Anastrozol

General characteristics. Structure:

Active ingredient: 1 mg of an anastrozol.

Excipients - sodium krakhmalgikolit (type A), K-25 povidone, calcium stearate, sodium lauryl sulfate, lactoses monohydrate, опадрай the II white (85 F);

Structure of a cover (опадрай the II white (85 F)): the polyvinyl alcohol which is partially hydrolyzed; macrogoal/polyethyleneglycol; talc (E553b); titanium dioxide (E171).

Pharmacological properties:

Pharmacodynamics. Anastrozol - the high-selection nonsteroid inhibitor of enzyme of aromatase which in an organism of women in a postmenopause turns androstendion in peripheral fabrics into estrone and further into oestradiol. The therapeutic effect at patients with cancer of a mammary gland is reached due to decrease in level of the circulating oestradiol. In a postmenopause анастрозол in a daily dose of 1 mg causes decrease in level of oestradiol by 80% in women.

Has no progestogenny, androgenic and oestrogenic activity. The daily dose to 10 mg does not make impact on secretion of cortisol and Aldosteronum. Replaceable introduction of corticosteroids is not required. Anastrozol can cause decrease in mineral density of a bone tissue in patients with a gormonpozitivny early breast cancer in a postmenopause. Anastrazol separately, and also in a combination from bisfosfonata does not change the level of lipids in plasma.

Pharmacokinetics. It is quickly soaked up, the maximum concentration in plasma is reached within 2 hours after intake on an empty stomach. Food slightly reduces absorption speed. Extent of decrease has no clinically significant influence on equilibrium concentration of drug in plasma at a single dose of a daily dose. About 90-95% of equilibrium concentration of an anastrozol are reached after 7 days of administration of drug. Data on dependence of pharmacokinetic parameters from time and a dose are absent. The age of women in a postmenopause does not influence pharmacokinetics. Communication with proteins of plasma – 40%.

Anastrozol is brought from an organism slowly. Plasma elimination half-life makes 40-50 hours. It is extensively metabolized at women in a postmenopause. In an invariable look 10% of a dose with urine within 72 hours after reception are allocated. It is metabolized by N-dealkylation, a hydroxylation and a glyukuronization. The main metabolite triazole has no activity. Removal of metabolites happens to urine. Cirrhosis or a renal failure does not change clearance of an anastrozol after oral administration.

Indications to use:

Adjuvant therapy of an early gormonopolozhitelny breast cancer in a postmenopause. A widespread breast cancer at women in a postmenopause.

Adjuvant therapy of an early gormonopolozhitelny breast cancer at women in a postmenopause after therapy by Tamoxifenum within 2-3 years.

Route of administration and doses:

Inside, the tablet is swallowed entirely, washing down with water. Use at the same time is recommended.

The daily dose for adults, including elderly, makes 1 mg of 1 times a day. At emergence of signs of progressing of a disease administration of drug should be stopped. At adjuvant therapy the recommended duration of treatment makes 5 years.

At a renal failure of easy and moderate extent of correction of a dose it is not required.

At an abnormal liver function of easy extent of correction of a dose it is not required.

Features of use:

Safety and efficiency at children is not established.

At women with a retseptorootritsatelny tumor to estrogen efficiency of an anastrozol was not shown, except those cases when there was a previous affirmative clinical answer on Tamoxifenum. In case of doubts in the hormonal status of the patient the menopause has to be confirmed with definition of sex hormones in blood serum. There are no data on use of drug for patients with the moderated or expressed liver failure and at patients with the expressed renal failure (clearance of creatinine less than 20 ml/min.).

In case of the remaining uterine bleeding against the background of reception of an anastrozol consultation and observation of the gynecologist is necessary.

Estrogensoderzhashchy drugs should not be appointed at the same time.

Decrease in level of the circulating oestradiol can cause liquefaction of mineral density of a bone tissue with the subsequent increase in risk of a change, patients with such high risk are subject to treatment according to the guide to therapy of these complications. Combined use of bisfosfonat at patients with average and high risk of developing of fractures promotes the prevention of changes of bone system. The supporting treatment by vitamin D and calcium of patients with low risk prevents changes in structure of a bone.

