Siterone

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Siterone

Medically reviewed

Marina Burgos

Last updated on 10/01/2026

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 Siterone

Property Description
Active ingredient Cyproterone acetate
Form Tablet (Oral)
Pharmacological class Antiandrogen (with Progestogen activity)
Common use (General) Management of androgen-dependent conditions
Origin Synthetic, Steroidal compound

Defining the Product: Active Ingredient and Type

Siterone is a prescription medicine that contains the single active ingredient Cyproterone acetate. This compound is administered in the standard dosage form of a tablet designed for oral intake. The foundation of this active ingredient is entirely synthetic, placing it in the category of manufactured steroidal compounds.

Chemically, Cyproterone acetate is formally identified as a synthetic steroidal antiandrogen. As a single-ingredient product, Siterone delivers a focused, systemic dose of this agent, which requires a prescription (Rx status) due to its high potency and specific hormonal targets.


Pharmacological Classification: Dual Hormonal Modulator

Cyproterone acetate belongs primarily to the pharmacological class of Antiandrogens, classifying it as a potent hormone antagonist that counteracts the effects of androgens (male sex hormones).

What provides its distinctive therapeutic profile is its dual activity: it also possesses significant secondary progestogen characteristics. This combined hormonal influence confirms its specialized role; Cyproterone acetate's progestational properties are clinically recognized for contributing to its overall effectiveness as a hormone modulator.


General Purpose: Targeted Androgen Suppression

Siterone's fundamental role is the therapeutic management of medical conditions driven by excessive or overactive male hormones, broadly termed androgen-dependent conditions. It achieves this through the primary mechanism of androgen receptor blockade, where the active ingredient occupies the receptor sites, preventing androgens from initiating their effects on target tissues.

This action, combined with a secondary mechanism of reducing the body's overall androgen production through gonadotropin inhibition, leads to a systemic reduction in androgen influence. This targeted suppression is essential for managing conditions where the body requires hormonal stabilization.

What side effects are possible with Siterone?

Possible Side Effects and Safety Information

The regulatory safety profile for Siterone (cyproterone acetate) classifies potential adverse reactions by frequency and the body system affected. These classifications clarify the expected range of effects from very common reactions to rare, serious adverse events.

Frequency-Classified Adverse Reactions

Adverse effects are categorized based on how frequently they are documented in clinical use:

  • Very Common (affecting ge 1 in 10): Headache, fatigue, decreased libido, and reversible effects on fertility in both men (inhibition of spermatogenesis) and women (inhibition of ovulation).
  • Common (affecting ge 1 in 100): Depressed mood, restlessness, weight changes, gynecomastia (in men), and irregular menstruation (in women).
  • Rare to Very Rare: Serious events such as thromboembolic events (blood clots) and severe hypersensitivity reactions are classified in these lower frequency tiers.

Key Safety Constraints

The most significant documented constraint relates to the Hepatobiliary system. The medicine is formally contraindicated for individuals with severe hepatic impairment due to the potential for severe and fatal liver toxicity. Monitoring of liver function is a documented safety necessity.

Additionally, the risk of developing Meningioma is officially associated with prolonged use of cyproterone acetate. Specific caution is also advised for patients with pre-existing conditions like diabetes mellitus and a history of cardiovascular or thrombotic events.

Overdose and Emergency Response

Overdose and when to seek help

The information regarding Siterone (Cyproterone acetate) overdose is derived strictly from official regulatory documentation, such as the Summary of Product Characteristics (SmPC) and approved labeling.

Documented Overdose Profile

Official regulatory sources note that there have been no reports of serious illness following the ingestion of an excessive amount of Cyproterone acetate in a single acute dose. Specific signs or symptom clusters that define an acute overdose beyond this observation are not explicitly detailed in the regulatory texts.

Overdose Component Regulatory Statement
Antidote Availability No specific antidotes are known for Cyproterone acetate.
Management Approach Treatment, if deemed necessary, should be strictly symptomatic and supportive.

When to Seek Help

In the event of a suspected overdose, the regulatory labeling mandates that the patient talk to a doctor or seek medical advice as soon as possible for immediate guidance on necessary procedures. The official guidance emphasizes that management must be symptomatic due to the lack of a known antidote. There are no population-specific considerations (e.g., for pediatric or geriatric patients) mentioned within the official acute overdose documentation.

