Selana tablets p / o 1mg, No. 30

• Adjuvant therapy for early breast cancer with positive hormone receptors in postmenopausal women, including after adjuvant therapy with tamoxifen for 2-3 years.

• First line therapy for locally advanced or metastatic breast cancer, with positive or unknown hormone receptors in postmenopausal women.

• The second line of therapy for advanced breast cancer, progressing after treatment with tamoxifen, in postmenopausal women.

The tablet should be swallowed whole and washed down with water.
It is recommended to take the drug at the same time of the day.

For adults, including elderly patients, the drug is prescribed 1 mg orally 1 time per day, for a long time. If signs of disease progression appear, the drug should be discontinued. As an adjuvant therapy, the recommended duration of treatment is 5 years.

Patients with mild to moderate renal failure do not require dose adjustment.

Patients with mild hepatic impairment do not require dose adjustment.

1 film-coated tablet contains:

Active substance:
Anastrozole 1.0 mg
Excipients:
Magnesium aluminometasilicate 9.0 mg
Croscarmellose sodium 3.0 mg
Colloidal silicon dioxide 3.0 mg
Magnesium stearate 0.5 mg
Ludipress 83.5 mg in terms of components:
- lactose monohydrate 77 , 7 mg
- povidone 2.9 mg
- crospovidone 2.9 mg
Sheath:
Opadray II white 85F48105 5.0 mg (polyvinyl alcohol from 35.0 to 49.00%, talc from 9.80 to 25.00%, macrogol 3350 from 7.35 to 35.20%, titanium dioxide from 15.15 to 30.00%)

• Hypersensitivity to anastrozole and other components of the drug.

• Severe renal failure (creatinine clearance less than 20 ml / min).

• Severe hepatic impairment (safety and efficacy have not been established).

• Concomitant therapy with tamoxifen or drugs containing estrogens.

• Childhood (safety and efficacy have not been established).

• Premenopausal period.

• Pregnancy and the period of breastfeeding.

Carefully

Osteoporosis, hypercholesterolemia, lactase deficiency, lactose intolerance, glucose-galactose malabsorption (the dosage form of the drug contains lactose), ischemic heart disease, liver dysfunction.

Trade name of the drug:

SelanaЃ

International non-proprietary name:

anastrozole (anastrozol)

Chemical name:

2,2 '- [5- (1H-1,2,4-triazol-1-ylmethyl) -1,3-phenylene] bis (2-methyl-propionitrile)

Dosage form:

film-coated tablets

Composition

1 film-coated tablet contains:

Active substance:
Anastrozole 1.0 mg
Excipients:
Magnesium aluminometasilicate 9.0 mg
Croscarmellose sodium 3.0 mg
Colloidal silicon dioxide 3.0 mg
Magnesium stearate 0.5 mg
Ludipress 83.5 mg in terms of components:
- lactose monohydrate 77 , 7 mg
- povidone 2.9 mg
- crospovidone 2.9 mg
Sheath:
Opadray II white 85F48105 5.0 mg (polyvinyl alcohol from 35.0 to 49.00%, talc from 9.80 to 25.00%, macrogol 3350 from 7.35 to 35.20%, titanium dioxide from 15.15 to 30.00%)

Description:

round biconvex film-coated tablets of white color, on a cross-section the core is white.

Pharmacotherapeutic group

Antineoplastic, estrogen synthesis inhibitor.

ATX code: L02BG03

Pharmacological properties

Pharmacodynamics

Anastrozole is a highly selective non-steroidal aromatase inhibitor. Aromatase is an enzyme by which, in postmenopausal women, androstenedione in peripheral tissues is converted into estrone and then into estradiol. Anastrozole has antitumor activity against estrogen-dependent breast tumors in postmenopausal women. In the postmenopausal period, the drug in a daily dose of 1 mg causes a decrease in the concentration of estradiol by 80%.

Anastrozole has no progestogenic, androgenic and estrogenic activity. Anastrozole in a daily dose of up to 10 mg has no effect on the secretion of cortisol and aldosterone (therefore, the use of the drug does not require replacement of corticosteroids).

Pharmacokinetics

Absorption After oral administration, anastrozole is rapidly absorbed from the gastrointestinal tract. The maximum concentration (Cmax) in plasma is reached within 2 hours (on an empty stomach). Food slightly reduces the rate of absorption, but not its degree, and does not lead to a clinically significant effect on the equilibrium concentration of the drug in plasma with a single daily dose.

