Have you heard of a menopause hormone therapy (MHT) called tibolone? It is a type of combined HRT that has estrogenic, androgenic effects (testosterone) and progesterone effects. Find out how tibolone treatment works, the benefits and risks and who would benefit from it's use.
What is Tibolone?
Tibolone is a type of synthetic hormone replacement therapy (HRT) drug. It is derived from the Mexican yam. It is metabolized in the body by the liver. Some of the tibolone metabolites act at the estrogen receptor exerting estrogen effects, especially at the alpha receptor. Another metabolite has androgenic effects (testosterone) and progesterone effects.
How does Tibolone work as HRT?
Tibolone is a synthetic hormone that is used to treat menopause symptoms. It works by mimicking the effects of estrogen, progesterone and testosterone in the female body.
In the brain it acts like estrogen to support circadian rhythm and sleep, and sexual desire, and reduces hot flashes, night sweats and brain fog.
It helps maintain bone strength and reduce fracture risk.
In the vulva/vagina/perineum it maintains the skin integrity, reduces urinary tract infections, and pain with sex.
Mood and libido are thought to be improved by the testosterone-like effect.
Tibolone comes in a 2.5mg tablet.
Who can use tibolone as HRT?
Tibolone is usually used as HRT for women who have not had a natural period for over 12 months. If it is used in women who are still having natural periods, it may cause irregular vaginal bleeding.
Who should not use tibolone?
Tibolone is not recommended to be used in women who are undergoing breast cancer treatment as it can interfere with treatments.
It is not used in people who have had a history of breast cancer.
If you have an increased risk of beast cancer you should check with your health practitioner if this is a suitable option for the treatment of your perimenopause/menopause symptoms.
How do I start taking tibolone?
Women who are using cyclical HRT with estrogen and progesterone can begin to use at the end of their estrogen + progesterone cycle.
Women who are using continuous can substitute the estrogen + progesterone for tibolone.
If you are not currently using any HRT or you have had a hysterectomy, or you are using only estrogen therapy, you can start using Tibolone as soon as you get your prescription.
What are the benefits of taking tibolone?
Tibolone is a hormone therapy used to treat conditions related to menopause. It is a good options for people who want to use a single pill for their HRT.
It is less effective that actual use of estrogen and progesterone, but for some women it can help improve the symptoms of perimenopause including:
hot flashes/hot flushes
female sexual dysfunction associated with vaginal dryness, pain or low libido.
Tibolone has also been shown to help protect against bone loss (osteoporosis), and reduces the risk of spine fractures.
What is the breast cancer risk of using Tibolone?
Tibolone HRT does not change the breast tissue density and the randomized trials indicate that tibolone either has a neutral effect or reduces risk of breast cancer in women without prior breast can.
In women who have had prior breast cancer there does appear to be an increased risk of recurrence of breast cancer (Lancet Oncol 2009).
What are the side effects of tibolone?
Side effects can occur with any medication, but are reasonably uncommon with tibolone. Look out for the following side effects:
Spotting or irregular bleeding. This should settle down within a few months and if it is ongoing, you should see your health provider.
There is a slight increase in risk of stroke 4 extra cases per 1000 in women aged 50-60 and 13 extra cases per 1000 in women aged over 60.
In observational studies from Denmark, there appears to be a small risk of endometrial cancer and ovarian cancer with the use of Tibolone (Løkkegaard 2018).
However the Cochrane systematic review showed no significant difference in women who used tibolone vs women who did not for any of the following:
Blood clots (ie in the legs or the lungs)
Heart attacks or other events relationg to cardiovascular disease
Strokes/brain bleeds or brain blood clots
Younger age at death from any cause.
Why is tibolone banned in sports?
Tibolone is considered a performance-enhancing drug in sport and is banned by the World Anti-Doping Agency (WADA). It is a synthetic anabolic steroid that can increase muscle mass and strength, as well as promote recovery. Therefore it is prohibited in competitive sports.
Is tibolone the same as HRT?