Therapeutic Uses of Siterone

What Siterone Treats: Main Uses and Benefits

Cyproterone acetate is a prescription therapeutic agent used to manage medical conditions where symptoms are related to systemic imbalance from excessive hormone activity, providing targeted support across several symptom domains. The core uses remain focused on conditions sensitive to hormone influence.

The medicine is considered relevant in the palliative management of advanced prostate carcinoma for men, and in women, it addresses conditions like severe acne, excessive hair growth (hirsutism), pathological oiliness (seborrhoea), and androgenetic scalp hair thinning. Quick Fact: Relief for Symptoms Related to Hormonal Imbalance

For patients with advanced cancer, Siterone provides support relevant for long-term disease management, and is applied in contexts where supportive symptomatic management of disease activity is needed, assisting with specific concerns such as incapacitating hot flushes. Siterone is also commonly used to assist men seeking therapeutic control over an abnormal or significantly heightened sexual urge (hypersexuality), which supports patients in maintaining a sense of stability.

Eligibility and Restrictions for Use

Siterone (cyproterone acetate) is an anti-androgen medication used to treat conditions in men and women that are caused by the effects of male sex hormones (androgens).

Who Can Use Siterone?

  • Men: Primarily for the palliative treatment of advanced prostatic carcinoma (prostate cancer) and for the reduction of drive in sexual deviations (severe hypersexuality) when other interventions are not appropriate.
  • Women: For severe signs of androgenization, such as very severe hirsutism (excessive hair growth), severe androgenic alopecia (scalp hair loss), and severe forms of acne and seborrhea.

Who Cannot Use Siterone? (Contraindications)

Siterone is generally contraindicated (should not be used) for certain patient groups and those with specific pre-existing conditions due to the risk of serious side effects. These include:

  • Pregnancy and Lactation: Must be excluded before starting therapy in women of childbearing age, as it can feminize a male fetus. It is also contraindicated during breastfeeding.
  • Liver Disease: Previous or existing liver tumors (except for metastases from prostate cancer), Dubin-Johnson and Rotor syndromes, or a history of jaundice or persistent itching during a prior pregnancy.
  • Thromboembolic Processes: Patients with a history of or existing blood clots (thromboembolic events).
  • Meningioma: A history of or existing benign brain tumor (meningioma). Treatment must be stopped if a meningioma is diagnosed.
  • Other Conditions: Severe chronic depression, certain wasting diseases (excluding inoperable prostate cancer), and patients who have not yet completed puberty (due to potential for unfavorable influence on growth).

Healthcare professionals will carefully assess the risk-benefit ratio for patients with conditions like severe diabetes with vascular changes or sickle-cell anemia before prescribing Siterone.

What should I know about interactions with other medicines?

Interactions with other medicines and products

The official regulatory interaction profile for Siterone (Cyproterone acetate) is defined primarily by its involvement in the CYP3A4 enzyme system as both a substrate for clearance and a potential inhibitor.


Metabolic Clearance Interactions

Co-administration with strong CYP3A4 inhibitors, such as ketoconazole or ritonavir, is expected to increase the plasma concentration of Cyproterone acetate by inhibiting its metabolism. Conversely, CYP3A4 inducers, including rifampicin, phenytoin, and the herbal product St. John’s Wort, may accelerate Siterone’s clearance, thereby reducing its plasma levels and potentially decreasing its efficacy.


Pharmacodynamic and Risk Interactions

A clinically relevant pharmacodynamic interaction is noted with antidiabetic agents (such as insulin and oral hypoglycemics), where Siterone may officially decrease their therapeutic efficacy. The combination with anticoagulants is documented to carry an increased risk of adverse events due to the drug's activity. Furthermore, co-administration with HMG-CoA Reductase Inhibitors (statins) that are CYP3A4 substrates may increase the risk of statin-associated muscle effects.


Substance and Population Notes

The official label notes that alcohol consumption may reduce the antiandrogenic effect in the indication of hypersexuality. The risk of all interactions is officially heightened in patients with hepatic impairment due to documented slower metabolic clearance.

