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What are the active ingredients in Anterone?

4 min read

Over 50% of prostate cancers are androgen-dependent, making antiandrogens a crucial treatment option. This article details what are the active ingredients in Anterone, exploring how this medication uses its primary compound to treat conditions like prostate cancer and severe androgenisation in women.

Quick Summary

Anterone's main active component is cyproterone acetate, a powerful antiandrogen that blocks male sex hormones to treat conditions like prostate cancer and excessive androgen-related symptoms in women, such as hirsutism.

Key Points

  • Single Active Ingredient: The only active component in Anterone is cyproterone acetate.

  • Antiandrogenic Action: Cyproterone acetate works by blocking androgen receptors and suppressing androgen production, reducing the effects of male sex hormones.

  • Diverse Applications: Anterone is used to treat prostate cancer in men and severe androgenisation symptoms, such as hirsutism and acne, in women.

  • Potential for Serious Side Effects: Long-term, high-dose use carries risks like liver toxicity and an increased risk of meningioma, a benign brain tumour.

  • Strict Medical Supervision: Due to significant side effect risks and interactions, Anterone requires regular monitoring and should only be used under a doctor's care.

  • Inactive Ingredients: Anterone tablets also contain inactive ingredients such as lactose monohydrate, maize starch, and povidone.

In This Article

Anterone is a brand-name medication that relies on a single, potent active compound to exert its therapeutic effects: cyproterone acetate. This steroidal antiandrogen is used to manage a variety of androgen-related conditions in both men and women. Understanding its mechanism of action, specific uses, and associated risks is crucial for anyone considering or undergoing treatment with this medication.

The Active Ingredient: Cyproterone Acetate

Cyproterone acetate is a synthetic steroidal antiandrogen with distinct hormonal properties. As the sole active ingredient in Anterone tablets, its function is central to the medication's purpose. The primary role of this compound is to counteract the effects of androgens, which are male sex hormones that are also produced in smaller amounts in females. By doing so, it can help manage conditions where an excess of, or sensitivity to, these hormones is a problem.

How Cyproterone Acetate Works

Cyproterone acetate employs a dual-action mechanism to combat the effects of androgens. This is what makes it so effective for its varied indications:

  • Androgen Receptor Blockade: The compound directly competes with natural androgens, such as testosterone and its more potent metabolite, dihydrotestosterone, for binding to androgen receptors in target tissues. By occupying these receptors, it prevents androgens from initiating cellular activity and promoting the growth of androgen-dependent cells.
  • Suppression of Gonadotropin Production: Cyproterone acetate also possesses progestational properties. This means it acts on the hypothalamic-pituitary axis, exerting a negative feedback effect that reduces the release of gonadotropins. This, in turn, diminishes the production of testosterone by the testes.

Indications and Uses

Anterone's use varies depending on the patient's sex and the specific condition being treated. For both men and women, it is a prescription-only medication.

For Men

  • Prostate Cancer: For men with inoperable prostate carcinoma, cyproterone acetate is used as an antiandrogen treatment. Some types of prostate cancer are androgen-dependent, and by blocking these hormones, Anterone can help slow or stop the cancer's growth. It can also be used to manage side effects like hot flushes that can occur during other hormonal therapies.
  • Reduction of Sex Drive: In cases of sexual deviations, Anterone is used to reduce sex drive. It is most effective when used alongside psychotherapeutic or sociotherapeutic measures.

For Women

  • Signs of Androgenisation: Anterone is prescribed to women suffering from severe symptoms of androgenisation, which may include:
    • Moderately severe to severe hirsutism (excessive hairiness)
    • Androgenic alopecia (hair loss from the scalp)
    • Severe forms of acne and seborrhoea (oily skin)

Inactive Ingredients and Formulations

In addition to the active ingredient, Anterone tablets contain several inactive components that aid in its formulation and stability. It is essential for individuals with allergies or specific intolerances to be aware of these inactive ingredients, as they can differ between brands. For example, Anterone 50 tablets are known to contain:

  • Lactose monohydrate
  • Starch-maize
  • Povidone
  • Magnesium stearate
  • Silica-colloidal anhydrous
  • Starch-pregelatinised maize

Important Considerations and Risks

Before starting treatment with Anterone, a doctor will perform a thorough assessment to determine if the benefits outweigh the risks. Regular monitoring may be necessary, especially for long-term use.

