Doses of estradiol of as high as 200 mg per day by intramuscular injection for several weeks have been administered to humans in studies. Serious adverse effects have not been described following acute overdose of large doses of estrogen- and progestogen-containing birth control pills by small children. Symptoms of estrogen overdosage may include nausea, vomiting, bloating, increased weight, water retention, breast tenderness, vaginal discharge, vaginal bleeding, heavy legs, and leg cramps. These side effects can be diminished by reducing the estrogen dosage. Interactions
Inducers of cytochrome P450 enzymes like CYP3A4 such as St. Johns wort, phenobarbital, carbamazepine and rifampicin decrease the circulating levels of estradiol by accelerating its metabolism, whereas inhibitors of cytochrome P450 enzymes like CYP3A4 such as erythromycin, cimetidine, clarithromycin, ketoconazole, itraconazole, ritonavir and grapefruit juice may slow its metabolism resulting in increased levels of estradiol in the circulation. There is an interaction between estradiol and alcohol such that alcohol considerably increases circulating levels of estradiol during oral estradiol therapy and also increases estradiol levels in normal premenopausal women and with parenteral estradiol therapy. This appears to be due to a decrease in hepatic 17β-hydroxysteroid dehydrogenase type 2 (17β-HSD2) activity and hence estradiol inactivation into estrone due to an alcohol-mediated increase in the ratio of NADH to NAD in the liver. Spironolactone may reduce the bioavailability of high doses of oral estradiol. Pharmacology
Pharmacodynamics
Estradiol is an estrogen, or an agonist of the estrogen receptors (ERs), the ERα and ERβ. It is also an agonist of membrane estrogen receptors (mERs), including the GPER, Gq-mER, ER-X, and ERx.
Prognosis is generally poor, and the 5 year survival rate of patients with lymphangiosarcoma is less than 5%. Incidence
In the 1960s, the incidence five years after a radical mastectomy varied from 0.07% to 0.45%. Today, it occurs in 0.03% of patients surviving 10 or more years after radical mastectomy. History
It was discovered by Fred W. Stewart and Norman Treves in 1948. See also
Angiosarcoma
List of cutaneous conditions
Lymphangiosarcoma
Lymphedema
Postcardiotomy syndrome

References


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