Anastrozole
Indications
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.
Description
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.
Pharmacology
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.
Dosage & Administration
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.
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.
Interaction
Tamoxifen and/or other therapies containing estrogen should not be co-administered with Anastrozole.
Side Effects
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.
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.
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.
Therapeutic Class
Hormonal Chemotherapy
Storage Conditions
Store in a cool & dry place, protected from light and moisture. Keep out of reach of children.
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