Tibolone

What it is and how it works

Tibolone is rapidly metabolised into compounds with oestrogenic, progestogenic and androgenic activity that act in a tissue-specific manner. It relieves vasomotor symptoms and preserves bone mass through oestrogenic effects, while its progestogenic action on the endometrium generally prevents endometrial stimulation.

Indications

Treatment of oestrogen-deficiency symptoms in postmenopausal women more than one year after the last natural menstrual period; prevention of osteoporosis in postmenopausal women at high fracture risk who cannot use other medicines.

Dosage and administration (summary)

Orally, 2.5 mg once daily, preferably at the same time each day; treatment should be reviewed regularly and continued at the lowest effective duration.

Contraindications

Pregnancy and lactation; known, past or suspected breast cancer or other oestrogen-dependent tumours; undiagnosed genital bleeding; untreated endometrial hyperplasia; history of venous or arterial thromboembolism (including stroke and myocardial infarction); acute or past liver disease with abnormal liver tests; porphyria.

Warnings and precautions

Tibolone increases the risk of stroke (particularly in women over 60) and is associated with an increased risk of breast cancer recurrence and possibly endometrial cancer; the benefit–risk balance should be assessed at least annually. Irregular bleeding after the first months of treatment requires investigation. Not to be used as a contraceptive.

Pregnancy

Contraindicated in pregnancy.

Storage and supply

Store below 25 °C in the original package, protected from light and moisture.

Source: reference summary prepared from the EU SmPC/EPAR, BNF and WHO Model Formulary. The approved product information in Iran governs.