Arimidex 1

• Adjuvant treatment of hormone receptor-positive early breast cancer in postmenopausal women
• First-line treatment of hormone receptor-positive or unknown locally advanced or metastatic breast cancer in postmenopausal women
• Second-line treatment of advanced breast cancer in postmenopausal women with disease progression following tamoxifen therapy

Anastrozole is a non-steroidal aromatase inhibitor. The growth of many breast cancers is stimulated or maintained by estrogens. In postmenopausal women, estrogens are mainly derived from the action of the aromatase enzyme, which converts adrenal androgens (primarily androstenedione and testosterone) to estrone and estradiol. Anastrozole specifically inhibits the aromatase enzyme, suppressing estrogen biosynthesis in peripheral tissues and in cancer tissue itself.

Anastrozole prevents the conversion of androstenedione to estrone and testosterone to estradiol, leading to significantly reduced serum estradiol concentrations.

Adult Dose:

• Recommended dose: 1 mg tablet once daily
• Adjuvant treatment of early breast cancer: Optimal duration unknown
• Advanced breast cancer: Continue until tumor progression

Hepatic Dose: No dose adjustment needed for mild-to-moderate hepatic impairment. Not studied in severe hepatic impairment.

Renal Dose: No dose adjustment necessary for renal impairment.

Special Populations: Pharmacokinetics not affected by age. Safety and efficacy in pediatric patients not established.

Common (>10%):

• Hot flashes
• Asthenia
• Arthritis
• Pain
• Arthralgia
• Hypertension
• Depression
• Nausea and vomiting
• Rash
• Osteoporosis
• Fractures
• Back pain
• Insomnia
• Headache
• Bone pain
• Peripheral edema
• Increased cough
• Dyspnea
• Pharyngitis
• Lymphedema

Rare (<0.01%):

• Skin reactions (lesions, ulcers, blisters)
• Allergic reactions (swelling of face, lips, tongue, throat - difficulty swallowing and/or breathing)
• Liver function changes (jaundice, liver pain or swelling)

[CONSULT YOUR DOCTOR] Anastrozole is unsafe to use during pregnancy (Category X). There is definite evidence of risk to the developing baby. Discontinue if pregnancy is detected.

Serious Precautions:

• Do not use during pregnancy or in premenopausal women
• Caution in pre-existing ischemic heart disease (increased risk of ischemic cardiovascular events)
• Bone density decrease and osteoporosis may occur - regular bone density testing recommended
• Cholesterol may increase - regular monitoring needed
• May cause weakness and sleepiness - do not drive if affected
• If nausea bothers you, take after meals
• Regular Vitamin D and bone mineral density monitoring recommended

Single doses up to 60 mg in healthy males and 10 mg daily in advanced breast cancer patients were well tolerated. Life-threatening dose not established. No specific antidote; symptomatic treatment required.

Store below 30°C, away from light & moisture. Keep out of reach of children.