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

    1 film-coated tablet contains: active substance: anastrozole 1.0 mg; Excipients: lactose monohydrate, povidone, sodium carboxymethyl starch, magnesium stearate; film shell: opadray white (macrogol 400, hypromellose, titanium dioxide).

    Description:

    White, round, biconvex tablets, covered with a film sheath, with engraving "ANA 1 "on one side of the tablet.At the break - white or almost white

    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 strong and highly selective non-steroidal aromatase inhibitor-enzyme, 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 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%.

    Anastrozole is 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 glucuronation.

    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 of early breast cancer with positive 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:

    - Hypersensitivity to anastrozole or other components of the drug.

    - Pregnancy and lactation.

    - Premenopause.

    - Severe hepatic impairment (safety and efficacy not established).

    - Concomitant therapy with tamoxifen or preparations containing estrogens.

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

    Carefully:

    Osteoporosis, hypercholesterolemia, ischemic heart disease, impaired hepatic 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 kidney: correction of the dose 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:

    Determination of the frequency of adverse reactions: 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: very often - "hot flashes".

    From the musculoskeletal and connective tissue: very often - arthralgia / joint stiffness, arthritis, often - bone pain, myalgia, infrequently - trigger finger.

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

    From the skin and subcutaneous tissues: very often skin rash, often thinning of hair (alopecia), allergic reactions, infrequent 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-glutamyl transferase 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 increased concentration 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 observed during clinical trials that are not associated with taking anastrozole: anemia, constipation, dyspepsia, back pain, abdominal pain, increased blood pressure, weight gain, depression, insomnia, dizziness, anxiety, paresthesia.

    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 antidote does not exist, 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 (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.

    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.

    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 persisting uterine bleeding against the background of receiving 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, 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. At the moment, there is insufficient data on the positive effect of bisphosphonates on the loss of bone mineral density caused by anastrozole, or their usefulness 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 concomitantly with anastrozole, as 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 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 driving andmechanisms.

    Form release / dosage:

    Film-coated tablets 1 mg.

    Packaging:

    10 tablets in a blister of PVC / PE / PVDC / aluminum foil. 3 or 9 blisters together with instructions for medical use are packed in a cardboard box.

    For 14 tablets in a blister of PVC / PE / PVDC / aluminum foil. 2 blisters together with instructions for medical use are packed in a cardboard box.
    Storage conditions:

    At a temperature of no higher than 30 ° C.

    Keep out of the reach of children.

    Shelf life:

    4 years. Do not use after the expiration date printed on the package.

    Terms of leave from pharmacies:On prescription
    Registration number:LSR-009050/10
    Date of registration:31.08.2010
    The owner of the registration certificate:Egis Pharmaceutical Plant OJSCEgis Pharmaceutical Plant OJSC Hungary
    Manufacturer: & nbsp
    Representation: & nbspEGIS ZAO Pharmaceutical Plant EGIS ZAO Pharmaceutical Plant Hungary
    Information update date: & nbsp16.04.2015
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