Distribution
Anastrozole binds to plasma proteins by 40%. After 7 days of taking the drug, approximately 90 - 95% of the equilibrium plasma concentration of anastrozole is achieved. There is no information on the dependence of pharmacokinetic parameters on time and dose.

Metabolism
Anastrozole is metabolized by N-dealkylation, hydroxylation and glucuronidation. Triazole, the major plasma metabolite, does not inhibit aromatase.

Withdrawal
Anastrozole is excreted slowly, the half-life (T1 / 2) is 40-50 hours. Anastrozole and its metabolites are excreted mainly in the urine. Less than 10% of the dose is excreted in the urine unchanged within 72 hours after taking the drug.

Pharmacokinetics in special clinical situations The
determined clearance of anastrozole after oral administration in patients with liver cirrhosis or impaired renal function does not differ from the clearance determined in healthy people.
The pharmacokinetics of anastrozole does not depend on age in postmenopausal women.

Indications for use

• Adjuvant therapy for early breast cancer with positive hormone receptors in postmenopausal women, including after adjuvant therapy with tamoxifen for 2-3 years.

• First line therapy for locally advanced or metastatic breast cancer, with positive or unknown hormone receptors in postmenopausal women.

• The second line of therapy for advanced breast cancer, progressing after treatment with tamoxifen, in postmenopausal women.

Contraindications

• Hypersensitivity to anastrozole and other components of the drug.

• Severe renal failure (creatinine clearance less than 20 ml / min).

• Severe hepatic impairment (safety and efficacy have not been established).

• Concomitant therapy with tamoxifen or drugs containing estrogens.

• Childhood (safety and efficacy have not been established).

• Premenopausal period.

• Pregnancy and the period of breastfeeding.

Carefully

Osteoporosis, hypercholesterolemia, lactase deficiency, lactose intolerance, glucose-galactose malabsorption (the dosage form of the drug contains lactose), ischemic heart disease, liver dysfunction.

Application during pregnancy and during breastfeeding

The use of the drug during pregnancy and during breastfeeding is contraindicated.

Method of administration and dosage

The tablet should be swallowed whole and washed down with water.
It is recommended to take the drug at the same time of the day.

For adults, including elderly patients, the drug is prescribed 1 mg orally 1 time per day, for a long time. If signs of disease progression appear, the drug should be discontinued. As an adjuvant therapy, the recommended duration of treatment is 5 years.

Patients with mild to moderate renal failure do not require dose adjustment.

Patients with mild hepatic impairment do not require dose adjustment.

Side effect

Side effects, registered more often than single observations, are listed below by organs and systems, indicating the frequency of their occurrence.
Determination of the frequency of adverse reactions: very often (> 10%); often (> 1% and 0.1% and 0.01% and Blood and lymphatic system disorders:
very often - lymphedema;
infrequently - anemia.

Metabolic and nutritional disorders:
very often - peripheral edema;
often - anorexia, hypercholesterolemia; increase in body weight;
infrequently - hypercalcemia (with or without an increase in the concentration of parathyroid hormone).
Taking the drug can cause a decrease in bone mineral density due to a decrease in the concentration of circulating estradiol, thereby increasing the risk of osteoporosis and bone fractures.

Nervous system disorders:
very often - headache, dizziness, sleep disturbances, depression;
often - drowsiness, carpal tunnel syndrome (mainly observed in patients with risk factors for this disease), sensitivity disorders (including paresthesia, loss or perversion of taste), anxiety.

Violations of the organ of vision:
infrequently - cataract.

Vascular disorders:
very often - 'hot flushes' of blood to the face, increased blood pressure;
often - vasodilation, ischemic cardiovascular diseases.

Disturbances from the respiratory system, chest and mediastinal organs:
very often - pharyngitis, increased cough, shortness of breath;
infrequently - chest pain, sinusitis, bronchitis.

Disturbances from the gastrointestinal tract:
very often - nausea, vomiting;
often - diarrhea, constipation, dyspepsia;
infrequently - abdominal pain, dry mouth.

Liver and biliary tract disorders:
often - increased activity of alkaline phosphatase, alanine aminotransferase, aspartate aminotransferase;
infrequently, an increase in the activity of gamma-glutamyltransferase and the concentration of bilirubin, hepatitis.

Skin and subcutaneous tissue disorders:
very often - skin rash;
often - thinning hair, alopecia, allergic reactions;
infrequently - urticaria;
rarely, erythema multiforme, anaphylactoid reaction, cutaneous vasculitis (including isolated cases of purpura (Schonlein-Henoch syndrome)),
very rarely - Stevens-Johnson syndrome, angioedema.

