Селана®

General characteristics. Structure:

Active ingredient: 1 mg of an anastrozol in 1 tablet.

Excipients: алюмометасиликат magnesium, croscarmellose sodium, silicon dioxide colloid, magnesium stearate, лудипресс in terms of components: lactoses monohydrate, povidone, кросповидон.

Cover: Опадрай the II white 85F48105 (alcohol of polyvinyl from 35,0 to 49,00%, talc from 9,80 to 25,00%, macrogoal of 3350 from 7,35 to 35,20%, titanium dioxide from 15,15 to 30,00%).

Pharmacological properties:

Pharmacodynamics. Anastrozol - the high-selection nonsteroid inhibitor of aromatase. Aromatase - enzyme by means of which at women in the post-menopausal period androstendion in peripheral fabrics turns into estrone and further into oestradiol. Anastrozol has antineoplastic activity concerning estrogenzavisimy tumors of a mammary gland at women in the post-menopausal period. In the post-menopausal period drug in a daily dose of 1 mg causes decrease in concentration of oestradiol by 80%.

Anastrozol has no progestagenny, androgenic and oestrogenic activity.

Anastrozol in a daily dose to 10 mg does not render effect on secretion of cortisol and Aldosteronum (therefore, at use of drug replaceable introduction of corticosteroids is not required).

Pharmacokinetics. Absorption. After intake анастрозол it is quickly soaked up from digestive tract. The maximum concentration (Cmax) in plasma is reached within 2 hours (on an empty stomach). Food slightly reduces the absorption speed, but not its degree and does not lead to clinically significant influence on equilibrium concentration of drug in plasma at a single dose of a daily dose.

Distribution. Anastrozol contacts proteins of plasma for 40%. After 7-day administration of drug about 90 - 95% of equilibrium concentration of an anastrozol in plasma are reached. There are no data on dependence of pharmacokinetic parameters from time and a dose.

Metabolism. Anastrozol is metabolized by N-dealkylation, a hydroxylation and a glyukuronization. Triazole, the main metabolite defined in plasma does not inhibit aromatase.

Removal. Anastrozol is brought slowly, the elimination half-life (T1/2) makes 40 – 50 hours.

Anastrozol and his metabolites are removed preferential with urine. Less than 10% of a dose are allocated with urine in an invariable look within 72 hours after administration of drug. Pharmacokinetics in special clinical cases

The defined clearance of an anastrozol after oral administration at patients with cirrhosis or a renal failure does not differ from the clearance defined at healthy people.

The pharmacokinetics of an anastrozol does not depend on age at women in a postmenopause.

Indications to use:

- Adjuvant therapy of an early gormonopolozhitelny breast cancer at women in the post-menopausal period.
- Treatment of a widespread breast cancer at women in the post-menopausal period.
- Adjuvant therapy of an early gormonopolozhitelny breast cancer at women in the post-menopausal period after therapy by Tamoxifenum within 2 – 3 years.

Route of administration and doses:

The tablet should be swallowed entirely and to wash down with water. It is recommended to accept drug at the same time days. The adult, including elderly patients, drug is appointed on 1 mg in 1 times a day, it is long.

At emergence of signs of progressing of a disease administration of drug should be stopped. As adjuvant therapy the recommended treatment duration – 5 years.

Patients from easy and average degree of a renal failure do not need dose adjustment.

Patients with easy degree of a liver failure do not need dose adjustment.

Features of use:

Use at pregnancy and during breastfeeding. Use of drug at pregnancy and during breastfeeding is contraindicated.

The hormonal status of a menopause at the patient has to be confirmed with definition of sex hormones in blood serum.

Efficiency of an anastrozol at women with a retseptorootritsatelny tumor to estrogen is noted, except cases when there was a previous affirmative clinical answer on use of Tamoxifenum.

There are no data on safety of use of an anastrozol for patients with the expressed abnormal liver functions or at patients with a renal failure of heavy degree (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.

It is not necessary to appoint the drugs containing estrogen along with anastrozoly.

Reducing concentration of the circulating oestradiol, анастрозол can cause decrease in mineral density of a bone tissue.

At patients with osteoporosis or with risk of development of osteoporosis the mineral density of a bone tissue has to be estimated by a densitometry method (for example, DEXA scanning) in an initiation of treatment and in dynamics. Treatment or prevention of osteoporosis under careful observation of the doctor have to be in case of need begun. There are no data on simultaneous use of an anastrozol and drugs of analogs of gonadotrophin-rileasing-hormone (GNRG). It is unknown whether improves анастрозол results of treatment at combined use with chemotherapy.

Data on safety at prolonged treatment anastrozoly are not obtained yet.

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 manage vehicles and mechanisms. It is necessary to be careful at control of vehicles and mechanisms since some side effects of drug, such as an adynamy, a headache, dizziness and sleep disorders, can negatively influence ability to performance of the work demanding the increased concentration of attention and speed of psychomotor reactions. At emergence of these side effects it is necessary to refrain from performance of the specified types of activity.

