Tibolone: Uses, Side Effects, Dosage - Drugvu

ℹ️ Compiled from public regulatory records · Last regulator revision: April 10, 2026🚩 Report this page

Tibolone

Other Estrogens

Sold as TIBELLA

GB MHRACA Health Canada

Drug class: Other Estrogens
Availability: See label
Routes: Oral
Markets covered: 2
Products on record: 9

Overview

Tibolone is an active pharmaceutical ingredient in the Other Estrogens group (G03CX). The information below is compiled per regulator from the product labels on record, with direct links to the original documents.

Regulatory status by market

Market	Regulator	Products	Last revision
GB United Kingdom	MHRA	8	April 10, 2026
CA Canada	Health Canada	1	July 2, 2025

GBUnited Kingdom· MHRA

8 products

Uses

GBOfficial regulatory label· revised May 23, 2025[1]

• Treatment of oestrogen deficiency symptoms in postmenopausal women, more than one year after menopause. 1). 8).

How to take

CACanada· Health Canada

1 product

Uses

CAOfficial regulatory label· revised July 2, 2025[2]

Tibella (tibolone) is indicated for short-term treatment of vasomotor symptoms due to estrogen deficiency in postmenopausal women, more than one year after menopause. For all women the decision to prescribe Tibella should be based on an assessment of the individual patient’s overall risks and, particularly in the over 60s, should include consideration of the risk of stroke (see WARNINGS AND PRECAUTIONS and ADVERSE REACTIONS).
After careful selection of users, Tibella should be prescribed for the shortest duration consistent with treatment goals. Review the need for continuation of treatment after 6 months, taking into account the risk-benefit ratio for the individual user at that moment (including cardiovascular disease, endometrial cancer and breast cancer, see ADVERSE REACTIONS and WARNINGS AND PRECAUTIONS).
Tibella should only be continued for as long as the benefit outweighs the risks. Tibella should be prescribed only to women with intact uteri since the medication includes progestogenic activity. 1 Pediatrics Pediatrics (≤ 18 years of age): There is no relevant use of Tibella in the pediatric population.

Sources & citations

[1]MHRA (UK) · PL000250599 · revised May 23, 2025
[2]Health Canada (DPD) · 02488361 · revised July 2, 2025

Information on this page is compiled from public regulatory records. Drugvu is not affiliated with any regulator or pharmaceutical manufacturer. This is not medical advice. Always consult a qualified healthcare professional.

Side effects & warnings

GBOfficial regulatory label· Adverse reactions· revised May 23, 2025[1]

