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

    1 film-coated tablet contains:

    active substance: anastrozole 1.0 mg;

    auxiliary substances: lactose monohydrate 79.95 mg, ascorbic acid 18.0 mg, citric acid monohydrate 4.0 mg, butyl hydroxytoluene 3.0 mg, corn starch 18.5 mg, microcrystalline cellulose 29.0 mg, povidone (K30) 2.5 mg, sodium carboxymethyl starch 15.0 mg, magnesium stearate 3.0 mg;

    film membrane: instacoate (hypromellose - 60%, macrogol - 12%, talc -10%, titanium dioxide -18%).

    Description:

    Round, biconvex tablets, covered with a film shell of white or almost white color.

    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 highly selective non-steroidal aromatase inhibitor-enzyme, with with which androstenedione and testosterone in tissues are converted into estrone and estradiol respectively. 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 affect 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 slightly reduces the rate of absorption, but not its degree and does not lead to a clinically significant effect on the equilibrium concentration of anastrozole in plasma blood with a single daily dose. After a 7-day treatment, approximately 90-95 % 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 is extensively metabolized in postmenopausal women, with less than 10% excreted by the kidneys unchanged for 72 hours after taking the drug. Period half-life Anastrozole from plasma-blood is 40-50 hours. Anastrozole metabolism is carried out N-dealkylation, hydroxylation and glucuronation.

    Metabolites of anastrozole are excreted mainly by the kidneys. Main metabolite - 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.

    The first line of therapy for locally advanced or metastatic breast cancer, with a positive or unidentified hormone receptor status in women in postmenopausal women.

    The second line of therapy for advanced breast cancer, progressing after previous therapy with tamoxifen.

    Contraindications:

    Hypersensitivity to anastrozole or other components of the drug.

    Pregnancy and lactation.

    Premenopause.

    Severe hepatic impairment (safety and efficacy not installed).

    Concomitant therapy with tamoxifen or preparations containing estrogens.

    Child age (safety and efficacy in children not established).

    Carefully:Osteoporosis, hypercholesterolemia, ischemic heart disease, impaired liver function,severe renal failure (creatinine clearance <20 ml / min), lactase insufficiency, lactose intolerance, glucose-galactose malabsorption (in the drug form of the drug contains lactose).
    Dosing and Administration:

    Inside. The tablet is swallowed whole, washed down 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.

    Dysfunction of the kidneys: dose adjustment in patients with impaired renal function it takes.

    Dysfunction of the liver: dose adjustment in patients with mild to moderate degree liver function 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, 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 cardio-vascular system: very often - the "tides" of blood to the face.

    From the musculoskeletal system: very often - arthralgia; rarely a trigger finger.

    On the part of the reproductive system: often - dryness of the vaginal mucosa, vaginal bleeding (mainly during the first weeks after the cancellation or change of previous hormonal therapy on anastrozole).

    From the skin and skin appendages: very often - skin rash; often thinning hair, alopecia, very rarely - malignant exudative erythema (Stevens-Johnson syndrome)

    On the part of the digestive system: very often - nausea; often diarrhea, vomiting, anorexia.

    From the hepatobiliary system: often - increased activity of alanine aminotransferase, aspartate aminotransferase and alkaline phosphatase; rarely - increased activity of gamma-glutamyltransferase and bilirubin concentration, hepatitis.

    From the nervous system: very often - headache; often - increased drowsiness, carpal tunnel syndrome (mainly observed in patients with risk factors for this disease).

    From the side of metabolism: often - hypercholesterolemia.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.

    Allergic reactions: often - allergic reactions; very rarely anaphylactoid reactions, angioedema, hives, anaphylactic shock.

    Other: very often - asthenia.

    Overdose:Single cases of accidental drug overdose are described. A single dose of anastrozole, which could lead to life-threatening symptoms is not established. Specific there is no 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 vital organs and systems are recommended.
    Interaction:

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

    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, since 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 with anastrozole consultation and supervision of the gynecologist is necessary.

    There is no data on the use of anastrozole in patients with severe liver function disorders.

    Because the anastrozole reduces the concentration of circulating estradiol, this can lead to a decrease in bone mineral density. Therefore, in patients with osteoporosis or an increased risk of osteoporosis, the mineral density The bone tissue should be evaluated by densitometry, for example, DEXAScanning (dual-energy X-ray absorptiometry), at the beginning of treatment and regularly on its length. When it is necessary to prescribe the treatment or prevention of osteoporosis and carefully monitor the patient's condition. At the moment, there is insufficient data on positive effects of bisphosphonates on loss bone mineral density caused by anastrozole, or their benefits for prevention.

    There is no data on the simultaneous use of anastrozole and analog preparations of gonadotropin releasing hormone.

    With receptor-negative breast cancer or with ineffectiveness of previous therapy with tamoxifen, the efficacy of anastrozole is low.

    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 combined 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 potentially hazardous activities requiring increased concentration, attention and speed of psychomotor reactions. In this regard, recommended When these symptoms appear, use caution when operating vehicles and mechanisms.
    Form release / dosage:

    Tablets, film-coated, 1 mg each.

    Packaging:

    10 tablets per contour non-cellular package made of aluminum foil (strip); 3 strips each - together with instructions for use in a pack of cardboard.

    For 14 tablets in a contour non-jawed package of aluminum foil (strip); 2 strips together with instructions for use in a pack of cardboard.
    Storage conditions:

    Store in a dry place, at a temperature not exceeding 30 ° C.

    Keep out of the reach of children.
    Shelf life:3 years. Do not use after the expiration date printed on the package.
    Terms of leave from pharmacies:On prescription
    Registration number:PL-000785
    Date of registration:03.10.2011
    The owner of the registration certificate:ANSTAR, AG ANSTAR, AG Switzerland
    Manufacturer: & nbsp
    Representation: & nbspANSTAR AG ANSTAR AG Switzerland
    Information update date: & nbsp03.10.2011
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