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

    1 tablet, film-coated, contains:

    active substance: anastrozole 1.0 mg; Excipients: lactose monohydrate 93.0 mg, sodium carboxymethyl starch 3.0 mg, povidone 2.0 mg, magnesium stearate 1.0 mg;

    composition of the shell: Drop off white (Y-1-7000): macrogol (PEG 400) 0.16 mg, hypromellose (HPMC) 1.56 mg, titanium dioxide 0.78 mg.

    Description:White round biconvex tablets, covered with a film membrane. One side of the tablet is engraved "ANA" and "1". On the fracture, the core is 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 highly selective non-steroidal aromatase inhibitor, an enzyme, with which, in women, 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 replace 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 anastrozole in the blood plasma with a single intake of a daily dose. 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.

    Metabolism anastrozole 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:Indications for use

    - 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:

    - Hypersensitivity to anastrozole or other components of the drug;

    - Premenopause;

    - Severe hepatic impairment (safety and efficacy not installed);

    - Concomitant therapy with tamoxifen or preparations containing estrogens;

    - Pregnancy and the period of breastfeeding;

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

    Carefully:

    With caution: 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 monohydrate).

    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:

    Frequency of adverse reactions given 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: very often - the "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 - dryness of the vaginal mucosa, 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 hair, alopecia, allergic reactions; infrequently - hives; 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 excretory ways: 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 not associated with anastrozole use: anemia, constipation, indigestion, 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 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.

    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:Precautions for use

    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.

    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. At the moment, there is insufficient data on the positive effect of bisphosphonates on the lossbone mineral density caused by anastrozole or their benefits when used for the purpose of prevention.

    There is no data on simultaneous anastrozole and preparations - analogues of gonadotropin - releasing hormone.

    With receptoronegative 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 the 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 10 or 14 tablets per blister PVC / PE / PVDC. For 3 blisters for 10 tablets and 2 blisters for 14 tablets in a cardboard box with instructions for use.
    Storage conditions:

    At a temperature of no higher than 25 ° C. Keep out of the reach of children!

    Shelf life:30 months. Do not use after the expiration date printed on the package.
    Terms of leave from pharmacies:On prescription
    Registration number:LP-000138
    Date of registration:12.01.2011
    Date of cancellation:2016-12-09
    The owner of the registration certificate:Actavis PTS ehf GroupActavis PTS ehf Group Iceland
    Manufacturer: & nbsp
    Representation: & nbspACTAVIS GROUP AO ACTAVIS GROUP AO Iceland
    Information update date: & nbsp09.12.2016
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