Tibolone
Rx
Generic NameTibolone
Therapeutic ClassHormone Replacement Therapy (HRT)
Max / 24h2.5 mg
Common Dose2.5 mg once daily
PregnancyContraindicated
Indications ▼
Relief of menopausal vasomotor symptoms such as hot flushes and night sweats
Treatment of urogenital atrophy including vaginal dryness and dyspareunia
Improvement of mood changes and sleep disturbances associated with menopause
Prevention of postmenopausal osteoporosis in women at increased fracture risk
Improvement of sexual well-being and libido in postmenopausal women
Mechanism & Pharmacokinetics ▼
Mechanism: Tibolone is metabolized into active metabolites with estrogenic, progestogenic, and androgenic activity. These metabolites act selectively on target tissues to relieve menopausal symptoms without stimulating endometrium.
Pharmacokinetics: Rapid oral absorption. Extensively metabolized in liver. Active metabolites exert tissue-specific effects. Excreted mainly via urine and feces. Elimination half-life approximately 45 hours.
Dosage & Administration ▼
| Indication | Dose | Frequency |
|---|---|---|
| Menopausal symptoms | 2.5 mg | Once daily |
| Osteoporosis prevention | 2.5 mg | Once daily |
Note: Treatment should begin at least 12 months after last natural menstruation.
Side Effects ▼
Abdominal pain, nausea
Weight gain, fluid retention
Breast tenderness
Vaginal bleeding or spotting
Headache, dizziness
Contraindications ▼
Known or suspected breast cancer
Estrogen-dependent malignancies
Undiagnosed vaginal bleeding
History of venous thromboembolism
Severe liver disease
Pregnancy and lactation
Drug Interaction ▼
Enzyme inducers (rifampicin, carbamazepine): reduce effect
Anticoagulants: may alter coagulation response
Herbal St John’s wort: reduces efficacy
Pregnancy & Lactation ▼
Contraindicated in pregnancy
Not indicated during breastfeeding
Clinical / Research Summary ▼
Clinical Role: Alternative to conventional estrogen–progestin HRT for menopausal symptom control.
Benefit: Relieves vasomotor symptoms while minimizing endometrial stimulation.
Safety: Risk of stroke may increase in elderly women; use lowest effective dose.
Research Focus: Long-term cardiovascular and breast safety evaluation.
Patient Counseling Points ▼
Take tablet at the same time every day
Do not use before menopause is complete
Report any abnormal vaginal bleeding
Regular breast and gynecological check-up recommended
Storage & Handling ▼
Store below 25°C
Protect from moisture and light
Keep out of reach of children
Brand Names (Bangladesh & Global) ▼
Medical Disclaimer: For educational purposes only. Not a substitute for professional medical advice.
Menorest® 2.5 mg