No, Tibolone is a hormone therapy (HRT) but it is not the same as traditional HRT. It acts in a similar way to estrogen, progesterone, and testosterone.
Does tibolone make you gain weight?
In a study that looked at women using tibolone for 2 years, there was an increase in weight of 1.5-2kg (Potdar 2010). Some of this many have been due to water retention as progesterone effects can induce this. If you are have have concerns about weight gain with tibolone, discuss with your healthcare provider.
Is tibolone safer than HRT?
The risks of Tibolone are similar to traditional HRT. Talk to your healthcare provider to see if it could be useful for your menopause symptoms.
Can you just stop taking tibolone?
Yes, you can stop taking tibolone at any time. However, if you have been using it for a long period of time and then suddenly discontinue it, this could result in menopausal symptoms returning. These symptoms would be present for a shorter duration and less severity if your tibolone dose is reduced when you want to stop using it.
Can you drink alcohol with tibolone?
It is recommended that post-menopausal women limit the amount of alcohol that you drink when taking tibolone. Being post-menopausal in itself increases your risk for health conditions such as high blood pressure, heart disease, diabetes and stroke.
If you do choose to drink alcohol, it is best to have no more than 1-2 units of alcohol per day and to ensure you have at least 2 alcohol free days per week.
Does tibolone affect mood?
In studies, tibolone has positive effects on mood compared with the placebo group and improves many negative mood symptoms to a similar extent as conventional hormone replacement therapy.
Improved mood with tibolone use is associated with higher levels of beta-endorphins. TIbolone treatment is also is associated with better word memory (Davis 2002).
Does tibolone improve female sexual function?
Tibolone improves sexual function more than standard hormone replacement therapy does (Davis 2002). This is thought to be due to the testosterone effects which alongside estrogen increase the vulva and vaginal skin integrity and also improves sexual desire (libido).
How does Tibolone affect the hair?
Women taking tibolone may experience thinning of the hair or increased facial hair as these are two potential effects due to increased testosterone effects of the hormone therapy.
Is Tibolone Funded in New Zealand?
As of 9 April 2023, Tibolone is available in New Zealand, but it is not funded by PHARMAC.
Find out about more funded and non-funded HRT treatments available in New Zealand - here.
The Takeaways on Tibolone treatment
Tibolone is a form of hormone therapy (HRT) used to treat menopausal symptoms.
It acts in a similar way to estrogen, progesterone, and testosterone.
The Cochrane review does not show increased risk of cancers, heart disease, stroke or death with tibolone use.
There may be increased risk in women who have had
Where can I get started?
Tracking your perimenopause symptom patterns is a great place to start. Contact your health provider or menopause specialist if you would love to know more.
As a menopause doctor, Dr Deb Brunt @ Ōtepoti Integrative Health would love to support you through the perimenopause and menopausal stages of life, supporting all aspects of your health and wellbeing.
Dr Deb Brunt is a menopause specialist in New Zealand and Menopause health coaches internationally. She has a passion for supporting women adapt to their changing female physiology for optimum health so they are able to live their best life
Schedule a free health discovery call with her to learn more.
More about Perimenopause and Menopause
Løkkegaard ECL, Mørch LS. Tibolone and risk of gynecological hormone sensitive cancer. Int J Cancer. 2018 Jun 15;142(12):2435-2440.
Potdar J. Non-conventional hormone therapy - Tissue-specific Tibolone-Caution. J Midlife Health. 2010 Jul;1(2):59-62.
Davis SR. The effects of tibolone on mood and libido. Menopause. 2002 May-Jun;9(3):162-70.
Kenemans P, Bundred NJ, Foidart JM, et al. LIBERATE Study Group. Safety and efficacy of tibolone in breast-cancer patients with vasomotor symptoms: a double-blind, randomised, non-inferiority trial. Lancet Oncol. 2009 Feb;10(2):135-46.
Formoso G, Perrone E, Maltoni S, et al. Short-term and long-term effects of tibolone in postmenopausal women. Cochrane Database Syst Rev. 2016 Oct 12;10(10):CD008536.