leuprolide; leuprorelin (Lupron, Eligard)
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Introduction
Tradename: Lupron.
Indications
- endometriosis
- uterine leiomyoma (fibroids)
- palliative treatment of advanced prostate carcinoma
- precocious puberty
- ovarian cancer[4]
- in combination with aromatase inhibitor for ER/PR+ breast cancer
Contraindications
Dosage
- endometriosis: 3.75 mg IM once a month for 6 months
- uterine leiomyoma: 11.25 mg IM once (3 month depot)
- advanced prostate carcinoma:
- children:
- precocious puberty: 20-45 ug/kg/day SC
- 0.3 mg/kg (minimun 7.5 mg) IM monthly
Do NOT use needles smaller than 22 guage when administering depot form. Use only diluent provided.
Store unopened vials in refrigerator.
Vial in use can be kept at room temperature for months.
Reconstituted suspension stable for 24 hours
Injection: 5 mg/mL (2.8 mL) Suspension, Depot (1 month):
Adverse effects
- common (> 10%)
- hot flashes, depression, weight gain, pain, nausea/vomiting
- less common (1-10%)
- edema, cardiac arrhythmias, dizziness, paresthesias, lethargy, insomnia, headache, rash, estrogenic effects (gynecomastia, breast tenderness), diarrhea, GI bleed, anemia, myalgia, blurred vision
- uncommon (< 1%)
- other
- osteoporosis: supplement calcium & vitamin D[6]
- bisphosphonat if bone metastases[6]
- osteoporosis: supplement calcium & vitamin D[6]
Test interactions
- interferes with pituitary gonadoropic & gonadal function test during & up to 4-8 weeks after therapy
Mechanism of action
- GnRH analog
- affects LH & FSH release from the pituitary
- decline in testosterone & estradiol production
- transient decline in estradiol production for > 1 month
- causes chemical castration
- retards growth of hormone-sensitive tissue
More general terms
- synthetic peptide
- gonadotropin-releasing hormone agonist (GnRH analog)
- antineoplastic endocrine agent
More specific terms
Component of
References
- ↑ The Pharmacological Basis of Therapeutics, 9th ed. Gilman et al, eds. Permagon Press/McGraw Hill, 1996
- ↑ Kaiser Permanente Northern California Regional Drug Formulary, 1998
- ↑ DrugDex Drug Evaluation, vol 105, 2000
- ↑ 4.0 4.1 Deprecated Reference
- ↑ Kaunitz AM Nocturnal Hot Flashes, Sleep Disturbances, and Worsening Mood: The Perfect Storm? NEJM Journal Watch. Oct 11, 2016 Massachusetts Medical Society (subscription needed) http://www.jwatch.org
- ↑ 6.0 6.1 6.2 Geriatric Review Syllabus, 10th edition (GRS10) Harper GM, Lyons WL, Potter JF (eds) American Geriatrics Society, 2019
Database
- PubChem: http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?cid=3911
- PubChem: http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?cid=3033055
- PubChem: http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?cid=441410
- PubChem: http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?cid=82154
- PubChem: http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?cid=657181