Treatment of symptoms resulting from the natural or surgical menopause in post menopausal women. Prevention of osteoporosis in women who have gone through the menopause & are at high risk of fractures, but cannot take other medicines used to prevent osteoporosis.
Tibolone is a synthetic steroid that has estrogenic, androgenic and progestagenic properties. After oral administration, Tibolone is rapidly metabolized into three compounds which contribute to the pharmacological effects of Tibolone. Two of these metabolites (the 3α−OH and 3β−OH metabolite) have predominantly estrogenic activity; a third metabolite (δ4-isomer of Tibolone) and the parent compound have predominantly progestagenic and androgenic activities. Tibolone substitutes for the loss of estrogen production in postmenopausal women and alleviates menopausal symptoms. It prevents bone loss following menopause or ovariectomy. It has estrogenic effects on the vagina, on bone and on the thermoregulatory centers in the brain (hot flushes). It improves vaginal dryness and vaginal atrophy. Tibolone has also effects on mood and libido.
Treatment of symptoms resulting from the natural or surgical menopause. Prevention of post-menopausal bone mineral density loss: The recommended dose is 2.5 mg once daily. Improvement of symptoms generally occurs within a few weeks, but optimal results are obtained when therapy is continued for at least 3 months. Women experiencing a natural menopause should commence treatment with tibolone at least 12 months after their last natural bleed. In case of a surgical menopause, treatment with tibolone may commence immediately.
No examples of interactions between Tibolone and other medicines have been reported in clinical practice. However, the following potential interactions should be considered on a theoretical basis: Enzyme-inducing compounds such as barbiturates, carbamazepine, hydantoins, and rifampicin may enhance the metabolism of Tibolone and thus decrease its therapeutic effect. Since Tibolone may increase blood or fibrinolytic activity (lower fibrinogen levels; higher AT III, plasminogen, and fibrinolytic activity values), it may enhance the effect of anticoagulants.
Contraindicated in - pregnancy & lactation; known, past or suspected breast cancer; known or suspected estrogen dependent malignant tumors (e.g. endometrial cancer); undiagnosed genital bleeding; untreated endometrial hyperplasia; previous idiopathic or current venous thromboembolism (deep venous thrombosis, pulmonary embolism); arterial thromboembolic disease (e.g. angina, myocardial infarction, stroke or TIA); acute liver disease or a history of liver disease as long as liver function tests have failed to return to normal; porphyria Precautions should be taken in - uterine fibroids or endometriosis, thromboembolic disorders, estrogen dependent tumors, hypertension, liver disorders (e.g. liver adenoma), diabetes, asthma, epilepsy etc.
Gastrointestinal disorders like abdominal pain, skin & subcutaneous tissue disorders like abnormal hair growth, acne, reproductive system & breast disorders like vaginal discharge, genital pruritus, vaginal candidiasis etc.
US-FDA pregnancy category D. Tibolone is contraindicated in lactating women.
The acute toxicity of Tibolone in animals is very low. Therefore, toxic symptoms are not expected to occur if several tablets are taken simultaneously. In cases of acute overdose - nausea, vomiting, and withdrawal bleeding in females may develop. Symptomatic treatment can be given if necessary.
Keep in a cool & dry place. Protect from light. Keep out of the reach of children.
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