Each film-coated tablet contains: Anastrozole 1 mg.
Anastrozole is a non-steroidal aromatase inhibitor. It is chemically described as 1,3-Benzene diacetonitrile, α, α, α', α'-tetramethyl-S-(IH-1.2,4-triazol-1-ylmethyl). Its molecular formula is C17H19N5.
Pharmacologic Classification: Antineoplastic (Aromatase Inhibitor). ATC code: L02B G03.
Pharmacology: Pharmacodynamics: Mechanism of action: Many breast cancers have estrogen receptors and growth of these tumors can be stimulated by estrogen. In postmenopausal women, the principal source of circulating estrogen (primarily estradiol) is conversion of adrenally generated androstenedione to estrone by aromatase in peripheral tissues with further conversion of estrone to estradiol. Many breast cancers also contain aromatase. Treatment of breast cancers included efforts to decrease oestrogen levels. Anastrozole is a potent and highly selective non-steroidal aromatase inhibitor. As with other aromatase inhibitors, Anastrazole lowers oestrogen levels in postmenopausal women by inhibiting conversion of adrenally-generated androstenedione (adrenal androgens) to estrone by aromatase in peripheral tissues. Estrone is subsequently converted to estradiol. Adrenally generated androstenedione is the chief source of circulating estrogen in postmenopausal women. Reducing circulating estradiol levels has been shown to produce a beneficial effect in women with breast cancer.
Pharmacokinetics: Anastrozole is rapidly and almost completely absorbed from the gastrointestinal tract after oral doses, with peak plasma concentrations within about 2 hours. Food decreases the rate of absorption, though this is not considered clinically significant. Anastrozole is 40% bound to plasma proteins. It is metabolised in the liver, and excreted in urine, chiefly as metabolites. The terminal plasma elimination half-life is about 40 to 50 hours, and steady-state concentrations are achieved after about 7 days in patients receiving once-daily doses.
For the treatment of breast cancer in post-menopausal women.
One (1 mg) tablet should be taken once a day. For patients with advanced breast cancer, anastrozole should be continued until tumor progression.
Patients with Hepatic Impairment: no change in dose are recommended. For patients with mild-to-moderate hepatic impairment, although patients should be monitored for side effects. Anastrozole has not been studied in patients with severe hepatic impairment.
Patients with Renal impairment: No changes in dose are necessary for patients with renal impairment.
Use in the Elderly: No dosage adjustment is necessary.
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 patients is alert. Dialysis may be helpful because anastrozole is not highly protein bound. General supportive care, including frequent monitoring of vital signs and close observation of the patient, is indicated.
Anastrozole is contraindicated in any patient who has shown a hypersensitivity reaction to the drug or to any of the excipients.
Anastrozole can cause fetal harm when administered to a pregnant woman. Anastrozole has been found to cross the placenta following oral administration of 0.1 mg/g in rats and rabbits (about 1 and 1.9 times the recommended human dose, respectively, on a mg/m2 basis). Studies in both rats and rabbits at doses equal to or greater than 0.1 and 0.02 mg/kg/day, respectively (about 1 and 1/3, respectively, the recommended human dose on a mg/m2 basis), administered during the period of organogenesis showed that anastrozole increased pregnancy loss (increased pre- and/or post-implantation loss, increased resorption, and decreased numbers of live fetuses); effects were dose related in rats. Placental weights were significantly increased in rats at doses of 0.1 mg/kg/day or more. Evidence of fetotoxicity, including delayed fetal development (i.e., incomplete ossification and depressed fetal body weights), was observed in rats administered doses of 1 mg/kg/day (which produced plasma anastrozole Cmax and AUC0-24 hr that were 19 times and 9 times higher than the respective values found in postmenopausal volunteers at the recommended dose). There was no evidence of teratogenicity in rats administered doses up to 1.0 mg/kg/day.
In rabbits, anastrozole caused pregnancy failure at doses equal to or greater than 1.0 mg/kg/day (about 16 times the recommended human dose on a mg/m2 basis); there was no evidence of teratogenicity in rabbits administered 0.2 mg/kg/day (about 3 times the recommended human dose on a mg/m2 basis). If anastrozole is used during pregnancy, or if the patient becomes pregnant while receiving this drug, the patient should be apprised of the potential hazard to the fetus or potential risk for loss of the pregnancy.
Anastrozole can cause fetal harm when administered to a pregnant woman. Anastrozole has been found to cross the placenta following oral administration of 0.1 mg/g in rats and rabbits (about 1 and 1.9 times the recommended human dose, respectively, on a mg/m2 basis). Studies in both rats and rabbits at doses equal to or greater than 0.1 and 0.02 mg/kg/day, respectively (about 1 and 1/3, respectively, the recommended human dose on a mg/m2 basis), administered during the period of organogenesis showed that anastrozole increased pregnancy loss (increased pre- and/or post-implantation loss, increased resorption, and decreased numbers of live fetuses); effects were dose related in rats. Placental weights were significantly increased in rats at doses of 0.1 mg/kg/day or more. Evidence of fetotoxicity, including delayed fetal development (i.e., incomplete ossification and depressed fetal body weights), was observed in rats administered doses of 1 mg/kg/day (which produced plasma anastrozole Cmax and AUC0-24 hr that were 19 times and 9 times higher than the respective values found in postmenopausal volunteers at the recommended dose). There was no evidence of teratogenicity in rats administered doses up to 1.0 mg/kg/day.
In rabbits, anastrozole caused pregnancy failure at doses equal to or greater than 1.0 mg/kg/day (about 16 times the recommended human dose on a mg/m2 basis); there was no evidence of teratogenicity in rabbits administered 0.2 mg/kg/day (about 3 times the recommended human dose on a mg/m2 basis). If anastrozole is used during pregnancy, or if the patient becomes pregnant while receiving this drug, the patient should be apprised of the potential hazard to the fetus or potential risk for loss of the pregnancy.
The most frequent adverse effects are gastrointestinal disturbances including anorexia, nausea and vomiting, and diarrhoea; asthenia; hot flushes; dizziness; drowsiness; headache; and rash. Other reported effects include hair thinning, vaginal dryness or bleeding, myalgia, arthralgia, and bone fractures. Abnormalities in liver enzyme values, thromboembolism, and increases in total cholesterol, have occurred in some patients receiving anastrozole. Very rare cases of erythema multiforme, Stevens-Johnson syndrome, and allergic reactions (including angioedema, urticaria, and anaphylaxis) have occurred. Reductions in bone mineral density can occur during use of anastrozole. Patients with or at risk of osteoporosis should therefore have their bone density assessed at the start of therapy and at regular intervals thereafter. Treatment or prophylaxis for osteoporosis should be started as appropriate and carefully monitored. The use of anastrozole is contra-indicated in premenopausal women (particularly in pregnancy).
Store at temperatures not exceeding 30°C. Protect from light and moisture.
Shelf Life: 24 Months.
L02BG03 - anastrozole ; Belongs to the class of enzyme inhibitors. Used in treatment of neoplastic diseases.
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