Products
Anastrozole is commercially available in the form of film-coated tablets (Arimidex, generic). It has been approved in many countries since 1996.
Structure and properties
Anastrozole (C17H19N5, Mr = 293.4 g/mol) exists as a white powder that is very sparingly soluble in water. It is a triazole derivative with a non-steroidal structure.
Effects
Anastrozole (ATC L02BG03) has antitumor and antiproliferative properties. The effects are due to competitive inhibition of the enzyme aromatase, which catalyzes the biosynthesis of estrogens from androgens such as androstenedione. This lowers serum estradiol concentrations. Anastrozole has a long half-life of 40 to 50 hours.
Indications
For adjuvant treatment of breast cancer and for treatment of advanced breast cancer in postmenopausal women.
Dosage
According to the SmPC. Tablets are taken once daily at the same time of day, regardless of meals.
Abuse
Anastrozole can be abused as a doping agent and for bodybuilding. It is prohibited during and outside of athletic competition.
Contraindications
- Hypersensitivity
- Pregnancy, lactation
Full precautions can be found in the drug label.
Interactions
Estrogens may reverse the effects of anastrozole and should not be administered concomitantly.
Adverse effects
Adverse effects are largely a result of reduced estrogen levels and resemble menopausal symptoms. The most common possible adverse effects include:
- Hot flashes
- Headache
- Muscle pain, joint pain, fractures, joint stiffness, arthritis.
- Nausea
- Mood swings
- Fatigue
- Skin rash