No

Antineoplastic Agent, Miscellaneous; Gonadotropin Releasing Hormone Analog; Luteinizing Hormone-Releasing Hormone Analog

Prostate carcinoma: Palliative treatment of advanced carcinoma of the prostate. An alternative treatment of prostatic cancer when orchiectomy or estrogen administration are either not indicated or unacceptable to the patient. Combination with flutamide for the management of locally confined stage T2b-T4 (stage B2-C) carcinoma of the prostate.

3.6 mg implant only:

Endometriosis: Management of endometriosis, including pain relief and reduction of endometriotic lesions for the duration of therapy

Advanced breast cancer: Palliative treatment of advanced breast cancer in pre- and perimenopausal women. Estrogen and progesterone receptor values may help to predict whether goserelin therapy is likely to be beneficial.

Note: The 10.8 mg implant is not indicated in women as the data are insufficient to support reliable suppression of serum estradiol

X

In women who are or may become pregnant, patients who are hypersensitive to the drug

Initially, goserelin, transiently increases serum levels of testosterone. Transient worsening of signs and symptoms, usually manifested by an increase in cancer-related pain which was managed symptomatically, may develop during the first few weeks of treatment. Isolated cases of ureteral obstruction and spinal cord compression have been reported; patient's symptoms may initially worsen temporarily during first few weeks of therapy, cancer-related pain can usually be controlled by analgesics

General: Worsening of signs and symptoms may occur during the first few weeks of therapy and are usually manifested by an increase in bone pain, increased difficulty in urinating, hot flashes, injection site irritation, and weakness; this will subside, but patients should be aware

Endocrine & metabolic: Gynecomastia, postmenopausal symptoms, sexual dysfunction, loss of libido, hot flashes

Genitourinary: Impotence, decreased erection

1% to 10%:

Cardiovascular: Edema

Central nervous system: Headache, spinal cord compression (possible result of tumor flare), lethargy, dizziness, insomnia

Dermatologic: Rash

Gastrointestinal: Nausea and vomiting, anorexia, diarrhea, weight gain

Genitourinary: Vaginal spotting and breakthrough bleeding, breast tenderness/enlargement

Local: Pain on injection

Neuromuscular & skeletal: Bone loss, increased bone pain

Miscellaneous: Diaphoresis

Symptomatic management

Zoladex® should be stored at room temperature not to exceed 25°C or 77°F; must be dispensed in an amber bag

LHRH synthetic analog of luteinizing hormone-releasing hormone also known as gonadotropin-releasing hormone (GnRH) incorporated into a biodegradable depot material which allows for continuous slow release over 28 days; mechanism of action is similar to leuprolide

Absorption: Oral: Inactive when administered orally; S.C.: Rapid and can be detected in the serum in 10 minutes

Distribution: V_d: 13.7 L

Time to peak serum concentration: S.C.: 12-15 days

Half-life: Following a bolus S.C. dose: 5 hours

Elimination: By the kidney; elimination time: 4.2 hours (prolonged in impaired renal function - 12 hours)

Adults: S.C.:

Monthly implant: 3.6 mg injected into upper abdomen every 28 days; do not try to aspirate with the goserelin syringe; if the needle is in a large vessel, blood will immediately appear in syringe chamber. While a delay of a few days is permissible, attempt to adhere to the 28-day schedule.

3-month implant: 10.8 mg injected into the upper abdominal wall every 12 weeks; do not try to aspirate with the goserelin syringe; if the needle is in a large vessel, blood will immediately appear in syringe chamber. While a delay of a few days is permissible, attempt to adhere to the 12-week schedule.

Prostate carcinoma: Intended for long-term administration

Endometriosis: Recommended duration: 6 months; retreatment is not recommended since safety data is not available. If symptoms recur after a course of therapy, and further treatment is contemplated, consider monitoring bone mineral density. Currently, there are no clinical data on the effect of treatment of benign gynecological conditions with goserelin for periods >6 months.

Dosing adjustment in renal/hepatic impairment: No adjustment is necessary

Serum alkaline phosphatase, serum acid phosphatase, serum testosterone, serum LH and FSH, serum estradiol

May cause sedation or insomnia

Sexual dysfunction is common; concurrent use with SSRIs may produce additive dysfunction

No information available to require special precautions

No effects or complications reported

This drug must be implanted into your stomach every 28 days; it is important to maintain appointment schedule. You may experience systemic hot flashes (cool clothes and temperatures may help), headache (analgesic may help), constipation (increased bulk and water in diet or stool softener may help), sexual dysfunction (decreased libido, decreased erection). Symptoms may worsen temporarily during first weeks of therapy. Report unusual nausea or vomiting, any chest pain, respiratory difficulty, unresolved dizziness, or constipation. Pregnancy/breast-feeding precautions: Inform prescriber if you are pregnant; do not get pregnant 1 month before, during, or for 1 month following therapy. Consult prescriber for instruction on appropriate contraceptive measures. This drug may cause severe fetal defects. Do not donate blood during or for 1 month following therapy (same reason). Do not breast-feed.

Do not try to aspirate with the goserelin syringe, if the needle is in a large vessel, blood will immediately appear in syringe chamber

Stability: Protect from light; store at room temperature

Injection, implant: 3.6 mg single dose disposable syringe with 16-gauge hypodermic needle; 10.8 mg single dose disposable syringe with 14-gauge hypodermic needle

Ahmann FR, Citrin DL, deHaan HA, et al, "Zoladex: A Sustained-Release, Monthly Luteinizing Hormone-Releasing Hormone Analog for the Treatment of Advanced Prostate Cancer," J Clin Oncol, 1987, 5(6):912-7.

Brogden RN and Faulds D, "Goserelin. A Review of Its Pharmacodynamic and Pharmacokinetic Properties and Therapeutic Efficacy in Prostate Cancer," Drugs Aging, 1995, 6(4);324-43.

Goldspiel BR and Kohler DR, "Goserelin Acetate Implant: A Depot Luteinizing Hormone-Releasing Hormone Analog for Advanced Prostate Cancer," DICP, 1991, 25(7-8):796-804.

Jeffrey LP, Chairman, National Study Commission on Cytotoxic Exposure. Position Statement. "The Handling of Cytotoxic Agents by Women Who Are Pregnant, Attempting to Conceive, or Breast-Feeding," January 12, 1987.

Peeling WB, "Phase III Studies to Compare Goserelin (Zoladex) With Orchiectomy and With Diethylstilbestrol in Treatment of Prostatic Carcinoma," Urol, 1989, 33(5 Suppl):45-52.

Robertson JF, Nicholson RI, Walker KJ, et al, "Zoladex in Advanced Breast Cancer," Horm Res, 1989, 32 (Suppl 1):206-8.