Anastrozole tablet is a potent and highly selective nonsteroidal aromatase inhibitor. Anastrozole selectively inhibits the conversion of androgens to estrogens, without affecting synthesis of adrenal corticosteroid, aldosterone or thyroid hormone. Suppression of estrogen biosynthesis in all tissues reduces serum concentrations of circulating estrogens, including estrone, estradiol, and estrone sulphate with a subsequent beneficial effect in breast cancer.

Anastrazole exerts its anti-estrogenic effects via selective and competitive inhibition of the aromatase enzyme found predominantly in the adrenal glands, liver, and fatty tissues. Many breast cancers are hormone receptor-positive, meaning their growth is stimulated and/or maintained by the presence of hormones such as estrogen or progesterone. In postmenopausal women, estrogen is primarily derived from the conversion of adrenally-produced androgens into estrogens by the aromatase enzyme- by competitively inhibiting the biosynthesis of estrogen at these enzymes, anastrozole effectively suppresses circulating estrogen levels and, subsequently, the growth of hormone receptor-positive tumours.

Anastrozole is indicated in-

• Treatment of early breast cancer in hormone receptor positive post-menopausal women.
• Adjuvant treatment of early breast cancer in hormone receptor positive
• postmenopausal women who have received 2 to 3 years of adjuvant tamoxifen.
• Reduction in the incidence of contralateral breast cancers in post menopausal women receiving Anastrozole as adjuvant treatment for early breast cancer.
• Treatment of advanced breast cancer in post-menopausal women.

Adults Including the Elderly: One tablet (1 mg) to be taken orally once a day.

Children: The use of Anastrozole is not recommended in children, as efficacy has not been established

Renal Impairment: No dose change is recommended.

Hepatic Impairment: No dose change is recommended.

Very common side effects: Hot flushes, asthenia, joint stiffness, arthritis, headache, nausea, rash etc. Common side effects: Hair thinning, allergic reactions, diarrhea, vomiting, somnolence etc.

Overdose Effects

There is limited clinical experience of overdose of Anastrozole. There are no reports where a patient has taken a dose in excess of 60 mg. No toxicity was observed and no clinically relevant adverse effects have been seen.

Pregnancy & Lactation

Anastrozole must not be administered during pregnancy or lactation.

Precautions & Warnings

Anastrozole is not recommended for use in children or in pre-menopausal women as safety and efficacy have not been established in these groups of patients.

• Anastrozole has not been investigated in patients with severe hepatic or severe renal impairment. The potential risk/benefit to such patients should be carefully considered before administration of Anastrozole.
• As Anastrozole lowers circulating estrogen levels, it may cause a reduction in bone mineral density with a possible consequent increased risk of fracture.