Estradiol

Indications

Estradiol is used for: Moderate to severe vasomotor symptoms associated with menopause, Prophylaxis of osteoporosis in postmenopausal women, Hypogonadism, Atrophic vaginitis

Adult Dose

Oral Vulvar and Vaginal Atrophy in Menopause Adult: 1-2 mg PO once daily for 3 weeks, followed by 1 week off Prevention of osteoporosis: 0.5 mg PO once daily for 3 weeks, followed by 1 week off Metastatic breast cancer: 10 mg PO q8hr for 3 months Prostate cancer: 1-2 mg PO q8hr for ?3 months

Child Dose

Renal Dose

Administration

May be taken with or without food.

Contra Indications

Hypersensitivity; undiagnosed vag bleeding; thrombophloebitis or thromboembolic disorders; breast carcinoma except in selected patients being treated for metastatic disease; oestrogen-dependent tumor; porphyria; pregnancy.

Precautions

Conditions exacerbated by fluid retention; hypercalcaemia, cerebrovascular diorders, coronary artery disease, gall bladder diseases; lipid effects; familial defects of lipoprotein metabolism. May increase BP, risk of venous thromboembolism, breast cancer, benign hepatic adenoma, endometrial cancer and size of preexisting uterine leiomyomata. Dosage should be reduced in hepatic impairment. Lactation. Child. Lactation: Drug enters breast milk; use with caution

Pregnancy-Lactation

Pregnancy Therapy not indicated for use in pregnancy; there are no data with use in pregnant women; however, epidemiologic studies and meta-analyses have not found an increased risk of genital or nongenital birth defects (including cardiac anomalies and limb-reduction defects) following exposure to combined hormonal contraceptives (estrogen and progestins) before conception or during early pregnancy Lactation Therapy not indicated for use in females of reproductive potential; estrogens present in human milk and can reduce milk production in breast-feeding females; reduction can occur at any time but is less likely to occur once breast-feeding is well- established

Interactions

CYP1A2 and CYP3A4 inducers e.g. aminoglutethimide, carbamazepine, phenobarbital, and rifampin may decrease the effects of estradiol. May enhance the effects of hydrocortisone and prednisolone when used together.

Adverse Effects

Side effects of Estradiol : Anxiety, Abdominal cramping, Amenorrhea, Bloating, Breakthrough bleeding, Breast enlargement, Breast tenderness, Delayed ejaculation, Depression, Dry mouth, Headache, Hypertension, Impotency, Influenza, Leukorrhea, Melasma, Muscle cramps, Nausea, Nervousness, Peripheral edema, Polydipsia, Pruritus, Rash, Swelling, Spotting, Syncope, Toothache, Vaginal discomfort, vaginal erosion, vaginal ulceration, adherence of the vaginal ring to the vaginal wall (Estring), Vomiting, Weight changes

Mechanism of Action

Estradiol is a naturally occurring oestrogen. Oestrogens are responsible for the development and maintenance of the female reproductive system and secondary sexual characteristics. They modulate the pituitary secretion of gonadotrophins, LH and FSH through a negative feedback system.