8. After stopping treatment, the excess risk will decrease with time and the time needed to return to baseline depends on the duration of prior HRT use. When HRT was taken for more than 5 years, the risk may persist for 10 years or more.
No data for persistence of risk after stopping are available for tibolone, but a similar pattern cannot be ruled out. Ovarian cancer Ovarian cancer is much rarer than breast cancer. Epidemiological evidence from a large meta-analysis suggests a slightly increased risk in women taking oestrogen-only or combined oestrogen- progestagen HRT, which becomes apparent within 5 years of use and diminishes over time after stopping.
8). In the Million Women Study it was shown that the relative risk for ovarian cancer with use of tibolone was similar to the risk associated with use of other types of HRT. e. deep vein thrombosis or pulmonary embolism. 8). In an epidemiological study using a UK database, the risk of VTE in association with tibolone was lower than the risk associated with conventional HRT, but only a small proportion of women were current users of tibolone and a small increase in risk compared with non-use cannot be excluded.
• Patients with known thrombophilic states have an increased risk of VTE and HRT or tibolone may add to this risk. 3). • Generally recognised risk factors for VTE include use of oestrogens, older age, major surgery, prolonged immobilisation, obesity (BMI > 30 kg/m2), pregnancy/postpartum period, systemic lupus erythematosus (SLE), and cancer.
There is no consensus about the possible role of varicose veins in VTE. As in all postoperative patients, prophylactic measures need to be considered to prevent VTE following surgery. If prolonged immobilisation is to follow elective surgery temporarily stopping HRT or tibolone 4 to 6 weeks earlier is recommended, if possible.
Treatment should not be restarted until the woman is completely mobilised. • In women with no personal history of VTE but with a first degree relative with a history of thrombosis at young age, screening may be offered after careful counselling regarding its limitations (only a proportion of thrombophilic defects are identified by screening).
g, antithrombin, protein S, or protein C deficiencies or a combination of defects) HRT or tibolone is contraindicated. • Women already on anticoagulant treatment require careful consideration of the benefit-risk of use of HRT or tibolone.
• If VTE develops after initiating therapy, the drug should be discontinued. g. painful swelling of a leg, sudden pain in the chest, dyspnea). Coronary artery disease (CAD) There is no evidence from randomised controlled trials of protection against myocardial infarction in women with or without existing CAD who received combined oestrogen-progestogen or oestrogen-only HRT.
In an epidemiological study using the GPRD no evidence was found of protection against myocardial infarction in postmenopausal women who received tibolone. 8). The baseline risk of stroke is strongly age- dependent and so the effect of tibolone is greater with older age.
Other conditions • Patients with rare hereditary problems of galactose intolerance, the Lapp lactase deficiency or glucose-galactose malabsorption should not take this medicine. • Livial is not intended for contraceptive use. 5 mg dose after 2 years).
Total triglycerides and lipoprotein(a) levels were also reduced. The decrease in total cholesterol and VLDL-C levels was not dose-dependent. Levels of LDL-C were unchanged. The clinical implication of these findings is not yet known. • Oestrogens may cause fluid retention, and therefore patients with cardiac or renal dysfunction should be carefully observed.
• Women with pre-existing hypertriglyceridaemia should be followed closely during oestrogen replacement or hormone replacement therapy, since rare cases of large increases of plasma triglycerides leading to pancreatitis have been reported with oestrogen therapy in this condition.
• Treatment with Livial results in a very minor decrease of thyroid binding globulin (TBG) and total T4. Levels of total T3 are unaltered. Livial decreases the level of sex-hormone-binding globulin (SHBG), whereas the levels of corticoid binding globulin (CBG) and circulating cortisol are unaffected.
• HRT does not improve cognitive function. There is some evidence of increased risk of probable dementia in women who start using continuous combined or oestrogen-only HRT after the age of 65. 5 Interaction with other medicinal products and other forms of interaction Since Livial may increase blood fibrinolytic activity, it may enhance the effect of anticoagulants.
This effect has been demonstrated with warfarin. Caution should therefore be exercised during the simultaneous use of Livial and anticoagulants, especially when starting or stopping concurrent Livial treatment. If necessary, the dose of warfarin should be adjusted.
There is limited information regarding pharmacokinetic interactions with tibolone An […]

GBOfficial regulatory label· Warnings and precautions· revised May 23, 2025[1]

For the treatment of postmenopausal symptoms, Livial should only be initiated for symptoms that adversely affect quality of life. In all cases, a careful appraisal of the risks and benefits should be undertaken at least annually and Livial should only be continued as long as the benefit outweighs the risk.
8) for each woman should be carefully assessed, in the light of her individual risk factors and bearing in mind the frequency and characteristics of both cancers and stroke, in terms of their response to treatment, morbidity and mortality.
Evidence regarding the risks associated with HRT or tibolone in the treatment of premature menopause is limited. Due to the low level of absolute risk in younger women, however, the balance of benefits and risks for these women may be more favourable than in older women.
Medical examination/follow-up Before initiating or reinstituting HRT or tibolone, a complete personal and family medical history should be taken. Physical (including pelvic and breast) examination should be guided by this and by the contraindications and warnings for use.
• During treatment, periodic check-ups are recommended of a frequency and nature adapted to the individual woman. Women should be advised what changes in their breasts should be reported to their doctor or nurse (see ‘Breast cancer’ below).
g. mammography, should be carried out in accordance with currently accepted screening practices, modified to the clinical needs of the individual. Conditions which need supervision • If any of the following conditions are present, have occurred previously, and/or have been aggravated during pregnancy or previous hormone treatment, the patient should be closely supervised.
g. g. 8). In these studies risk increased with increasing duration of use. Tibolone increases endometrial wall thickness, as measured by transvaginal ultrasound. 1). Women should be advised to report any break- through bleeding or spotting if it is still present after 6 months of treatment, if it starts beyond that time or if it continues after treatment has been discontinued.
The woman should be referred for gynaecological investigation, which is likely to include endometrial biopsy to exclude endometrial malignancy. 5 mg dose. 8. After stopping treatment, the excess risk will decrease with time and the time needed to return to baseline depends on the duration of prior HRT use.

This is not medical advice. Consult a qualified healthcare professional.