Mechanism of Action

The drug's mechanism of action involves a dual interference with androgen signaling. Primarily, the molecule acts as a competitive antagonist at the Androgen Receptor (AR) inside target cells. By binding to the AR, the drug blocks natural androgens, such as testosterone, from activating the receptor. This action interrupts androgen-mediated gene transcription, causing a localized reduction in androgenic stimulation of tissues. The secondary mechanism involves the central hormonal system: the molecule functions as an agonist at the Progesterone Receptor (PR), particularly in the pituitary gland. This PR activation triggers a negative feedback signal, leading to the suppression of Luteinizing Hormone (LH) release. The reduction in LH subsequently decreases the biosynthesis and secretion of testosterone by the gonads, resulting in a systemic lowering of circulating androgen levels. This synergistic action—combining peripheral receptor blockade with central hormone supply reduction—determines the drug's overall profile of attenuated androgenic activity across multiple physiological systems.

Dosage and Administration Information

Administration Scope

Siterone (Cyproterone acetate) is primarily administered in the oral tablet form for systemic use, although an intramuscular (IM) injection depot is approved in some regions. Oral tablets must be taken with some liquid after meals to ensure correct administration, and a consistent daily timing is typically advised.


Labeled Dosing and Frequency Patterns

The specific dosing regimen is determined by the clinical scenario, adhering to two primary usage patterns:

  1. Continuous Use (Men): For advanced prostate carcinoma, the high oral dose is typically 200 mg to 300 mg daily, often divided into two or three administrations, and used without interruption. For hypersexuality management, the initial 100 mg daily dose must be followed by a prescribed gradual reduction (tapering) over several weeks to identify and maintain the lowest effective dose.
  2. Cyclic Use (Women): For severe androgen-dependent conditions in women of childbearing age, a 50 mg or 100 mg daily dose is administered on a cyclic regimen, restricted to a 10-day period within the menstrual cycle. This use is mandatory to be combined with a separate progestogen-oestrogen preparation.

Special Procedural Conditions

Guidelines include explicit rules for administration. The medicine is not recommended for use in children and adolescents who have not completed puberty. Furthermore, if a scheduled tablet is missed, instructions state that the missed dose should be omitted entirely; the patient should simply take the next scheduled dose at the designated time, rather than doubling the dose. This defines the strict schedule of intake required.

Recent Clinical Evidence

Research Evidence / Overview of Studies for Siterone

The research landscape for Siterone (Cyproterone acetate) is based on clinical evaluations conducted across different medical fields. The evidence describes group patterns observed in controlled and observational settings, providing context on what outcomes researchers have chosen to measure.


Evidence for Use in Advanced Prostate Carcinoma

Research examining the compound in the context of advanced prostate carcinoma has involved controlled studies, including randomized controlled trials (RCTs) and long-term follow-up analyses. These studies also included comparison arms with other hormonal therapies or surgical interventions.

Studies examined primary outcomes such as overall survival rates and measurements of biomarkers like PSA levels that indicate disease activity. Findings described patterns observed in these survival and progression outcomes, and research also measured patient-reported outcomes describing perceived discomfort or changes in functional imbalance.


Evidence for Androgen-Dependent Skin and Hair Conditions

The compound was studied for its effects in conditions characterized by symptoms of systemic or functional imbalance, such as excessive hair growth (hirsutism), severe acne, and androgenetic scalp hair thinning. This research base includes systematic reviews and randomized controlled trials, often applied in studies examining patient-reported experiences.

Studies monitored clinical grading scores for hirsutism, such as the Ferriman Gallwey scale, and research examined acne lesion counts and severity. Research describes changes measured during the study period for both hormonal markers and clinical symptom scores. Findings described patterns observed in these studies, contributing to understanding symptom patterns in women of reproductive age.


Key Areas of Uncertainty and Research Gaps

The overall evidence quality varies across the studied indications. While a large body of long-term RCTs exists for prostate carcinoma, comparative evidence is lacking or inconsistent against certain other established hormonal treatments. For the androgen-dependent conditions, sample sizes were modest in several trials, and the reliance on combination product data limits insight into the single-ingredient formulation. These limitations highlight what is known and what is still uncertain within the clinical research record.

