Source: Health Products Regulatory Authority (ZA) Revision Year: 2022 Publisher: Pharma Dynamics (Pty) Ltd, 1<sup>st</sup> Floor, Grapevine House, Steenberg Office Park, Silverwood Close, Westlake, Cape Town, 7945, South Africa
Pharmacological classification: A.21.13 Others
Pharmacotherapeutic group: Urogenital system (including sex hormones)
ATC code: G03CX01
Tibolone stabilises the hypothalamic-pituitary system after failure of ovarian function in the climacteric, which leads to the occurrence of vasomotor complaints as a result of the involvement of the thermoregulatory centre in the hypothalamus. The therapeutic central effect of tibolone is due to the combined estrogenic, progestogenic and weak androgenic activities of the medicine.
Tibolone has a moderate gonadotrophin suppressing effect in post-menopausal woman.
The peripheral effect of tibolone is the combination of hormonal activities which exerts a balanced effect and does not stimulate the endometrium in post-menopausal woman.
Following oral administration, tibolone is rapidly and extensively absorbed, appearing in the blood within 30 minutes of oral administration with peak levels between 1,5 and 4 hours. The consumption of foods has no significant effects on the extent of absorption.
Tibolone is metabolised in the liver and converted to metabolites. Some metabolites may contribute to the biological effects of the medicine. The elimination half-life of tibolone and active metabolites is less than 2 days, justifying once a day administration.
Excretion of tibolone is mainly in the form of conjugated (mostly sulphated) metabolites, which are excreted mainly in the faeces and to a lesser extent in the urine.
The pharmacokinetic parameters for tibolone and its metabolites were found to be independent of renal function.
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