What pill lowers testosterone levels? An overview of anti-androgen medications

October 10, 2025 •

5 min read

For many conditions, including prostate cancer and hormonal acne, targeted therapy to modulate hormone levels is necessary. A number of different types of pills that lower testosterone levels exist, and the appropriate medication depends on the underlying medical condition and individual patient goals.

Quick Summary

This guide covers various oral medications, such as anti-androgens and androgen synthesis inhibitors, that lower testosterone levels by blocking hormone production or action.

Key Points

Spironolactone: A commonly prescribed anti-androgen pill used primarily in women for conditions like hormonal acne and PCOS due to its ability to block testosterone's effects.
Relugolix (Orgovyx): The first oral GnRH antagonist used for advanced prostate cancer, known for its rapid and reversible testosterone reduction without causing an initial hormone flare.
Abiraterone (Zytiga): An androgen synthesis inhibitor that blocks testosterone production and is primarily used for treating castration-resistant prostate cancer.
Anti-androgens (e.g., bicalutamide): These pills block testosterone from attaching to receptors and are frequently combined with other treatments for prostate cancer.
Underlying Condition: The choice of medication is dependent on the specific condition being treated, emphasizing the need for professional medical guidance before starting or stopping any treatment.
Secondary Effects: Medications for other conditions, such as long-term opioid use, certain antidepressants, or statins, can also affect testosterone levels as a secondary or off-target effect.
Side Effect Management: Many testosterone-lowering medications carry a risk of side effects like hot flashes, fatigue, and potential cardiovascular or electrolyte issues, requiring ongoing monitoring.

Understanding the mechanisms of action

Testosterone, the primary male sex hormone, is vital for several bodily functions in both men and women. In men, it is responsible for the development of masculine characteristics. In women, it is present in smaller amounts and plays a role in bone density and libido. Conditions such as prostate cancer, polycystic ovary syndrome (PCOS), and gender dysphoria may necessitate lowering testosterone levels. Medications designed to achieve this work through several distinct mechanisms. Some block the production of testosterone, while others block its action at the cellular level by interfering with hormone receptors. The following sections detail several types of oral medications used for this purpose.

Anti-androgens: Blocking the effects of testosterone

Anti-androgens, also called androgen receptor blockers, prevent testosterone and its more potent form, dihydrotestosterone (DHT), from binding to cellular receptors. This effectively neutralizes their biological impact, even if circulating hormone levels remain high. This is a common strategy for treating hormone-sensitive conditions.

Spironolactone (Aldactone): This medication, also a potassium-sparing diuretic, is a widely used anti-androgen. While FDA-approved for conditions like high blood pressure and heart failure, its anti-androgenic properties are used off-label for several conditions.
- Uses: Treatment of hormonal acne in women, PCOS management, and as part of gender-affirming hormone therapy for transgender women.
- Side Effects: Potential side effects include increased urination, menstrual irregularities, dizziness, and elevated potassium levels (hyperkalemia), which requires monitoring.
Bicalutamide (Casodex): A potent, nonsteroidal anti-androgen primarily used to treat prostate cancer. It is often used in combination with other treatments that suppress testosterone production to block any remaining androgen activity.
- Uses: Advanced prostate cancer, often combined with LHRH agonists or surgical castration.
- Side Effects: Hot flashes, breast tenderness, and gynecomastia (breast tissue enlargement) are common. Bicalutamide is generally well-tolerated, but some side effects are possible.

Androgen synthesis inhibitors: Stopping production altogether

Another approach involves inhibiting the enzymes necessary for testosterone synthesis throughout the body, including the adrenal glands and testicles. This drastically reduces the total amount of testosterone in the body.

Abiraterone (Zytiga, Yonsa): This oral medication is a potent inhibitor of the CYP17 enzyme, a key player in androgen synthesis. It is used to treat advanced prostate cancer that has become castration-resistant.
- Uses: Metastatic castration-resistant prostate cancer.
- Side Effects: Abiraterone is typically taken with a corticosteroid like prednisone to manage side effects, which can include hot flashes, fatigue, joint pain, and potential liver problems.

GnRH antagonists: A new oral option

Luteinizing hormone-releasing hormone (LHRH), also known as gonadotropin-releasing hormone (GnRH), triggers testosterone production in the testicles. Traditional LHRH agonists are injections, but newer oral antagonists provide a pill-based alternative.

Relugolix (Orgovyx): The first and only oral GnRH antagonist, relugolix offers a rapid, profound, and reversible reduction of testosterone. Unlike LHRH agonists, it does not cause an initial testosterone flare, making it safer for certain prostate cancer patients.
- Uses: Advanced prostate cancer.
- Side Effects: Common side effects include hot flashes, fatigue, and increased blood sugar levels. It also has a lower risk of major adverse cardiovascular events compared to LHRH agonists.

Other medications with testosterone-modulating effects

Several other prescription medications can impact testosterone levels, sometimes as a secondary or side effect of their primary purpose.

