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Published on: August 13, 2019
Cardiovascular effects of tibolone: a selective tissue estrogenic activity regulator
Roxana Campisi1, Fernando D Marengo
1Fundación Centro Diagnóstico Nuclear and Instituto Argentino de Diagnóstico y Tratamiento S.A., Argentina. rcampisi@fcdn.org.ar
Insights
Traditional hormone replacement therapy (HRT) shows no cardiovascular benefit in postmenopausal women. This review examines tibolone, an alternative HRT, and its cardiovascular effects in women with or at risk for coronary artery disease (CAD).
Area of Science:
- Cardiovascular Science
- Endocrinology
- Pharmacology
Background:
- Long-term hormone replacement therapy (HRT) was previously thought to benefit cardiovascular health in postmenopausal women.
- Randomized trials contradict this, showing no cardiovascular benefit for traditional HRT (estrogen and progesterone) in primary or secondary prevention of cardiovascular events.
- This has prompted research into alternative HRT options for women with or at risk for coronary artery disease (CAD).
Purpose of the Study:
- To review the effects of tibolone, a synthetic selective estrogen receptor modulator (SERM), on the cardiovascular system.
- To discuss clinical investigations of tibolone's impact on cardiovascular disease in postmenopausal women.
- To evaluate tibolone as a potential alternative to traditional HRT for cardiovascular health.
Main Methods:
- Review of existing clinical investigations and studies on tibolone's cardiovascular effects.
- Analysis of tibolone's tissue-selective mechanism of action and the role of its metabolites.
- Focus on studies involving postmenopausal women, particularly those with or at risk for CAD.
Main Results:
- Tibolone, unlike traditional HRT, has a tissue-selective mechanism of action.
- Its metabolites play a crucial role in its mode of action.
- Clinical impact of tibolone on cardiovascular disease is still under ongoing investigation.
Conclusions:
- Concerns regarding traditional HRT's cardiovascular safety necessitate exploring alternatives like tibolone.
- Tibolone's unique pharmacological profile warrants further investigation into its cardiovascular effects.
- More clinical data is needed to establish tibolone's role in managing cardiovascular health in postmenopausal women.
Abstract:
Traditionally, it was accepted that long-term hormone replacement therapy (HRT) has a cardiovascular beneficial effect in postmenopausal women with and without coronary artery disease (CAD). However, randomized trials in postmenopausal women have not shown any benefit in either primary or secondary prevention of cardiovascular events. Therefore, these findings have raised the question of whether traditional HRT (i.e., estrogen and progesterone) has a cardioprotective effect in women at risk for or with established CAD. Concerns about the use of conventional HRT have led to a search for alternatives. Tibolone is a synthetic compound with estrogenic, androgenic, and progestogenic properties that relieves climacteric symptoms and prevents postmenopausal bone loss. Tibolone possesses a tissue-selective mechanism of action that differs from that of estrogen and/or progestogen. Unlike these compounds, tibolone's metabolites play a central role in its mode of action. Tibolone is widely used for HRT. However, its clinical impact on cardiovascular disease is still under study. The current review focuses on the effects of tibolone on the cardiovascular system and discusses clinical investigations with this compound in postmenopausal women.
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