estradiol
Sources réglementaires consultées
Indications approuvées
- Traitement des symptômes de déficit en œstrogènes chez la femme ménopausée.
- Prévention de l’ostéoporose postménopausique chez les femmes à haut risque de fracture qui ne tolèrent pas les autres médicaments autorisés ou chez lesquelles ils sont contre-indiqués.
Contre-indications
Absolues
- Cancer du sein actuel, antérieur ou suspecté ; tumeur maligne œstrogénodépendante ; saignement génital non diagnostiqué ; hyperplasie endométriale non traitée.
- Thromboembolie veineuse actuelle ou antérieure, thrombophilie connue, maladie thromboembolique artérielle active ou récente.
- Maladie hépatique aiguë ou antécédent sans normalisation des tests, porphyrie ou hypersensibilité.
Mises en garde cliniques
- Mise en garde majeure · Réévaluer au moins chaque année la nécessité du traitement hormonal. Évaluer les risques de cancer du sein et de l’endomètre, de thromboembolie veineuse, d’AVC et cardiovasculaires ; arrêter en cas de thrombose ou d’ictère. — CIMA/AEMPS, ficha técnica 82115
- Mise en garde majeure · Chez la femme ayant un utérus, les œstrogènes non opposés augmentent le risque d’hyperplasie et de cancer de l’endomètre ; ajouter un progestatif et évaluer tout saignement inattendu. — CIMA/AEMPS, ficha técnica 82115
Interactions médicamenteuses
- ModéréeInducteurs enzymatiques tels que phénobarbital, phénytoïne, carbamazépine, rifampicine, éfavirenz ou millepertuis
Mécanisme: Ils augmentent le métabolisme de l’estradiol et peuvent réduire l’effet ou modifier les saignements.
Recommandation: Surveiller la réponse clinique et le profil des saignements ; ajuster le traitement avec l’équipe soignante.
CIMA/AEMPS, ficha técnica 82115https://cima.aemps.es/cima/dochtml/ft/82115/FT_82115.html
- SévèreLamotrigineN03AX09
Mécanisme: Les œstrogènes induisent la glucuronidation de la lamotrigine et peuvent diminuer ses concentrations. Bien que l’interaction avec le traitement hormonal substitutif n’ait pas été étudiée directement, un effet similaire à celui observé avec les contraceptifs hormonaux est attendu.
Recommandation: Surveiller le contrôle des crises et réévaluer le traitement avec l’équipe soignante lors de l’instauration ou de l’arrêt de l’estradiol.
CIMA/AEMPS, ficha técnica 82115https://cima.aemps.es/cima/dochtml/ft/82115/FT_82115.html
- ModéréeSchémas antiviraux à action directe contre le VHC
Mécanisme: Les données disponibles avec l’estradiol sont limitées ; la prudence est recommandée avec ombitasvir/paritaprévir/ritonavir et dasabuvir, avec ou sans ribavirine, glécaprévir/pibrentasvir ou sofosbuvir/velpatasvir/voxilaprévir en raison du signal d’élévation des ALAT observé avec les œstrogènes.
Recommandation: Utiliser avec prudence et suivre le RCP de l’antiviral ainsi que la surveillance hépatique indiquée.
CIMA/AEMPS, ficha técnica 82115https://cima.aemps.es/cima/dochtml/ft/82115/FT_82115.html
Effets indésirables
Communs (≥1%)
Sensibilité ou douleur mammaire · Saignement vaginal ou spottings · Nausées ou douleur abdominale · Céphalées · Variations de poids · Dépression ou humeur dépressive
Rares mais graves
Thromboembolie veineuse · AVC ou infarctus du myocarde · Cancer de l’endomètre ou du sein
Grossesse et allaitement
Il n’est pas indiqué pendant la grossesse ; arrêter immédiatement en cas de grossesse. Il n’est pas indiqué pendant l’allaitement.
Bibliographie récente (PubMed)
Soy contains genistein and daidzein isoflavones. Isoflavones are phytoestrogens, with a similarity in structure to human 17-β estradiol hormone. They imitate the action of estrogen on organs by binding and activating estrogen receptors. Numerous studies have examined the relationship between soy consumption and breast cancer but not the amount of consumption itself. We performed a systematic review of the literature in order to determine whether the amount of soy and isoflavones consumed has a positive effect in pre- and post-menopausal women. Data gathering was performed following PRISMA guidelines. Narrowing down the result set for all relevant data was performed via title, abstract, full-text evaluation and the snowball procedure. The selected articles had all relevant data extracted. Analysis of the data was performed using Cochrane's Review Manager statistical analysis tool in order to draw conclusions regarding the positive effect for the amount of soy and isoflavones consumed. Significant results were found when statistically analyzing data from prospective studies which compared soy isoflavones consumption, breast cancer risk and occurrence. The data were indicative of a clear inverse correlation between the amount of isoflavones consumed and breast cancer occurrence in pre- and post-menopausal women. The consumption of soy isoflavones can reduce the risk of breast cancer in pre-menopausal and post-menopausal women.
