Generic Name : estradiol , estradiol ,estradiol acetate , estradiol cypionate ,estradiol hemihydrate ,estradiol valerate
- Oral: Estrace, Gynodiol
- Transdermal system: Alora, Climara, Esclim, Estraderm, Menostar, Vivelle, Vivelle Dot
- Topical vaginal cream: Estrace
- Vaginal ring: Estring
- Topical emulsion: Estrasorb
- Gel: Estrogel
- Tablets: Femtrace
- Vaginal ring: Femring
- Injection in oil: Depo-Estradiol
- Vaginal tablet: Vagifem
- Injection in oil: Delestrogen
Classification: Hormone , Estrogen
Pregnancy Category X
Dosage & Route
- Moderate to severe vasomotor symptoms, atrophic vaginitis, kraurosis vulvae associated with menopause: 1–2 mg/day PO. Adjust dose to control symptoms. Cyclic therapy (3 wk on/1 wk off) is recommended, especially in women who have not had a hysterectomy. 1–5 mg estradiol cypionate in oil IM every 3–4 wk. 10–20 mg estradiol valerate in oil IM, every 4 wk. The 0.014–0.05-mg system is applied to the skin weekly or twice weekly. If oral estrogens have been used, start transdermal system 1 wk after withdrawal of oral form. Given on a cyclic schedule (3 wk on/1wk off). Attempt to taper or discontinue medication every 3–6 mo.
- Female hypogonadism, female castration, primary ovarian failure: 1–2 mg/day PO. Adjust dose to control symptoms. Cyclic therapy (3 wk on/1 wk off) is recommended. 1.5–2 mg estradiol cypionate in oil IM at monthly intervals. 10–20 mg estradiol valerate in oil IM every 4 wk. 0.05-mg system applied to skin twice weekly as above.
- Vaginal cream: 2–4 g intravaginally daily for 1–2 wk, then reduce to one-half dosage for similar period followed by maintenance doses of 1 g one to three times/wk thereafter. Discontinue or taper at 3- to 6-mo intervals.
- Vaginal ring: Insert one ring high into vagina. Replace every 90 days.
- Vaginal tablet: 1 tablet inserted vaginally daily for 2 wk; then twice weekly.
- Prostatic cancer (inoperable): 1–2 mg PO tid. Administer long-term. 30 mg or more estradiol valerate in oil IM every 1–2 wk.
- Breast cancer (inoperable, progressing): 10 mg tid PO for at least 3 mo.
- Prevention of postpartum breast engorgement: 10–25 mg estradiol valerate in oil IM as a single injection at the end of the first stage of labor.
- Osteoporosis prevention: 0.5 mg/day PO given cyclically—23 days on, 5 days rest—starting as soon after menopause as possible or 0.05 mg/24 hr applied to skin once or twice weekly.
- Relief of menopausal symptoms: Apply lotion to legs, thighs, or calves once daily apply gel to one arm once daily.
- Not recommended due to effect on the growth of the long bones.
- 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.
- Femtrace, Estrasorb, estradiol cypionate, estradiol valerate: Vasomotor symptoms
- Estradiol acetate tablets (Femtrace): Treatment of moderate to severe vasomotor symptoms associated with menopause
- Vagifem, Estrace, Estring: Vaginal atrophy
- Femring, tablets, transdermal (except Menostar), Estrogel: Vasomotor symptoms amd vaginal atrophy
- Estradiol oral, transdermal, estradiol valerate: Prevention of postmenopausal osteoporosis
- Estradiol oral, transdermal, estradiol cypionate, valerate: Treatment of female hypogonadism, female castration, primary ovarian failure
- Estradiol oral, estradiol valerate: Palliation of inoperable prostatic cancer
- Estradiol oral: Palliation of inoperable, progressing breast cancer
- GI disturbances, genitourinary changes, haematologic disorders, CV and CNS effects, endocrine and metabolic disorders, cholestatic jaundice, local skin reactions, chorea, contact lens intolerance, steeping of corneal curvature, pulmonary thromboembolism, carbohydrate intolerance.
- Hypersensitivity; undiagnosed vag bleeding; thrombophloebitis or thromboembolic disorders; breast carcinoma except in selected patients being treated for metastatic disease; oestrogen-dependent tumor; porphyria; pregnancy.
- History: Allergy to estrogens, tartrazine; breast cancer, estrogen-dependent neoplasm; undiagnosed abnormal genital bleeding; active or previous thrombophlebitis or thromboembolic disorders; pregnancy; lactation; metabolic bone disease; renal insufficiency; CHF
- Physical: Skin color, lesions, edema; breast examination; injection site; orientation, affect, reflexes; P, auscultation, BP, peripheral perfusion; R, adventitious sounds; bowel sounds, liver evaluation, abdominal examination; pelvic examination; serum calcium, phosphorus; LFTs, renal function tests; Pap smear; glucose tolerance test
- BLACK BOX WARNING: Arrange for pretreatment and periodic (at least annual) history and physical, which should include BP, breasts, abdomen, pelvic organs, and a Pap smear; may increase risk of endometrial cancer.
- BLACK BOX WARNING: Do not use to prevent CV events or dementia; may increase risks including thrombophlebitis, pulmonary embolism, CVA, MI.
- BLACK BOX WARNING: Caution patient of the risks of estrogen use, the need to prevent pregnancy during treatment, for frequent medical follow-up, and for periodic rests from drug treatment.
- Administer cyclically for short-term only when treating postmenopausal conditions because of the risk of endometrial neoplasm; taper to the lowest effective dose, and provide a drug-free week each month.
- Apply transdermal system to a clean, dry area of skin on the trunk of the body, preferably the abdomen; do not apply to breasts; rotate the site at least 1 wk between applications; avoid the waistline because clothing may rub the system off; apply immediately after opening and compress for about 10 sec to attach.
- Insert vaginal ring as deeply as possible into upper one-third of vagina. Ring will remain in place for 3 mo. Then, remove and evaluate need for continued therapy. If a ring falls out during 3 mo, rinse with warm water and reinsert.
- WARNING: Arrange for the concomitant use of progestin therapy during long-term estrogen therapy in women with a uterus; this will mimic normal physiologic cycling and allow for a cyclic uterine bleeding that may decrease the risk of endometrial cancer. Women without a uterus do not need progestin.
- Administer parenteral preparations by deep IM injection only. Monitor injection sites and rotate with each injection to decrease development of abscesses.
- Use this drug in cycles or short term; prepare a calendar of drug days, rest days, and drug-free periods.
- Apply transdermal system and vaginal cream properly; insert vaginal tablet as high into the vagina as is comfortable.
- Insert vaginal ring high in vagina; it should remain in place for 3 months. If it falls out before that time, rinse with warm water and reinsert.
- Potentially serious side effects include cancers, blood clots, and liver problems; it is very important to have periodic medical examinations throughout therapy.
- This drug cannot be given to pregnant women because of serious toxic effects to the baby.
- You may experience these side effects: Nausea, vomiting, bloating; headache, dizziness, mental depression (use caution if driving or performing tasks that require alertness); sensitivity to sunlight (use a sunscreen and wear protective clothing); rash, loss of scalp hair, darkening of the skin on the face; changes in menstrual patterns.
- Report pain in the groin or calves of the legs, chest pain or sudden shortness of breath, abnormal vaginal bleeding, lumps in the breast, sudden severe headache, dizziness or fainting, changes in vision or speech, weakness or numbness in the arm or leg, severe abdominal pain, yellowing of the skin or eyes, severe mental depression, pain at injection site.