How to take

CAOfficial regulatory label· revised July 2, 2025[2]

1 Dosing Considerations Starting Tibella  Any irregular/unscheduled vaginal bleeding, either on or off Hormone Replacement Therapy (HRT), should be investigated to exclude malignancy before starting Tibella. (see WARNINGS AND PRECAUTIONS)  Women experiencing a natural menopause should commence treatment with Tibella at least 12 months after their last natural bleed.
In case of a surgical menopause, treatment with Tibella may commence immediately. Women being treated with gonadotrophin Serious Warnings and Precautions Tibella may increase the risk of stroke, breast cancer and, in women with an intact uterus, endometrial cancer and can be dependent on individual risk factors (See Clinical Trial Adverse Reactions).
A complete personal and family medical history should be taken before starting treatment with Tibella. Periodic check-ups are recommended while on the treatment. The Women’s Health Initiative (WHI) trial examined the health benefits and risks of oral combined estrogen plus progestin therapy (n=16,608) and oral estrogen -alone therapy (n=10,739) in postmenopausal women aged 50 to 79 years.
2 years compared to those receiving placebo. 8 years compared to those receiving placebo. Therefore, the following should be given serious consideration at the time of prescribing:  Estrogens with or without progestins should not be prescribed for primary or secondary prevention of cardiovascular diseases.
 Estrogens with or without progestins should be prescribed at the lowest effective dose for the approved indication.  Estrogens with or without progestins should be prescribed for the shortest period possible for the approved indication.
TIBELLA (tibolone) Page 6 of 40 releasing hormone (GnRH) analogues, for example, for endometriosis, may commence treatment with Tibella immediately. Switching from a sequential or continuous combined HRT preparation  If changing from a sequential HRT preparation, treatment with Tibella should start the day following completion of the prior regimen.
If changing from a continuo us combined HRT preparation, treatment can start at any time. 5 mg) per day. 5 mg. The tablets should be swallowed whole with some water or other drink, preferably at the same time every day. When a pack is complete, patients should start a new pack the next day without missing any days on the drug.
Tibella may be administered with or without food. A separate progestogen should not be added with Tibella treatment. For initiation and continuation of treatment of postmenopausal symptoms, the lowest effect ive dose for the shortest duration (see WARNINGS AND PRECAUTIONS) should be used.
There is no relevant use of Tibella in the pediatric population; therefore, Health Canada has not authorized an indication for pediatric use. 3 Reconstitution Not applicable. 4 Administration For oral use. 5 Missed Dose A missed dose should be taken as soon as remembered, unless it is more than 12 hours overdue.
In the latter case, the missed dose should be skipped and the next dose s hould be taken at the normal time. Missing a dose may increase the likelihood of breakthrough bleeding and spotting.

This is not medical advice. Consult a qualified healthcare professional.

Side effects & warnings

CAOfficial regulatory label· Adverse reactions· revised July 2, 2025[2]