Male infertility is a prevalent and worldwide problem with various difficulties in treatment. Clomiphene citrate is a selective estrogen receptor modulator and may improve semen quality by stimulating hormone synthesis and spermatogenesis. There is lack of evidence on the efficacy of clomiphene citrate as therapy for male infertility. Therefore, a systematic review and meta-analysis was performed to assess the efficacy of clomiphene citrate on sperm quality in infertile men. A search was conducted in the PubMed, EMBASE and Cochrane databases for effectiveness in infertile males treated with clomiphene citrate. Both intervention and observational studies were included. Primary outcome measures were semen parameters (concentration, motility and morphology). Secondary outcomes included hormonal evaluation, pregnancy rate and side effects. Studies were included for meta-analysis if they provided absolute numbers for outcomes before and during treatment with appropriate SD or SE. Total 1799 studies were identified during the search, 18 studies remained for qualitative analysis (n = 731) and 15 studies for meta-analysis (n = 566). Study populations ranged between 11 and 140 participants. Sperm concentration was higher during treatment, with a mean difference 8.38 × 106 /ml (95% confidence interval: 5.17-11.59; p < 0.00001; I2 = 87%). Total sperm motility was higher during treatment, with a mean difference of 8.14% (95% confidence interval: 3.83-12.45; p < 0.00001; I2 = 76%). There was no difference in sperm morphology before and during treatment. Total testosterone, follicle-stimulating hormone, luteinizing hormone and estradiol were higher during clomiphene citrate treatment. During follow-up, no serious adverse effects occurred. In 10 studies, pregnancy rate was reported and yielded a mean of 17% during clomiphene citrate treatment (range: 0%-40%). Clomiphene citrate increased sperm concentration and motility and could be considered as a safe therapy for improving spe
Transdermal estradiol is licensed to treat estradiol deficiency symptoms and prevent osteoporosis in postmenopausal women. There is no one-size-fits-all estradiol dose or serum concentration that will achieve symptom relief and bone protection in all women. Dose is usually titrated to symptom response, but measurement of serum estradiol concentration can be used to support or inform dose decisions in certain clinical scenarios. The optimal level for an individual varies according to tissue sensitivity (pharmacodynamic effects), the method used for estradiol quantitation (immunoassay vs. mass spectrometry), the clinical endpoint (symptoms vs. bone protection), and treatment goals, including patient preferences. An understanding of transdermal estradiol pharmacokinetics and pharmacodynamics, and the limitations of the methods used to measure serum estradiol, is essential to ensure that all women who choose to use menopausal hormone therapy (MHT) can reap the benefits and avoid the harms of over-treatment and under-treatment. Achieving and maintaining optimal estradiol levels for all MHT users is consistent with menopause guidelines that promote high-quality, patient-centred, personalized menopause care.
Male hypogonadism is a clinical and biochemical androgen insufficiency syndrome, becoming more prevalent with age. Exogenous testosterone is first-choice therapy, with several side effects, including negative feedback of the hypothalamic-pituitary-gonadal axis, resulting in suppression of intratesticular testosterone production and spermatogenesis. To preserve these testicular functions while treating male hypogonadism, clomiphene citrate is used as off-label therapy. This systematic review and meta-analysis aimed to evaluate the effectiveness and safety of clomiphene citrate therapy for men with hypogonadism. The EMBASE, PubMed, Cochrane databases were searched in May 2021, for effectiveness studies of men with hypogonadism treated with clomiphene citrate. Both intervention and observational studies were included. The Effective Public Health Practice Project Quality Assessment Tool, a validated instrument, was used to assess methodological study quality. The primary outcome measure was the evaluation of serum hormone concentration. Secondary outcomes were symptoms of hypogonadism, metabolic and lipid profile, side effects, safety aspects. We included 19 studies, comprising four randomized controlled trials and 15 observational studies, resulting in 1642 patients. Seventeen studies were included in the meta-analysis, with a total of 1279 patients. Therapy and follow-up duration varied between one and a half and 52 months. Total testosterone increased with 2.60 (95% CI 1.82-3.38) during clomiphene citrate treatment. An increase was also seen in free testosterone, luteinizing hormone, follicle stimulating hormone, sex hormone-binding globulin and estradiol. Different symptom scoring methods were used in the included studies. The most frequently used instrument was the Androgen Deficiency in Aging Males questionnaire, whose improved during treatment. Reported side effects were only prevalent in less than 10% of the study populations and no serious adverse events were r
Estrogens (estradiol, estriol, and estrone) are important hormones that directly and indirectly regulate the metabolism and function of bone and skeletal muscle via estrogen receptors. Menopause causes a dramatic reduction in the concentration of estrogen in the body. This contributes to a decline in bone and skeletal muscle function, thereby resulting in osteoporosis and sarcopenia. Menopausal women often experience osteoporosis and muscle wasting, and clinicians recognize estrogen as playing an important role in these conditions, particularly in women. Bone and muscle are closely related endocrine tissues that synthesize and produce various cytokines. These bone- and muscle-derived cytokines, including interleukin-6, irisin, β-aminoisobutyric acid, osteocalcin, fibroblast growth factor-23, and sclerostin, regulate both local and distant tissues, and they mediate the crosstalk between bone and skeletal muscle. This review examines the metabolic effects of estrogen on bone and skeletal muscle and describes cytokine-mediated bone-muscle crosstalk in conditions of estrogen deficiency.