Tibolone

1. Introduction

Tibolone is a synthetic steroid hormone with oestrogenic, progestogenic, and androgenic properties, used primarily in postmenopausal hormone replacement therapy (HRT). It helps alleviate menopausal symptoms and prevent osteoporosis in postmenopausal women.

2. Indications

  • Hormone Replacement Therapy (HRT): Treatment of oestrogen deficiency symptoms in postmenopausal women.
  • Osteoporosis Prevention: In postmenopausal women at high risk of fractures who cannot take other osteoporosis medications.

3. Dosage

Adults (Postmenopausal Women):

  • Standard Dose: 2.5 mg once daily, taken at the same time each day.

Elderly:

  • No dose adjustment required.

Renal Impairment:

  • No dose adjustment required, but use with caution in severe renal impairment.

Hepatic Impairment:

  • Contraindicated in severe liver disease.

4. Administration

  • Take orally, once daily at the same time each day.
  • Can be taken with or without food.
  • If a dose is missed, take it as soon as remembered, unless it’s almost time for the next dose. Do not double dose.

5. Forms Available

  • Tablets: 2.5 mg

6. Side Effects

6.1 Common Side Effects:

  • Weight gain
  • Breast tenderness
  • Abdominal pain
  • Vaginal bleeding or spotting
  • Headache

6.2 Less Common Side Effects:

  • Acne
  • Fluid retention
  • Mood changes

6.3 Rare but Serious Side Effects:

  • Increased risk of breast cancer
  • Increased risk of endometrial hyperplasia or cancer
  • Thromboembolism (DVT, PE)
  • Stroke or cardiovascular events

7. Warnings

  • Breast Cancer Risk: Tibolone slightly increases the risk of breast cancer; avoid in women with a history of hormone-sensitive cancers.
  • Endometrial Cancer Risk: Can stimulate the endometrium; unexplained vaginal bleeding should be investigated.
  • Cardiovascular & Thromboembolic Risks: Increased risk of deep vein thrombosis (DVT), pulmonary embolism (PE), and stroke, especially in older women.
  • Liver Disease: Avoid in women with severe hepatic dysfunction.

8. Precautions

  • Not for use in premenopausal women.
  • Regular mammograms and gynaecological check-ups recommended.
  • Use for the shortest duration necessary to relieve menopausal symptoms.
  • Avoid in women with uncontrolled hypertension or cardiovascular disease.

9. Interactions

  • CYP3A4 Inducers (e.g., rifampin, carbamazepine, phenytoin): May reduce tibolone efficacy.
  • CYP3A4 Inhibitors (e.g., ketoconazole, erythromycin): May increase tibolone levels, enhancing side effects.
  • Anticoagulants (e.g., warfarin): May increase bleeding risk.

10. Monitoring Parameters

  • Blood pressure: Regular monitoring in women with hypertension.
  • Breast cancer screening: Annual mammograms recommended.
  • Endometrial monitoring: Unexplained vaginal bleeding should be evaluated.
  • Liver function: Monitor in women with a history of liver disease.

11. Use in Children

  • Not indicated for use in children or premenopausal women.

12. Use in Pregnancy

  • Contraindicated in pregnancy (Category X).

13. Use in Elderly

  • Safe for use but monitor for cardiovascular risks and breast cancer risk.

14. Use in Kidney Disease

  • No dose adjustment required, but use cautiously in severe renal impairment.

15. Use in Liver Disease

  • Contraindicated in severe liver impairment.

16. Patient Counselling Points

  • Take daily at the same time for the best effect.
  • Report unexplained vaginal bleeding to your doctor.
  • Maintain regular breast and gynaecological exams while on treatment.
  • Stop immediately if signs of a blood clot appear (e.g., leg swelling, chest pain, shortness of breath).
  • Do not use for longer than necessary; review treatment regularly.

17. Table of Brand Names, Manufacturer, and Prices in USD

Brand NameManufacturerStrength/Dosage FormPrice (USD)
LivialOrganon2.5 mg Tablet$50 (30 tablets)
Generic TiboloneVarious2.5 mg Tablet$30 (30 tablets)

18. 15 FAQs (Frequently Asked Questions)

1. What is Tibolone used for?
Tibolone is used for menopausal symptoms and osteoporosis prevention.

2. How does Tibolone work?
It mimics oestrogen, progesterone, and androgens, helping to relieve symptoms of menopause.

3. How long does Tibolone take to work?
Most women experience relief from symptoms within a few weeks, but full effects may take up to 3 months.

4. Can Tibolone cause weight gain?
Yes, weight gain is a common side effect.

5. Can Tibolone cause breast cancer?
It may slightly increase the risk of breast cancer, especially with prolonged use.

6. Can Tibolone be taken long-term?
It should be used for the shortest duration necessary and reviewed regularly.

7. Does Tibolone affect libido?
Yes, it may increase libido due to its androgenic effects.

8. Can Tibolone cause blood clots?
Yes, it increases the risk of deep vein thrombosis (DVT) and stroke.

9. Can Tibolone be taken with food?
Yes, it can be taken with or without food.

10. Can I take Tibolone if I have a uterus?
Yes, but any unexplained vaginal bleeding should be investigated for endometrial hyperplasia.

11. Can Tibolone help with osteoporosis?
Yes, it can prevent osteoporosis in postmenopausal women.

12. Can Tibolone be stopped suddenly?
Yes, but symptoms may return; consult your doctor before stopping.

13. Does Tibolone interact with alcohol?
No significant interaction, but limit alcohol intake to reduce cardiovascular risks.

14. Is Tibolone better than traditional HRT?
Tibolone has lower breast cancer risk than combined HRT but still carries some risks.

15. How should Tibolone be stored?
Store at room temperature, away from moisture and heat.