Climafen

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Medically reviewed

Rosario Oropesa

Last updated on 22/12/2025

This page provides general, reference-level information compiled from official medical sources. It is not a substitute for professional medical advice, diagnosis, or treatment. For decisions about your health, please consult a qualified healthcare professional.

Overview of Climafen

Climafen: Classification and Composition of the Synthetic Steroid Tibolone

Property Description
Active ingredient Tibolone (INN)
Form Oral Tablet
Pharmacological class Selective Tissue Estrogenic Activity Regulator (STEAR)
General purpose Hormonal support in postmenopausal women
Origin Synthetic steroidal agent

Climafen is a prescription medicinal product whose single active ingredient is Tibolone (INN: Tibolonum). This unique compound is chemically classified as a synthetic steroidal agent and belongs to the pharmacological group known as a Selective Tissue Estrogenic Activity Regulator (STEAR). Tibolone is designed for systemic action and is manufactured as an oral tablet. This identity as a single-component agent provides hormonal support via a selective mechanism that is recognized for its use in managing postmenopausal changes.

The drug's formulation is defined by its monotherapy status, containing only the active Tibolone component. This differs from many conventional Hormone Replacement Therapy (HRT) regimens which often necessitate the combined or sequential use of separate estrogen and progestogen compounds. Tibolone is metabolized in the body, where its active compounds collectively exhibit properties that offer protection and structural maintenance in target tissues. This tissue-selective action is a primary differentiator compared to non-selective estrogen therapies.

What is the General Purpose of Climafen (Tibolone)?

The general purpose of Climafen is to provide hormonal support and stabilization for postmenopausal women managing the physiological consequences of declining endogenous hormone levels. Its pharmacological activity as a STEAR is specifically engineered to replace estrogenic benefits where needed, such as in maintaining the density and integrity of the skeletal structure. It is designed to help reduce the risk of non-vertebral fractures.

A typical application involves providing essential hormonal stabilization to help women maintain their mobility and avoid age-related bone fragility. This tissue-selective action is crucial as it enables the medication to stabilize hormone-sensitive systems vulnerable to deficiency, contributing to the overall general therapeutic context of restoring well-being and maintaining structural functions.

What side effects are possible with Climafen?

Possible Side Effects and Safety Information for Climafen (Tibolone)

The official safety profile of Climafen is structured by regulatory authorities (such as the EMA and FDA) to classify potential adverse reactions based on their frequency and the body system affected.

Frequency-Classified Adverse Reactions

Adverse reactions are grouped by frequency, based on clinical trial data and regulatory standards. Common effects, which may affect up to 10 users in 100, include irregular vaginal bleeding or spotting, weight gain, abdominal pain, and breast discomfort. Other common effects involve the skin, such as acne and unnatural hair growth (hirsutism). Reactions classified as uncommon include general rash or pruritus (itching).


Serious Adverse Reaction Risks

Regulatory documents emphasize the risk of serious, clinically significant conditions associated with the use of Tibolone. These risks include an increased incidence of Venous Thromboembolism (VTE), such as Deep Vein Thrombosis and Pulmonary Embolism, and arterial thromboembolic events, including Stroke and Myocardial Infarction. An increased risk of certain hormone-sensitive malignancies, specifically Endometrial cancer and Breast cancer, is also documented.


Safety Constraints and Time-Related Patterns

The safety profile includes specific constraints related to exposure and duration. The risk of Endometrial cancer increases with the duration of use. The elevated risk of Stroke has been mainly observed in postmenopausal women over 60 years of age at the start of treatment. Furthermore, the risk of VTE is noted to be highest during the first year of use. The medication is generally constrained in individuals with known severe hepatic dysfunction or a history of thromboembolic disorder.

Overdose and Emergency Response

Climafen Overdose and when to seek help

The official regulatory profile for Climafen (Tibolone) indicates that acute overexposure is expected to be of low toxicity. The clinical manifestations associated with taking an amount higher than the recommended dose are documented as gastrointestinal disturbance, including nausea and vomiting, and reports of unscheduled vaginal bleeding. Treatment is officially designated as symptomatic and supportive treatment, as no specific antidote is known for the compound.

Feature Regulatory Description
Manifestations Gastrointestinal disturbance; Unscheduled vaginal bleeding.
Toxicity Classification Expected to be of low acute toxicity.
Antidote Status No specific antidote is known.
Monitoring Hospital monitoring may be required.

