Tuesday, June 13, 2023

Tibolone – Alternative to HRT

 

Tibolone (brand name Livial) is a prescription medicine that is similar to taking combined HRT (oestrogen and progestogen). Actually, Tibolone is a synthetic hormone medication that is primarily used in hormone replacement therapy (HRT) for postmenopausal women, mimicking the actions of estrogen, progesterone, and testosterone in the body.

Advantages

Tibolone is commonly prescribed to alleviate menopausal symptoms such as hot flashes, night sweats, vaginal dryness, and mood swings. It can also help prevent bone loss and reduce the risk of osteoporosis - a condition characterized by weakened bones.

Here are some potential advantages of tibolone:

  • Menopausal Symptom Relief: Tibolone can effectively alleviate menopausal symptoms such as hot flashes, night sweats, vaginal dryness, and mood swings. It acts as a hormonal substitute, providing relief from these symptoms and improving overall quality of life.
  • Bone Health: Tibolone has been shown to help prevent bone loss and reduce the risk of osteoporosis, a condition characterized by weakened bones. By mimicking the effects of estrogen, tibolone can help maintain bone density and reduce the risk of fractures associated with osteoporosis.
  • Hormonal Balance: Tibolone acts as a combined hormonal therapy, providing estrogenic, progestogenic, and androgenic effects. This can help restore hormonal balance in postmenopausal women, potentially improving various aspects of health and well-being.
  • Convenience: Compared to traditional hormone replacement therapies that involve separate estrogen and progestogen medications, tibolone is a single tablet that combines both hormones. This can be more convenient for women who prefer a simpler treatment regimen.
  • Endometrial Protection: Tibolone has progestogenic effects, which can help protect the endometrium (the lining of the uterus) from the potential overstimulation by estrogen alone. This reduces the risk of endometrial hyperplasia and may lower the risk of endometrial cancer associated with unopposed estrogen therapy.



How it works?

The exact mechanism of action of tibolone is not fully understood, but it is believed to exert its effects by binding to estrogen, progesterone, and androgen receptors in the body. This allows it to act as an agonist (mimicking the effects) on certain tissues and as an antagonist (blocking the effects) on others.

When tibolone is taken orally, it undergoes metabolic conversion in the body, resulting in the formation of various metabolites with different hormonal effects. These metabolites contribute to the overall effects of tibolone.

The exact mechanism of action of tibolone is not fully understood, but it is believed to act through the following mechanisms:

  • Estrogenic Activity: Tibolone metabolites have estrogenic effects on certain tissues in the body, such as bone, the brain, and the vagina. By binding to estrogen receptors in these tissues, tibolone can help alleviate menopausal symptoms and prevent bone loss.
  • Progestogenic Activity: Tibolone also has progestogenic effects, meaning it can bind to progesterone receptors in the body. This helps provide endometrial protection, reducing the risk of endometrial hyperplasia and potentially lowering the risk of endometrial cancer associated with estrogen therapy alone.
  • Androgenic Activity: Tibolone metabolites have weak androgenic effects, similar to testosterone. This can help improve sexual well-being, libido, and mood in some women.

The overall effects of tibolone depend on the balance of its metabolites and their interactions with different tissues and receptors in the body. It's important to note that tibolone is a systemic hormone therapy and can affect multiple organs and systems.

Protocol and dosage

It's taken as a tablet once a day. It can help relieve symptoms such as hot flushes, low mood and reduced sex drive, although some studies have suggested it may not be as effective as combined HRT. It's only suitable for women who had their last period more than a year ago (known as the post-menopause).

Side effects

It's important to note that tibolone is not recommended for all women, especially those with a history of certain medical conditions such as breast cancer, liver disease, or unexplained vaginal bleeding. Like any medication, tibolone carries potential risks and side effects, which should be discussed with a healthcare professional before starting treatment.

Here are some commonly reported side effects associated with tibolone:

  • Menstrual Irregularities: Tibolone can cause changes in menstrual bleeding patterns, including irregular or unpredictable bleeding. Some women may experience spotting or breakthrough bleeding.
  • Breast Discomfort: Breast tenderness or pain can occur as a side effect of tibolone. It is recommended to monitor any changes in the breasts and report them to a healthcare professional.
  • Headaches: Some individuals may experience headaches or migraines while taking tibolone. If headaches become severe or persistent, it's important to consult with a healthcare professional.
  • Mood Changes: Tibolone can affect mood and may lead to changes such as depression, irritability, or mood swings. It is essential to discuss any mood changes with a healthcare professional.
  • Gastrointestinal Symptoms: Tibolone can cause digestive symptoms such as nausea, abdominal discomfort, bloating, or changes in appetite.
  • Skin Reactions: In some cases, tibolone can lead to skin reactions such as rash or itching. If you experience any skin changes or allergic reactions, it's important to seek medical attention.
  • Weight Changes: Some individuals may experience weight changes while taking tibolone. This can include weight gain or weight loss.
  • Other Side Effects: Additional side effects that have been reported with tibolone include dizziness, fatigue, muscle pain, changes in libido, and changes in hair growth.