Δ4-Tibolone

Δ4-Tibolone is a synthetic steroid used in the treatment of menopausal syndrome. It is marketed under several brand names, including Livial and Tibofem, and is available in over 60 countries worldwide.

Pharmacology

Δ4-Tibolone is a prodrug that is converted in the body to three active metabolites, each with its own mode of action. These metabolites contribute to the overall therapeutic effects of the drug, which include relief from hot flashes, vaginal dryness, and prevention of osteoporosis.

Mechanism of Action

Δ4-Tibolone and its metabolites act on several different types of receptors, including estrogen, progesterone, and androgen receptors. This broad spectrum of activity allows it to have a range of effects that are beneficial in the treatment of menopausal symptoms.

Clinical Use

Δ4-Tibolone is used primarily in the treatment of menopausal symptoms, such as hot flashes and vaginal dryness. It is also used in the prevention of osteoporosis in postmenopausal women.

Side Effects

Like all medications, Δ4-Tibolone can cause side effects. These may include nausea, breast tenderness, and weight gain. In rare cases, it may increase the risk of breast cancer and stroke.

See Also

• Menopause
• Osteoporosis
• Estrogen
• Progesterone
• Androgen

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