Key Studies & References Pharmacological treatment of hypersexuality in men: a systematic review of the evidence

Frequently Asked Questions (FAQ)

Common questions about Siterone (FAQ)


Q: Is Siterone considered a hormone therapy?

Siterone's active ingredient, cyproterone acetate, is officially classified as a hormone modulator. This is because it is a synthetic steroidal antiandrogen, meaning it blocks male hormones, but it also has secondary progestogen characteristics. This dual activity gives it a specialized role in hormone management, according to official regulatory classification.


Q: Can Siterone affect liver function?

Yes, according to official warnings, Siterone has the potential for severe and fatal liver toxicity. Because of this risk, the drug is contraindicated (is generally not recommended) for people with severe liver problems. Regular liver function monitoring is a necessary safety check documented in official guidance.


Q: Is it safe to drink alcohol in moderation while taking Siterone?

Official regulatory information notes a potential interaction between Siterone and alcohol. Specifically, alcohol consumption may reduce the intended antiandrogenic effect of the medication when it is used for the management of hypersexuality.


Q: Does having a history of heart issues affect eligibility for Siterone?

Yes, official safety documentation advises specific caution for people with a history of cardiovascular or thrombotic events (blood clots). Siterone is generally contraindicated for those who currently have or have a history of blood clots, due to the documented risk of serious thromboembolic events.


Q: What kind of monitoring or regular tests are usually needed when taking Siterone?

Official product information states that certain monitoring is a necessity during treatment. This includes checks of liver function, adrenocortical function, and red blood cell count.


Q: Is Siterone safe to take if I have diabetes?

Official warnings advise specific caution when the drug is prescribed for people with pre-existing diabetes mellitus. The medication is also noted to potentially decrease the therapeutic efficacy of antidiabetic drugs (like insulin), according to interaction profiles.


Q: Can Siterone affect fertility?

Yes, official safety information states that Siterone commonly causes reversible effects on fertility in both men and women. This includes the inhibition of sperm production in men and the inhibition of ovulation in women. These effects are expected to cease after treatment is stopped.


Q: Is Siterone known to cause changes in mood or emotional state?

Yes, changes to mood are documented in official safety information. Depressed mood and restlessness are listed as common adverse reactions. Fatigue (tiredness) and decreased libido (sex drive) are also very common effects noted in regulatory documents.


Q: Are there different brand names for the medicine Siterone?

The medicine Siterone contains the active ingredient Cyproterone acetate. This compound is manufactured and marketed under various brand names internationally, depending on the regulatory region and the specific product formulation authorized for use.


Q: Is there a generic version of Siterone available?

Yes, in many regions, the active ingredient Cyproterone acetate is available in generic formulations.


Q: What happens if a severe side effect occurs while taking Siterone?

Official patient information advises seeking immediate medical attention if signs of a severe adverse event are noticed (such as signs of liver changes, a blood clot, or a severe allergic reaction). In such cases, the treatment may need to be stopped immediately, as directed by the healthcare professional.


Q: Does Siterone have any known interactions with herbal supplements?

Yes, regulatory documentation explicitly lists the herbal product St. John’s Wort as a known interaction. It is classified as an enzyme inducer that may reduce the efficacy of Siterone by speeding up its breakdown in the body.


Q: What are the official warnings and precautions listed for Siterone?

Official regulatory information includes specific risk warnings and precautions. Key areas of caution relate to the potential for liver toxicity, the risk of thromboembolic events (blood clots), and the need for careful management in people with diabetes mellitus. Additionally, the development of Meningioma (a benign brain tumor) is associated with prolonged use.


Q: Are there specific symptoms that require immediate medical attention while on Siterone?

Symptoms that may indicate a serious event are important to be aware of. These can include signs of a blood clot, such as throbbing pain or swelling in a limb or sudden breathlessness. Symptoms of severe liver problems, such as yellowing of the skin or eyes (jaundice) or pain in the upper abdomen, are also symptoms that warrant immediate medical evaluation.


Q: Is Siterone available in different strengths?

Yes, Siterone tablets are manufactured in different strengths, as indicated in official product documentation. These various strengths are prescribed to accommodate the different dosage requirements for men (high doses for prostate cancer) and women (lower doses for androgen-dependent conditions).


Q: Does Siterone typically cause weight gain or weight loss?

