Synthetic Steroid (Tissue-Selective Oestrogen Activity) Pregnancy: CONTRAINDICATED — not for use before or during the reproductive years

Tibolone

Brand names: Livial

Adult dose

Dose: 2.5 mg once daily continuously

Route: Oral

Frequency: Once daily

Max: 2.5 mg/day

Menopausal symptoms and osteoporosis prevention; only suitable ≥12 months post-menopause (otherwise erratic bleeding); not for perimenopausal or premenopausal women

Paediatric dose

Dose: Not applicable N/A/kg

Route: N/A

Frequency: N/A

Max: N/A

Not for use before menopause

Dose adjustments

Renal

No dose adjustment required

Hepatic

Contraindicated in severe hepatic impairment or liver disease

Paediatric weight-based calculator

Patient weight (kg)

Not for use before menopause

Clinical pearls

LIFT trial (Cummings et al. NEJM 2008): tibolone reduced vertebral fracture risk by 45% and non-vertebral fracture by 26% vs placebo in osteoporotic postmenopausal women — also reduced breast cancer incidence; BUT increased stroke risk (2.19 RR) led to trial suspension
Tibolone metabolites have tissue-selective activity: oestrogenic in bone and brain (reduces hot flushes), progestogenic in endometrium (no endometrial hyperplasia, so no monthly progestogen needed), androgenic in peripheral tissue — explains libido improvement
Stroke risk: LIFT trial terminated early due to excess strokes in women over 60; MHRA advises caution in women with cardiovascular risk factors; not recommended >60 years without clear individual risk-benefit discussion
Does not stimulate breast as much as standard HRT: Million Women Study and LIBERATE trial suggest lower breast cancer risk than standard combined HRT but higher than no HRT — relevant counselling point
Unlike standard HRT (which requires progestogen add-back if uterus present), tibolone alone is sufficient for women with intact uterus — no progestogen required due to endometrial progestogenic effects

Contraindications

History of breast cancer
Thromboembolic disease
History of cardiovascular disease or stroke
Undiagnosed vaginal bleeding
Endometrial cancer
Pregnancy/lactation

Side effects

Vaginal bleeding/spotting (particularly in perimenopause — avoid)
Weight gain
Breast tenderness
Headache
Facial hair
Lower leg pain (VTE)
Increased stroke risk in older women

Interactions

Anticoagulants (warfarin) — tibolone can potentiate anticoagulant effect; monitor INR
CYP enzyme inducers — reduce tibolone levels
Antidiabetics — tibolone may alter glucose tolerance; monitor

Monitoring

Annual breast examination/mammogram
Blood pressure
Endometrial assessment if unexpected bleeding
Cardiovascular risk factors
Bone density (DEXA if osteoporosis indication)

Reference: BNFc; BNF 90; LIFT trial (Cummings et al. NEJM 2008); LIBERATE trial (Sismondi et al. Lancet Oncol 2011); MHRA SPC Livial; NICE NG23 (Menopause). Verify against your local formulary and the latest BNF before prescribing.

Curated clinical cross-links plus same-class fallbacks.

Calculators