Tibolone

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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 and are at high risk of fractures, but cannot take other medicines used to prevent osteoporosis.

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Contraindicated in pregnancy and lactation, known or suspected hormone-dependent tumours, cardiovascular or cerebrovascular disorders, active deep vein thrombosis, thromboembolic disorders, vaginal bleeding of unknown etiology and severe liver disorders.

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.

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.

Occasionally, vaginal bleeding or spotting may occur, mainly during the first months of treatment. Other adverse effects are headache and migraine, oedema, dizziness, pruritus, increase in body weight, nausea, abdominal pain, rash, and depression.

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.

Tibolone tablet is contraindicated during pregnancy. If pregnancy occurs during medication with this tablet, treatment should be withdrawn immediately. For this tablet no clinical data on exposed pregnancies are available. Tibolone tablet is contraindicated in lactating women.

In patients with renal dysfunction, history of liver disease, epilepsy, migraine, hypercholesterolemia, impaired carbohydrate metabolism, diabetes mellitus and cholestatic jaundice.