Tibolone

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

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.