Anastrozole
Indications
Anastrozole is used for:
Breast cancer, Ovulation induction
Adult Dose
Oral
Advanced or locally advanced breast cancer, Adjuvant treatment in early breast cancer
Adult: In postmenopausal women: 1 mg daily. Adjuvant treatment may be continued for up to 5 yr.
Hepatic Impairment
Mild-to-moderate impairment or stable hepatic cirrhosis: Dose adjustment not necessary
Severe hepatic impairment: Not studied
Child Dose
Renal Dose
Administration
May be taken with or without food.
Contra Indications
Pregnancy. Hypersensitivity, premenopausal women.
Precautions
Moderate or severe hepatic impairment, hyperlipidaemias. Laboratory test for menopause if status is doubtful. Bone mass density test should be conducted at the start of the therapy and at regular intervals thereafter.
Lactation: Unknown whether drug is excreted in milk; not recommended given potential for serious adverse reactions in nursing infants
Pregnancy-Lactation
Interactions
Efficacy decreased by oestrogens. Plasma concentrations decreased by tamoxifen.
Adverse Effects
Side effects of Anastrozole :
>10%
Hot flashes (12-36%),Vasodilation (25-36%),Fatigue (19%),Mood disturbances (19%),Nausea and vomiting (19%),Weakness (16-19%),Arthritis (17%),Pain (17%),Arthralgia (2-15%),Pharyngitis (14%),Depression (13%),Hypertension (2-13%),Bone pain (11%),Increased cough (11%),Osteoporosis (11%),Rash (8-11%)
1-10%
Accidental injury (10%),Back pain (10%),Fracture (10%),Headache (10%),Insomnia (10%),Peripheral edema (10%),Dyspnea (8-10%),Abdominal pain (9%),Infection (9%),Lymphedema (9%),Diarrhea (8-9%),Constipation (7-9%),Breast pain (8%),Dizziness (8%),Urinary tract infection (8%),Chest pain (7%),Dyspepsia (7%),Paresthesia (5-7%),Anxiety (6%),Cataracts (6%),Flu syndrome (6%),Sinusitis (6%),Vulvovaginitis (6%),Xerostomia (6%),Breast neoplasm (5%),Bronchitis (5%),Cyst (5%),Diaphoresis (5%),Neoplasm (5%),Vaginal bleeding (5%),Fractures of spine, hip, or wrist (4%),Ischemic cardiovascular disease (4%),Vaginal hemorrhage (4%),Vaginitis (4%),Leukorrhea (3-4%),Deep vein thrombosis (2%),Endometrial cancer (intact uterus at baseline) (2%),Ischemic cerebrovascular event (2%),Weight gain (2%),Lethargy (1%)
Mechanism of Action
Anastrozole prevents conversion of androstenedione to estrone and testosterone to oestradiol by inhibiting aromatase, thus leading to significantly reduced serum oestradiol concentrations.