Severe vasomotor symptoms associated with the menopause; primary ovarian failure; atrophic vaginitis.
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
Absorption: well absorbed, Effect of food: not significant. Distribution: Vd-widely distributed, Protein binding- largely bound to sex hormone-binding globulin and albumin. Metabolism: Hepatic- partially by P450 CYP3A4. Excretion: Renal- primary, Biliary- conjugates secreted into the intestine. Elimination Half Life: Estrone: oral, 26.5 to 26.7 hr
•Baseline adjusted total estrone: oral, 14.8 hr to 17.5 hr
•Equilin: oral, 11.4 to 12.5 hr
禁忌症
Breast cancer; estrogen dependent neoplasia, pregnancy, active thrombophlebitis, or thromboembolic disorders, abnormal vaginal bleeding.
懷孕分類
X [FDA]
哺乳分類
Probably safe, but it can decrease milk production, if breast feeding is desired, the smallest possible estrogen dose should be used and the infant should be monitor for weigh gain and the need for formular supplementation.
副作用
Breast tenderness, enlargement and secretion, melasma, erythema multiforme erythema nodosum, migraine, dizziness, mental depression and chorea.
劑量和給藥方法
1. Moderate to severe vasomotor symptoms associated with the menopause: 1.25 mg/day. If the patient is menstruating, begin administration on day 5 of bleeding.
2. Atrophic vaginitis and kraurosis vulvae: 0.3 to 1.25 mg or more per day.
3. Female hypogonadism: 2.5-7.5 mg/day, TID for 20 days, followed by a rest period of 10 days.
4. Female castration and primary ovarian: 1.25 mg/day.
5. Mammary carcinoma (for palliation): 10 mg TID for at least 3 months.
6. Prevention of postpartum breast engorgement: 3.75 mg Q4H for 5 doses or 1.25 mg Q4H for 5 days.