← Search & browse all drugs
GENITO URINARY SYSTEM AND SEX HORMONES › SEX HORMONES AND MODULATORS OF THE GENITAL SYSTEM › ESTROGENS › Other estrogens
tibolone
G03CX01
Adult Dosing
- Postmenopausal osteoporosis prevention and menopausal symptom relief: 2.5 mg orally once daily
- Treatment should be initiated at least 12 months after the last natural menstrual period
Pediatric Dosing
- Not indicated for pediatric use
Indications
- Short-term relief of vasomotor symptoms associated with menopause
- Prevention of postmenopausal osteoporosis in women at risk of future fractures who are intolerant to other approved osteoporosis medications
Mechanism of Action
- Synthetic steroid with estrogenic, progestogenic, and weak androgenic properties
- Metabolized in the liver and intestine into active 3-alpha and 3-beta-hydroxy metabolites (which act primarily as estrogens) and a delta-4 isomer (which acts as a progestin and androgen)
Contraindications
- Known or suspected breast cancer
- Known or suspected estrogen-dependent malignant tumors (e.g., endometrial cancer)
- Undiagnosed genital bleeding
- Active or previous venous thromboembolism (deep vein thrombosis, pulmonary embolism)
- Active or recent arterial thromboembolic disease (e.g., angina, myocardial infarction, stroke)
- Known hepatic dysfunction or liver disease with abnormal liver function tests
- Known hypersensitivity to tibolone or excipients
- Porphyria
- Known or suspected pregnancy
Adverse Reactions
- Weight gain
- Abnormal hair growth
- Vaginal bleeding or spotting
- Breast pain or tenderness
- Abdominal pain
- Dizziness
- Headache
- Seborrhea
- Endometrial hypertrophy
- Increased risk of stroke
Drug Interactions
- Enhanced anticoagulant effect of warfarin and other coumarin derivatives due to increased fibrinolytic activity
- Potential decreased efficacy when co-administered with strong CYP3A4 inducers (e.g., barbiturates, carbamazepine, hydantoins, rifampicin)
Curated Content: Needs Vetting Before Put to Clinical Use