tibolone: clinical use

Prescribing considerations

• Confirm established postmenopausal status and investigate unexplained genital bleeding before initiation.
• Assess individual stroke, breast-cancer and, with an intact uterus, endometrial-cancer risks; stroke risk becomes more important with increasing age.
• Use particular caution with thromboembolic risk factors, hypertension, migraine, diabetes, liver disorders, fibroids, endometriosis, epilepsy, asthma, systemic lupus erythematosus and hypertriglyceridaemia.
• Tibolone is not contraceptive and is not intended for paediatric use.

Contraindications and cautions

• Pregnancy or breastfeeding
• Known, previous or suspected breast cancer
• Known or suspected oestrogen-dependent malignancy
• Unexplained genital bleeding or untreated endometrial hyperplasia
• Current or previous venous thromboembolism or a known thrombophilic disorder
• History of arterial thromboembolic disease, including angina, myocardial infarction, stroke or transient ischaemic attack
• Acute liver disease, or previous liver disease before liver tests have normalised
• Porphyria or hypersensitivity to an ingredient

Monitoring

• Document relevant personal and family history; perform breast and pelvic assessment where clinically indicated.
• Review symptom benefit, adverse effects and evolving risks regularly.
• Maintain appropriate breast screening and advise reporting new breast changes.
• Investigate persistent, newly developing or post-treatment vaginal bleeding.
• Monitor anticoagulant response closely when tibolone is introduced or withdrawn in a person taking warfarin.

Clinical pharmacology

Tibolone is rapidly and extensively absorbed and converted to oestrogenic, progestogenic and androgenic metabolites. Food does not materially alter absorption; metabolites are eliminated mainly as conjugates, predominantly in faeces.

Formulation and product differences

• The selected product is an uncoated oral tablet containing lactose; check excipient suitability and tablet appearance against current product information.

Tablet

Route: Oral

Strengths: 2.5 mg