Yes, regulatory information lists weight changes as a common adverse reaction for Siterone. This can manifest as either weight gain or weight loss and is sometimes associated with fluid retention.


Q: Can Siterone be taken long-term for several years?

While some indications may involve long-term treatment, official warnings advise that the risk of developing a Meningioma (a type of benign brain tumor) is associated with prolonged use of the medication, which may involve treatment over multiple years.


Q: Can I stop taking Siterone suddenly, or does it require tapering?

Official dosing patterns indicate that for the management of hypersexuality, a gradual reduction (tapering) of the dose is required. Discontinuation protocols for other indications are not specified and should be handled under professional guidance.


Q: Why is Siterone sometimes prescribed alongside another drug?

Official regulatory documentation states that for the treatment of severe androgen-dependent conditions in women, Siterone is mandatory to be combined with a separate progestogen-oestrogen preparation. It is also used in combination with other hormonal therapies for the treatment of prostate cancer.


Q: How does Siterone impact bone health?

Official drug information indicates a potential for impact on bone health. Osteoporosis, which is the weakening and thinning of the bones, is listed as a possible adverse effect of the medication.


Q: Does Siterone affect sleep patterns?

Yes, regulatory documents list sleep disturbances as an uncommon side effect of Siterone. This is distinct from general tiredness, which is listed as a very common effect.


Q: Is Siterone commonly used in older adults?

The use of Siterone is based on the specific condition being treated. One of the primary indications for men is the palliative treatment of advanced prostatic carcinoma, a condition most frequently managed in the older adult population.


Q: What is the research evidence summary regarding Siterone's long-term use?

Official documents confirm that research includes long-term follow-up analyses, particularly for the prostate carcinoma indication. Regulatory documents also note where long-term comparative data may be inconsistent or lacking for other uses.


Q: Can Siterone cause skin problems or rashes?

Although Siterone is used to treat skin conditions like severe acne, the side effects list includes the potential risk of an allergic reaction. Such a reaction can manifest as a rash on the skin.


Q: How quickly does Siterone typically start working?

The timeline for observed effects varies by indication. Initial feelings of tiredness or loss of energy often occur at first but may lessen after about the third month of treatment. For conditions like severe acne or excessive hair growth, clinical improvement is typically seen after 3 to 6 months of use.


Q: Is the benefit of Siterone seen immediately or over time?

Clinical benefits from Siterone are typically seen over time, rather than immediately. Studies and regulatory guidance indicate that typical improvement for androgen-dependent conditions often occurs after 3 to 6 months of treatment.


Q: Are there any known issues with Siterone for people with kidney problems?

The medication is primarily processed by the liver, but professional monitoring guidelines may include checks of kidney function. This suggests a general need for careful monitoring of overall system health when taking Siterone.


Q: Does Siterone increase or decrease blood pressure?

While official regulatory information does not list blood pressure changes as a common side effect, blood pressure monitoring is included in the routine documented checks associated with Siterone therapy.


Q: Is it true that Siterone can sometimes affect cholesterol levels?

Yes, according to professional monitoring guidelines, the recommended checks for Siterone therapy include a Full Lipid profile test. This monitoring procedure includes the measurement of lipid levels, which suggests that metabolic effects are assessed.


Q: Does Siterone cause long-term side effects that go away after stopping the drug?

Regulatory documents list that Siterone commonly causes reversible effects on fertility in both men and women. Being reversible, these effects should typically cease once the medication is stopped.

How should Siterone be stored and disposed of?

How to Store and Dispose of Siterone

Official regulatory documents define strict requirements for storing and disposing of Siterone (cyproterone acetate).


Storage Requirements

The tablets must be stored in a cool, dry place at a temperature below 30 C (86 F). The medicine must be kept in its original pack until it is needed to maintain stability and should be protected from heat, moisture, and direct light. It is prohibited to store the medicine in environments like the bathroom, and it must be kept from freezing.


Handling and Disposal

The medication must be secured out of the sight and reach of children. Due to its potency, individuals who are pregnant or who may become pregnant should not handle the tablets. Unused or expired Siterone must not be kept and should be returned to a pharmacist or healthcare professional for proper disposal. The product should not be released into the environment, such as drains or wastewater.

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

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