Atrophic vulva - Atrophy of vagina
Dyspareunia (Moderate to Severe) - Menopause
藥理
Estrogens bind to nuclear receptors in estrogen-responsive tissues. It modulates the pituitary secretion of the gonadotropins, luteinizing hormone (LH) and follicle stimulating hormone (FSH), through a negative feedback mechanism reducing the levels of these hormones seen in postmenopausal women.
藥動學
Distribution
Vd: widely distributed [4]
Protein binding: largely bound to sex hormone-binding globulin and albumin [4]
Metabolism
Hepatic; partially by P450 CYP3A4 [4]
Metabolites: estrone, estriol, and estrone sulfate [4]
禁忌症
anaphylactic reaction or angioedema to conjugated estrogens, known [2]
arterial thromboembolic disease, active, recent, or history (eg, stroke, myocardial infarction) [2][10][11]
breast cancer, known, suspected, or history [2][11][10]; except in appropriately selected patients being treated for metastatic disease [2]
DVT/pulmonary embolism, active or history [2][10][11]
estrogen-dependent neoplasia, known or suspected [2][10][11]
genital bleeding, undiagnosed abnormal [2][10][11]
hypersensitivity to conjugated estrogens or any other component of the product [10]
liver dysfunction or disease, known [2][10][11]
pregnancy, known or suspected [2][10][11]
protein C, protein S, antithrombin deficiency, or other known thrombophilic disorders [2]
懷孕分類
X (FDA)
D (AUS)
哺乳分類
WHO: Avoid breastfeeding if possible. May inhibit lactation.[18]
Micromedex: Milk effects are possible.
副作用
N/A
(僅有Oral & Inj)
劑量和給藥方法
Atrophic vulva - Atrophy of vagina
initial, 0.5 g INTRAVAGINALLY daily for 21 days, off for 7 days; may increase to 2 g based on clinical response [3]
Dyspareunia (Moderate to Severe) - Menopause
cyclic regimen: 0.5 g INTRAVAGINALLY once daily for 21 days, then off for 7 days [3]
continuous regimen: 0.5 g INTRAVAGINALLY twice a week continuously [3]
小兒調整劑量
safety and efficacy of oral conjugated estrogen in children not established; however, estrogen therapy has been used for the induction of puberty in adolescents with some forms of pubertal delays [2]
conjugated estrogen vaginal cream is not indicated for use in children [3]