goserelin (Zoladex)
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Introduction
Tradename: Zoladex.
Indications
- palliative treatment of prostate cancer, usually in combination with other agents
- management of endometriosis
- estrogen receptor positive breast cancer[4]
- precocious puberty[4] 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)
Mechanism of action
- GnRH analog
- affects LH & FSH release from the pituitary
- 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 endocrine agent
Additional terms
References
- ↑ The Pharmacological Basis of Therapeutics, 9th ed. Gilman et al, eds. Permagon Press/McGraw Hill, 1996
- ↑ AHFS Drug Information, American Society of Health-System Pharmacists, Bethesda, 1998
- ↑ Drug Information & Medication Formulary, Veterans Affairs, Central California Health Care System, 1st ed., Ravnan et al eds, 1998
- ↑ 4.0 4.1 4.2 Deprecated Reference