Side effects:

The side effects registered more often than single observations are listed below on bodies and systems with the indication of frequency of their emergence. Determination of frequency of side reactions: very often (> 10%); often (1-10%); infrequently (0,1 - 1%); seldom (0,01 - 0,1%); very seldom (<0,01%).

From cardiovascular system: very often - heat "inflows", increase in arterial pressure; often – a vazodilatation, ischemic cardiovascular diseases.

From a musculoskeletal system: very often - an arthralgia, constraint of joints, arthritis, a dorsodynia, decrease in mineral density of a bone tissue, osteoporosis and fractures of bones; often - an ostealgia, a mialgiya; infrequently - "a trigger finger" or "the clicking finger" (disturbance of ability to straighten a finger, usually average or anonymous).

From reproductive and urinogenital 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 with drugs of an anastrozol), a vulvovaginitis, a vaginitis, pelvic pain; infrequently – mucous allocations from a vagina, infections of urinary tract, a stethalgia; seldom – endometrial cancer, new growths in a breast.

From blood and lymphatic system: very often – a limfedema; infrequently – anemia.

From the alimentary system: very often – nausea, vomiting; often - diarrhea, a lock, dyspepsia, increase in activity of an alkaline phosphatase, alaniaminotranferaza, aspartate aminotransferase; infrequently – abdominal pains, increase in activity of gamma glutaminetransferase and concentration of bilirubin, hepatitis, dryness in a mouth.

From a nervous system: very often - a headache, dizziness, sleep disorders, a depression; often - a syndrome of a carpal tunnel (it was generally observed at patients with risk factors to this disease), feeling of alarm, paresthesia.

From sense bodys: infrequently – a cataract.

From respiratory system: very often – pharyngitis, strengthening of cough, short wind; infrequently – a stethalgia, sinusitis, bronchitis.

From a metabolism: very often - peripheral hypostases; often - anorexia, a hypercholesterolemia, a hypercalcemia (with increase or without increase in concentration of parathormone), increase in body weight.

From skin and appendages: very often - skin rash; often - thinning of hair, an alopecia; infrequently - a multiformny erythema (Stephens-Johnson's syndrome), a skin vasculitis (including separate cases of a purpura (Shenleyn's syndrome - Genokh)).

Allergic reactions: often - allergic reactions; infrequently – a small tortoiseshell; seldom - anaphylactoid reaction; very seldom - a Quincke's disease.

Others: very often – an adynamy. If you noticed any other side effects which are not specified in the instruction, report about it to the doctor.

Interaction with other medicines:

Medicinal interaction with phenazone (Antipyrine) and Cimetidinum is pointed that combined use of an anastrozol with other drugs will hardly lead to clinically significant interaction caused by P450 cytochrome.

There are no data on clinically significant medicinal interaction at a concomitant use of an anastrozol with other often used drugs.

At the moment there are no data on use of an anastrozol in a combination with other antineoplastic drugs.

The drugs containing estrogen should not be applied along with anastrozoly since they reduce pharmacological action of the last.

It is not necessary to apply Tamoxifenum along with anastrozoly as it can weaken pharmacological action of the last.

Contraindications:

- Hypersensitivity to an anastrozol and other components of drug.
- Heavy renal failure (clearance of creatinine less than 20 ml/min.).
- A heavy liver failure (safety and efficiency are not established).
- The accompanying therapy by Tamoxifenum or drugs containing estrogen.
- Children's age (safety and efficiency are not established).
- Premenopauzalny period.
- Pregnancy and period of breastfeeding.

With care. Osteoporosis, a hypercholesterolemia, insufficiency of lactase, a lactose intolerance, glyukozo-galaktozny malabsorption (the dosage form of drug contains lactose), coronary heart disease, an abnormal liver function.

Overdose:

Isolated clinical cases of overdose of an anastrozol are described. The single dose of an anastrozol at which life-threatening symptoms develop is not established.

Treatment: the specific antidote does not exist. If necessary carry out symptomatic therapy. Initiate vomiting (if the patient in consciousness), carry out the general maintenance therapy and observation of the patient, control of functions of vitals and systems. Carrying out dialysis is possible.

Storage conditions:

Period of validity – 3 years. Not to apply after the period of validity specified on packaging. To store in the dry, protected from light place at a temperature not above 25 °C. To store in places unavailable to children.

Issue conditions:

According to the recipe

Packaging:

Tablets, film coated, 1 mg. On 7 tablets in a blister strip packaging from a film of polymeric and aluminum foil, on the 4th blister strip packagings together with the application instruction place in a cardboard pack. On 10 tablets in a blister strip packaging from a film of polymeric and aluminum foil, on the 3rd blister strip packagings together with the application instruction place in a cardboard pack. On 14 tablets in a blister strip packaging from a film of polymeric and aluminum foil, on the 2nd blister strip packagings together with the application instruction place in a cardboard pack.