List of marketed estradiol benzoate formulations

Estradiol Benzoate Formulations are a group of pharmaceutical drugs used in hormone therapy for their estrogenic effects. Estradiol benzoate, a synthetic form of the naturally occurring female hormone estrogen, is used in various formulations for medical purposes, including but not limited to, menopausal symptom management, hormone replacement therapy (HRT), and in some cases, for contraception. This article provides a detailed list of marketed estradiol benzoate formulations, highlighting their diverse applications and formulations.

Formulations

Estradiol benzoate is available in several formulations, each designed for specific therapeutic needs and administration routes. These include:

• Injectable Solutions: Often used in hormone therapy, especially in transgender hormone therapy, to induce feminization or suppress testosterone production.
• Topical Creams and Gels: Applied directly to the skin, these formulations are used for systemic hormone replacement therapy or for local symptoms like vaginal atrophy.
• Transdermal Patches: These patches are applied to the skin and release estradiol steadily over time, used in hormone replacement therapy.
• Vaginal Rings and Tablets: Specifically designed for local treatment of menopausal symptoms such as vaginal dryness and atrophy.

List of Marketed Estradiol Benzoate Formulations

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• Note: Specific brand names and formulations are subject to change and may vary by country and regulatory approval status.

Clinical Uses

Estradiol benzoate formulations are primarily used in:

• Menopause symptom management, including hot flashes, night sweats, and vaginal atrophy.
• Hormone replacement therapy (HRT) in postmenopausal women or those with estrogen deficiency due to other causes.
• Part of transgender hormone therapy for transgender women and non-binary individuals seeking feminization.
• Certain formulations may be used in contraception methods, though this is less common.

Mechanism of Action

Estradiol benzoate mimics the action of natural estrogen in the body. It binds to estrogen receptors, activating them and inducing the transcription of estrogen-responsive genes. This leads to the proliferation of estrogen-dependent tissues and the modulation of various biochemical pathways involved in reproductive and non-reproductive systems.

Safety and Side Effects

While estradiol benzoate formulations are generally safe and well-tolerated, they may cause side effects in some individuals. Common side effects include nausea, headache, breast tenderness, and mood changes. Long-term use of estrogen therapy has been associated with an increased risk of certain conditions, such as breast cancer, thrombosis, and stroke, especially in older women and those with specific health risks.

Regulatory Status

The availability and regulatory approval of estradiol benzoate formulations vary by country. In many regions, these formulations are available by prescription only and are subject to regulatory oversight to ensure their safety and efficacy.