Anastrozole

Registered South African indications:

• Early and late breast cancer in postmenopausal women

• Receptor-positive metastatic breast cancer in postmenopausal women

Contraindications

• Hypersensitivity to the active ingredient or any of its excipients
• Pregnancy
• Breastfeeding

Cautions

• Severe renal impairment
• Moderate to severe hepatic impairment
• Children and adolescents
• Pre-menopausal women
• Osteoporosis or risk thereof
• Galactose intolerance
• Total lactase deficiency
• Glucose-galactose malabsorption
• May impair ability to drive or operate machinery

Forms avail. in SA and covered in this monograph: tab

Early and late breast cancer in postmenopausal women

• Oral (tab): 1mg, dly

Receptor-positive metastatic breast cancer in postmenopausal women

• Oral (tab): 1mg, dly

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5 years of hormonal blockade is recommended, this can be achieved with 5 years of continuous anastrozole treatment

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Use is also indicated in postmenopausal women who have received 2 to 3 years of adjuvant tamoxifen

Not established for use in children

Pregnancy

• Contraindicated
• There are no data from the use of anastrozole in pregnant women. Studies in animals have shown reproductive toxicity; thus anastrozole is contraindicated during pregnancy

Breastfeeding

• Contraindicated
• There are no data on the use of anastrozole during breastfeeding; thus anastrozole is contraindicated during breastfeeding

Fertility

• The effects of anastrozole on fertility in humans have not been studied. Studies in animals have shown reproductive toxicity

Renal Impairment

• Mild to moderate: No dose adjustment recommended
• Severe: Caution; no dose adjustment recommended 

Hepatic Impairment

• Mild: No dose adjustment recommended
• Moderate to severe: Caution; no dose adjustment recommended

Elderly

• No dose adjustment recommended

Porphyria Information

• Probably not porphyrinogenic (PNP)

Drugs in Sport

• Prohibited - At all times

Central Nervous System Disorders

• Mood disturbances
• Headache
• Depression
• Weakness
• Somnolence
• Paraesthesia
• Asthenia

Cardiovascular Disorders

• Ischaemic cardiovascular disease
• Myocardial infarct
• Coronary artery disorder
• Myocardial ischaemia
• Venous thromboembolic events including pulmonary embolism
• Ischaemic cerebrovascular events
• Angina pectoris
• Hot flushes

Gastrointestinal Disorders

• Nausea and vomiting
• Diarrhoea

Hepatobiliary Disorders

• Increased alkaline phosphatase
• Increased alanine aminotransferase
• Increased aspartate aminotransferase
• Increased gamma-GT
• Increased bilirubin
• Hepatitis

Genitourinary Disorders

• Vaginal dryness
• Vaginal bleeding
• Vaginal discharge
• Endometrial cancer

Endocrine and Metabolic Disorders

• Decreased bone mineral density
• Anorexia
• Hypercholesterolaemia
• Hypercalcaemia (with or without an increase in parathyroid hormone)

Musculoskeletal Disorders

• Arthritis
• Arthralgia
• Joint stiffness
• Bone pain
• Myalgia
• Trigger finger
• Osteoporosis
• Fractures

Skin and Subcutaneous Tissue Disorders

• Rash
• Urticaria
• Aloplecia
• Erythema multiforme
• Cutaneous vasculitis
• Henoch-Schönlein purpura
• Steven-Johnson syndrome

Immune, Blood and Lymphatic Disorders

• Allergic reactions
• Anaphylactoid reaction
• Angioedema
• Leucopenia

Sensory Disorders

• Sensory disturbances
• Taste loss
• Taste perversion
• Cataracts

Others

• Carpal tunnel syndrome

• Tamoxifen
• Oestrogen-containing therapy

• Bone mineral density
• Lipid profile
• Pregnancy test

Specific cases may require

• Luteinizing hormone (LH), follicle stimulating hormone (FSH), and/or estradiol levels

Premenopausal women

• Anastrozole should not be used in premenopausal women. The menopause should be defined biochemically with luteinizing hormone (LH), follicle stimulating hormone (FSH), and/or estradiol levels in any patient where there is doubt about menopausal status

Paediatric population

• Anastrozole is not recommended for use in children and adolescents as safety and efficacy have not been established in this group of patients
• Anastrozole should not be used in boys with growth hormone deficiency in addition to growth hormone treatment
• Since anastrozole reduces estradiol levels, it must not be used in girls with growth hormone deficiency in addition to growth hormone treatment

Anastrozole is a potent and highly selective non-steroidal aromatase inhibitor. In postmenopausal women, estradiol is produced primarily from the conversion of androstenedione to estrone through the aromatase enzyme complex in peripheral tissues. Estrone is subsequently converted to estradiol. Reducing circulating estradiol levels has been shown to produce a beneficial effect in women with breast cancer. Anastrozole does not possess any progestogenic, androgenic or estrogenic activity.

Tablet 1mg 

• Accord anastrozole fct (Accord)
• Anabrez 1 fct (Ranbaxy)
• Anastrozole sandoz (Sandoz)
• Arimidex (AstraZeneca) originator
• Castra 1 (Zydus)
• Everdex (AstraZeneca)
• Medivision anastrozole (Medivision)
• Mylan anastrozole (Xixia)
• Stradexa fct (Eurolab)
• Teva anastrozole fct (Teva)
• Zostracol (Hetero Drugs South Africa)