Tibolone itself is devoid of activity, but it is metabolized in a tissue-selective manner to three metabolites. These metabolites have predominantly estrogenic, progestogenic, and androgenic activities, providing a combined hormonal effect.
Alleviating menopausal symptoms (e.g., vaginal atrophy, vasomotor instability)Prevention of postmenopausal osteoporosisEarly natural or surgical menopause (before age 45 years) in women at high risk of osteoporosistreatment of vasomotor symptoms (in E.U.)prevention of osteoporosis (in E.U.)Hormone replacement therapy (HRT) for menopausal symptoms
- Adult
- Hormone replacement therapy (HRT) with small doses of an oestrogen (together with a progestogen in women with a uterus) is appropriate for alleviating menopausal symptoms such as vaginal atrophy or vasomotor instability.…
Metabolism
Metabolized in a tissue-selective manner to three metabolites.
- Increased risk of irregular bleeding (unopposed estrogen)
- Existing breast cancer
- Pregnancy
- Thromboembolic, coronary and cerebrovascular disease or history
- Moderate-to-severe hypertension
- Hyperlipidaemia
- Active liver disease, hepatoma or history of jaundice during past pregnancy
- Suspected/overt malignancy of genitals/breast
- Porphyria
- Impending major surgery (to avoid excess risk of postoperative thromboembolism)
Common
Weight gainIncreased facial hairOccasional vaginal spotting
Serious
- Venous thromboembolism
- Stroke
- Endometrial cancer
- Breast cancer
- Ovarian cancer
- Endometrial hyperplasia
AnastrozoleModerate
Database
Oestrogenic activity may antagonise AI
Avoid
Source: Kimi deep-research + Cla