Goserelin

Introduction: Goserelin is a synthetic decapeptide GnRH analogue used for prostate cancer, breast cancer, endometriosis and uterine fibroids. It is a potent inhibitor of pituitary gonadotrophin secretion.

How it works: Goserelin initially causes an increase in serum FSH and LH levels but chronic administration leads to sustained suppression of pituitary gonadotrophin release causing regression of the sex organs.

Important Information: Administered as subcutaneous injection into the anterior abdominal wall every 28 days. Hot flashes are a common side effect. Long-term use may cause decreased bone mineral density.

• Stage B2-C Prostatic Carcinoma: in combination with flutamide prior to and during radiation therapy
• Advanced Prostatic Carcinoma: palliative treatment
• Endometriosis: pain relief and reduction of lesions (6 months)
• Endometrial Thinning: prior to endometrial ablation
• Advanced Breast Cancer: palliative treatment in pre- and perimenopausal women

Hormonal Therapy

GnRH Analogue

Goserelin is a synthetic decapeptide analogue of GnRH. Goserelin acts as an inhibitor of pituitary gonadotropin secretion when administered in the biodegradable formulation. In animal and in vitro studies, administration of goserelin resulted in the regression or inhibition of growth of the hormonally sensitive dimethylbenzanthracene (DMBA)-induced rat mammary tumor and Dunning R3327 prostate tumor.

Goserelin binds to GnRH receptors, initially increasing gonadotropin secretion, then through receptor desensitization with chronic use, reduces testosterone and estradiol levels.

Goserelin 3.6 mg:

• SC injection into anterior abdominal wall every 28 days
• Prostate cancer: long-term administration
• Endometriosis: 6 months
• Endometrial thinning: 1 or 2 depots (4 weeks apart)
• Breast cancer: long-term administration

Goserelin 10.8 mg:

• SC injection into anterior abdominal wall every 12 weeks
• Prostate cancer: long-term administration

* Use as directed by the registered physician

Subcutaneous (SC) injection - into the anterior abdominal wall below the navel line. Your doctor or nurse will give you this medicine. Do not self-administer. Use aseptic technique.

If you miss a dose, consult your doctor.

Common Side Effects (Men >10%):

• Hot flashes
• Sexual dysfunction
• Decreased erections
• Lower urinary tract symptoms

Common Side Effects (Women >20%):

• Hot flushes
• Headache
• Sweating
• Acne
• Emotional lability
• Depression
• Decreased libido
• Vaginitis
• Breast atrophy

Precautions:

• Tumor Flare Phenomenon - symptoms may temporarily worsen in first few weeks
• Hyperglycemia and diabetes risk - monitor blood glucose
• Cardiovascular disease risk - monitor and manage
• Hypercalcemia - monitor in patients with bone metastases
• QT interval may be prolonged - consider risks and benefits

Contraindications:

• Hypersensitivity to Goserelin or GnRH analogues
• Pregnancy

Drug Interactions: No significant interactions known.

Food Interactions:

• It is not known whether it is safe to consume alcohol. Please consult your doctor.

Use in Pregnancy: Highly unsafe during pregnancy. Studies have shown significant harmful effects to the developing baby.

Use in Lactation: Probably unsafe during breastfeeding. Limited data suggests the drug may pass into breastmilk and harm the baby.

Pediatric Use: Safety and efficacy in pediatric patients have not been established.

Geriatric Use: No specific dosage adjustment is necessary for elderly patients.

Renal Impairment: Safe in kidney disease. No dose adjustment required.

Hepatic Impairment: Safe in liver disease. No dose adjustment required.

Overdose: Limited information available on overdose. Employ usual supportive measures.

Storage: Keep away from light and moisture. Keep out of reach of children.

Goserelin Injection