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Drug Details

Nastrosa 1mg film-coated tablets

• Presentation
  Film-coated tablet. White, round, biconvex, film-coated tablets. Debossed with '1' on one side and plain on the reverse side
• Description
  Each tablet contains 1 mg anastrozole as active substance. Excipients: Each tablet contains 90.3 mg lactose (as lactose monohydrate).
• Indications
  Treatment of advanced breast cancer in postmenopausal women. Efficacy has not been demonstrated in oestrogen receptor-negative patients unless they had a previous positive clinical response to tamoxifen.
• Adult Dosage
  

  Adults including the elderly:	One 1 mg tablet to be taken orally once a day.
  Children:	Not recommended for use in children.
  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

• Contra Indications
  

  Anastrozole is contraindicated in:

  - premenopausal women.

  - pregnant or lactating women.

  - patients with severe renal impairment (creatinine clearance less than 20 ml / min)

  - patients with moderate or severe hepatic disease

  - patients with hypersensitivity to anastrozole or to any of the excipients as referenced in section 6.1.

  Oestrogen-containing therapies should not be co-administered with anastrozole as they would negate its pharmacological action.

  Concurrent tamoxifen therapy

• Special Precautions
  

  Anastrozole is not recommended for use in children as safety and efficacy have not been established in this group of patients.

  The menopause should be defined biochemically in any patient where there is doubt about hormonal status.

  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 formally assessed by bone densitometry e.g. DEXA scanning at the commencement of treatment and at regular intervals thereafter. Treatment or prophylaxis for osteoporosis should be initiated as appropriate and carefully monitored.

  There are no data available for the use of anastrozole with LHRH analogues. This combination should not be used outside clinical trials.

  As anastrozole lowers circulating oestrogen levels it may cause a reduction in bone mineral density. Adequate data to show the effect of bisphosphonates on bone mineral density loss caused by anastrozole, or their utility when used prophylactically, are not currently available.

  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.

• Interactions
  

  Anastrozole inhibited cytochrome P450 1A2, 2C8/9 and 3A4 in vitro. A clinical interaction study indicated that anastrozole at a 1 mg dose does not significantly alter the pharmacokinetics of warfarin, a CYP2C9 substrate.

  No clinically significant interactions between anastrozole and bisphosphonates have been identified.

  Antipyrine and cimetidine clinical interaction studies indicate that co-administration of anastrozole with other drugs is unlikely to result in clinically significant drug interactions mediated by cytochrome P450.

  A review of the clinical trial safety datatbase did not reveal evidence of clinically significant interaction in patients treated with anastrozole who also received other commonly prescribed drugs.

  Tamoxifen should not be co-administered with anastrozole, as this may diminish its pharmacological action.

• Adverse Drug Reactions
  

  The assessment of the side effects is based on the following frequencies:

  Very common (1/10)

  Common (1/100 to <1/10)

  Uncommon (1/1,000 to<1/100)

  Rare (1/10,000 to<1/1,000)

  Very rare (<1/10,000), not known (cannot be estimated from the available data).

  Within each frequency grouping, undesirable effects are presented in order of decreasing seriousness.

   

  Nervous system disorders

  Common: Headache, mainly mild or moderate in nature

  Carpal Tunnel Syndrome

  Uncommon: Somnolence, mainly mild or moderate in nature

   

  Gastrointestinal disorders

  Common: Nausea, mainly mild or moderate in nature, diarrhoea, mainly mild or moderate

  Uncommon: Vomiting, mainly mild or moderate in nature

   

  Skin and subcutaneous tissue disorders

  Common: Hair thinning, mainly mild or moderate in nature, Rash, mainly mild or moderate in nature

  Very rare: Erythema multiforme, Stevens-Johnson syndrome, allergic reactions including angiooedema, urticaria and anaphylaxis

   

  Musculoskeletal and connective tissue disorders

  Common: Joint pain/stiffness, mainly mild or moderate in nature

   

  Metabolism and nutrition disorders

  Uncommon: Anorexia, mainly mild in nature, hypercholesterolaemia, mainly mild or moderate in nature

   

  Vascular disorders

  Very common: Hot flushes, mainly mild or moderate in nature

   

  General disorders and administration site conditions

  Common: Asthenia, mainly mild or moderate in nature

   

  Hepatobiliary disorders

  Common: Increases in alkaline phosphatase, alanine aminotransferase and aspartate aminotransferase

  Uncommon: Increases in gamma-GT and bilirubin, hepatitis

   

  Reproductive system and breast disorders

  Common: Vaginal dryness, mainly mild or moderate in nature

  Uncommon: Vaginal bleeding, mainly mild or moderate in nature*

  *Vaginal bleeding has been reported uncommonly, mainly in patients with advanced breast cancer during the first few weeks after changing from existing hormonal therapy to treatment with anastrozole. If bleeding persists, further evaluation should be considered.

  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 section 4.4).

  Elevated gamma-GT has been reported uncommonly (0.1% and <1%). A causal relationship for these this changes has not been established.

  The table below presents the frequency of pre-specified adverse events in the ATAC study, irrespective of causality, reported in patients receiving trial therapy and up to 14 days after cessation of trial therapy.

   

  Adverse effects	Anastrozole (N=3092)	Tamoxifen (N=3094)
  Hot flushes	1104 (35.7%)	1264 (40.9%)
  Joint pain/stiffness	1100 (35.6%)	911 (29.4%)
  Mood disturbances	597 (19.3%)	554 (17.9%)
  Fatigue/asthenia	575 (18.6%)	544 (17.6%)
  Nausea and vomiting	393 (12.7%)	384 (12.4%)
  Fractures	315 (10.2%)	209 (6.8%)
  Fractures of the spine, hip, or wrist/Colles	133 (4.3%)	91 (2.9%)
  Wrist/Colles fractures	67 (2.2%)	50 (1.6%)
  Spine fractures	43 (1.4%)	22 (0.7%)
  Hip fractures	28 (0.9%)	26 (0.8%)
  Cataracts	182 (5.9%)	213 (6.9%)
  Vaginal bleeding	167 (5.4%)	317 (10.2%)
  Ischaemic cardiovascular disease	127 (4.1%)	104 (3.4%)
  Angina pectoris	71 (2.3%)	51 (1.6%)
  Myocardial infarct	37 (1.2%)	34 (1.1%)
  Coronary artery disorder	25 (0.8%)	23 (0.7%)
  Myocardial ischaemia	22 (0.7%)	14 (0.5%)
  Vaginal discharge	109 (3.5%)	408 (13.2%)
  Any venous thromboembolic event	87 (2.8%)	140 (4.5%)
  Deep venous thromboembolic events including PE	48 (1.6%)	74 (2.4%)
  Ischaemic cerebrovascular events	62 (2.0%)	88 (2.8%)
  Endometrial cancer	4 (0.2%)	13 (0.6%)

  Fracture rates of 22 per 1000 patient-years and 15 per 1000 patient-years were observed for the anastrozole and tamoxifen groups, respectively, after a median follow-up of 68 months. The observed fracture rate for anastrozole is similar to the range reported in age-matched postmenopausal populations. It has not been determined whether the rates of fracture and osteoporosis seen in ATAC in patients on anastrozole treatment reflect a protective effect of tamoxifen, a specific effect of anastrozole, or both. The incidence of osteoporosis was 10.5% in patients treated with anastrozole and 7.3% in patients treated with tamoxifen.