Active substanceAnastrozoleAnastrozole
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  • Dosage form: & nbspfilm-coated tablets
    Composition:

    1 tablet contains:

    Active substance

    Anastrozole 1.00 mg

    Excipients

    Lactose monohydrate 91.25 mg

    Sodium carboxymethyl starch 4.0 mg

    Povidone K-30 3.00 mg

    Magnesium stearate 0.75 mg

    Shell

    Fill white (Y-1-7000): 2.5 mg

    - hypromellose 5 cP 1.5625 mg

    - titanium dioxide 0.78125 mg

    - Macrogol-400 0.15625 mg

    Description:

    Round biconvex tablets covered with a film shell, white or almost white with engraving DB02 on one side. On a cross-section of a tablet of white or almost white color.

    Pharmacotherapeutic group:Antitumor agent, estrogen synthesis inhibitor
    ATX: & nbsp

    L.02.B.G   Enzyme Inhibitors

    L.02.B.G.03   Anastrozole

    Pharmacodynamics:Anastrozole is a highly selective non-steroidal aromatase inhibitor, an enzyme that, with the help of which, in postmenopausal women, androstenedione in peripheral tissues is converted to estrone and further into estradiol. Reducing the concentration of circulating estradiol in patients with breast cancer has a therapeutic effect. In postmenopausal women anastrozole in a daily dose of 1 mg causes a decrease in the concentration of estradiol by 80%. Anastrozole does not possess progestogen, androgenic and estrogenic activity. In daily doses up to 10 mg does not have an effect on the secretion of cortisol and aldosterone, therefore, when anastrozole is used, it is not necessary to substitute corticosteroids.
    Pharmacokinetics:

    After oral administration anastrozole quickly absorbed from the gastrointestinal tract. The maximum concentration in the blood plasma is usually achieved within 2 hours after ingestion (fasting). Food insignificantly 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 the blood plasma with a single daily intake of anastrozole. After a 7-day treatment, approximately 90 to 95% the equilibrium concentration of anastrozole in the blood plasma. There is no information on the dependence of pharmacokinetic parameters of anastrozole on time or dose. The pharmacokinetics of anastrozole does not depend on the age of postmenopausal women. Connection with blood plasma proteins - 40%. Anastrozole Extensively metabolized in postmenopausal women, with less than 10% excreted by the kidneys unchanged for 72 hours after taking the drug. The half-life of anastrozole from the blood plasma is 40-50 hours. Anastrozole metabolism is carried out N-dealkylation, hydroxylation and glucuronidation. Metabolites of anastrozole are excreted mainly by the kidneys.The main metabolite of anastrozole - triazole, determined in blood plasma, does not have pharmacological activity. The clearance of anastrozole after oral administration with liver cirrhosis or renal dysfunction does not change.

    Indications:

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

    - the first line of therapy for locally advanced or metastatic breast cancer, with positive or unknown hormonal receptors in postmenopausal women;

    - the second line of treatment of advanced breast cancer, progressing after treatment with tamoxifen, in postmenopausal women.

    Contraindications:

    - Hypersensitivity to anastrozole or other components of the drug;

    - pre-menopausal period;

    - severe hepatic insufficiency (safety and efficacy not established);

    - concomitant therapy with tamoxifen or preparations containing estrogens;

    - pregnancy and the period of breastfeeding;

    - children's age (safety and efficacy in children not established).

    Carefully:

    ABOUTstenosis, hypercholesterolemia, ischemic heart disease, impaired hepatic function, severe renal failure (creatinine clearance <20 ml / min), lactase insufficiency, lactose intolerance, glucose-galactose malabsorption (lactose in the drug form).

    Dosing and Administration:

    Inside, 1 mg once a day. Tablet, swallowed whole, washed down with water. It is recommended to take the drug at the same time, regardless of food intake.

    The duration of treatment depends on the form and severity of the disease (with adjuvant therapy, the recommended duration of treatment is 5 years). If signs of disease progression appear, the drug should be discontinued.

    Side effects:

    The frequency of adverse reactions listed below was determined according to the following criteria: very often (not less than 1/10), often (more than 1/100 less than 1/10): sometimes (more than 1/1000, less than 1/100); rarely (more than 1/10000, less than 1/1000): very rarely (less than 1/10000), including individual messages.

    From the side of the vessels: Often - "tides" of blood to the face.

    From the side of the musculoskeletal and connective tissue: very often - arthralgia / joint stiffness, arthritis; often - pain in the bones, myalgia; infrequently - a trigger finger.

    From the genitals and the breast: often - dry mucous sheaths of the vagina, vaginal bleeding (mainly during the first weeks after cancellation or replacement of previous hormonal therapy on anastrozole).

