Leuprolide
Leuprolide Acetate (Lupron)
A synthetic GnRH agonist that, with continuous administration, paradoxically suppresses LH and FSH secretion, leading to reduced sex hormone production. Used clinically for prostate cancer, endometriosis, and precocious puberty.
Mechanism of Action
Leuprolide initially stimulates GnRH receptors causing a testosterone flare, but continuous exposure desensitizes and downregulates pituitary GnRH receptors, ultimately suppressing LH, FSH, and gonadal steroid production to castrate levels.
Health Claims & Evidence
Suppresses testosterone to castrate levels in prostate cancer
Reduces endometriosis-related pain
Treats central precocious puberty
Short-Term Effects
Initial testosterone flare followed by suppression within 2–4 weeks.
Long-Term Effects
Sustained hormonal suppression; bone density loss with prolonged use requires monitoring.
Side Effects
Hot flashes, decreased libido, erectile dysfunction, bone density loss, mood changes, injection site reactions.
Contraindications
Pregnancy, undiagnosed vaginal bleeding. Use with caution in patients with cardiovascular disease.
This profile is provided for educational research only. It is not a treatment recommendation or dosing guide. Human evidence, safety information and regulatory status vary by substance. Verify primary sources and consult a qualified healthcare professional for medical decisions.
Research Papers
Leuprolide acetate in prostate cancer
Crawford et al. · New England Journal of Medicine · 1989
Educational research only. This profile is not a treatment recommendation or dosing guide. Human evidence, safety information and regulatory status vary by substance. Consult a qualified healthcare professional for medical decisions.
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