Tibolone
Generic Details
Generic Name
Tibolone
Other Names
- Livial
- Tibofem
Drug Class
- Hormone replacement therapy
- Progestogen
Chemical Formula
C21H28O2
Molecular Weight
312.45 g/mol
Mechanism of Action
- Tibolone is a synthetic steroid hormone with a tissue-specific effect. It has estrogenic, progestogenic, and weak androgenic activity. It acts by interacting with estrogen, progesterone, and androgen receptors.
Indications
- Treatment of symptoms associated with menopause, such as hot flashes, vaginal dryness, and mood swings
- Prevention of osteoporosis in postmenopausal women
Common Dosage Forms
- Tablet
Typical Dosage
- 2.5 mg once daily
Pediatric Dosage
- Not recommended for use in children
Geriatric Dosage
- Dose adjustment may be needed in elderly patients
Side Effects
- Headache
- Breast pain
- Vaginal bleeding
- Mood changes
- Edema
- Acne
- Liver dysfunction
Contraindications
- Pregnancy
- Breastfeeding
- History of breast cancer or other estrogen-dependent tumors
- Severe liver disease
Pregnancy Category
- X - Contraindicated in pregnancy
Lactation Safety
- Not recommended during breastfeeding
Drug Interactions
- Concomitant use with enzyme-inducing drugs may decrease tibolone efficacy
Overdose Symptoms
- Nausea
- Vomiting
- Breast tenderness
Antidote for Overdose
- No specific antidote, symptomatic and supportive treatment
Storage Conditions
- Store at room temperature away from moisture and heat
Pharmacokinetics
- Absorption: Rapidly and almost completely absorbed from the gastrointestinal tract
- Distribution: Tibolone and its metabolites are extensively bound to plasma proteins
- Metabolism: Metabolized in the liver to active metabolites
- Excretion: Excreted primarily in the urine and feces
Precautions
- Regular monitoring of liver function tests is recommended during treatment
Warnings
- Increased risk of endometrial and breast cancer
- Risk of venous thromboembolism
- Should not be used as a contraceptive
Others
- May take several weeks to see the full benefit of the medication