Tibolone

What is Tibolone?

Tibolone is a type of hormone replacement therapy (HRT) which is used to treat the symptoms of menopause in women, including hot flushes, mood swings, reduced libido, pain or discomfort during sex, and vaginal irritation, inflammation or dryness. Tibolone may also be prescribed to prevent the onset of osteoporosis in women who are unable to take other forms of HRT.

How does Tibolone work?

During menopause, the amount of oestrogen produced by the ovaries decreases, resulting in symptoms such as mood swings, reduced libido, pain or discomfort during sex, vaginal irritation and dryness, spotting, and recurrent urinary tract infection (UTI). Tibolone is a synthetic steroid which mimics the activity of the female sex hormones oestrogen and progesterone, and of the androgen hormone testosterone. When absorbed, Tibolone is broken down into three compounds which act similarly to the body’s natural oestrogen, progesterone and testosterone, restoring the body’s hormonal balance and relieving the symptoms of menopause. 

Will I have to use HRT forever?

Many women continue to use HRT for several years. However, the potential health risks associated with HRT do increase slightly with time and age, so a doctor will usually prescribe the lowest dose necessary for the patient’s symptoms and for the shortest amount of time. While HRT delays the onset of osteoporosis, it does not prevent it altogether. Deciding when to come off of HRT is a personal decision that should be discussed with a doctor beforehand.

Active ingredients

The active ingredient in Tibolone is tibolone.

Inactive ingredients

The inactive ingredients in Tibolone are potato starch, lactose monohydrate, ascorbyl palmitate and magnesium stearate.

The recommended dose of Tibolone is 1 x 2.5mg tablets taken once daily at the same time each day.

How to start Tibolone?

You should only start taking Tibolone following consultation with a doctor. You can start taking it straight away if:

• You are changing from a period-free HRT

• You have never used HRT before

• It was prescribed to you following a hysterectomy

• You are being treated for endometriosis

If you are changing over from a type of HRT which allows for monthly withdrawal bleeds (such as Elleste Duet), wait for your next bleed and start taking Tibolone as soon as your bleed ends. 

You should NOT take Tibolone if you have experienced a natural period within the last 12 months.

How to take Tibolone

Always take Tibolone as instructed by a doctor. Swallow each tablet with water, without chewing or breaking it, at the same time each day. To help you remember, try and make this a part of your daily routine - for example, take your tablet with breakfast each day, or when you brush your teeth in the morning or evening. Each strip of tablets is marked with the days of the week to help you keep track. When you finish a strip, start a new one on the next day without leaving a gap.

If you forget to take a tablet, try and take it within 12 hours of the normal time. If 12 hours has already passed, just skip the dose and take the next tablet at the normal time. Never take a double dose to make up for a missed one.

Like all medications, Tibolone can cause side effects in some patients. If you experience any of the following, stop taking Tibolone immediately and see a doctor straight away:

• A significant rise in blood pressure

• Jaundice (yellowing of the skin or whites of the eyes)

• Sudden migraines 

• Signs of a blood clot

Common side effects, which can affect up to 1 in 10 people, include:

• Breast pain

• Stomach or pelvic pain

• Unusual hair growth

• Vaginal bleeding or spotting (this is common in the first few months of using HRT and usually stops over time)

• Thrush, vaginal irritation or itching, or an increase in vaginal discharge

• Thickening of the lining of the womb or the lining of the cervix

• Weight gain

Uncommon side effects (affecting up to 1 in 100 women) can include:

• Signs of fluid retention (swelling of the hands, ankles or feet)

• Stomach upset

• Acne

• Painful nipples

• Vaginal infections

Rarely, women taking Tibolone may experience itchy skin. The following have also been reported by women taking Livial:

• Depression, headaches, dizziness

• Joint or muscle pain

• Rash or itching of the skin

• Loss of vision or blurred vision

• Changes in liver tests

Tibolone slightly increases the risk of developing breast cancer or endometrial cancer. It is important to go for regular health checks (breast screening and cervical smear tests) while taking this medication. Speak to your doctor for more information if you are worried.

