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ANTINEOPLASTIC AND IMMUNOMODULATING AGENTS › ENDOCRINE THERAPY › HORMONES AND RELATED AGENTS › Gonadotropin releasing hormone analogues
leuprorelin
L02AE02
Forms & Strengths
- 1mg, 3.75mg, and 6mg prefilled syringe
- 1mg, 3.75mg, 6mg, 11.25mg, and 18.75mg vial
- 7.5mg, 11.25mg, 15mg, and 22.5mg depot injection
- 1mg, 2mg, 3mg, and 4mg/mL solution
Adult Dosing
- Prostate cancer: 1mg SC/IM qd or 7.5mg, 11.25mg, 15mg, or 22.5mg IM q1-3mos
- Endometriosis: 3.75mg IM qmo
- Uterine fibroids: 3.75mg IM qmo
- Precocious puberty: 0.05-1.28mg/kg q4wks
Pediatric Dosing
- Central precocious puberty: 0.05-1.28mg/kg q4wks
- Adjust dose based on response and IGF-1 levels
- Max dose: 40mg q28d
Indications
- Palliative treatment of advanced prostate cancer
- Management of endometriosis
- Treatment of uterine fibroids
- Treatment of precocious puberty
Mechanism of Action
- Agonist at gonadotropin-releasing hormone (GnRH) receptors
- Initially increases LH and FSH, then downregulates receptors
- Reduces sex hormone production
- Decreases LH/FSH with chronic administration
Contraindications
- Hypersensitivity to leuprorelin or GnRH agonists
- Pregnancy
- Undiagnosed vaginal bleeding
Adverse Reactions
- Hot flashes
- Injection site reactions
- Mood changes
- Decreased libido
- Erectile dysfunction
- Bone density loss with long-term use
Drug Interactions
- Androgens, estrogens: may counteract effects of leuprorelin
- Other GnRH agonists or antagonists: may intensify or diminish leuprorelin effects
Curated Content: Needs Vetting Before Put to Clinical Use