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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.

Indications
  • Symptoms of natural or surgical menopause
  • Prevention of postmenopausal osteoporosis (high-risk women)
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.

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
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
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.

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
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.

Tibolone — see the full informationPharmacology, precautions, pregnancy, overdose and the rest on the generic page
⚠️ This information is for educational purposes only — not a substitute for medical advice. Consult a registered physician before taking any medicine.