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

    One film-coated tablet contains: active substance: anastrozole 1 mg;

    Excipients: lactose monohydrate - 65.00 mg, corn starch - 13.00 mg, povidone K-30 - 2.00 mg, microcrystalline cellulose pH 102 - 12.00 mg, sodium carboxymethyl starch type A - 4,00 mg, silicon dioxide colloidal anhydrous 0,30 mg, magnesium stearate - 0,70 mg, talc - 2,00 mg;

    sheath: hypromellose 5 siz - 1,875 mg, macrogol 400 - 0,197 mg, titanium dioxide - 0,711 mg, talc - 0,217 mg.

    Description:

    White round tablets covered with a film sheath, with a diameter of approximately 6.6 mm.

    Pharmacotherapeutic group:An antineoplastic agent, an estrogen synthesis inhibitor.
    ATX: & nbsp

    L.02.B.G   Enzyme Inhibitors

    L.02.B.G.03   Anastrozole

    Pharmacodynamics:

    Anastrozole is a potent and highly selective nonsteroidal aromatase inhibitor - an enzyme, whereby in postmenopausal women androstenedione in peripheral tissues is converted into estrone and then to estradiol. Reduction of circulating concentrations of estradiol, as it turned out, has a positive effect on women with breast cancer. In postmenopausal women anastrozole in a daily dose of 1 mg suppresses the level of estradiol by more than 80%.

    Anastrozole does not possess progestagen, androgenic or estrogenic activity. Regular use of anastrozole daily doses up to 10 mg did not affect the secretion of cortisol or aldosterone, therefore, when administered in corticoid additives unnecessary.

    Pharmacokinetics:

    The pharmacokinetics of anastrozole does not depend on the age of postmenopausal women. Absorption of anastrozole is fast, the maximum concentration in the plasma is reached within two hours after ingestion (on an empty stomach). Food slightly reduces the rate of absorption, but not its degree, and does not lead to a clinically significant effect of achieving an equilibrium plasma anastrozole concentration with a single daily dose of anastrozole. After taking 7 daily doses, the concentration of anastrozole in plasma is 90-95% of the equilibrium concentration. There is no evidence that the pharmacokinetic parameters of anastrozole depend on time and dose.

    Anastrozole binds to plasma proteins by 40%.

    Anastrozole is withdrawn slowly, the half-life from the plasma is 40-50 hours. Intensively metabolized in postmenopausal women. Less than 10% of the dose taken is excreted unchanged in urine within 72 hours after admission. Anastrozole metabolism occurs through stages N-dealkylation, hydroxylation and glucuronization. Triazole, the main metabolite of anastrozole in plasma, does not inhibit aromatase. Metabolites are excreted mainly by the kidneys.In volunteers with stable cirrhosis of the liver or impaired function of the nights, the clearance of anastrozole after oral administration remained within the limits observed in healthy volunteers.

    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 therapy for advanced breast cancer, progressing after treatment with tamoxifen, in postmenopausal women.

    Contraindications:

    AXASTROL® is contraindicated in the following cases:

    with increased sensitivity to anastrozole or to any auxiliary substance of the drug,

    during pregnancy and lactation,

    in premenopausal women,

    with severe form of renal failure (creatinine clearance less than 20 ml / min),

    with moderate or severe forms of liver disease,

    with simultaneous administration of tamoxifen,

    childhood.

    Carefully:With caution: osteoporosis, hypercholesterolemia, ischemic heart disease.
    Dosing and Administration:

    Inside. Swallow the whole tablet with water. It is recommended to take the drug at the same time, regardless of food intake.

    Adults, including the elderly: 1 mg orally once a 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.

    Impaired renal function: no dose adjustment is required.

    Dysfunction of the liver: no dose adjustment is required.

    The duration of treatment depends on the form and severity of the disease.

    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), infrequently (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: very often - the "tides" of blood to the face.

    From 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 breast: often - dryness of the mucous membrane of the vagina, vaginal bleeding (mainly during the first weeks after cancellation or change of previous hormone therapy on anastrozole).

    From the skin and subcutaneous tissues: very often - skin rash; often, hair loss, 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.

    On the part of the liver and bile ducts: often - increased activity of alkaline phosphatase, alanine aminotransferase, aspartate aminotransferase and, rarely - increased activity of gamma-glutamintransferase; infrequently - excess of 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), sensitivity disorders (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). Reception of 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.

    Common disorders: very often - plants 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:

    Single clinical cases of accidental drug overdose are described. A single dose of anastrozole, which could lead to symptoms threatening life, is not established. Specific antidote does not exist, in case of an overdose, treatment should be symptomatic.

    Dialysis may be performed. If the patient is conscious, vomiting is recommended.

    General supportive therapy is recommended, including frequent monitoring of vital signs and careful monitoring of the patient.

    Interaction:

    Studies on the drug interaction with antipyrine and cimetidine indicate that the combined use of anastrozole with other drugs is unlikely to lead to a clinically significant drug interaction mediated by cytochrome P450.

    There is no data on the simultaneous use of the drug with other antitumor drugs.

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

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

    Special instructions:

    The safety and efficacy of anastrozole in children is not established.

    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.

    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.

    There is no data on the use of anastrozole in patients with moderate or severe liver function disorders. In the case of persisting uterine bleeding against the background of receiving anastrozole, consultation and supervision of the gynecologist is necessary.

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

    Reducing the concentration of circulating estradiol, anastrozole can cause a decrease in bone mineral density. In patients with osteoporosis or at risk of this disease, it is necessary to check bone density by densitometry at the beginning of therapy and in dynamics. If necessary, preventive and adjuvant therapy is recommended under strict control.

    There is no data on the simultaneous administration of anastrozole with analogues of gonadotropin-releasing hormone. It is not known whether anastrozole results of treatment when used in conjunction with chemotherapy.

    Tablets AXASTROLA® contain lactose.Patients with a rare congenital intolerance to galactose, a deficiency of lactase or malabsorption of glucose-galactose should not be prescribed this medicine.

    Effect on the ability to drive transp. cf. and fur:

    Some side effects of anastrozole (asthenia and drowsiness) can adversely affect the ability to drive vehicles and manage mechanisms. Therefore, during the treatment period, care must be taken when driving vehicles and engaging in other potentially hazardous activities that require an increased concentration of attention and speed of psychomotor reactions.

    Form release / dosage:

    Film-coated tablets 1 mg.

    Packaging:

    For 14 tablets in a planar cell packaging made of polyvinylchloride film and aluminum foil.

    2 contour packs of 14 tablets together with the instructions for use are placed in a cardboard box.
    Storage conditions:

    Store at a temperature not exceeding 25 ° C.

    Keep out of the reach of children.

    Shelf life:

    3 years.

    Do not use after the expiry date printed on the package.

    Terms of leave from pharmacies:On prescription
    Registration number:LP-001096
    Date of registration:03.11.2011
    The owner of the registration certificate:GRINDEX, JSC GRINDEX, JSC Latvia
    Manufacturer: & nbsp
    Representation: & nbspGrindeks Rus, Open CompanyGrindeks Rus, Open CompanyRussia
    Information update date: & nbsp13.04.2015
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