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Document Type

Drug Monographs
Treatment Regimens

Scientific Name:
ANASTROZOLE
Brand Name(s):
Arimidex®

Drug Monograph

Pharmacology

Mechanism of Action

Selective, nonsteroidal aromatase inhibitor, with no detectable effect on synthesis of adrenal corticosteroids or aldosterone. It inhibits the activity of aromatase enzyme responsible for the conversion of androstenedione to estrone, and testosterone to estradiol. Causes an 85% reduction in estrone sulfate levels.

Pharmacokinetics

Oral Absorption:
well absorbed (80%), may be absorbed in the presence of food
Distribution:
crosses the placenta; Excretion in breast milk unknown
Cross blood brain barrier?  No information
Vd: No information    PPB: 40%
Metabolism:
hepatic- N-deallylation, hydroxylation, glucuronidation
metabolite(s): active- no information
inactive- triazole (1o metabolite)
Excretion:
biliary 85%, renal 11% (~10% unchanged, 60% as metabolites)
urine   yes
t½ : 50 hours
Cl   no information

Side Effects

IMMEDIATE ONSET (hours to days)
   vasodilatation (36%)
   hypertension (13%)
EARLY ONSET
(days to weeks)
   hot flashes (13-36%)
   weakness (asthenia- 19%), arthralgia (15%)
   back pain (12%), bone pain (11%), osteoporosis (11%), fractures (10%)
   nausea (11-19%),
vomiting (8%)
   headache (9%), depression (5%), mood disturbance (19%)
   skin rash (8-11%)
   lymphedema (10%), peripheral edema (10%)
   dyspnea (8%), cough (8%)
* ischemic cardiovascular events (4%), chest pain (7%)
   cataracts (6%)
   trouble breathing (8%), increased coughing (8%)
   pharyngitis (14%), sinusitis (6%)
   insomnia (10%), dizziness (8%), anxiety (6%)
   diarrhea (8%), constipation (7%), weight gain (2%), anorexia (7%)
   dry mouth (6%), dyspepsia (7%)
   vaginal bleeding (1-5%), vaginitis (6%), vaginal discharge (4%), vaginal dryness (2%)
* blood clots, venous thromboembolic events (3-4%)
   general pain (11%)

Therapeutics

Approved Indications

Breast cancer

Routes

Oral

Dosing

1 mg PO once daily. 
• Administer with food or on empty stomach.

Pediatric: Limited data on the use of this drug in pediatric patients

Contraindications

• Pregnant or lactating women • Patients with thromboembolic conditions, pulmonary emboli, DVT, thromboembolic stroke

Monitoring

Clinical Monitoring

RECOMMENDED CRITERIA
NO RECOMMENDED TOXICITY RATINGS

SUGGESTED CRITERIA
NO ADDITIONAL TOXICITY RATINGS

Significant Interactions

• ARIPiprazole: may increase serum concentration of ARIPiprazole by inhibiting CYP3A4. Aripiprazole dose adjustments may be required. • Digoxin: may decrease absorption of Digoxin. • Estrogen derivatives: may decrease therapeutic effect of Anastrozole (avoid combination) • Methadone: may increase the serum concentration of Methadone • Pimozide: may increase the serum concentration of Pimozide by inhibiting CYP3A4 (avoid combination) • Tamoxifen: may decrease the serum concentration of Anastrozole • Vitamin K Antagonists (e.g. Warfarin): may increase or decrease the anticoagulant effect of Vitamin K antagonists.

Product Information

Commercial Product Description

White tablets with 1mg Anastrozole.

Pharmaceutical Considerations

Tablet
1 mg; inactive ingredient includes lactose. Store at room temperature.

Handling Risk Level

Pregnancy CPOSSIBLE HAZARDOUS DRUG
FDA Pregnancy Risk Factor C

  • Consider handling this drug using precuations outlined in CCNS Policies for Occupational Safety, Preparing Cancer Chemotherapy and Administering Cancer Chemotherapy

Note

HANDLING RISK LEVEL:
HAZARD RISK LEVEL 3
FDA Pregnancy Risk Factor C
• Consider handling this drug using precuations outlined in CCNS Policies for Preparing Cancer Chemotherapy and Administering Cancer Chemotherapy and the CCNS Standard for Oral Systemic Therapy for Cancer
Go to "Additional Information" tab (above) for links to CCNS Policies

Availability & Funding

Administrative Information (Nova Scotia)

• CCNS Provincial Formulary Status- Community Level Take Home Prescription • Go to "Additional Information" tab (above) for links to Provincial Formulary of Cancer Drugs • Pharmacare Formulary Status: Formulary



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