When Urgent Medical Help Must Be Sought Immediate medical attention must be sought for any suspected overdose event. Individuals who experience severe clinical manifestations, such as a loss of consciousness or any form of respiratory distress, are required to contact emergency services immediately. The necessary care involves general supportive measures provided under medical supervision until the clinical signs of overexposure fully resolve. This regulatory profile establishes the required response based solely on documented risk and management protocols.

Therapeutic Uses of Climafen

What Climafen Treats: Main Uses and Benefits

Climafen is commonly used to help with symptoms related to systemic imbalance in postmenopausal women, specifically in areas where short-term symptom management is appropriate. This includes: managing hot flushes and night sweats, easing symptoms related to vaginal dryness and dyspareunia, and providing support for low mood and fatigue.

A relevant therapeutic application is applied in addressing conditions involving systemic discomfort (the risk of bone loss and subsequent fragility). In women identified as being at high risk of a fracture, it is used in contexts characterized by periods of heightened symptoms related to low bone mineral density. By addressing these clusters, Climafen contributes to improved comfort during periods of heightened symptoms, assists with maintaining functional stability, and is a supportive option applied when symptoms become temporarily overwhelming.


Quick Fact: Management of Hot Flushes

Quick Fact: Management of Hot Flushes and Night Sweats is an area of use, helping patients cope more steadily with symptom fluctuations.

Eligibility and Restrictions for Use

Population Eligibility for Climafen (Tibolone)

Climafen is exclusively authorized for use in postmenopausal women and must only be initiated a minimum of one year after the last natural menstrual period. Women who have undergone surgical menopause may begin treatment immediately, provided all other eligibility criteria are met. There is no relevant use documented for pediatric or adolescent patients.

Absolute Contraindications (Must Not Use)

Use of Climafen is strictly contraindicated in patients with the following conditions, as defined by regulatory authorities:

  • Known or suspected breast cancer or other oestrogen-dependent malignant tumours.
  • Active or previous venous or arterial thromboembolic disease (e.g., DVT, stroke, heart attack, TIA) or certain thrombophilic disorders.
  • Undiagnosed vaginal bleeding or untreated endometrial hyperplasia.
  • Acute liver disease or a history of liver disease with abnormal function tests, or Porphyria.
  • The medicine is strictly contraindicated during pregnancy and lactation.

Conditional Use and Supervision

Treatment requires close medical supervision in the presence of certain conditions that may recur or worsen, including hypertension, diabetes mellitus, leiomyoma (uterine fibroids), and endometriosis. Regulatory documents note limited experience in treating women over 65 years of age.

What should I know about interactions with other medicines?

Interactions with other medicines and products

The regulatory information for Climafen (Tibolone) establishes specific interaction patterns with several medicinal products and substances. These officially documented interactions fall primarily into two categories: pharmacokinetic (metabolism-related) and pharmacodynamic (effect-related) interactions, which dictate constraints on co-administration.

Documented Interacting Substances and Classes

The interacting drug classes include Oral Anticoagulants, CYP3A4 Inducers, CYP3A4 Inhibitors, and certain hormonal agents such as Aromatase Inhibitors. Specific interacting medicines explicitly listed in regulatory guidance include Warfarin and Acenocoumarol, the anti-epileptics Phenytoin and Carbamazepine, and the anti-tuberculosis medicine Rifampicin.

Official Interaction Statements and Restrictions

  • Co-administration with Oral Anticoagulants is officially documented as a pharmacodynamic interaction that enhances the anticoagulant effect, requiring the close monitoring of coagulation status upon initiation or cessation of Climafen.
  • CYP3A4 Inducers (e.g., Rifampicin, Carbamazepine) cause a pharmacokinetic interaction that significantly decreases the plasma concentration of Tibolone's active metabolites, potentially resulting in a reduced therapeutic effect. Strong CYP3A4 Inhibitors are noted to theoretically increase exposure.
  • The herbal product St. John's Wort (Hypericum perforatum) is also officially cited as a potent inducer of CYP3A4 metabolism that may stop Climafen from working as well.
  • The co-administration of Climafen with Aromatase Inhibitors or a separate progestogen is consistently advised to be avoided in official prescribing information.

Mechanism of Action

Climafen, a non-steroidal compound, functions as a Selective Estrogen Receptor Modulator (SERM). Its primary biological targets are estrogen receptors (ERs), predominantly in the hypothalamus, but also in the pituitary gland, ovary, endometrium, and cervix. Climafen acts as a competitive inhibitor/partial agonist at these receptors.

