Estradiol Valerate/Dienogest

Abstract

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 17beta-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 1mg/norethisterone acetate 1mg 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 1mg/norethisterone acetate 1mg 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 multicentre 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.

Evaluation of Uterine Artery Doppler and Estrogen Milieu in Oocyte Donation Pregnancies—A Pilot Study

“…Fourth, it was impossible in this explorative preliminary study to evaluate maternal serum concentrations of other biological forms of estrogen and progestogen. The choice to analyze 17β-estradiol in OD was based on the pharmacokinetic and pharmacodynamics profile of estradiol valerate [25,26]. This study has several strengths.…”

The Effects of Progesterone Selection on Psychological Symptoms in Hormone Replacement Therapy

“…Their climacteric symptoms had been evaluated and Kupperman index scores were found to be 78.5%, 74.5% and 75% respectively [14][15][16]. Although a number of studies have reported physical side effects (constipation, bloating and breast pain) and psychological side effects (depression, fatigue, irritability) resulting from medroxyprogesterone acetate use, these were not observed in prospective randomized studies [17].…”

Acceptabilité par les patientes d'un THS combiné continu versus cyclique : une étude clinique randomisée multicentrique française

“…Commercialisé en France par les laboratoires Schering AG à la dose de 2 mg/jour en association au valé-rate d'estradiol depuis 2003, il s'administre à la dose d'un comprimé par jour en continu dans l'indication « traitement hormonal substitutif (THS) des symptômes de déficit en estrogènes chez les femmes ménopausées depuis au moins un an, et non hystérectomisées ». La tolérance de Climodiène ® sur le plan des saignements s'est avérée bonne [12], avec 67 et 85 % d'aménorrhées respectivement à trois et 12 mois de traitement. Climodiène ® s'est révélé efficace sur les plaintes climatériques et bien toléré dans une étude de phase III [13] sur 1501 femmes traitées pendant un an.…”