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

    From the gastrointestinal tract: very often - nausea; often - diarrhea, vomiting.

    From the liver and bile ducts: often - increased activity of alkaline phosphatase, alanine aminotransferase, aspartate aminotransferase; infrequently - increased activity of gamma-glutamyltransferase and bilirubin concentration, hepatitis.

    From the nervous system: very often - headache; often - drowsiness, carpal tunnel syndrome (mainly observed in patients with risk factors of the disease), impaired sensitivity (including paresthesia, loss or perversion of taste sensations).

    From the side of metabolism and nutrition: often - anorexia, hypercholesterolemia: infrequently - hypercalcemia (with / without increasing the concentration of parathyroid hormone). Admission of the drug may 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.

    General disorders: very often - asthenia of mild or moderate severity.

    Adverse events noted in clinical trials that are not associated with anastrozole use: anemia, constipation, dyspepsia, back pain, abdominal pain, increased blood pressure, weight gain, depression, insomnia, dizziness, anxiety, paresthesia.

    Overdose:

    A single dose of anastrozole, which could lead to symptoms threatening life, is not established.

    Treatment: induction of vomiting, dialysis, maintenance therapy, control of the function of vital organs and systems. There is no specific antidote.

    Interaction:

    Studies on the drug interaction with phenazone (Antipyrin) and cimetidine indicate that the combined use of anastrozole with others drugs is unlikely to lead to a clinically significant drug interaction mediated by cytochrome P450.

    Clinically significant drug interaction with the reception of anastrozole at the same time with other commonly prescribed drugs is absent.

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

    Preparations containing estrogens reduce the pharmacological effect of anastrozole, and therefore they should not be administered simultaneously with anastrozole.

    Do not assign tamoxifen simultaneously with anastrozole because it can weaken the pharmacological action of the latter.

    Special instructions:

    In case of doubt in the hormonal status of the patient, menopause should be confirmed by determining the concentration of sex hormones in the blood serum.

    In the case of persistent uterine bleeding background of admission, anastrozole consultation and supervision of the gynecologist is necessary.

    There are no data on the use of anastrozole in patients with severe degree violations function of the liver.

    In patients with osteoporosis or an increased risk of osteoporosis, bone mineral density should be assessed by densitometry, for example DEXAScanning (dual-energy X-ray absorptiometry) at the beginning of treatment and regularly throughout its duration. If necessary, prescribe the treatment or prevention of osteoporosis and carefully monitor the patient's condition. Because the anastrozole reduces the concentration of circulating estradiol, this can lead to a decrease in bone mineral density. Nowadays there is insufficient data on the positive effect of bisphosphonates on the loss of bone mineral density caused by anastrozole or their benefits when used for prophylaxis. There is no data on the simultaneous use of anastrozole and analogues of gonadotropin-releasing hormone.

    In women with a receptor-negative tumor to estrogens, the efficacy of anastrozole has not been demonstrated, except in cases where there was a previous positive clinical response to tamoxifen.

    Preparations containing estrogens should not be administered simultaneously with anastrozole, since these drugs will neutralize its pharmacological action.

    The efficacy and safety of anastrozole and tamoxifen in their simultaneous application, regardless of the status of the hormonal receptors, are comparable to those of a single tamoxifen. The exact mechanism of this phenomenon is not yet known.

    It is not known whether anastrozole results of treatment when used in conjunction with chemotherapy.

    Effect on the ability to drive transp. cf. and fur:Some side effects of anastrozole, such as asthenia and drowsiness, can adversely affect the ability to perform work that requires increased concentration and speed of psychomotor reactions. In this regard, it is recommended that when these symptoms occur, exercise caution in the management of vehicles and mechanisms.
    Form release / dosage:

    Tablets, film-coated 1 mg.

    Packaging:For 14 tablets in a blister of PVC / aluminum foil. For 1, 2, or 6 blisters are placed in a cardboard box together with instructions for use.
    Storage conditions:

    At a temperature of no higher than 30 ° C.

    KEEP OUT OF THE REACH OF CHILDREN.

    Shelf life:

    3 years.

    The drug should not be used after the expiry date indicated on the packaging.
    Terms of leave from pharmacies:On prescription
    Registration number:LP-001135
    Date of registration:03.11.2011 / 07.11.2016
    Expiration Date:Unlimited
    The owner of the registration certificate:Fresenius Kabi Deutschland GmbHFresenius Kabi Deutschland GmbH Germany
    Manufacturer: & nbsp
    Representation: & nbspFRESENIUS KABI DEYCHLAND GmbH FRESENIUS KABI DEYCHLAND GmbH Germany
    Information update date: & nbsp28.08.2017
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