Indications
Tibolone is prescribed for alleviating symptoms associated with natural or surgical menopause in postmenopausal women. It is also recommended for preventing osteoporosis in women who are postmenopausal and at high risk of fractures, but are unable to take other osteoporosis medications.
Pharmacology
Tibolone is a synthetic steroid with estrogenic, androgenic, and progestagenic properties. Upon oral administration, Tibolone is swiftly metabolized into three compounds, each contributing to its pharmacological effects. The metabolites exert estrogenic effects on the vagina, bone, and thermoregulatory centers in the brain, thereby reducing menopausal symptoms and preventing bone loss post-menopause or following ovariectomy. Tibolone also enhances vaginal moisture and alleviates vaginal atrophy, while influencing mood and libido.
Dosage & Administration
The recommended dosage is one Tibolone tablet daily (2.5 mg). It should be swallowed with water or another beverage, preferably at the same time each day. Symptom improvement is typically noticeable within a few weeks, with optimal results achieved after at least 3 months of continuous therapy.
Starting Tibolone Tablet:
- For natural menopause, treatment should begin at least 12 months after the last natural bleed.
- In cases of surgical menopause, treatment can commence immediately.
Switching from HRT (Hormone Replacement Therapy):
- If transitioning from sequential HRT, start Tibolone the day after completing the previous regimen.
- For continuous-combined HRT, Tibolone can be initiated at any time.
Missed Dose:
- If a dose is missed, take it as soon as remembered, unless it’s more than 12 hours overdue. In that case, skip the missed dose and resume with the next scheduled dose to avoid breakthrough bleeding.
Interactions
While no specific interactions with Tibolone have been reported clinically, theoretical considerations suggest that enzyme-inducing compounds like barbiturates, carbamazepine, hydantoins, and rifampicin may potentially decrease its effectiveness.
Contraindications
Tibolone is contraindicated in pregnancy, during lactation, and in individuals with known or suspected hormone-dependent tumors, cardiovascular or cerebrovascular disorders, active deep vein thrombosis, thromboembolic disorders, unexplained vaginal bleeding, and severe liver diseases.
Side Effects
Possible side effects include vaginal bleeding or spotting, particularly in the initial months of treatment, as well as headache, migraine, edema, dizziness, pruritus, weight gain, nausea, abdominal pain, rash, and depression.
Pregnancy & Lactation
Use of Tibolone is strictly contraindicated during pregnancy and lactation.
Precautions & Warnings
Special precautions should be observed in patients with renal dysfunction, history of liver disease, epilepsy, migraine, hypercholesterolemia, impaired carbohydrate metabolism, diabetes mellitus, and cholestatic jaundice.
Overdose Effects
Acute overdose of Tibolone is rare and typically results in mild symptoms such as nausea, vomiting, and withdrawal bleeding in females. Symptomatic treatment may be administered if necessary.
Therapeutic Class
Tibolone belongs to the therapeutic class of drugs used for managing menopausal symptoms, specifically hormone replacement therapy.
Storage Conditions
Store Tibolone in a cool, dry place away from light, and keep it out of reach of children.
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