Goserelin

From Anvita Health Wiki

Contents 1 Introduction 2 Indications 3 Pharmacokinetics 4 Adverse-effects 5 Mechanism-of-action 6 More General Terms 7 Additional Terms 8 Internet Database 9 References

Introduction

• Tradename: Zoladex.

Indications

• palliative treatment of prostate cancer, usually in combination with other agents
• management of endometriosis Prostate cancer & endometriosis:
• 3.6 mg SC every 28 days (preferred)
• 10.8 mg SC every 3 months
• used in combination with androgen antagonist bicalutamide ( Casodex)

Pharmacokinetics

• slowly released from subcutaneously inserted pellet
• eliminated in urine
• 1/2life 5 hours, prolonged with renal insufficiency
  

• elimination via liver
• 1/2life = 5 hours

Adverse-effects

• local discomfort at the injection site
• hot flashes
• decreased libido
• spot bleeding in females
• muscle weakness
• tumor flare (mostly in 1st 2 weeks due to initial stimulation of hormone production)
  
• drug adverse effects of GnRH agonists

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)

Additional Terms

• prostate carcinoma (prostate cancer)

Internet Database

PubChem: 47725
PubChem: 5311128
PubChem: 3502

References

1. The Pharmacological Basis of Therapeutics, 9th ed. Gilman et al, eds. Permagon Press/McGraw Hill, 1996
2. AHFS Drug Information, American Society of Health-System Pharmacists, Bethesda, 1998
3. Drug Information & Medication Formulary, Veterans Affairs, Central California Health Care System, 1st ed., Ravnan et al eds, 1998

goserelin (Zoladex)