienogest is a reliable ovulation inhibitor with high contraceptive efficacy that is comparable with other combined oral contraceptives. It also provides effective cycle control, with reduced intensity and duration of menstrual bleeding, and improves dysmenorrhoea. The combination of ethinylestradiol and dienogest reduces serum androgen levels, and increases the levels of thyroid hormones; however, although thyroid hormone levels increase, there is no increased activity due to increases in transporter protein. Like other low-dose oral contraceptives, ethinylestradiol/dienogest has only minor influences on lipid and carbohydrate metabolism, adrenal hormones and blood pressure parameters, and appears to have a balanced effect on the haemostatic system. Ethinylestradiol/dienogest also has beneficial effects on hair and skin; a number of studies have reported decreased hair and skin greasiness, and improvements in acne vulgaris following treatment with ethinylestradiol/dienogest. After discontinuation of ethinylestradiol/dienogest, there may be a small delay in conception during the first three cycles, but there is no subsequent impairment of fertility. Furthermore, the duration of use of ethinylestradiol/dienogest does not seem to influence the rate of conception or time to conception. Ethinylestradiol/dienogest is well tolerated; adverse reactions associated with treatment include breast pain, headache and nausea/vomiting. These adverse reactions are rare and decrease in incidence over time.

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Acknowledgements

Dr Pérez-Campos has acted as a consultant, participated in advisory boards, provided expert testimony, received honoraria for lectures and symposia, and received grants for clinical research from the following companies: MSD, Bayer Schering Pharma, Juste Laboratories, Grunenthal and Wyeth Pharma, Merck Serono, HRA Pharma and Janssen-Cilag. Medical writing assistance for this article was provided by Lucy Ebden of inScience Communications. This assistance was funded by Effik.

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Correspondence to Ezequiel F. Pérez-Campos.

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Pérez-Campos, E.F. Ethinylestradiol/Dienogest in Oral Contraception. Drugs 70, 681–689 (2010). https://doi.org/10.2165/11536320-000000000-00000

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