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Tibolone

AEMPS

Synthetic steroid with estrogenic, progestogenic and weak androgenic activity

ATC code: G03CX01

Updated · Methodology

Indications

A

Hot flashes and night sweats

Second line

Reduces the frequency and severity of hot flushes and night sweats. According to Cochrane, tibolone is somewhat less effective than combined estrogen-progestogen MHT for symptom control, but it is convenient as a single tablet: women with an intact uterus need no separate progestogen and take 2.5 mg once daily continuously. In women over 60 it is not recommended because of an increased stroke risk (LIFT trial).

Use only in women at least 12 months after their last menstrual period.

Sources

  1. AEMPS: Ficha técnica de Tibolona (2024)
  2. Cochrane Database Syst Rev: Short-term and long-term effects of tibolone in postmenopausal women. (2016)
  3. Menopause: The 2022 hormone therapy position statement of The North American Menopause Society (2022)

ICD-10: N95.1 · ICD-11: GA30.4

B

Postmenopausal osteoporosis

Second line

Reduces vertebral and non-vertebral fracture risk by 45% and 26% respectively (LIFT). Bone mineral density gains are smaller than with bisphosphonates and denosumab, so tibolone is an alternative in women with climacteric symptoms for whom osteoporosis is a secondary goal. Not the first choice once osteoporosis is the established diagnosis.

Sources

  1. AEMPS: Ficha técnica de Tibolona (2024)

ICD-10: M81.0 · ICD-11: FB83.11

Marketing claims without evidence base

The drug is promoted for these uses outside international guidelines. Each entry below is analyzed against AEMPS, FDA, EMA, Cochrane and major RCTs.

F

Anti-aging and longevity

Not recommended

Tibolone is a synthetic steroid with estrogenic, progestogenic, and weak androgenic activity. It is prescribed for marked vasomotor symptoms of menopause and for postmenopausal osteoporosis prevention in women more than one year after menopause (NAMS 2022, NG23). In anti-aging practice, tibolone is positioned as a universal anti-aging drug for postmenopausal women to rejuvenate skin and libido. In women without marked menopausal symptoms, no clinical studies of prophylactic anti-aging use exist. The LIFT trial (2008) showed increased stroke risk in women over 60 on tibolone. Also: increased breast cancer recurrence (LIBERATE 2009), venous thromboembolism, and gallbladder disease. If tibolone was prescribed for anti-aging, consider seeking a second opinion.

Sources

  1. AEMPS: Ficha técnica de Tibolona (2024)
  2. Cochrane: Antioxidant supplements for prevention of mortality in healthy participants and patients with various diseases (2012)
How to read tiers A–F
  • AStrong evidence – first or second line in international guidelines
  • BRecommended in selected cases
  • CStudy data contradict each other
  • DBenefit not proven, no documented harm
  • FDocumented harm, or risk without benefit

Mechanism of action

Tibolone is metabolized to three active forms: 3α-OH-tibolone and 3β-OH-tibolone act as estrogens on bone and the vulvovaginal mucosa, while the Δ4-isomer carries progestogenic and weak androgenic activity. Tissue-selective action delivers estrogenic effect on bone and vagina without significant stimulation of the endometrium and breast. Effect on hot flashes is comparable to low-dose combined MHT. Evidence rests on the LIBERATE and LIFT trials.

Safety

Contraindications

  • History or suspicion of breast cancer
  • Estrogen-dependent malignancies (endometrial cancer)
  • Undiagnosed vaginal bleeding
  • Active or prior venous thromboembolism
  • Prior arterial thromboembolism (stroke, MI)
  • Severe hepatic disease
  • Pregnancy and lactation
  • Porphyria

Serious adverse effects

  • Ischemic stroke (higher risk in women over 60)
  • Venous thromboembolism
  • Breast cancer with long-term use (lower risk than combined MHT, higher than placebo)
  • Endometrial cancer (risk rises after 5 years)

Common adverse effects

  • Breast tenderness
  • Light vaginal bleeding/spotting in early months
  • Weight gain
  • Vaginal discharge
  • Headache

Pregnancy: can you take Tibolone?

Pregnancy is an absolute contraindication. Stop the drug if pregnancy is suspected.

Breastfeeding: can you take Tibolone?

Breastfeeding is a contraindication. Active metabolites pass into milk and may affect the infant.

Calculate RID

Reference information, not a clinical decision. Discuss feeding pauses or changes with your physician or an IBCLC.

