Generic
Tibolone
9 brands available in the market
At a glance
Tibolone is a synthetic steroid used for menopausal symptoms (hot flushes, vaginal dryness) and prevention of osteoporosis in postmenopausal women. It has estrogenic, progestogenic, and weak androgenic properties.
Description
Tibolone is a synthetic steroid metabolized into three compounds: 3α-OH and 3β-OH metabolites (predominantly estrogenic), and δ4-isomer (predominantly progestogenic and androgenic). It replaces estrogen production loss in postmenopausal women, alleviates menopausal symptoms, and prevents bone loss.
Indications
- Symptoms of natural or surgical menopause
- Prevention of postmenopausal osteoporosis (high-risk women)
Therapeutic class
Drugs for Menopausal Symptoms: Hormone Replacement Therapy
Pharmacological class
Synthetic Steroid (Estrogenic/Progestogenic/Androgenic)
Pharmacology
Tibolone is rapidly metabolized into three active metabolites. 3α-OH and 3β-OH metabolites activate estrogen receptors; δ4-isomer activates progesterone and androgen receptors. It reduces hot flushes at thermoregulatory centers, improves vaginal dryness and atrophy, prevents bone loss, and improves mood and libido.
Mechanism of action
Replaces postmenopausal estrogen deficiency to relieve menopausal symptoms and prevent bone loss.
Dosage
Adult Dose (Oral):
- Menopausal symptoms: 2.5 mg/day
- Postmenopausal osteoporosis prevention: 2.5 mg/day (5-10 years)
- Natural menopause: Start 12 months after last natural bleed
- Surgical menopause: Start immediately
Administration
- Can be taken with or without food
- Swallow tablet whole; do not chew, crush, or break
- Take at the same time each day
Missed dose
If more than 12 hours until the next dose, take it immediately; if less than 12 hours, skip it; do not double the dose.
Side effects
Common Side Effects:
- Vaginal bleeding or spotting (especially in the first months)
- Headache, migraine
- Edema, dizziness
- Pruritus, weight gain
- Nausea, abdominal pain
- Rash, depression
Precautions & warnings
- Do not use in history of breast cancer or estrogen-dependent tumors
- Do not use in undiagnosed vaginal bleeding or severe liver disease
- Do not use in pregnancy and lactation
- Do not use in history of cardiovascular or cerebrovascular disorders
- Regular breast and cervical smear examinations required
Contraindications
- Estrogen-dependent tumors (breast cancer)
- Undiagnosed vaginal bleeding
- Severe liver disease
- Cardiovascular or cerebrovascular disorders
- Untreated endometrial hyperplasia
- Porphyria, pregnancy and lactation
- Premenopausal women
Drug interactions
- Enzyme inducers (barbiturates, phenytoin, carbamazepine, rifampicin): Accelerate tibolone metabolism
- Warfarin: Increased anticoagulant effect
Food interactions
Alcohol is unsafe with Tibolone; consult your doctor.
Use in pregnancy
Use in Pregnancy: Highly unsafe; discontinue immediately if pregnancy occurs; consult your doctor.
Pregnancy Category: X — always consult a doctor before taking during pregnancy.
Use in lactation
Use in Lactation: Information not available; do not use; consult your doctor.
Pediatric use
Not indicated for children (menopause medication)
Geriatric use
Indicated for elderly
Renal / hepatic impairment
Renal Impairment: Limited information; caution needed; consult your doctor.
Hepatic Impairment: Limited information; caution needed; consult your doctor.
Overdose effects
Overdose may cause nausea, vomiting, vaginal bleeding; provide symptomatic treatment.
Storage conditions
Store in a cool and dry place, protected from light; keep out of reach of children.
Chemical structure
Tibolone