Products
Tibolone is commercially available in tablet form (Livial, Germany: Liviella). It has been approved in many countries since 1998. Generic versions were registered in 2014.
Structure and properties
Tibolone (C21H28O2, Mr = 312.4 g/mol) is structurally related to 19-nortestosterone. It carries an ethynyl group like ethynylestradiol.
Effects
Tibolone (ATC G03CX01) is a prodrug. The metabolites have estrogenic, progestogenic, and androgenic effects. Tibolone relieves menopausal symptoms and prevents osteoporosis.
Indications
- Symptoms of estrogen deficiency due to natural or artificial menopause (at least 1 year ago).
- Prevention or delay of estrogen deficiency-induced osteoporosis in postmenopausal women at high risk of fracture.
Dosage
According to the professional information. The drug is taken once a day, regardless of meals and always at the same time of day.
Contraindications
For complete precautions, see the drug label.
Interactions
Drug-drug interactions are possible with CYP3A4 substrates and inducers. Tibolone may potentiate the effects of anticoagulants.
Adverse effects
The most common possible adverse effects include abdominal pain, abdominal pain, endometrial hypertrophy, breast pain, genital itching, vaginitis, vaginal thrush, vaginal bleeding, spotting, weight gain, and increased hairiness.