Potential Side Effects

Common and serious side effects have been reported with Anterone use. Some of the most frequently observed effects include:

  • Decreased Libido and Impotence: Particularly in men, this is an expected effect of the medication.
  • Tiredness and Fatigue: Can impair concentration and the ability to operate machinery.
  • Liver Toxicity: In rare cases, severe liver damage, including hepatitis and liver tumours, has been reported, especially with high doses.
  • Meningioma: A link has been established between long-term use (years) of cyproterone acetate at doses of 25 mg/day and above and the development of meningiomas, which are typically benign brain tumours.
  • Thromboembolic Events: An increased risk of blood clots has been reported, especially in patients with pre-existing risk factors.

Contraindications

Anterone should not be used in individuals with:

  • Liver disease or previous liver tumours (unless prostate cancer related)
  • Certain inherited syndromes, such as Dubin-Johnson or Rotor syndrome
  • Severe chronic depression
  • A history of thromboembolic processes
  • Severe diabetes with vascular changes
  • Pregnancy (due to risk of feminisation of male foetuses)

Comparison of Antiandrogen Medications

Cyproterone acetate is just one of several antiandrogen options available. Other medications may be used depending on the specific condition and patient profile. Here is a comparison of Anterone with other common antiandrogens mentioned in pharmacological contexts.

Feature Anterone (Cyproterone Acetate) Abiraterone Acetate (Zytiga) Bicalutamide (Casodex)
Mechanism Dual action: Blocks androgen receptors and suppresses gonadotropin release. Inhibits an enzyme (CYP17) needed to produce androgens. Primarily blocks androgen receptors.
Primary Use (Men) Inoperable prostate cancer, reduction of sex drive. A specific type of metastatic prostate cancer. Prostate cancer.
Primary Use (Women) Severe androgenisation symptoms like hirsutism and acne. Not indicated for women. Not indicated for women.
Important Side Effects Liver toxicity, meningioma risk (long-term, high dose), reduced libido. Increased blood pressure, hypokalemia, fluid retention, liver enzyme elevations. Gynaecomastia, hot flushes, liver enzyme changes.
Route of Administration Oral tablet. Oral tablet, usually with prednisone. Oral tablet.

Conclusion

In summary, the sole active ingredient in Anterone is cyproterone acetate, a synthetic steroid with powerful antiandrogen effects. It acts by both blocking androgen receptors and suppressing hormone production, making it effective for treating androgen-dependent conditions in both men and women. While it can be highly beneficial for conditions like prostate cancer, hirsutism, and severe acne, it is crucial to be aware of its potential side effects, including liver toxicity and the risk of meningioma with long-term, high-dose use. Treatment with Anterone should always be under the strict supervision of a medical professional, who will weigh the benefits against the risks and monitor the patient for any adverse effects.

Disclaimer: This information is for educational purposes only and should not replace advice from a qualified healthcare provider. Always consult a doctor or pharmacist for any medical concerns.

For more detailed product information, you can consult a consumer medicine information leaflet provided by health organizations like NPS MedicineWise: Anterone 50.

Frequently Asked Questions

Cyproterone acetate, the active ingredient in Anterone, is an antiandrogen that blocks the effect of male sex hormones (androgens) on the body and decreases their overall production.

Yes, Anterone is used to treat prostate cancer and reduce sex drive in men, and to manage severe symptoms of androgenisation like hirsutism and acne in women.

Yes, common inactive ingredients found in Anterone tablets include lactose monohydrate, starch-maize, povidone, magnesium stearate, and silica-colloidal anhydrous.

Serious side effects include liver toxicity, which can be fatal, and an increased risk of benign brain tumours (meningiomas) with long-term, high-dose use.

Anterone is contraindicated for individuals with liver diseases, severe chronic depression, a history of blood clots, or severe diabetes with vascular changes. It must also not be taken during pregnancy.

In men, Anterone can cause infertility and impotence, though this is usually reversible within a few months after discontinuing therapy. For women, the long-term effects on fertility are not well-established.

Yes, Anterone can interact with other medications metabolized by the CYP3A4 enzyme, such as certain antifungals, HIV treatments, and statins. It is important to inform your doctor about all medications you are taking.

References

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Medical Disclaimer

This content is for informational purposes only and should not replace professional medical advice.