Estrogens Clinical uses 1)Postmenopausal syndrome-tibolone Postmenpausal hormone replacement therapy (HrT) prevention of osteoporosIs, Fractures of the spine, wrist, and hips decrease by 50-70% and spinal bone density increases by x5% in women treated with estrogen within 3 years of the onset of menopause and for 5-10 years thereafter treat vasomotor CNs symptoms hot flushes, vaginal dryness, urinary stress incontinence, chilly sensations dizziness, fatigue, irritability, and sweating. prevention of cardiovasculardisease lowerS LDL. TG: raises hdl levels endothelial vasodilatation properties, anti-inflammatory
(1) Postmenopausalsyndrome-tibolone Postmenpausal hormone replacement therapy (HRT): • prevention of osteoporosis; - Fractures of the spine, wrist, and hips decrease by 50-70% and spinal bone density increases by ~5% in women treated with estrogen within 3 years of the onset of menopause and for 5–10 years thereafter. • treat vasomotor & CNS symptoms - hot flushes, vaginal dryness, urinary stress incontinence, chilly sensations, dizziness, fatigue, irritability, and sweating. • prevention of cardiovascular disease -lowers LDL ,TG; raises HDL levels -endothelial vasodilatation properties , anti-inflammatory Clinical uses Estrogens
Estrogens (2) Primary hypogonadism(卵巢功能不全 replacement vaginal atrophy, hypoestrogenism 3)Menstrual disorders amenorrhea, dysmenorrhea, and oligomenorrhea severe dysfunctional uterine bleeding (4)Contraception (5)Others: suppress lactation after c child birth advanced breast cancer(postmenopausal)and prostatic cancer -hormone-sensitive or hormone-receptor-positive cancers -hormone therapy, or anti-estrogen therapy (not to be confused with hormone replacement therapy) acne · neuroprotection
(2) Primaryhypogonadism (卵巢功能不全):replacement • vaginal atrophy, hypoestrogenism (3) Menstrual disorders • amenorrhea , dysmenorrhea, and oligomenorrhea; • severe dysfunctional uterine bleeding (4) Contraception (5) Others: • suppresslactation after child birth • advanced breast cancer (postmenopausal) and prostatic cancer -hormone-sensitive or hormone-receptor-positive cancers -hormone therapy, or anti-estrogen therapy (not to be confused with hormone replacement therapy) • acne • neuroprotection Estrogens
Estrogens 3. Adverse effects (1 Oral administration: nausea, vomiting, diarrhea (2)Cardiovascular effects risk of venous thromboembolisis plasma triglycerides↑ hypertension, edema (3)Others gallbladder disease risk of breast and endometrial carcinoma
3. Adverse effects (1) Oral administration: nausea,vomiting, diarrhea (2) Cardiovascular effects: • risk of venous thromboembolisis • plasma triglycerides • hypertension, edema (3) Others: • gallbladder disease • risk of breast and endometrial carcinoma Estrogens
Estrogens The estrogen-alone T stroke and deep vein thrombosis(dvt) in postmenopausal women>50y t dementia in postmenopausal women>65y using 0.625 mg of Premarin conjugated equine estrogens (Cee) The estrogen-plus-progestin T risk of myocardial infarction, stroke, invasive breast cancer, pulmonary emboli and dvt in postmenopausal women >50y dementia in postmenopausal women>65y using 0.625 mg of CeE with 2.5 mg of the progestin medroxyprogesterone acetate MPa)
The estrogen-alone • stroke and deep vein thrombosis (DVT) in postmenopausal women>50y • dementia in postmenopausal women>65y using 0.625 mg of Premarin conjugated equine estrogens (CEE). The estrogen-plus-progestin • risk of myocardial infarction, stroke, invasive breast cancer, pulmonary emboli and DVT in postmenopausal women >50y • dementia in postmenopausal women>65y using 0.625 mg of CEE with 2.5 mg of the progestin medroxyprogesterone acetate (MPA). Estrogens
Antiestrogens Clomifene 氯米芬(克罗米酚) CI NCH2CH20- C=C H5C2 (1)Effects: Partial agonist/antagonist for estrogen receptor
Antiestrogens (1) Effects: Partial agonist/antagonist for estrogen receptor H5C2 H5C2 NCH2CH2O C Cl C Clomifene 氯米芬 (克罗米酚)