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Medication Spotlight: Tibella

A relatively unknown form of hormone replacement therapy, Tibella is a convenient one pill a day option for short-term treatment of postmenopausal symptoms due to estrogen deficiency.


Tibella contains 2.5 mg of tibolone and is a prodrug which is metabolized in the body into its active metabolites. This gives Tibella a unique mechanism. Tibolone is metabolized into three compounds: 3α-hydroxy-tibolone, 3β-hydroxy-tibolone, and a Δ4-tibolone. The two hydroxylated versions of tibolone have an estrogenic effect on the brain, vagina and bone, allowing for relief of hot flashes, vaginal dryness and bone preservation. The third compound Δ4-tibolone has both progestin and androgen activity. Its progestin activity minimizes endometrial proliferation and hyperplasia, whereas its androgen activity could improve libido.


As mentioned before, its dosing is 1 tablet daily at the same time each day without regards to meals. Patients should not be taking any extra hormone therapy because this tablet already has all the activity.


Tibella has many contraindications such as endometrial cancer, breast cancer, history of clotting disorders and many more.

There are many concerns with hormone replacement therapy, such as increased risk of venous thromboembolisms, stroke, cardiovascular events, breast cancer and uterine cancer. Specifically, Tibella can cause common adverse effects such as weight gain, gastrointestinal symptoms, mood changes and amenorrhea. In addition, Tibella’s androgenic activity can cause acne and excess hair growth.

Tibella can increase the effect of anticoagulants. As well, Tibella is metabolized by CYP3A4, so CYP3A4 inducers such as phenytoin, carbamazepine and phenobarbital should be used with caution because it can lead to unpredictable bleeding patterns.

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