Estradiol Capsules

Overview of Estradiol Capsules

Dosage Strength

Compounded: 0.75 mg, 1.25 mg, 1.5 mg, 1.75 mg, 2.5 mg, 3 mg Capsules

General Information

The main intracellular human estrogen is estradiol, which is also far more active in cells than its metabolites, estrone and estriol. Estradiol can be made synthetically or from natural sources. No data exists to support the claims that “natural” estrogens are either more or less effective or secure than “synthetic” estrogens. 1 Estradiol must be administered in a micronized oral dose form to ensure therapeutic action due to practically full first-pass metabolism. The parenteral duration of action of estradiol is lengthened by esterification to estradiol cypionate or valerate, enabling parenteral intramuscular delivery. Estradiol is primarily used to treat female hypogonadism and other anomalies of female gonadotropin functioning, as well as to prevent osteoporosis and ease vasomotor and genitourinary symptoms associated with menopause (natural or surgical). Since 1938, numerous estrogen products have been sold in the United States. Oral pills, transdermal systems, topical emulsions, gels, and sprays, vaginal creams, vaginal rings, and parenteral depot injections are just a few of the dosage forms of estradiol that are offered. Due to lesser systemic absorption/exposure with most of these dose formulations, vaginal treatments are favored in postmenopausal women with just genitourinary complaints. 1 Since the 1990s, a large number of estradiol products have received FDA approval in compliance with the FDA’s recommendations to provide effective low-dose estrogen therapy in alternative drug delivery systems.


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