Peptide Library / Detail
Leuprolide
Half-life
3-4 hours (immediate release); extended for depot formulations (1-4 months)
Delivery
Subcutaneous or intramuscular injection
Dosage
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Description
Leuprolide is a synthetic nonapeptide analog of gonadotropin-releasing hormone (GnRH) that acts as a potent agonist. It is widely used in clinical medicine to regulate sex hormone production by initially stimulating and then suppressing pituitary gonadotropin secretion. Leuprolide has established therapeutic applications in hormone-sensitive conditions including prostate cancer, endometriosis, and precocious puberty.
Usage
Clinical dosing varies by indication and formulation. Depot injections typically range from 3.75 mg to 22.5 mg administered monthly to every 3-6 months. Daily subcutaneous injections of 1 mg may be used for certain conditions. Treatment duration depends on the specific therapeutic goal and is determined by healthcare providers.
Mechanism of Action
Leuprolide initially stimulates GnRH receptors in the pituitary gland, causing a transient increase in luteinizing hormone (LH) and follicle-stimulating hormone (FSH). With continuous administration, it causes receptor downregulation and desensitization, leading to suppression of gonadotropin secretion and subsequent reduction in testosterone and estrogen production to castration or menopausal levels within 2-4 weeks.
Benefits(6)
- Suppression of testosterone in androgen-dependent prostate cancer
- Reduction of endometriosis symptoms and lesion size
- Management of precocious puberty in children
- Treatment of uterine fibroids and associated symptoms
- Reduction of ovarian hormone production in hormone-sensitive conditions
- Improvement in pain and dysmenorrhea associated with endometriosis
Side Effects(8)
- Hot flashes and sweating
- Decreased libido and sexual dysfunction
- Bone density loss with prolonged use
- Initial tumor flare in prostate cancer patients
- Mood changes and depression
- Headache and dizziness
- Injection site reactions
- Fatigue and weakness