Anastrozol

Anastrozol – drug with antineoplastic action.

Form of release and structure

Dosage form of release of Anastrozol – a tablet, film coated: round, biconvex, almost white or white; on a break two layers – white or almost white color a kernel and a film cover (on 7, 10, 14 or 30 pieces in blisters or blister strip packagings, till 1-10 blisters/packagings in a cardboard pack; on 7, 10, 14, 20, 28, 30, 40, 50, 60, 100 or 120 pieces in banks, after 1 bank in a cardboard pack).

Structure of 1 tablet:

• active ingredient: анастрозол – 1 mg;
• auxiliary components: sodium carboxymethylstarch – 2 mg, microcrystallic cellulose – 15,6 mg, monohydrate of lactose (milk sugar) – 72 mg, magnesium stearate – 0,9 mg, polyvinylpirrolidone (povidone) – 3 mg, colloid silicon dioxide – 0,5 mg;
• cover: titanium dioxide – 0,9 mg, a macrogoal of 4000 - 0,45 mg, a gipromelloza – 1,65 mg.

Indications to use

• early gormonopolozhitelny breast cancer at women in the period of a postmenopause (adjuvant therapy);
• early gormonopolozhitelny breast cancer at women in the period of a postmenopause after use for 2-3 years of Tamoxifenum (adjuvant therapy);
• widespread breast cancer at women in the period of a postmenopause (treatment).

Contraindications

Absolute:

• premenopauzalny period;
• liver failure in average/heavy degree (the safety profile for this group of patients is not studied);
• renal failure in heavy degree (at clearance of creatinine <20 ml/min.);
• the combined use with Tamoxifenum or the medicines containing estrogen;
• pregnancy and period of feeding by a breast;
• age up to 18 years (the safety profile for this group of patients is not studied);
• hypersensitivity to drug components.

Relative (Anastrozol appoint with care in the presence of the following diseases / states):

• coronary heart disease;
• hypercholesterolemia;
• osteoporosis;
• functional disturbances of a liver;
• intolerance lactose/insufficiency of lactase / глюкозо-галактозная malabsorption (lactose is a part of drug).

Route of administration and dosage

Anastrozol accept inside, it is more preferable – at the same time. Tablets need to be swallowed entirely and to wash down with water. Meal does not influence efficiency of drug.

Anastrozol appoint on 1 tablet a day. Long therapy is shown. Drug is cancelled in cases of emergence of signs of progressing of a disease. The recommended duration of adjuvant therapy – 5 years.

Dose adjustment at easy/average degree of renal and easy degree of a liver failure is not required.

Side effects

• respiratory system, bodies of a thorax and mediastinum: bronchitis, pharyngitis, sinusitis, short wind;
• lymphatic system and blood: limfedema, anemia, venous thrombembolia;
• urinogenital system: dryness of a mucous membrane of a vagina, a vulvovaginitis, infections of urinary tract, vulval bleedings (as a rule, for the first weeks after cancellation or when changing of the previous hormonal treatment on Anastrozol);
• nervous system: drowsiness, a headache, paresthesia, a depression, dizziness, sleeplessness, concern, a syndrome of a carpal tunnel (as a rule, it was observed with risk factors of a course of a disease);
• cardiovascular system: increase in arterial pressure, rushes of blood to the person;
• skeletal and muscular system and connecting fabrics: arthralgia/constraint of joints, arthritis, trigger finger, muscle/bones pain;
• alimentary system: nausea, dyspepsia, diarrhea, lock, vomiting, gastrointestinal frustration;
• gepatobiliarny system: hepatitis, increase in activity of an alkaline phosphatase, aspartate aminotransferase, alaninaminotranspherase, increase in concentration of bilirubin and activity gamma глутамилтрансферазы;
• skin and hypodermic fabrics: thinning of hair, skin rash, alopecia, sweating;
• organ of sight: cataract;
• metabolism and food: anorexia, increase in body weight, a hypercholesterolemia, a hypercalcemia (with/without increase in concentration of parathormone); decrease in mineral density of a bone tissue because of decrease in concentration of the circulating oestradiol is possible that increases risk of development of fractures of bones and osteoporosis;
• allergic reactions: a small tortoiseshell, anaphylactoid reaction, a multiformny erythema, Stephens-Johnson's syndrome, a skin vasculitis (including separate cases of a purpura), a Quincke's disease;
• others: consecutive infections, adynamy, spin/stomach/breast pain, new growths, grippopodobny syndrome.

Special instructions

Anastrozol's efficiency at a retseptorootritsatelny tumor to estrogen was not shown, except for cases when there is a previous affirmative clinical answer on Tamoxifenum. In the presence of doubts in the hormonal status of the patient the menopause needs to be confirmed with definition of sex hormones in blood serum.

The combined use with the drugs containing estrogen is contraindicated (as they level Anastrozol's action).

At preservation during therapy of uterine bleeding it is necessary to consult at the gynecologist.

At osteoporosis or existence of the increased risk of development of osteoporosis in an initiation of treatment and regularly on its extent the mineral density of a bone tissue needs to be estimated by a densitometry method, for example, a two-power x-ray absorbtsiometriya (DEXA scanning). In cases of need it is necessary to appoint therapy or prevention of osteoporosis, and also to make careful observation of a condition of the patient. Anastrozol lowers concentration of the circulating oestradiol that can lead to reduction of mineral density of a bone tissue. At the moment there are no sufficient data of rather positive action of bisfosfonat on the loss of mineral density of a bone tissue connected with Anastrozol's reception or efficiency of their use for prevention.

Data on the combined Anastrozol's use with drugs analogs of the luteinizing hormone of rileasing-hormone (LHRH) are absent.

Efficiency of the combined use with chemotherapy is not established.

Data on safety of prolonged treatment by Anastrozol are not obtained.

At Anastrozol's use more often than at therapy by Tamoxifenum, development of ischemic diseases was noted, however the statistical importance at the same time was not noted.

As during Anastrozol's use development of such disturbances as dizziness, drowsiness, an adynamy, a headache is possible, it can have an adverse effect on ability to control of motor transport and mechanisms, and also performance of other works demanding the increased concentration of attention and bystry psychomotor reactions (respect for care is necessary).

Medicinal interaction

Clinically significant medicinal interaction of Anastrozol with other often appointed drugs is absent.

The medicines containing estrogen reduce pharmacological action of Anastrozol (the combination is contraindicated).

The combined use with Tamoxifenum is not recommended (because of probability of weakening of pharmacological action of an anastrozol).

Terms and storage conditions

To store in protected from light, the place, unavailable to children, at a temperature up to 25 °C.

Period of validity – 3 years.