ATZ

White film coated tablet, round, biconvex tablet with the inscription ANA and 1 on one side.
Each film coated tablet contains 1 mg anastrozole.
Excipients/Inactive Ingredients: Lactose monohydrate, povidone, sodium starch glycolate, magnesium stearate, hypromellose, macrogol 400, titanium dioxide.

Pharmacotherapeutic group: Enzyme inhibitors. ATC Code: L02B G03.
Pharmacology: Pharmacodynamics: Anastrozole is a potent and highly selective nonsteroidal aromatase inhibitor. In postmenopausal women, oestradiol is produced primarily from the conversion of androstenedione to oestrone through the aromatase enzyme complex in peripheral tissues. Oestrone is subsequently converted to oestradiol. Reducing circulating oestradiol levels has been shown to produce beneficial effects in women with breast cancer.
In postmenopausal women, Anastrozole at a daily dose of 1 mg produced oestradiol suppression of greater than 80% using a highly sensitive assay.
Anastrozole does not possess any progestogenic, androgenic or oestrogenic activity.
Daily doses of Anastrozole up to 10 mg do not have any effect on cortisol or aldosterone secretion, measured before or after standard ACTH challenge testing. Corticoid supplements are therefore not needed.
Pharmacokinetics: The pharmacokinetics parameters of 24 subjects were calculated and results were statistically analyzed to demonstrate bioequivalence in a randomized, 2-period, crossover design study. After oral administration of Anastrozole 1 mg film coated tablets (test product), the mean of the maximum plasma concentration (C_max) (rate of absorption) was 15.47 ng/mL, the median t_max was 1.43 h. The extent of absorption is expressed in Area Under the Curve (AUC)_0-t and AUC_0-inf, the mean values were 575.58 ng.h/mL and 628.47 ng.h/mL respectively. The mean elimination half-life (t_½) of Anastrozole 1 mg film coated tablets was 41.01 h.
The T/R ratios and confidence intervals between test and reference product were as follows: for C_max the T/R ratio was 99.94% (96.01%-104.02%). For AUC_0-t the T/R ratio was 98.57% (95.35%-101.90%). The results of the study showed that the T/R ratios and confidence intervals are within the acceptance range for bioequivalence, therefore it can be concluded that the test product, Anastrozole 1 mg film coated tablets, is bioequivalent with the reference product.

Treatment of advanced breast cancer in postmenopausal women with oestrogen receptor positive and or progesterone receptor positive.

Adults including elderly: One 1 mg tablet to be taken orally once a day. For patients with advanced breast cancer, Anastrozole should be continued until tumor progression.
Children: The use of Anastrozole is not recommended in children, as efficacy has not been established.
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 disease.

There is no specific antidote to overdosage and treatment must be symptomatic. In the management of an overdose, consideration should be given to the possibility that multiple agents may have been taken. Vomiting may be induced if the patient 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: Pre-menopausal women.
Pregnant or lactating women.
Patients with severe renal impairment (creatinine clearance less than 20 ml/min).
Patient with moderate or severe hepatic disease.
Patients with known hypersensitivity to anastrozole or to any of the excipients as referenced on Description.
Oestrogen-containing therapies should not be co-administered with Anastrozole as they would negate its pharmacological action.
Concurrent tamoxifen therapy (see Interactions).

Anastrozole is not recommended for use in children, as safety and efficacy have not been established in this group of patients.
Anastrozole should not be used in pre-menopausal women (see Contraindications). The menopause should be defined biochemically (luteinizing hormone [LH], follicle stimulating hormone [FSH] and/or estradiol levels) in any patient where there is doubt about hormonal status. There are no data available for the use of Anastrozole with LHRH analogues.
This combination should not be used outside clinical trials.
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).
As Anastrozole lowers circulating oestrogen levels it may cause a reduction in bone mineral density with a possible consequent increased risk of fractures. This possible increased risk should be managed according to treatment guidelines or managing bone health in postmenopausal women.
Women with osteoporosis or at risk of osteoporosis should have their bone mineral density formally assessed by bone densitometry at the commencement of treatment and at regular intervals thereafter.
Treatment or prophylaxis for osteoporosis should be initiated as appropriate and carefully monitored.
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.
Effects on ability to drive and operate machinery: Anastrozole is unlikely to impair the ability of patients to drive and operate machinery. However, asthenia and somnolence have been reported with the use of Anastrozole and caution should be observed when driving or operating machinery while such symptoms persist.

Anastrozole is contraindicated in pregnant or lactating women.

(See table.)


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As Anastrozole lowers circulating oestrogen levels, it may cause a reduction in bone mineral density placing some patients at a higher risk of fracture (see Precautions).
Ischaemic cardiovascular events were reported more frequently in patients treated with Anastrozole compared to those treated with tamoxifen, although the difference was not statistically significant. The observed difference was mainly due to more reports of angina pectoris and was associated with a subgroup of patients with pre-existing ischaemic heart disease.

Co-administration of Anastrozole with other drugs such as Antipyrine and Cimetidine is unlikely to result in clinically significant drug interactions mediated by cytochrome P450.
Oestrogen-containing therapies should not be co-administered with Anastrozole as they would negate its pharmacological action.
Tamoxifen and/or other therapies containing oestrogen should not be co-administered with Anastrozole, as they may diminish its pharmacological action (see Contraindications).

Incompatibilities: Not applicable.

Store below 30°C.
Shelf-life: 36 months.

Cancer Hormone Therapy

L02BG03 - anastrozole ; Belongs to the class of enzyme inhibitors. Used in treatment of neoplastic diseases.

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