tibolone

Action and Spectrum

Actions and Spectrum: 

• Estrogenic Activity: tibolone has estrogenic effects on various tissues in the body, meaning it can mimic the actions of natural estrogen. This helps in relieving symptoms such as hot flashes, night sweats, and vaginal dryness. 
• Progestogenic Activity: tibolone also has progestogenic properties, which means it can counteract the effects of estrogen on the uterine lining (endometrium). This helps reduce the risk of endometrial hyperplasia (excessive growth of the uterine lining) and the potential for uterine cancer in women with an intact uterus who are using tibolone. 
• Androgenic Activity: tibolone has weak androgenic effects, similar to male sex hormones (androgens). This can contribute to increased sexual desire and overall well-being in some women. 
• Bone Health: tibolone positively affects bone density and can help prevent osteoporosis by reducing bone resorption (breakdown).  
• Lipid Profile: tibolone can influence lipid metabolism, leading to a decrease in LDL (low-density lipoprotein) and an increase in HDL (high-density lipoprotein), which can favor cardiovascular health. 
• Brain Function: Some studies suggest that tibolone may have neuroprotective properties, which can benefit cognitive function and mood. 

Drug Interaction

Adverse Reaction

Frequency not defined 

Breast cancer 

Venous thromboembolism 

Bleeding 

Spotting 

Hyperplasia 

Ovarian cancer 

Fluid retention 

Decreased HDL 

Pancreatitis 

Black Box Warning

Black Box Warning: 

None 

Contraindication / Caution

Contraindication/Caution: 

Contraindications: 

• Breast cancer 
• Liver disease 
• Thromboembolic disorders 
• Undiagnosed vaginal bleeding 
• Hypersensitivity 

Cautions: 

• Cardiovascular risk 
• Migraine 
• Endometrial hyperplasia 
• Breast examination 
• Bone health 
• Drug interactions 

Pregnancy / Lactation

Pregnancy consideration:  

Pregnancy Category: D 

Breastfeeding warnings:  

The drug is excreted in breast milk. The effect on lactating infants is not known.  

Pregnancy category: 

Category A: Well-controlled and satisfactory studies show no risk to the fetus in the initial or later trimester. 

Category B: There was no evidence of risk to the fetus in animal studies, and there were not enough studies on pregnant women. 

Category C: There was evidence of risk of adverse effects in animal reproduction studies, and no adequate evidence in human studies must take care of potential risks in pregnant women.    

Category D: adequate data with sufficient evidence of human fetal risk from various platforms, but despite the potential risk, and used only in emergency cases for potential benefits.    

Category X: Drugs listed in this category outweigh the risks over benefits. Hence, these categories of drugs need to be avoided by pregnant women.    

Category N: No data is available for the drug under this category. 

Pharmacology

Pharmacology:  

• tibolone exerts estrogenic effects in some tissues, meaning it can bind to estrogen receptors and mimic the actions of natural estrogen. These estrogenic effects include: 
• Relief of menopausal symptoms: tibolone can alleviate hot flashes, night sweats, vaginal dryness, and other menopausal symptoms by providing estrogen-like activity. 
• Preservation of bone density: tibolone can help maintain bone mineral density and reduce the risk of osteoporosis by promoting bone health. 
• Effects on the urogenital tract: It can support the health of the vaginal lining and improve vaginal lubrication. 

Pharmacodynamics: 

• Progestogenic Activity: tibolone also has progestogenic properties. This means it can counteract the estrogenic effects on the uterine lining (endometrium). This helps reduce the risk of endometrial hyperplasia and uterine cancer in women with an intact uterus who use tibolone as part of hormone replacement therapy (HRT). 
• Androgenic Activity: tibolone has weak androgenic properties, similar to male sex hormones (androgens). This can contribute to increased sexual desire and overall well-being in some women. However, the androgenic effects are generally weaker than the estrogenic effects. 
• Lipid Profile: tibolone can influence lipid metabolism. It has been shown to decrease low-density lipoprotein cholesterol and increase high-density lipoprotein (HDL) cholesterol (often referred to as “good” cholesterol), which can have a favorable impact on cardiovascular health. 
• Liver Metabolism: tibolone is metabolized by the liver, and its metabolites can have varying degrees of estrogenic, progestogenic, and androgenic activity. 

Pharmacokinetics: 

Absorption 

tibolone is typically administered orally in the form of tablets. 

After oral administration, the drug gets rapidly absorbed from the GIT. 

Distribution 

tibolone is highly lipophilic, which means it has an affinity for fat tissues. 

It is extensively bound to plasma proteins, primarily to albumin and sex hormone-binding globulin (SHBG). 

Metabolism 

tibolone undergoes extensive metabolism in the liver. 

It is metabolized into several active and inactive metabolites, including 3α-hydroxy tibolone, 3β-hydroxy tibolone, and δ4-isomer tibolone. 

Elimination and Excretion 

tibolone and its metabolites are primarily excreted in the urine. 

The elimination half-life of tibolone varies between individuals but is approximately 16-31 hours. This means it takes this amount of time for half of the drug to be cleared from the body. 

Adminstartion

Administration: 

tibolone is typically administered orally in the form of tablets.  

tibolone can be taken with or without food, as food intake does not significantly affect it. 

The duration of tibolone treatment can vary. 

Patient Information Leaflet

Patient information leaflet 

Generic Name: tibolone 

Pronounced as: tee-bo-lone 

Why do we use tibolone? 

tibolone is used primarily in hormone replacement therapy (HRT) for postmenopausal women. It is prescribed to address menopausal symptoms and other health concerns. Here are some common reasons why tibolone may be used: 

Relief of Menopausal Symptoms: tibolone is often prescribed to alleviate the uncomfortable symptoms of menopause, which can include hot flashes, night sweats, vaginal dryness, mood swings, and sleep disturbances. tibolone’s estrogenic activity can help reduce these symptoms and improve overall quality of life. 

Prevention of Osteoporosis: tibolone helps maintain bone density and reduces the risk of osteoporosis. This is especially important for postmenopausal women, as estrogen levels decline after menopause, increasing bone loss risk. 

Urogenital Health: tibolone can support the health of the urogenital tract, including the vaginal lining. It can help alleviate vaginal dryness and discomfort, making sexual intercourse more comfortable. 

Libido and Sexual Function: Some women experience declining sexual desire and satisfaction during menopause. tibolone’s weak androgenic properties may improve sexual function and libido in some women. 

Mood and Well-Being: tibolone’s estrogenic and potential neuroprotective effects may positively impact mood and overall well-being in postmenopausal women.