What is Tibolone?

Tibolone is a synthetic steroid medicine used for hormone replacement therapy (HRT). It mimics the activity of the female sex hormones oestrogen and progesterone in the body.

How does Tibolone work?

Oestrogen is the main sex hormone in the female body. Certain parts of the body such as the vagina, bones and breasts rely on oestrogens to function normally. When the levels of oestrogen are low, these tissues can slowly degenerate, as is experienced during menopause. In addition low levels of oestrogen can cause distressing symptoms such as hot flushes, night sweats, mood swings or depressed mood, reduced sex drive and vaginal dryness. Oestrogen levels decrease naturally during the menopause, but also decrease following a hysterectomy (surgical menopause) and in women taking medicines called gonadorelin analogues, eg leuprorelin for endometriosis.

What is Tibolone used for?

Tibolone's oestrogenic effect on bone density also allows it to be used to prevent osteoporosis in oestrogen deficient women who are at risk of fractures. Women considered to be at risk of developing fractures due to osteoporosis include those who have had an early menopause, those with a family history of osteoporosis, those who have had recent prolonged corticosteroid (eg prednisolone) therapy, those with a small thin frame, and smokers.

Tibolone mode of action

Tibolone when taken by mouth is broken down into three compounds which act in a similar way to the natural oestrogen and progesterone found in the body. This helps restore the balance of hormones in the body and reduces the symptoms of menopause, whether natural or otherwise.

Tibolone side effects

It is important to be aware that all women using HRT have an increased risk of being diagnosed with breast cancer compared with women who don't use HRT. This risk needs to be weighed against the personal benefits to you of taking HRT. There is more detailed information about the risks and benefits associated with HRT in the factsheet about the menopause linked above. You should discuss these with your doctor before starting HRT. Women on HRT should have regular breast examinations and mammograms and practice breast self-examination. Report any changes in your breasts to your doctor or nurse.

It is important to be aware that women taking HRT have a slight increase in the risk of abnormal blood clot formation (deep vein thrombosis and pulmonary embolism) compared with women not taking HRT. At present it is unclear whether tibolone carries the same risk as other types of HRT in this respect. Women should carefully discuss this with their doctor before starting treatment, particularly those with a personal or family history of thrombosis or other risk factors (eg obesity, recent surgery, immobility).

Medicines and their possible side effects can affect individual people in different ways. The following are some of the side effects that are known to be associated with Tibolone. Because a side effect is stated here, it does not mean that all people using this medicine will experience that or any side effect.

-Depression

-Disturbances of the gut such as diarrhoea, 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 (oedema)

-Weight changes

-Vaginal bleeding

-Pain in the muscles and joints

-Rash or itching

-Seborrhoeic dermatitis

-Headache

-Dizziness

-Growth of facial hair

Chemical Structure

Molecular Formula C21H28O2

Disclaimer:

Information on this page is provided for general information purposes. You should not make a clinical treatment decision based on information contained in this page without consulting other references including the package insert of the drug, textbooks and where relevant, expert opinion. We cannot be held responsible for any errors you make in administering drugs mentioned on this page, nor for use of any erroneous information contained on this page.