Mesterolone is a synthetic, orally active androgen derived from dihydrotestosterone (DHT). It is a pure androgen with minimal to no estrogenic, progestogenic, or anabolic activity. Unlike testosterone, it does not undergo aromatization to estradiol, making it a preferred choice in specific clinical scenarios in India, particularly for male hypogonadism and infertility, where estrogenic side effects are a concern.
Adult: For hypogonadism: 25 mg to 75 mg per day, divided into 2-3 doses. For infertility: 50 mg to 100 mg per day, divided into 2 doses. Typical starting dose is 25 mg twice daily.
Note: Tablet should be swallowed whole with water, preferably with or after food to minimize gastric discomfort. Doses should be evenly spaced. Therapy duration for infertility should be at least 3-6 months to assess efficacy.
Mesterolone binds to and activates intracellular androgen receptors in target tissues (e.g., prostate, seminal vesicles, skin, hair follicles, central nervous system). The hormone-receptor complex translocates to the nucleus, binds to specific DNA sequences (androgen response elements), and modulates gene transcription, leading to androgenic effects.
Pregnancy: CATEGORY X. Contraindicated. May cause virilization of the female fetus.
Driving: Usually no effect. However, patients should be cautioned that dizziness or visual disturbances, though rare, can occur and may impair driving ability.
| Warfarin/Acenocoumarol | Mesterolone may potentiate anticoagulant effect, increasing INR and bleeding risk. | Major |
| Oral Hypoglycemics (e.g., Glimepiride) & Insulin | Androgens may alter glucose tolerance, requiring dose adjustment of anti-diabetic drugs. | Moderate |
| Corticosteroids (e.g., Prednisolone) | Additive risk of fluid retention and edema. | Moderate |
| Cyclosporine, Tacrolimus | Increased risk of nephrotoxicity due to potential additive renal impairment. | Moderate |
| Thyroid Hormones (e.g., Levothyroxine) | Mesterolone may decrease thyroxine-binding globulin, altering thyroid function test results. | Minor |
Same composition (Mesterolone (25mg)), different brands: