Active substanceAnastrozoleAnastrozole
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  • Dosage form: & nbsptfilm-covered laths
    Composition:

    1 tablet, film-coated, contains:

    active substance: anastrozole 1 mg;

    Excipients: lactose monohydrate, corn starch, povidone (polyvinylpyrrolidone K-30), sodium carboxymethyl starch, magnesium stearate;

    shell composition: Opaprai II white: giprolose (hydroxypropyl cellulose) 28-40%, lactose monohydrate 21-40%, macrogol (polyethylene glycol 4000) 8-14%; titanium dioxide (E171) 20-30%.

    Description:

    White or almost white, round, biconvex tablets, covered with a film membrane.

    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 level 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 level of estradiol by 80%.

    Anastrozole does not possess progestogen, androgenic and estrogenic activity.

    Anastrozole 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:

    Absorption of anastrozole is fast, the maximum concentration in the blood plasma is reached within 2 hours after ingestion (on an empty stomach). 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 7 days of taking the drug, approximately 90-95% of the equilibrium concentration of anastrozole in the blood plasma is reached. 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%.

    Anastrazole is withdrawn slowly, the half-life of plasma is 40-50 hours. Extensively metabolized in postmenopausal women. Less than 10% of the dose is excreted with urine unchanged for 72 hours after taking the drug. Metabolism is carried out in the process N-dealkylation, hydroxylation and glucuronization. Metabolites are excreted mainly by the kidneys. Triazole, the main metabolite, determined in blood plasma,does not possess pharmacological activity.

    The total clearance of anastrozole after oral administration with 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 therapy for advanced breast cancer, progressing after tamoxifen treatment, in women in postmenopause.

    Contraindications:

    - Hypersensitivity to anastrozole or other constituents of the drug;

    - in premenopausal women;

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

    - concomitant therapy with tamoxifen;

    - pregnancy and the period of breastfeeding;

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

    Carefully:

    Insufficiency of lactase, galactose intolerance, glucose-galactose malabsorption (in the drug form of the drug contains lactose).

    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. As adjuvant therapy the recommended duration of treatment is 5 years. If signs of disease progression appear, the drug should be discontinued.

    Renal impairment: dose adjustment in patients with impaired renal function is not required.

    Dysfunction of the liver: dose adjustment in patients with mild to moderate liver function impairment is not required.

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

    From the genitals and breast: often - dryness of the vaginal mucosa, vaginal bleeding (mainly during the first weeks after cancellation or change of previous hormonal therapy on anastrozole).

    From the skin and subcutaneous tissues: very often - skin rash; often thinning hair, alopecia, allergic reactions; infrequently - hives; rarely - erythema multiforme, anaphylactoid reaction, skin vasculitis (including individual 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 biliary tract: often - increased activity Alkaline phosphatase, alanine aminotransferase, aspartate aminotransferase; infrequently - increased activity of gamma-glutamintransferase 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). 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.

    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:

    Single clinical cases of accidental drug overdose are described. A single dose of anastrozole, which could lead to symptoms threatening life, is not established.

    There is no specific antidote; In case of an overdose, treatment should be symptomatic. You can induce vomiting if the patient is conscious. Dialysis may be performed. General supportive therapy, patient monitoring and monitoring of the function of vital organs and systems are recommended.

    Interaction:

    Clinically significant drug interaction with the administration of anastrozole concomitantly 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.

    Studies on the drug interaction with phenazone 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.

    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:

    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 the determination of sex hormones in the blood serum.

    There is no data on the use of anastrozole in patients with 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 level of circulating estradiol, anastrozole can cause a decrease in bone mineral density

    In patients who suffer from osteoporosis or who are at risk for developing osteoporosis, bone mineral density should be assessed by densitometry (for example, DEXA scanning) at the beginning of treatment and in dynamics. If necessary, treatment or prevention of osteoporosis should be initiated under the close supervision of a physician.

    There is no data on the simultaneous use of anastrozole and analogue preparations of the luteinizing hormone releasing hormone (LHRH).

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

    Efficacy and safety with simultaneous use with tamoxifen, regardless of the status of hormonal receptors, are comparable to those with one tamoxifen.

    Effect on the ability to drive transp. cf. and fur:Some of the side effects of anastrozole, such as asthenia and drowsiness, can adversely affect the ability to perform potentially hazardous activities requiring 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 or 15 tablets in a blister of Al / PVC.

    2 blisters together with instructions for use in a cardboard bundle.

    Storage conditions:

    In a dry place, at a temperature of no higher than 30 ° 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:LS-002171
    Date of registration:03.11.2009 / 12.12.2016
    Expiration Date:Unlimited
    The owner of the registration certificate:Laboratory Tutor SAASIFAALaboratory Tutor SAASIFAA Argentina
    Manufacturer: & nbsp
    Representation: & nbspGENPHA LTD.GENPHA LTD.Russia
    Information update date: & nbsp14.08.2017
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