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Indications and Dosage
Oral
Menopausal hormone replacement therapy Adult: In menopausal women: 10-20 mcg daily in conjunction with a progestogen in women with uterus. Oral Palliative treatment of breast carcinoma Adult: In postmenopausal women: 0.1-1 mg tid. Oral Part of combined oral contraceptive Adult: As the oestrogenic component of combined oral contraceptive: 20-40 mcg/day. Oral Female hypogonadism Adult: 10-50 mcg daily in a cyclical regimen. Oral Palliative treatment of prostatic carcinoma Adult: 0.15-3 mg daily.
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Administration
May be taken with or without food.
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Contraindications
Uterine, liver and mammary carcinoma, thromboembolic disorders. Pregnancy, lactation, untreated endometriosis, jaundice, undiagnosed vag bleeding.
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Special Precautions
Asthma; epilepsy; migraine; DM; cardiac or renal dysfunction; hepatic disease; familial defects of lipoprotein metabolism. Increased risk of endometrial cancer in unopposed oestrogen therapy. Increased risk of gallbladder disease in women on postmenopausal oestrogens. Large doses may increase CV risk, BP, risk of thrombophlebitis and pulmonary embolism.
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Adverse Reactions
Oedema, hypertension; dizziness; headache; thromboembolism; cholestatic jaundice; nausea, vomiting; disturbance of menstrual cycle; fluid retention, discomfort in breast, wt gain/loss; increased appetite, increased tendency for vag candidiasis; mental depression; alteration in libido; rashes; alopoecia, hirsutism; gynaecomastia and impotence.
Potentially Fatal: Endometrial cancer (prolonged use). |
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Drug Interactions
CYP1A2 and CYP3A4 inducers such as aminoglutethimide, carbamazepine, phenobarbital, and rifampin may decrease the effects of estradiol. May enhance the effects of hydrocortisone and prednisolone when used together. Altered anticoagulant effect when used with dicoumarol.
Potentially Fatal: Antibiotics (ampicillin, tetracycline, sulphonamides and chloramphenicol) can cause intermenstrual bleeding or failure of contraception. Reduced efficacy of antihypertensives or hypoglycaemic drugs. |
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Food Interaction
Folic acid absorption may be decreased. Black cohosh, dong quai, red clover, saw palmetto, ginseng, St John's wort.
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Lab Interference
Reduced response to metyrapone test.
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Action
Description: Oestradiol is the major oestrogen in pre-menopausal women. Ethinylestradiol has similar actions as oestradiol. It is responsible for the development and maintenance of female reproductive system and secondary sexual characteristics. It also inhibits anterior pituitary by negative feedback effect and causes capillary dilation, fluid retention and protein anabolism.
Pharmacokinetics: Absorption: Rapidly and well absorbed from the GI tract. Systemic bioavailability: About 40%. Distribution: Highly protein bound. Metabolism: Hepatically metabolised. Excretion: Urine and faeces. |
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Storage
Oral:
Menopausal hormone replacement therapy: Store at 25°C. Palliative treatment of breast carcinoma: Store at 25°C. Female hypogonadism: Store at 25°C. Palliative treatment of prostatic carcinoma: Store at 25°C. |
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