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Tibolone may enhance the blood fibrinolytic activity of anticoagulants such as warfarin. Use with caution during concomitant use especially when starting or stopping concurrent tibolone treatment.
In vivo, the pharmacokinetics of midazolam (cytochrome P450 3A4 substrate) may be affected to a moderate extent and therefore drug interactions with other CYP3A substrates may be expected. However, the clinical relevance is dependent on the pharmacological and pharmacokinetic properties of the substrate involved.
The metabolism of tibolone may be enhanced and its activity reduced by compounds that induce liver enzymes (e.g., phenytoin, carbamazepine and rifampicin).
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