About Tibolone A synthetic steroid hormone,Selective tissue estrogenic activity regulator, Female sexual dysfunction drug. Mechanism of Action of Tibolone The drug metabolized in a tissue selective manner in to three metabolites which have estrogenic, progestogenic and weak androgenic properties. It restores plasma endorphin level in post menopausal women and stabilizes the hypothalamic pituitary systems. It increases bone mineral density and raises gonadotropin levels. It decreases vasomotor symptoms with out stimulating endometrium. It improves urogenital atrophy, psychological symptoms, libido and osteoporosis. Indications for Tibolone 1.Menopausal vasomotor symptoms due to estrogen deficiency, 2.Osteoporosis. Interactions for Tibolone Antibacterials: Rifampicin: Accelerates metabolism (reduced plasma concentration). Antiepileptics: Carbamazapine, phenobarbitone, phenytoin, primidone: Accelerate metabolism.