Estradiol

Details About Generic Salt ::  Estradiol 

Main Medicine Class:: Endocrine,Steroid Hormones , Metabolic System   Sub Medicine Class ::  Estrogens and Anti Estrogens

8E. ESTROGENS AND ANTI-ESTROGENS in 8. ENDOCRINE/STEROID HORMONES & METABOLIC SYSTEM
ESTRADIOL
ESTROGEN | HORMONE
also comes under 10H. Vaginal Urethral Preparations in 10. Genito-Urinary System
PK: A: Well absorbed D: Extensive M: Hepatic E: Urine

Indications & Dose: ADVANCED PROSTATE CANCER Palliative therapy PO Adult 1-2mg TID (as estradiol) | Palliative therapy IM Adult >30mg once q1 or 2wk (as valerate) | ATROPHIC VAGINITIS VAG Adult Cream: 2-4g (as estradiol) applied OD for 1-2 wk & gradually reduced to one half the initial dosage for the similar period, MD 1g 1-3 times weekly or 1 vaginal tablet (25µg of estradiol) is inserted intravaginally OD for 2 wk, MD 1 tablet twice weekly | FEMALE HYPOGONADISM PO Adult Initially 1 or 2mg/day (as estradiol) adjust dose based on response | IM Adult 1.5-2mg once monthly (as cypionate) or 10-20mg once q4wk as required (as valerate) | METASTATIC BREAST CANCER IN MEN/POSTMENOPAUSAL WOMEN Palliative therapy PO Adult 10mg TID (as estradiol) 3 months | OSTEOPOROSIS PO Adult 0.5mg/day in cyclic regimen | OSTEOPOROSIS IN POSTMENOPAUSAL WOMEN Prophylactic therapy TD Adult Once-weekly patch: Apply a single patch/wk (0.014/0.025mg OD, dose may vary based on preparation), adjust dose according to response. In women with a uterus, progestin is given for 2 wk q6-12month. Twice-weekly patch: Apply 0.025mg/0.05mg patch twice weekly, adjust the dose based up on response | OVARIECTOMY/PRIMARY OVARIAN FAILURE PO Adult Initially 1 or 2mg/day (as estradiol) adjust dose based on response | IM Adult 10-20mg once q4wk as required (as valerate) | VASOMOTOR MENOPAUSAL SYMPTOMS Moderate-to-severe PO Adult Initially 1 or 2mg/day (as estradiol) in cyclic regimen or 450µg/day (as acetate) | Moderate-to-severe IM Adult 1-5mg once q3-4wk (as cypionate) or 10-20mg once q4wk as required (as valerate) | Moderate-to-severe TD Adult Preparations containing various strength of estradiol are available | VASOMOTOR SYMPTOMS ASSOCIATED WITH MENOPAUSE TP Adult Initially 1 spray (1.53mg) per day, adjust dose based on patient response (usually 1-3 sprays/day) | VASOMOTOR SYMPTOMS IN MENOPAUSE Moderate-to-severe TP Adult Once-weekly patch: Apply 0.025mg/day patch once weekly. Adjust dose control symptoms as required, dose may vary based on preparations available May be used continuously in patients without an intact uterus or used continuously/in cycles (3 wk on, 1 wk off) in patients with an intact uterus. Twice-weekly patch: Apply 0.05mg patch twice weekly. Titrate to lowest dose possible to control symptoms, adjusting initial dose after the first month of therapy, dose may vary based on preparations available | VULVAR/VAGINAL ATROPHY IN MENOPAUSE/FEMALE HYPOEST Moderate-to-severe TP Adult Once-weekly patch: Apply 0.025mg/day patch once weekly. Adjust dose control symptoms as required, dose may vary based on preparations available. May be used continuously in patients without an intact uterus or used continuously/in cycles (3 wk on, 1 wk off) in patients with an intact uterus. Twice-weekly patch: Apply 0.05mg patch twice weekly. Titrate to lowest dose possible to control symptoms, adjusting initial dose after the first month of therapy, dose may vary based on preparations available | VULVULAR/ATROPHIC VAGINITIS IN MENOPAUSE PO Adult Initially 1 or 2mg/day (as estradiol)in cyclic regimen | IM Adult 10-20mg once q4wk as required (as valerate)

Contra: Hypersensitivity, undiagnosed abnormal vaginal bleeding, active/recent arterial thromboembolic disease, breast carcinoma, estrogen-dependent tumor, hepatic dysfunction/disease, venous thromboembolic disorders

Precautions: CVD, history of cholestatic jaundice, hepatic hemangiomas, severe hypocalcemia, migraine, porphyria, asthma, severely atrophic vaginal mucosa, SLE, diseases exacerbated by fluid retention

ADR: Serious: Chest pain, MI, DVT, HTN, stroke, venous thromboembolism, hemorrhagic eruption, thrombophlebitis, asthma exacerbation, pulmonary thromboembolism, hypersensitivity reactions, endometrial cancer, erythema multiforme, retinal vascular thrombosis, ovarian, breast & uterine cancer, cholestatic jaundice, endometrial hyperplasia, hepatic hemangioma enlargement, myalgia, arthralgia, blindness, Others: contact lens intolerance, vaginal discharge, vaginitis, urogenital pruritus, toxic shock syndrome, skeletal pain, weakness, blindness, contact lens intolerance, urinary incontinence, muscle cramps, corneal curvature steepening, ovarian cyst, dysmenorrhea, metrorrhagia, vaginal candidiasis, leukorrhea, mood disturbances, uterine enlargement, anxiety, dementia, dizziness, epilepsy exacerbation, insomnia, mental depression, migraine, hirsutism, nervousness, erythema, aggravation of porphyria

DDI: Serious Phenobarbital/Carbamazepine decreases drug levels, leads to decrease therapeutic effects, Tacrine/Selegiline levels increased, Corticosteroids metabolism decreased, Bupropion metabolism inhibited, Erythromycin/Diltiazem/Ketoconazole raises drug levels