Arodex

Arodex Tablet

The growth of many cancers of the breast is stimulated or maintained by estrogens. In postmenopausal women, estrogens are mainly derived from the action of the aromatase enzyme, which converts adrenal androgens (primarily androstenedione and testosterone) to estrone and estradiol. The suppression of estrogen biosynthesis in peripheral tissues and in the cancer tissue itself can therefore be achieved by specifically inhibiting the aromatase enzyme.

Arodex is a selective non-steroidal aromatase inhibitor. It significantly lowers serum estradiol concentrations and has no detectable effect on formation of adrenal corticosteroids or aldosterone.

Uses

Adjuvant treatment of post-menopausal women with hormone receptor-positive early breast cancer, and also advanced breast cancer in post-menopausal women. First-line treatment of hormone receptor-positive post-menopausal women who have received 2 to 3 years of adjuvant tamoxifen.

Arodex is also used to associated treatment for these conditions: Advanced Breast Cancer, Early Breast Cancer, Locally Advanced Breast Cancer (LABC), Metastatic Breast Cancer, Invasive, early Breast Cancer

Arodex

Trade Name Arodex
Generic Anastrozole
Anastrozole Other Names Anastrozol, Anastrozole
Weight 1 mg
Type Tablet
Formula C17H19N5
Weight Average: 293.3663
Monoisotopic: 293.164045633
Protein binding

Anastrozole is 40% protein bound in plasma and appears to be independent of plasma concentration.

Therapeutic Class Hormonal Chemotherapy
Manufacturer Techno Drugs Ltd
Available Country Bangladesh
Last Updated: June 23, 2021 at 11:16 am

Structure

Arodex
Anastrozole Structure

Dosage

Arodex dosage

Adults and elderly: 1 mg tablet to be taken orally once a day.

Side Effects

More common side effects are: Blurred vision chest pain or discomfort, dizziness, headache nervousness, pounding in the ears, shortness of breath, slow or fast heartbeat, swelling of the feet or lower legs

Precaution

There are no data to support the safe use of anastrozole in patients with moderate or severe hepatic impairment, or patients with severe impairment of renal function (creatinine clearance less than 20 mL/min). Women with osteoporosis or at risk of osteoporosis should have their bone mineral density at regular intervals monitored.

There are no data available for the use of anastrozole with LHRH analogues. This product contains lactose. Patients with rare hereditary problems of galactose intolerance, the lapp lactase deficiency or glucose-galactose malabsorption should not take this medicine.

Interaction

Antipyrine and cemetidine clinical interaction studies indicate that the co administration of anastrozole with other drugs is unlikely to result in clinically significant drug interactions mediated by cytochrome P450. Tamoxifen should not be co-administered with anastrozole as this may reduce its pharmacological action.

Food Interaction

  • Take with or without food. Co-administration with food reduces the rate, but not the overall extent, of absorption.

Volume of Distribution

The volume of distribution of anastrozole into brain tissue in mice is 3.19 mL/g. Distribution into the CNS is limited due to the activity of P-gp efflux pumps at the blood brain barrier, of which anastrozole is a substrate.

Half Life

The elimination half-life of anastrozole is approximately 50 hours.

Clearance

Arodex's clearance is mainly via hepatic metabolism and can therefore be altered in patients with hepatic impairment - patients with stable hepatic cirrhosis exhibit an apparent oral clearance approximately 30% lower compared with patients with normal liver function. Conversely, renal impairment has a negligible effect on total drug clearance as the renal route is a relatively minor clearance pathway for anastrozole. In volunteers with severe renal impairment, renal clearance was reduced by 50% while total clearance was only reduced by approximately 10%.

Pregnancy & Breastfeeding use

Arodex is contraindicated in pregnant and lactating women.

Contraindication

Patients with severe renal impairment (Creatinine clearance less than 20 mL/min), patients with moderate to severe hepatic disease and known hypersensitivity to anastrozole or to any of the excipients. Oestrozen-containing therapies should not be co-administered with anastrazole as they would negate its pharmacological action.

Special Warning

Renal impairment: No dose change is recommended in patients with mild or moderate renal impairment.

Hepatic impairment: No dose change is recommended in patients with mild hepatic impairment. For early disease, the recommended duration of treatment should be 5 years.

Acute Overdose

Clinical trials have been conducted with Arodex tablets, up to 60 mg in a single dose given to healthy male volunteers and up to 10 mg daily given to postmenopausal women with advanced breast cancer; these dosages were tolerated. A single dose of Arodex tablets that results in life-threatening symptoms has not been established. There is no specific antidote to overdosage and treatment must be symptomatic.

In the management of an overdose, consider that multiple agents may have been taken. Vomiting may be induced if the patient is alert. Dialysis may be helpful because Arodex tablet is not highly protein bound. General supportive care, including frequent monitoring of vital signs and close observation of the patient, is indicated.

Storage Condition

Product should be stored within 30°C

Innovators Monograph

Arodex contains Anastrozole see full prescribing information from innovator // generic/anastrozole/anastrozole-prescribing-information" Monograph