In the hypothalamus, Climafen occupies ERs, preventing the binding of endogenous estradiol. This interaction results in an anti-estrogenic effect in this specific tissue. This receptor occupancy leads to a disruption of the normal estrogenic negative feedback inhibition on the hypothalamic-pituitary-gonadal (HPG) axis.

The central consequence is a molecular signal interpreted as systemic estrogen deficiency. This modified feedback loop initiates an upstream cascade resulting in increased pulsatile release of gonadotropin-releasing hormone (GnRH) from the hypothalamus. Subsequently, the pituitary gland increases the secretion of both luteinizing hormone (LH) and follicle-stimulating hormone (FSH) into the systemic circulation.

This elevated downstream cascade of gonadotropins modulates ovarian follicular development and steroidogenesis, representing a system-level physiological consequence of modified neuroendocrine signaling.

Dosage and Administration Information

Standard Administration Overview for Climafen (Tibolone)

Climafen is a medicinal product available as a 2.5 mg oral tablet, defining its exclusive route and form of use.


Administration Scope

The established regimen is a fixed, continuous dose:

Instruction Detail
Route of administration Oral use (swallowed)
Dosing schedule One 2.5 mg tablet per day
Timing in relation to meals May be taken with or without food
Preparation requirements Tablet must be swallowed whole with liquid
Age-group rules No dose adjustment is necessary for the elderly

Procedural and Scheduling Rules

Treatment follows a consistent, once-daily pattern that should be taken preferably at the same time every day.

The initiation of treatment for women experiencing natural menopause is structured so that use commences only at least 12 months after the last natural menstrual bleed. When starting Climafen, a separate progestogen should not be added to the regimen.

In the event of a missed dose, the standard protocol includes a 12-hour window: the dose should be taken if remembered within 12 hours of the usual time. If more than 12 hours have passed, the missed dose is typically skipped, and the regular schedule resumed with the next tablet at the normal time. Missing a dose may increase the likelihood of unexpected bleeding or spotting.

Recent Clinical Evidence

Research Evidence / Overview of Studies for Climafen


Evidence for Use in Managing Vasomotor Symptoms

Research was studied for how the frequency and intensity of hot flashes and night sweats were measured in randomized controlled trials (RCTs) and subsequent meta-analyses. These symptoms fall under outcomes related to physical discomfort. The findings describe patterns observed in the studies where measured changes in symptom severity were monitored over the initial treatment period. Research highlights how symptoms evolved in the observed populations. What remains uncertain is the long-term persistence of any reported symptomatic changes, as follow-up durations were limited in many trials.


Evidence for Use in Supporting Bone Health and Skeletal Structure

Research was studied for how changes in bone mineral density (BMD) and fracture incidence were monitored. Studies include intermediate-term RCTs that measured BMD at sites like the spine and hip. The populations observed in these studies included women in early postmenopausal status as well as older women presenting with conditions associated with bone fragility. The data show patterns related to measured changes in bone density over approximately two years. There is limited information for long-term outcomes regarding the absolute rate of fractures, as many early trials focused primarily on density changes.


Evidence for Use in Addressing Urogenital and Sexual Function Symptoms

Research was evaluated in women symptomatic for outcomes linked to inflammatory or irritative states in the urogenital area. Researchers explored patient-reported outcomes describing perceived discomfort, such as vaginal dryness and pain during intercourse (dyspareunia). The studies report how symptoms evolved in the observed populations, but findings related to specific psychological components of sexual function (like libido) were mixed across different trials. Sample sizes were modest in some trials, and there is limited information for long-term outcomes regarding the durability of these observations.

Key Studies & References

  1. Effect of Tibolone on Bone Mineral Density in Postmenopausal Women: Systematic Review and Meta-Analysis

Frequently Asked Questions (FAQ)

Common questions about Climafen (FAQ)

Q: Is Climafen the same type of medication as other common treatments for this condition?

A: Official documents describe Climafen (Tibolone) as a Selective Tissue Estrogenic Activity Regulator (STEAR). This classification means it is chemically different from conventional Hormone Replacement Therapy (HRT), which often involves a combination of separate estrogen and progestogen compounds. Despite this difference in composition, its overall effects and benefits are described as similar to those of combined HRT.

Q: How quickly does Climafen typically start working?

A: While individual response times vary, official patient information describes an initial period of adjustment. During this time, which may last during the first 3 to 6 months of taking the medication, you may experience common side effects like irregular bleeding or spotting.

