TIBOFEM

• Brand Name: TIBOFEM

• Generic Name: Tibolone

• Therapeutic Class: Synthetic Steroid with estrogenic, progestogenic, and androgenic activity

• Presentation: 2.5 mg film-coated tablets

2. Composition

• Active Ingredient: Tibolone 2.5 mg

• Excipients:

  • Lactose monohydrate

  • Maize starch

  • Magnesium stearate

  • Hypromellose

3. Mechanism of Action

Tibolone is metabolized into 3 active compounds:

1. Δ4-isomer (progestogenic/androgenic effects)

2. 3α-OH & 3β-OH metabolites (estrogenic effects)

Key Effects: ✔ Relieves menopausal symptoms (hot flashes, vaginal dryness) ✔ Prevents bone loss (osteoporosis) ✔ Endometrial protection (no need for additional progestogen) ✔ Improves libido (mild androgenic activity)

4. Dosage & Administration

• Standard Dose: 2.5 mg once daily (oral)

• Initiation: Start at least 12 months after last menstrual period

• Missed Dose: Take as soon as remembered (skip if next dose is due)

• Administration: Can be taken with/without food

5. Indications

✅ Postmenopausal symptom relief (vasomotor, urogenital) ✅ Prevention of osteoporosis in high-risk women ✅ Libido enhancement in postmenopausal women

6. Storage & Stability

• Temperature: Below 30°C

• Humidity: Keep in original packaging

• Shelf Life: 3 years

• Protection: Avoid moisture

7. Key Recommendations

✔ Not for perimenopausal women (wait ≥1 year after last period) ✔ Monitor breast health annually (mammography as needed) ✔ Assess venous thromboembolism risk before prescribing ✔ Consider non-hormonal alternatives for women with CVD risk

8. Important Safety Notes

⚠ Contraindications: ❌ Active/past hormone-dependent cancers ❌ Undiagnosed vaginal bleeding ❌ History of venous thromboembolism ❌ Severe hepatic disease

⚠ Adverse Effects:

• Common: Headache, vaginal bleeding, weight gain

• Serious:

  • Increased risk of stroke in women >60 years

  • Possible breast cancer risk (similar to other HRT)

⚠ Drug Interactions:

• Strong CYP3A4 inducers (e.g., rifampicin) → reduced efficacy

• Anticoagulants → may require dose adjustment

9. Comparison with Traditional HRT

10. Patient Counseling

✔ Take at the same time daily for consistent effects ✔ Report unusual vaginal bleeding immediately ✔ Attend regular breast/gynecological check-ups ✔ Combine with calcium/vitamin D for bone health

Conclusion

TIBOFEM offers unique tissue-selective benefits for postmenopausal women, combining symptom relief, bone protection, and libido support in a single tablet. However, it requires careful patient selection and monitoring due to potential risks.