Musculoskeletal and connective tissue disorders:
very common - arthralgia, joint stiffness, arthritis, back pain, osteoporosis and bone fractures;
often - bone pain, myalgia; infrequently - 'trigger finger' or 'snapping finger' (violation of the ability to straighten the finger, usually the middle or ring finger).

Violations of the genitals and mammary gland:
often - dryness of the vaginal mucosa, vaginal bleeding (mainly during the first weeks after the cancellation or change of previous hormonal therapy with anastrozole preparations), vulvovaginitis, vaginitis, pelvic pain;
infrequently - mucous vaginal discharge, urinary tract infections, chest pain;
rarely - endometrial cancer, breast neoplasms.

General disorders and disorders at the injection site:
very often - mild or moderate asthenia. If any of the side effects indicated in the instructions are aggravated or you notice any other side effects not listed in the instructions, inform your doctor.

Overdose

Isolated clinical cases of anastrozole overdose are described. A single dose of anastrozole at which life-threatening symptoms develop has not been established.

Treatment: there is no specific antidote. If necessary, symptomatic therapy is performed. Vomiting is initiated (if the patient is conscious), general supportive therapy and observation of the patient are carried out, the functions of vital organs and systems are monitored. Dialysis is possible.

Interaction with other medicinal products

Drug interactions with phenazone (Antipyrin) and cimetidine indicate that the combined use of anastrozole with other drugs is unlikely to lead to a clinically significant interaction caused by cytochrome P450.

There are no data on clinically significant drug interactions while taking anastrozole with other commonly used drugs.

At the moment, there is no information on the use of anastrozole in combination with other anticancer drugs.

Preparations containing estrogens should not be used concomitantly with anastrozole, because they reduce the pharmacological action of the latter.

Tamoxifen should not be used concomitantly with anastrozole, as it can weaken the pharmacological effect of the latter.

special instructions

The hormonal status of the patient's menopause should be confirmed by the determination of sex hormones in the blood serum.
The efficacy of anastrozole in women with a receptor-negative tumor to estrogens was not noted, except in cases where there was a previous positive clinical response to the use of tamoxifen.
There is no data on the safety of using anastrozole in patients with severe hepatic impairment or in patients with severe renal failure (creatinine clearance less than 20 ml / min).
In the case of persisting uterine bleeding while taking anastrozole, consultation and supervision of a gynecologist is necessary.
Preparations containing estrogens should not be administered concurrently with anastrozole. By decreasing the concentration of circulating estradiol, anastrozole can cause a decrease in bone mineral density.
In patients with osteoporosis or at risk of developing osteoporosis, bone mineral density should be assessed by densitometry (for example, DEXA scanning) at the beginning of treatment and over time. If necessary, treatment or prevention of osteoporosis should be initiated under close medical supervision. There is no data on the simultaneous use of anastrozole and drugs of analogs of gonadotropin-releasing hormone (GnRH). It is not known whether anastrozole improves treatment outcomes when used with chemotherapy.
Safety data for long-term treatment with anastrozole have not yet been obtained. The efficacy and safety of anastrozole and tamoxifen when used simultaneously, regardless of the status of hormonal receptors, are comparable to those when using tamoxifen alone. The exact mechanism of this phenomenon is not yet known.

Influence on the ability to drive vehicles and mechanisms
Care should be taken when driving vehicles and mechanisms, because some side effects of the drug, such as asthenia, headache, dizziness and sleep disturbances, can adversely affect the ability to perform work that requires increased concentration and psychomotor speed. When these side effects appear, you should refrain from performing these activities.

‘орма выпуска

“аблетки, покрытые пленочной оболочкой, 1 мг.
ѕо 7 таблеток в контурной ¤чейковой упаковке из пленки полимерной и фольги алюминиевой, по 4 контурные ¤чейковые упаковки вместе с инструкцией по применению помещают в картонную пачку.
ѕо 10 таблеток в контурной ¤чейковой упаковке из пленки полимерной и фольги алюминиевой, по 3 контурные ¤чейковые упаковки вместе с инструкцией по применению помещают в картонную пачку.
ѕо 14 таблеток в контурной ¤чейковой упаковке из пленки полимерной и фольги алюминиевой, по 2 контурные ¤чейковые упаковки вместе с инструкцией по применению помещают в картонную пачку.

—рок годности

3 года.
Ќе примен¤ть по истечении срока годности, указанного на упаковке.

”слови¤ хранени¤

Store in a dark place at a temperature not exceeding 25 ? C.
Keep out of the reach of children.

Vacation conditions

Dispensed by prescription.