Estrogen Therapy: For transgender women and nonbinary people, estrogen is often combined with anti-androgens. Estrogen itself can suppress endogenous testosterone production by creating a negative feedback loop with the pituitary gland, in addition to promoting feminizing characteristics.
Opioid Pain Medications: Long-term use of opioids can inhibit the hypothalamic-pituitary axis, leading to lower levels of testosterone.
Certain Antidepressants (SSRIs): Some SSRIs have been shown to inhibit testosterone synthesis and increase prolactin levels, which can also lower testosterone.
Statins: These cholesterol-lowering drugs can slightly decrease testosterone levels, as cholesterol is a precursor for testosterone production. The effect is typically minor.

Comparison of oral testosterone-lowering medications


Drug Type	Example	Mechanism	Primary Use	Key Side Effects
Anti-androgen	Spironolactone	Blocks androgen receptors	Hormonal acne, PCOS, gender-affirming therapy	Hyperkalemia, dizziness, menstrual irregularities
Anti-androgen	Bicalutamide	Blocks androgen receptors	Prostate cancer	Gynecomastia, hot flashes, fatigue
Androgen Synthesis Inhibitor	Abiraterone	Blocks CYP17 enzyme	Castration-resistant prostate cancer	Hot flashes, fatigue, liver issues
Oral GnRH Antagonist	Relugolix	Blocks GnRH receptors	Advanced prostate cancer	Hot flashes, fatigue, high blood sugar

Which pill is right for you?

Choosing the correct oral medication to lower testosterone is a complex decision that must be made in consultation with a healthcare professional. The underlying medical condition, the severity of symptoms, potential side effects, and the desired outcome all play a critical role. For example, a patient with advanced prostate cancer requires different medication than a woman with hormonal acne. Side effect profiles can also influence the choice; while spironolactone is effective, its risk of hyperkalemia requires careful monitoring. It is crucial to have an open discussion with a doctor to weigh the benefits and risks of each option.

Considerations for long-term use

Many of these medications are prescribed for long-term use, especially for chronic conditions like prostate cancer or ongoing hormonal management. Long-term treatment necessitates consistent medical supervision and monitoring. Regular blood tests may be required to check hormone levels, liver and kidney function, and electrolytes, especially with spironolactone. Patients should also be aware of the potential for medication interactions and discuss all other drugs or supplements they are taking with their physician. For conditions like gender dysphoria, the medication regimen is highly individualized and depends on the patient's transition goals. Regardless of the reason, it is important for individuals to discuss the potential impact on fertility and sexual function with their healthcare provider before beginning treatment. The specific medication and treatment plan must be tailored to the individual to ensure both effectiveness and safety.

Note: Medications should never be started or stopped without the explicit guidance and supervision of a qualified healthcare professional. For more information on hormone therapy options, resources like the Mayo Clinic can provide additional detail.

Conclusion

Various oral medications exist for lowering testosterone levels, each with a unique mechanism and application. Anti-androgens, such as spironolactone and bicalutamide, block hormone receptors, making them useful for conditions like PCOS, acne, and prostate cancer. Androgen synthesis inhibitors like abiraterone block the production of testosterone, primarily for treating advanced prostate cancer. Relugolix is a newer oral GnRH antagonist that provides a fast-acting, non-injection option for prostate cancer patients. Other drugs, including estrogen therapy and certain medications for cholesterol, pain, or depression, may also impact testosterone levels. The selection of the most suitable medication depends heavily on the specific medical condition and should always involve a detailed discussion with a healthcare provider to understand the benefits and risks involved.

Frequently Asked Questions

Spironolactone is a very common oral medication for lowering testosterone's effects, particularly in women being treated for conditions like hormonal acne or polycystic ovary syndrome (PCOS).

No, spironolactone is generally not recommended for men for the treatment of acne, as it can cause significant anti-androgenic side effects like gynecomastia (enlargement of breast tissue) and other feminizing effects.

Relugolix is an oral GnRH antagonist, which means it rapidly and reversibly lowers testosterone without causing the initial testosterone surge (flare) seen with older injectable LHRH agonists.

Yes, some common medications, particularly long-term opioid pain relievers and certain statins, have been shown to potentially lower testosterone levels, though the effect from statins is typically minor.

Common side effects vary by medication but can include hot flashes, fatigue, decreased libido, breast tenderness or enlargement, and mood changes. Spironolactone, for example, can cause elevated potassium levels.

The time it takes for a pill to work depends on the specific medication. Relugolix, for example, shows significant testosterone reduction within two weeks, while others like spironolactone may take several months to produce noticeable effects on symptoms like acne.

Stopping these medications should only be done under a doctor's supervision. For some, like Relugolix for prostate cancer, stopping can reverse the effects, but for others, the treatment is long-term. Abrupt cessation can cause a rebound of symptoms.

Yes, in women, oral contraceptives can decrease ovarian androgen production and increase sex hormone-binding globulin (SHBG), which reduces free testosterone levels. They are often used to manage conditions caused by excess androgens, such as acne and hirsutism.