1 Adverse Reaction Overview See WARNING AND PRECATIONS regarding potential induction of malignant neoplasms and adverse effects similar to those of oral contraceptives. The following adverse reactions have been reported with estrogen/progestin combination in general: Blood and lymphatic system disorders Altered coagulation tests (see Warnings and Precautions, Drug-Laboratory Tests Interactions).
Cardiac disorders Palpitations; increase in blood pressure (see Warnings and Precautions); coronary thrombosis. Endocrine disorders Increased blood sugar levels; decreased glucose tolerance. , retinal thrombosis, optic neuritis); visual disturbances; steepening of the corneal curvature; intolerance to contact lenses.
TIBELLA (tibolone) Page 16 of 40 Gastrointestinal disorders Nausea; vomiting; abdominal discomfort (cramps, pressure, pain, bloating). General disorders and administration site conditions Fatigue; changes in appetite; changes in body weight; change in libido.
Hepatobiliary disorders Gallbladder disorder; asymptomatic impaired liver function; cholestatic jaundice. Musculoskeletal and connective tissue disorders Musculoskeletal pain including leg pain not related to thromboembolic disease (usually transient, lasting 3-6 weeks) may occur.
Nervous system disorders Aggravation of migraine episodes; headaches; dizziness; neuritis. Psychiatric disorders Mental depression; nervousness; irritability. Renal and urinary disorders Cystitis; dysuria; sodium retention; edema. Reproductive system and breast disorders Breakthrough bleeding; spotting; change in menstrual flow; dysmenorrhea; vaginal itching/discharge; dyspareunia; endometrial hyperplasia; pre-menstrual-like syndrome; reactivation of endometriosis; changes in cervical erosion and amount of cervical secretion; breast swelling and tenderness.
Skin and subcutaneous tissue disorders Chloasma or melasma, which may persist when drug is discontinued; erythema multif orme; erythema nodosum; hemorrhagic eruption; loss of scalp hair; hirsutism and acne. Vascular disorders Isolated cases of: thrombophlebitis; thromboembolic disorders.
2 Clinical Trial Adverse Reactions Clinical trials are conducted under very specific conditions. The adverse reaction rates observed in the clinical trials; therefore, may not reflect the rates observed in practice and should not be compared to the rates in the clinical trials of another drug.
Adverse reaction information from clinical trials may be useful in identifying and approximating rates of adverse drug reactions in real-world use. 5 mg) of tibolone and 3476 women receiving placebo. 5 years. Table 2 shows the undesirable effects that occurred statistically significantly more frequently during treatment with tibolone than with placebo.
TIBELLA (tibolone) Page 17 of 40 Table 2:
Common Adverse Reactions System Organ Class Common (≥1/100 to <1/10) Gastrointestinal disorders Lower abdominal pain Skin and subcutaneous tissue disorders Abnormal hair growth Reproductive system and breast disorders Vaginal discharge Endometrial thickening Breast tenderness Genital pruritus Vaginal candidiasis Vaginal hemorrhage* Pelvic pain Cervical dysplasia Genital discharge Vulvovaginitis Investigations Weight increase Abnormal cervical smear * Bleeding that happens at least 12 months after periods have stopped.
Breast cancer An up to 2-fold increased risk of having breast cancer diagnosed is reported in women taking combined estrogen-progestogen therapy for more than 5 years. Any increased risk in users of estrogen-only and tibolone therapies is substantially lower than seen in users of estrogen-progestogen combinations.
The level of risk is dependent on the duration of use. Results of the largest epidemiological study (Million Women Study) are presented. 3 3 (0-6) a: Taken from baseline incidence rates in developed countries b: Overall risk ratio. The risk ratio is not constant but will increase with increasing durat ion of use Endometrial cancer risk Postmenopausal women with a uterus The endometrial cancer risk is about 5 in every 1000 women with a uterus not using HRT or tibolone.
The randomised placebo-controlled trial that included women who had not been screened for endometrial abnormalities at baseline, and therefore reflected clinical practice, identified the highest risk of endometrial cancer (LIFT study, mean age 68 years).
9 years compared with 4 cases of endometrial cancer in the tibolone group (n=1,746). 8 additional case of endometrial cancer in every 1000 women who used tibolone for one year in this study. Ovarian cancer Use of estrogen-only or combined estrogen-progestogen HRT has been associated with a slightly increased risk of having ovarian cancer diagnosed.
56). For women aged 50 to 54 years taking 5 years of HRT, this results in about 1 […]

CAOfficial regulatory label· Warnings and precautions· revised July 2, 2025[2]

Please see the Serious Warnings and Precautions Box at the beginning of Part I:
Health Professional Information. General For the treatment of postmenopausal symptoms, Tibella should only be initiated for symptoms that adversely affect quality of life. In all cases, a careful appraisal of the risks and benefits should be undertaken at least annually and Tibella should only be continued as long as the benefit outweighs the risk.
The risks of stroke, breast cancer and, in women with an intact uterus, endometrial cancer for each woman should be carefully assessed, in the light of her individual risk factors and bearing in mind the frequency and characteristics of both cancers and stroke, in terms of their respon se to treatment, morbidity and mortality.
Evidence regarding the risks associated with HRT or tibolone in the treatment of premature menopause is limited. Due to the low level of absolute risk in younger women, however, the balance of benefits and risks for these women may be more favorable than in older women.
Tibella is not intended for contraceptive use. Conditions which need supervision If any of the following conditions are present, have occurred previously, and/or have been aggravated during pregnancy or previous hormone treatment, the patient should be closely supervised.
g. g. 5 mg Ascorbyl palmitate, lactose monohydrate, magnesium stearate, mannitol, and potato starch. TIBELLA (tibolone) Page 8 of 40  Systemic lupus erythematosus  A history of endometrial hyperplasia (see below)  Epilepsy  Asthma  Otosclerosis Reasons for immediate withdrawal of therapy: Therapy should be discontinued in case a contra-indication is discovered and in the following situations:  Jaundice or deterioration in liver function  Significant increase in blood pressure  New onset of migraine-type headache  Pregnancy Carcinogenesis and Mutagenesis (also see ADVERSE REACTIONS) Endometrial hyperplasia and carcinoma The available data from randomised controlled trials are conflicting, however, observational studies have consistently shown that women who are prescribed Tibella in normal clinical practice are at an increased risk of having endometrial cancer diagnosed.
In these studies, risk increased with increasing duration of use. Tibolone increases endometrial wall thickness, as measured by transvaginal ultrasound. Break-through bleeding and spotting may occur during the first months of treatment.

This is not medical advice. Consult a qualified healthcare professional.