Estradiol Valerate/Dienogest

- ▴ Estradiol valerate 2mg/dienogest 2mg is an oral estrogen/progestogen formulation that has been approved throughout the European Union for the treatment of climacteric symptoms in postmenopausal women. - ▴ Dienogest is a progestogen that combines the properties of both progesterone and 19-nortestosterone derivatives. It has moderate affinity for the progesterone receptor, significant antiproliferative and antiandrogenic activity, and produces secretory transformation of the endometrium. - ▴ Estradiol valerate is an esterified form of natural 17β-estradiol, the most potent endogenous human ovarian estrogen, and is hydrolysed to estradiol soon after oral administration. - ▴ Results from a randomised, double-blind, multicentre trial showed that oral estradiol valerate 2mg/dienogest 2mg and estradiol valerate 2mg/dienogest 3mg once daily for 1 year were each as effective as estradiol 2mg/estriol lmg/norethisterone acetate lmg in the treatment of climacteric symptoms in 581 postmenopausal women; reductions from baseline in Kupperman Index scores were 78.5, 74.5 and 75.0%, respectively. - ▴ The number of days without any type of bleeding was lowest in patients treated with estradiol valerate 2mg/dienogest 2mg (8.7 days), and highest in the estradiol valerate 2mg/dienogest 3mg group (12.1 days). During the twelfth month of treatment with estradiol valerate 2mg/dienogest 2mg, the percentage of patients who reported bleeding was 14.5%. - ▴ Endometrial biopsy results were similar in patients treated with estradiol valerate 2mg/dienogest 2mg, estradiol valerate 2mg/dienogest 3mg or estradiol 2mg/estriol lmg/norethisterone acetate lmg once daily for 1 year; 90.8, 87.4 and 87.5% of samples, respectively, contained atrophic material. Proliferative material was found in 4.2, 2.5 and 4.4% of the biopsies, respectively; there was no incidence of hyperplasia in any of the treatment groups. - ▴ A noncomparative muticentre study in 1501 postmenopausal women demonstrated that adverse events associated with estradiol valerate 2mg/dienogest 2mg once daily for 48 weeks included breakthrough bleeding, mastalgia, headache, abdominal pain, hypertension, thrush, migraine, weight gain, increase in endometrial thickness and metrorrhagia. Similar content being viewed by others

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Continuous-combined treatment of the menopause with combinations of oestradiol valerate and dienogest: a dose-ranging study. Maturitas 2000 Jun 30; 35(3): 253–61 Author information Authors and Affiliations Corresponding author Rights and permissions About this article Cite this article Wellington, K., Perry, C.M. Estradiol Valerate/Dienogest. Drugs 62, 491–504 (2002). https://doi.org/10.2165/00003495-200262030-00006 Published: Issue date: DOI: https://doi.org/10.2165/00003495-200262030-00006