Q: How long does the effect of one dose of Climafen last?

A: Climafen is prescribed as a once-daily tablet, which is designed to provide continuous support over a 24-hour period. Regulatory documents detailing the medication’s metabolism note that the half-life of its active components is approximately 45 hours, which relates to how long the substance remains active in the body.

Q: Do the side effects of Climafen usually go away over time?

A: Patient information provided by official health bodies indicates that side effects often improve as the body adjusts to the medication. For example, some common effects such as breast tenderness may improve after 4 to 6 weeks, and vaginal bleeding or spotting may improve after one or two months of use.

Q: Is it normal to feel tired or dizzy after starting Climafen?

A: Dizziness and tiredness (fatigue) are effects that have been reported by some women taking Climafen. However, official safety classification indicates these are not among the most common adverse reactions. If these or other effects are experienced, regulatory documents advise consulting a healthcare professional.

Q: Can Climafen cause weight changes?

A: Regulatory documents classify weight gain as a common side effect of Climafen. This means that weight gain may be experienced by up to 10 out of every 100 users.

Q: What should I do if a rash develops while using Climafen?

A: A rash is classified as an uncommon side effect of Climafen. Regulatory safety instructions indicate that signs of a serious allergic reaction, such as a rash accompanied by swelling or difficulty breathing, should be brought to the attention of a healthcare professional immediately.

Q: Does Climafen affect sleep patterns?

A: Research has been conducted on the effect of Climafen on sleep quality in postmenopausal women. Research findings have suggested associations between the medication and the relief of insomnia, potentially leading to observed improvements in sleep patterns in some studies.

Q: Can Climafen affect my ability to drive or operate machinery?

A: Climafen has been associated with certain side effects, such as dizziness and headache, which may affect attention and coordination. Official product information describes these potential effects, which may affect a patient’s ability to drive or operate machinery.

Q: Are there any known interactions between Climafen and birth control pills?

A: Regulatory guidance advises that Climafen should not be used as a form of birth control to prevent pregnancy. Furthermore, co-administration of Climafen with other hormonal agents, such as a separate progestogen, is generally advised to be avoided.

Q: What information is available about Climafen's use in pediatric populations?

A: Regulatory documents are clear that there is no relevant use documented or authorized for Climafen in pediatric or adolescent patients. The medication is exclusively authorized for use in postmenopausal women.

Q: How long after stopping Climafen does the drug stay in the system?

A: The elimination half-life of the active components of Climafen is described in regulatory documents as approximately 45 hours. This documented half-life is a key component of the pharmacokinetic data that determines how long the substance remains active in the body.

Q: Can I take Climafen with a daily multivitamin?

A: While regulatory documents on interactions do not specifically list multivitamins, official guidance indicates that dietary and herbal supplements are generally not tested in the same manner as prescription medicines for their effect on Climafen. For any supplements or vitamins being taken, reviewing this with a healthcare provider is generally recommended.

Q: Does Climafen have a generic version available?

A: Yes, the active ingredient in Climafen is Tibolone. Tibolone is the international non-proprietary name (INN), which is the official generic name for the substance. Climafen is one of several brand names used for medications containing Tibolone.

Q: What are the symptoms of an overdose of Climafen?

A: The official safety documentation for Climafen states that in case of swallowing too much of the medication, you should not induce vomiting and should immediately seek medical attention. The primary instruction from safety documentation is to immediately seek medical attention in such an event.

Q: How does Climafen affect blood sugar levels?

A: Official documents note that diabetes mellitus is a condition requiring close medical supervision when using Climafen. Because of this association, patients with diabetes are noted in official documents as requiring close medical supervision.

Q: Can I stop taking Climafen suddenly?

A: Patient information advises that stopping Climafen should be done in consultation with a doctor or pharmacist. This is the standard official guidance for discontinuing the medication.

How should Climafen be stored and disposed of?

Official Storage and Disposal Requirements

Climafen (Tibolone) tablets must be stored according to specific environmental conditions to maintain stability, as required by regulatory labeling. The medicine should be kept out of the sight and reach of children.


Storage Conditions

Requirement Description
Temperature Store below 30 C.
Protection Protect from moisture and store in the original package.
Handling Do not remove the tablet from the blister until the dose is required.

Disposal Instructions

Unused or expired Climafen must be disposed of in accordance with local requirements. The medicine should not be thrown away via wastewater or standard household waste to prevent environmental contamination.

Attention! Always consult to a doctor or pharmacist before using pills or medicines.

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