Leuprolide

From Anvita Health Wiki

Contents 1 More Specific Terms 2 Introduction 3 Indications 4 Contraindications 5 Dosage 6 Adverse-effects 7 Test-interactions 8 Mechanism-of-action 9 More General Terms 10 Internet Database 11 References

More Specific Terms

• implantable leuprolide (Viadur)

Introduction

• Tradename: Lupron.

Indications

• endometriosis
• uterine leiomyoma ( fibroids)
• palliative treatment of advanced prostate carcinoma
• precocious puberty

Contraindications

• pernicious anemia
• pregnancy
  

• pregnancy category = x
• safety in lactation = -

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:

• 7.5 mg IM monthly (1 month depot)
• 22.5 mg IM every 12 weeks (3 month depot)

• 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):

• 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

• 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%)

• pulmonary embolism, thrombophlebitis, myocardial infarction
  
• drug adverse effects of GnRH agonists

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

• initially stimulates LH & FSH release, then
• diminishes LH & FSH release via negative feed-back (loss of pulsatility)

• decline in testosterone & estradiol production
• causes chemical castration
• retards growth of hormone-sensitive tissue

More General Terms

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

Internet Database

PubChem: 3911
PubChem: 3033055
PubChem: 441410
PubChem: 82154
PubChem: 657181

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

leuprolide; leuprorelin (Lupron)