Goserelin
- Atc Codes:L02AE03
- CAS Codes:65807-02-5
- PHARMGKB ID:65807-02-5
Table of contents
- Brand Names
- Chemistry
- Pharmacologic Category
- Mechanism of Action
- Therapeutic Use
- Pregnancy and Lactation Implications
- Contraindications
- Warnings and Precautions
- Adverse Reactions
- Genes that may be involved
- Drug Interactions
- Dosage
- Pharmacokinetics and Pharmacodynamics
- Special Considerations
Brand Names
Europe
Austria: Goserelin, Novimp, Novogos, Zoladex; Belgium: Zoladex; Bulgaria: Zoladex; Cyprus: Zoladex; Czech Republic: Zoladex; Denmark: Zoladex; Estonia: Zoladex; Finland: Zoladex; France: Zoladex; Germany: Goserelin, Novimp, Novosis, Zoladex; Greece: Zoladex; Hungary: Zoladex; Ireland: Zoladex; Italy: Zoladex; Latvia: Zoladex; Lithuania: Zoladex; Luxembourg: Zoladex; Malta: Zoladex; Netherlands: Zoladex; Poland: Zoladex; Portugal: Zoladex; Romania: Zoladex; Slovakia: Zoladex; Slovenia: Zoladex; Spain: Zoladex; Sweden: Zoladex; UK: Novgos, Zoladex.
North America
Canada: Zoladex; USA: Zoladex.
Latin America
Argentina: Larmadex, Zoladex; Brazil: Zoladex; Mexico: Zoladex.
Asia
Japan: Zoladex.
Drug combinations
Chemistry
Goserelin: C~59~H~84~N~18~O~14~. Mw: 1269.41. (1) Luteinizing hormone-releasing factor (pig), 6-[O-(1,1-dimethylethyl)-D-serine]-10-deglycinamide-, 2-(aminocarbonyl)hydrazide; (2) 1-(5-Oxo-L-prolyl-L-histidyl-L-tryptophyl-L-seryl-L-tyrosyl-O-tert-butyl-D-seryl-L-leucyl-L-arginyl-L-prolyl)semicarbazide. CAS-65807-02-5 (1987).
Pharmacologic Category
Antineoplastic Agents; Endocrine Therapy. Gonadotropin-Releasing Hormone (GnRH). Luteinizing-Hormone-Releasing Hormone (LHRH) Agonist. (ATC-Code: L02AE03).
Mechanism of action
Goserelin is a synthetic analog of LHRH. Following initial increase in luteinizing hormone (LH) and follicle-stimulating hormone (FSH), chronic administration of goserelin results in sustained suppression of pituitary gonadotropins. Serum testosterone falls to levels comparable to surgical castration. Exact mechanism of this effect unknown, but may be related to changes in control of LH or down-regulation of LH receptors.
Therapeutic use
Palliative treatment of advanced prostate cancer, endometriosis, or advanced breast cancer in premenopausal and perimenopausal women. Used as endometrial-thinning agent prior to endometrial ablation procedures for treatment of dysfunctional uterine bleeding.
Pregnancy and lactiation implications
Goserelin has been found to be teratogenic, and increases pregnancy loss in animal studies. Women of childbearing potential should avoid pregnancy. Contraindicated during lactation.
Unlabeled use
Contraindications
Hypersensitivity to goserelin, LHRH, LHRH-agonist analogs, or any component of the formulation. Known or suspected pregnancy or lactation.
Warnings and precautions
Hazardous agent. Decreased bone density reported in women (may be irreversible). Hypercalcemia reported in prostate and breast cancer with bone metastases. Spinal cord compression and/or ureteral obstruction reported when used for prostate cancer. Transient worsening of signs and symptoms (tumor flare) may develop during first few weeks of treatment. Urinary tract obstruction reported when used for prostate cancer. May cause fetal harm. Continuous use of goserelin usually inhibits ovulation and stops menstruation. Hypercalcemia reported in prostate or breast cancer with bone metastases. Antibody formation, acute anaphylactic reactions, and urticaria reported with GnRH agonists. Possible increase in cervical resistance. Decreases in bone mineral density, osteoporosis, and bone fracture reported in men, and decreases in bone mineral density reported in women. Possible transient changes in blood pressure (hyper-/hypotension). Possible increased total and LDL-C and triglycerides, and decreased HDL-C.