Practical notes

Timing and administration

Take 2.5 mg once daily at the same time, preferably after a meal for better tolerability. The effect on hot flashes develops over 4–8 weeks. Annual review with the physician confirms whether to continue, including breast assessment and blood pressure check.

Common myths

Myth: «tibolone is not really a hormone, it is herbal.» Fact: tibolone is a synthetic steroid and is part of MHT. The same limitations apply as with estrogens: history of breast cancer, hormone-dependent tumors, active venous thromboembolism. Myth: «you can start at any age in menopause.» Fact: the optimal start window is before 60 and within the first 10 years from the last menstrual period; later initiation is linked with extra stroke and cardiovascular risk.
Label mentions8 mentions

Verbatim lines from the interaction sections, in the language of the label

From this drug’s label

  • anticoagulantesclass named in the label
    «Como tibolona puede potenciar la actividad fibrinolítica de la sangre, puede aumentarse el efecto de los anticoagulantes. Por tanto, el uso simultáneo de anticoagulantes y tibolona debería ser…»

    AEMPS, section 4.5 · Open on CIMA

  • anticonceptivos hormonalesclass named in the label
    «Los anticonceptivos hormonales con estrógenos han mostrado disminuir significativamente las concentraciones plasmáticas de lamotrigina cuando se administran conjuntamente debido a la inducción de la…»

    AEMPS, section 4.5 · Open on CIMA

  • barbitúricosclass named in the label
    «Los inductores del CYP3A4 tales como barbitúricos, carbamazepina, hidantoínas y rifampicina pueden potenciar el metabolismo de la tibolona y por tanto, afectar a su efecto terapéutico.»

    AEMPS, section 4.5 · Open on CIMA

  • Carbamazepine
    «Los inductores del CYP3A4 tales como barbitúricos, carbamazepina, hidantoínas y rifampicina pueden potenciar el metabolismo de la tibolona y por tanto, afectar a su efecto terapéutico.»

    AEMPS, section 4.5 · Open on CIMA

  • inductores del CYP3A4class named in the label
    «Los inductores del CYP3A4 tales como barbitúricos, carbamazepina, hidantoínas y rifampicina pueden potenciar el metabolismo de la tibolona y por tanto, afectar a su efecto terapéutico.»

    AEMPS, section 4.5 · Open on CIMA

  • Lamotrigine
    «Los anticonceptivos hormonales con estrógenos han mostrado disminuir significativamente las concentraciones plasmáticas de lamotrigina cuando se administran conjuntamente debido a la inducción de la…»

    AEMPS, section 4.5 · Open on CIMA

  • Rifampicin
    «Los inductores del CYP3A4 tales como barbitúricos, carbamazepina, hidantoínas y rifampicina pueden potenciar el metabolismo de la tibolona y por tanto, afectar a su efecto terapéutico.»

    AEMPS, section 4.5 · Open on CIMA

  • Warfarin
    «Como tibolona puede potenciar la actividad fibrinolítica de la sangre, puede aumentarse el efecto de los anticoagulantes. Por tanto, el uso simultáneo de anticoagulantes y tibolona debería ser…»

    AEMPS, section 4.5 · Open on CIMA

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Frequently asked

What is Tibolone used for?

Tibolone is evaluated for the following indications with varying evidence strength: Hot flashes and night sweats (evidence tier A), Postmenopausal osteoporosis (evidence tier B), Anti-aging and longevity (evidence tier F). See the full indication matrix with dosing and citations above on this page.

What are the side effects of Tibolone?

Common side effects of Tibolone (≥ 1 in 100): Breast tenderness, Light vaginal bleeding/spotting in early months, Weight gain, Vaginal discharge, Headache. See the Safety section for uncommon and serious reactions.

Is Tibolone safe during pregnancy?

Pregnancy is an absolute contraindication. Stop the drug if pregnancy is suspected.

Is Tibolone compatible with breastfeeding?

Breastfeeding is a contraindication. Active metabolites pass into milk and may affect the infant.

Who should not take Tibolone?

Tibolone is contraindicated in: History or suspicion of breast cancer; Estrogen-dependent malignancies (endometrial cancer); Undiagnosed vaginal bleeding; Active or prior venous thromboembolism; Prior arterial thromboembolism (stroke, MI). Full list in the Safety section.

Official sources

Direct links to regulator labels. Open in a new tab.

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