Search
goserelin (Zoladex)
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:
1) 3.6 mg SC every 28 days (preferred)
2) 10.8 mg SC every 3 months
3) used in combination with androgen antagonist bicalutamide (Casodex)
Pharmacokinetics:
1) slowly released from subcutaneously inserted pellet
2) eliminated in urine
3) 1/2life 5 hours, prolonged with renal insufficiency
Adverse effects:
1) local discomfort at the injection site
2) hot flashes
3) decreased libido
4) spot bleeding in females
5) muscle weakness
6) tumor flare (mostly in 1st 2 weeks due to initial stimulation of hormone production)
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
4) causes chemical castration
5) retards growth of hormone-sensitive tissue
Interactions
drug adverse effects of GnRH agonists
Related
prostate cancer
General
antineoplastic endocrine agent
gonadotropin-releasing hormone agonist (GnRH analog)
synthetic peptide
Properties
MISC-INFO: elimination route LIVER
1/2life 5 HOURS
pregnancy-category X
safety in lactation -
Database Correlations
PUBCHEM correlations
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
- Deprecated Reference