Tibolone

Chemical Name:(7α, 17β)-17-ethynyl-17-hydroxy-7-methylestr-5(10) en-3-one
Molecular Formula: C21H28O2
Molecular Weight: 312.446
CAS: 5630-53-5

Tibolone Description and Indication

Tibolone is a synthetic hormone-type drug which is used mainly for hormone replacement therapy in post-menopausal women. It is a synthetic steroid that has the same activity as the female sex hormones estrogen and progesterone and the androgen testosterone. Tibolone helps restore hormonal balance in the body.

When estrogen levels are low tissues can slowly degenerate, as is experienced during menopause. In addition, low levels of estrogen can cause distressing symptoms such as hot flushes, night sweats, mood swings, reduced sex drive and vaginal dryness.

Tibolone is broken down into three compounds which act in a similar way to the natural estrogen and progesterone found in the body. It restores plasma endorphin level in post-menopausal women and acts centrally to affect the thermo-regulatory system.

Tibolone Mechanism of Action

In itself Tibolone has no biological activity; the effects are produced mainly by the results of the activity of its metabolites on various tissues. After administration, Tibolone is quickly metabolized into 3α-hydroxytibolone and 3ß-hydroxytibolone compounds, which are also present in an inactive, sulfated form. A third compound, the Δ4- isomer is formed from Tibolone directly or from the 3ß hydroxymetabolite.

Tibolone has estrogenic effects on bone and vaginal tissue. The Δ4-isomer functions as a progestogen in endometrial tissue, whereas in the brain and liver it has androgenic effects.

In breast tissue, Tibolone acts by strongly inhibiting sulfate activity and weak inhibition of 17α-hydroxysteroid dehydrogenase activity, which results in blocking the conversion of estrone sulfate to E2.

Tibolone Contraindications

Tibolone is contraindicated in patients with the following conditions:

Tibolone Adverse Drug Effects

Tibolone Drug Interactions

Tibolone interacts with:

Tibolone Formulations

Tibolone Brands

These are the following brands available for Tibolone: