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leuprolide; leuprorelin (Lupron, Eligard)

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: 1) pernicious anemia 2) pregnancy Dosage: 1) endometriosis: 3.75 mg IM once a month for 6 months 2) uterine leiomyoma: 11.25 mg IM once (3 month depot) 3) advanced prostate carcinoma: a) 7.5 mg IM monthly (1 month depot) b) 22.5 mg IM every 12 weeks (3 month depot) 4) children: a) precocious puberty: 20-45 ug/kg/day SC b) 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): - 3.75 mg/mL, 7.5 mg/mL, 11,25 mg/mL, 15 mg/mL Suspension, Depot (3 months): 11.25 mg/mL, 22.5 mg/mL Adverse effects: 1) common (> 10%) - hot flashes, depression, weight gain, pain, nausea/vomiting 2) 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 3) uncommon (< 1%) - pulmonary embolism, thrombophlebitis, myocardial infarction 4) other - osteoporosis: supplement calcium & vitamin D [6] - bisphosphonat if bone metastases [6] Test interactions: - interferes with pituitary gonadoropic & gonadal function test during & up to 4-8 weeks after therapy Mechanism of action: 1) GnRH analog 2) affects LH & FSH release from the pituitary a) initially stimulates LH & FSH release, then b) diminishes LH & FSH release via negative feed-back (loss of pulsatility) 3) decline in testosterone & estradiol production - transient decline in estradiol production for > 1 month 4) causes chemical castration 5) retards growth of hormone-sensitive tissue

Interactions

drug adverse effects of GnRH agonists

Specific

implantable leuprolide (Viadur)

General

antineoplastic endocrine agent gonadotropin-releasing hormone agonist (GnRH analog) synthetic peptide

Properties

MISC-INFO: elimination route LIVER pregnancy-category X safety in lactation -

Database Correlations

PUBCHEM correlations

References

  1. The Pharmacological Basis of Therapeutics, 9th ed. Gilman et al, eds. Permagon Press/McGraw Hill, 1996
  2. Kaiser Permanente Northern California Regional Drug Formulary, 1998
  3. DrugDex Drug Evaluation, vol 105, 2000
  4. Deprecated Reference
  5. 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. Geriatric Review Syllabus, 10th edition (GRS10) Harper GM, Lyons WL, Potter JF (eds) American Geriatrics Society, 2019

Component-of

implantable leuprolide (Viadur) leuprolide/norethindrone