Estradiol is prescribed for symptomatic treatment of the usual symptoms associated with menopause (hot flushes, vaginal dryness, etc.), prevention of bone fractures associated with osteoporosis, reduction of the risk of heart attacks and strokes, and dysfunctional (excessive and painful) uterine bleeding. The vaginal cream is prescribed for vaginal or vulvar atrophy associated with menopause.

Estradiol enters cells freely and interacts with a cytoplasmic target cell receptor. When the estrogen receptor has bound its ligand it can enter the nucleus of the target cell, and regulate gene transcription which leads to formation of messenger RNA. The mRNA interacts with ribosomes to produce specific proteins that express the effect of estradiol upon the target cell.

Estradiol binds well to both estrogen receptors, ER&#945 and ER&#946, in contrast to certain other estrogens, notably medications that preferentially act on one of these receptors. These medications are called selective estrogen receptor modulators, or SERMs. 

 

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