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In itself Tibolone has no biological activity; the effects are produced mainly by the results of the activity of its metabolites on various tissues. After administration, Tibolone is quickly metabolized into 3¦Á-hydroxytibolone and 3--hydroxytibolone compounds, which are also present in an inactive, sulfated form. A third compound, the ¦¤4- isomer is formed from Tibolone directly or from the 3h hydroxymetabolite.
Tibolone has estrogenic effects on bone and vaginal tissue. The ¦¤4-isomer functions as a progestogen in endometrial tissue, whereas in the brain and liver it has androgenic effects.In breast tissue, Tibolone acts by strongly inhibiting sulfate activity and weak inhibition of 17¦Á-hydroxysteroid dehydrogenase activity, which results in blocking the conversion of estrone sulfate to E2.
Tibolone Contraindications;Tibolone is contraindicated in patients with the following conditions:,Women with hormone treated tumors,Undiagnosed vaginal bleeding,Pregnancy/lactation,Liver and/or cardiac disease,Tibolone Adverse Drug Effects,Depression,Diarrhea, constipation, nausea, vomiting or abdominal pain,Visual disturbances,Alteration in results of liver function tests,Excessive fluid retention in the body tissues resulting in swelling (edema),weight changes, vaginal bleeding, pain in the muscles and joints, rashes or itching,Seborrhoeic dermatitis,Headaches, dizziness, growth of facial hair
Tibolone interacts with:Rifampicin,Anti-epileptics such as phenytoin, primidone, Phenobarbitone



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