Gynecomastia Medication

Updated: Feb 14, 2022
  • Author: George Ansstas, MD; Chief Editor: George T Griffing, MD  more...
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Medication Summary

Clomiphene, [31] an antiestrogen, can be administered on a trial basis at a dose of 50-100 mg per day for up to 6 months. Approximately 50% of patients achieve partial reduction in breast size, and approximately 20% of patients note complete resolution. Adverse effects, while rare, include visual problems, rash, and nausea.

Tamoxifen, an estrogen antagonist, is effective for recent-onset and tender gynecomastia when used in doses of 10-20 mg twice daily. [32] Up to 80% of patients report partial to complete resolution. Tamoxifen is typically used for 3 months before referral to a surgeon. Nausea and epigastric discomfort are the main adverse effects. [34]

Other, less frequently used drugs include danazol. [35] Danazol, a synthetic derivative of testosterone, inhibits pituitary secretion of LH and follicle-stimulating hormone (FSH), which decreases estrogen synthesis from the testicles. The dose used for gynecomastia is 200mg twice daily. Complete resolution of breast enlargement has been reported in 23% of cases. Adverse effects include weight gain, acne, muscle cramps, fluid retention, nausea, and abnormal liver function test results.



Class Summary

Androgens suppress pituitary release of gonadotropic hormones.

These agents are used to inhibit the effects of estrogen. [6, 31, 32, 34, 35, 48]

Testosterone (Androderm, AndroGel, Axiron, Testim)

Testosterone is the predominant male sex hormone used for replacement therapy in male hypogonadism.


Danazol is a synthetic steroid analog with strong antigonadotropic activity (it inhibits LH and FSH) and weak androgenic action.


Selective Estrogen Receptor Modulators

Class Summary

Selective estrogen receptor modulators inhibit estrogen effects.

Clomiphene (Clomid, Serophene)

Clomiphene stimulates the release of pituitary gonadotropins.


Tamoxifen competitively binds to the estrogen receptor, producing a nuclear complex that decreases deoxyribonucleic acid (DNA) synthesis and inhibits estrogen effects.