Contraindications

Do NOT take Tibolone if:

• You are allergic to any of the ingredients in this medication

• You have, have ever had, or are suspected of having breast cancer

• You have a form of oestrogen-sensitive cancer

• You have unexplained vaginal bleeding

• You have endometrial hyperplasia (excessive thickening of the womb lining)

• You have or have ever had thrombosis (blood clot in a vein)

• You have a blood clotting disorder

• You have or have recently had a heart attack, angina, or any other disease caused by a blood clot in an artery

• You have or have ever had a liver disease

• You have porphyria 

• You are pregnant or think you  might be pregnant

• You are breastfeeding

You should tell your doctor before taking Tibolone if you have ever experienced any of the following:

• Fibroids inside the womb

• Endometriosis (growth of the womb lining outside of the womb) or endometrial hyperplasia (excessive growth of the womb lining)

• Increased risk of developing blood clots

• Increased risk of developing an oestrogen-sensitive cancer

• High blood pressure

• A liver disorder

• Diabetes

• Gallstones

• Migraines or severe headaches

• Systemic lupus erythematosus (a disease of the immune system affecting many organs of the body

• Epilepsy

• Asthma

• Otosclerosis (a disease affecting the eardrum and hearing)

• Triglycerides (high level of fat in the blood)

• Fluid retention due to kidney problems

Drug Interactions

Before taking Tibolone, tell your doctor or pharmacist if you are taking any other medications, including those purchased over the counter without a prescription. The following medications may interfere with the effect of Tibolone and lead to irregular bleeding:

• Medicines for blood clotting, such as warfarin

• Medicines for epilepsy, such as phenobarbital, phenytoin and carbamazepine

• Medicines for tuberculosis, such as rifampicin

• Herbal remedies containing St John’s Wort

Pregnancy and breastfeeding

Do not take Tibolone if you are breastfeeding, pregnant, think you might be pregnant, or are planning on becoming pregnant. If you become pregnant while taking Tibolone, stop taking it immediately and consult a doctor.

HRT

While Tibolone, brand name Livial, is a synthetic steroid, other forms of HRT contain either bioidentical or synthetic supplements of the hormones oestrogen and/or progesterone themselves.Tibolone is thought to carry a slightly lower risk of breast cancer than hormonal HRTs, but you can speak to your doctor to work out which option is best for you.

Oestrogen-only HRTs can be taken orally, applied to the skin as a transdermal patch, or applied topically as a gel or cream. They should only be used by women who have had a hysterectomy, or who have an alternative progesterone supplement such as an intrauterine device (IUD), as progesterone is required to prevent a dangerous build up of the uterine lining. Premarin and Elleste Solo are oestrogen-only HRTs that can be taken orally, while Elleste Solo MX80, Elleste Solo MX40 and Evorel are transdermal patches which are changed twice weekly. Patches have the benefit of bypassing the digestive system, reducing the likelihood of developing side effects. 

Women who have not had a hysterectomy, or who do not have an alternative supply of progesterone, will need to use a combined form of HRT containing both oestrogen and progesterone. Climesse, Elleste Duet Conti, and Prempak-C are continuous forms of HRT, while Kliovance and Elleste Duet allow for a monthly withdrawal bleed and are therefore more suitable for women who have experienced a natural period within the last 12 months.

If you are in the early days of your menopause and are suffering from vaginal symptoms such as dryness, irritation, inflammation, pain or discomfort during sex, spotting, and recurrent UTIs, you may wish to try a topical form of HRT. Ovestin, Estriol and Premarin Creams, and vaginal suppositories such as Vagifem contain an oestrogen supplement and work locally in the vaginal region to relieve these symptoms. They are also less likely to cause side effects, but bear in mind that they can have a weakening effect on latex condoms and diaphragms.

Alternatives to HRT

Although HRT is the most popular and accessible treatment for the symptoms of menopause, some women choose to try herbal supplements to help with hot flushes and mood swings. However, the effectiveness of herbal supplements in unknown, so you should make sure to consult a doctor or pharmacist for advice and information before trying a product. 

Lifestyle changes to improve menopause symptoms

Making a few lifestyle changes can help you to deal with the symptoms of menopause. To reduce the impact of hot flushes and night sweats, try cutting down on caffeine, alcohol and spicy foods, and quit smoking if you haven’t already done so. Meanwhile, exercising regularly and increasing your intake of vitamin D, which is vital for the production of calcium, can help to keep your bones strong and healthy. Although there is little evidence to suggest that eating an oestrogen-rich diet will significantly reduce symptoms of menopause, some women choose to increase their intake of plant-based foods containing oestrogen, such as sesame and flaxseed, died fruits, oranges, strawberries and apricots.

Is Tibolone safe?

Tibolone is considered a safe and effective first-line treatment for the symptoms of menopause, and a second-line treatment for preventing the onset of osteoporosis. HRT in general carries a very slight increase in the risk of developing oestrogen sensitive cancers, such as breast cancer, ovarian cancer and endometrial cancer, stroke, and blood clots, but for most women, the benefits of HRT outweigh this risk. Make sure to read the patient information carefully and inform your doctor of any previous or existing conditions you have.

Sources

Patient Information Leaflet

NHS - HRT

Health Direct - Livial 

GOV.UK - Tibolone: benefit-risk balance