Management of Hyperestrogenism in Men
The first-line treatment for men experiencing symptoms of hyperestrogenism is an aromatase inhibitor such as anastrozole, which significantly lowers serum estradiol concentrations by inhibiting the conversion of androgens to estrogens. 1
Clinical Presentation of Hyperestrogenism in Men
- Common symptoms include gynecomastia, sexual dysfunction (particularly erectile dysfunction and decreased libido), infertility, and hypogonadism 2, 3
- Hyperestrogenism affects approximately 17-20% of men seeking treatment for sexual health concerns, with higher prevalence in older men and those with comorbidities 4, 2
- Men with elevated estradiol levels show higher rates of severe erectile dysfunction (48.9% vs 29.9% in men with normal levels) 2
Diagnostic Evaluation
- Initial workup should include comprehensive hormonal panel:
- Additional testing may include:
- Complete blood count
- Lipid profile
- Liver function tests 5
Causes of Hyperestrogenism in Men
- Exogenous testosterone therapy (especially injectable forms) is a common cause, with approximately 20% of men on testosterone replacement developing high estradiol levels 4
- Obesity (increased aromatization in adipose tissue) 6
- Genetic disorders (rare familial hyperestrogenism due to increased aromatase activity) 3, 7
- Liver disease (impaired estrogen metabolism)
- Certain medications that affect hormone metabolism 5
Treatment Options
First-Line Treatment: Aromatase Inhibitors
- Anastrozole is the most commonly prescribed medication (62.3% of practitioners use it for symptomatic hyperestrogenemia) 1, 8
- Mechanism: Selectively inhibits the aromatase enzyme, preventing conversion of androgens to estrogens
- Dosing varies significantly in clinical practice, ranging from 1 mg weekly to 1 mg daily 8
- Effectively suppresses serum estradiol by approximately 70% within 24 hours and 80% after 14 days of daily dosing 1
Additional Treatment Options
- Selective estrogen receptor modulators (SERMs) may be used as an alternative or adjunct therapy 4
- For men with obesity, weight loss and lifestyle modifications should be recommended as they can help reduce aromatization of androgens to estrogens 6
- If hyperestrogenism is due to exogenous testosterone therapy:
- Adjust testosterone dosage or change administration route (transdermal may cause less estrogen conversion than injectable forms)
- Consider discontinuation if appropriate 5
Monitoring and Follow-up
- Regular laboratory monitoring of estradiol levels is essential during treatment 5, 8
- Approximately 50% of practitioners treating men with testosterone therapy monitor estrogen levels 8
- Monitor for potential side effects of aromatase inhibitors:
- Bone mineral density changes
- Lipid profile alterations
- Joint pain 5
Special Considerations
- For men with concurrent erectile dysfunction, PDE5 inhibitors may be used in combination with treatments for hyperestrogenism 6
- For men with fertility concerns, aromatase inhibitors may help improve semen parameters by restoring proper testosterone-to-estrogen ratio 6
- Breast cancer in men is associated with elevated estrogen levels; men with persistent gynecomastia should be monitored appropriately 6
Treatment Algorithm
- Confirm hyperestrogenism with laboratory testing (estradiol >42.6 pg/mL)
- Identify and address underlying causes when possible
- For symptomatic patients:
- Monitor estradiol levels every 3-6 months during treatment 5
- Adjust treatment based on symptom resolution and laboratory values
By following this approach, most men with hyperestrogenism can achieve symptom improvement and normalization of hormone levels.