At the patients having osteoporosis or having risk of development of osteoporosis, the mineral density of a bone tissue has to be estimated by a densitometry method, for example, of DEXA scanning (Dual-Energy X-ray Absorptiometry - a two-power x-ray absorbtsiometriya), in an initiation of treatment and in dynamics. If necessary treatment or prevention of osteoporosis, under careful observation of the doctor have to be begun.

There are no data on simultaneous use of an anastrozol and drugs analogs of luteinizing hormone of rileasing-hormone. It is unknown whether improves анастрозол results of treatment when sharing with chemotherapy. Data on safety at prolonged treatment anastrozoly are absent.

At use of an anastrozol more often than at therapy Tamoxifenum, observed ischemic diseases, however the statistical importance at the same time is noted.

Efficiency and safety of an anastrozol and Tamoxifenum at their simultaneous use regardless of the status of hormonal receptors are comparable with those when using one Tamoxifenum. The exact mechanism of this phenomenon is not known yet.

Influence on ability to control of motor transport and potentially dangerous mechanisms: it is necessary to be careful at control of motor transport and potentially dangerous mechanisms as анастрозол it is capable to cause an adynamy and drowsiness.

Side effects:

Frequency of development of side effects is specified in the following gradation: very often (> 1/10); often (> 1/100, <1/10); infrequently (> 1/1000, <1/100); seldom (> 1/10000, <1/1000); very seldom (<1/10000), including separate messages.

From vascular system: very often - inflows.

From a musculoskeletal system: very often - an arthralgia, constraint of joints, arthritis; often - an ostealgia; infrequently - a trigger finger.

From reproductive system: often - dryness of a mucous membrane of a vagina, vulval bleedings (generally within the first weeks after cancellation or change of the previous hormonal therapy on анастрозол).

From a track and skin appendages: very often - skin rash; often - an alopecia, allergic reactions; infrequently - a small tortoiseshell; seldom - a multiformny erythema, anaphylactoid reaction, a skin vasculitis (including separate cases of a purpura (Shenleyna-Genokh's syndrome)); very seldom - Stephens-Johnson's syndrome, a Quincke's disease.

From digestion: very often - nausea; often - diarrhea, vomiting.

From gepatobiliarny system: often - increase in activity of an alkaline phosphatase, alaninaminotranspherase, aspartate aminotransferase; infrequently - increase in activity gamma глютамилтрансферазы and concentration of bilirubin, hepatitis.

From a nervous system: very often – a headache; often – drowsiness, a syndrome of a carpal tunnel (it was generally observed at patients with risk factors of this disease).

From metabolism: often - anorexia, a hypercholesterolemia. Administration of drug can cause decrease in mineral density of a bone tissue in connection with decrease in concentration of the circulating oestradiol, thereby, increasing risk of developing of osteoporosis and fractures of bones.

Others: very often - an adynamy of easy and moderate degree of manifestation.

Interaction with other medicines:

Clinically significant interaction with phenazone (antipyrine), Cimetidinum and other often appointed drugs is noted.

There are no data on the combined use with other antineoplastic drugs.

The drugs containing estrogen reduce pharmacological action of an anastrozol in this connection, they should not be appointed along with drug.

Combined use of Tamoxifenum with anastrozoly can weaken pharmacological action of the last.

Contraindications:

Hypersensitivity to an anastrozol or other components of drug; a premenopauza at women; the expressed renal failure (clearance of creatinine less than 20 ml/min.); the moderated or expressed liver failure (safety and efficiency is not established); the accompanying therapy by Tamoxifenum or drugs containing estrogen. Pregnancy and period of a lactation; children's age (safety and efficiency at children is not established).

With care: osteoporosis, hypercholesterolemia, coronary heart disease, abnormal liver function, insufficiency of lactase, glyukozo-galaktozny malabsorption.

Overdose:

Cases of overdose are single and accidental. The single dose of drug which could lead to symptoms life-threatening, is not established.

Treatment: the specific antidote does not exist. Symptomatic treatment. Induction of vomiting (if the patient is in consciousness). Dialysis. General maintenance therapy, observation of the patient and control of function of vitals and systems.

Storage conditions:

To store in the place protected from moisture and light at a temperature not above 25 °C. To store in the place, unavailable to children. Period of validity 2 years. Not to use after the expiry date specified on packaging.

Issue conditions:

According to the recipe

Packaging:

On 10 tablets in a blister strip packaging from a film of polyvinyl chloride and aluminum foil. One or three planimetric packagings together with the application instruction place in a pack from a cardboard.