Titre du document / Document title

Estradiol valerate/dienogest

Auteur(s) / Author(s)

WELLINGTON Keri ⁽¹⁾ ; PERRY Caroline M. ⁽¹⁾ ;

Affiliation(s) du ou des auteurs / Author(s) Affiliation(s)

⁽¹⁾ Adis International Limited, Auckland, NOUVELLE-ZELANDE

Résumé / Abstract

A 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. A 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. A 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 I year were each as effective as estradiol 2mg/estriol I mg/norethisterone acetate 1 mg 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. A The number ofdays 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%. A Endometrial biopsy results were similar in patients treated with estradiol valerate 2mg/dienogest 2mg, estradiol valerate 2mg/dienogest 3mg or estradiol 2mg/estriol 1 mg/norethisterone acetate 1 mg 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 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.

Revue / Journal Title

Drugs   ISSN 0012-6667   CODEN DRUGAY 

Source / Source

2002, vol. 62, n^o3, pp. 491-504 (47 ref.)

Langue / Language

Anglais

Editeur / Publisher

Adis International, Auckland, NOUVELLE-ZELANDE  (1962) (Revue)

Mots-clés anglais / English Keywords

Review ; Toxicity ; Pharmacokinetics ; Oral administration ; Female ; Human ; Replacement therapy ; Chemotherapy ; Hormone replacement therapy ; Menopause ; Drug combination ; Estroprogestagen ; Progestagen ; Estrogen ; Dienogest ; Estradiol valerate ;

Mots-clés français / French Keywords

Article synthèse ; Toxicité ; Pharmacocinétique ; Voie orale ; Femelle ; Homme ; Traitement substitutif ; Chimiothérapie ; Traitement hormonal ; Ménopause ; Association médicamenteuse ; Oestroprogestatif ; Progestatif ; Oestrogène ; Diénogest ; Valérate d'estradiol ;

Mots-clés espagnols / Spanish Keywords

Artículo síntesis ; Toxicidad ; Farmacocinética ; Vía oral ; Hembra ; Hombre ; Tratamiento sustitutivo ; Quimioterapia ; Hormonoterapia ; Menopausia ; Asociación medicamentosa ; Estroprogestágeno ; Progestágeno ; Estrógeno ; Dienogest ; Valerato de estradiol ;

Localisation / Location

INIST-CNRS, Cote INIST : 15326, 35400010043421.0060