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, povidone 2.0 mg, carboxymethyl starch sodium 3.0 mg, magnesium stearate 1.0 mg

    composition of the film jacket: hypromellose 1.50 mg, macrogol 300 0.30 mg, titanium dioxide 0.45 mg.

    Description:

    Round, biconvex tablets of white color, covered with a film membrane; with engraving A - on one side and Adx another.

    Pharmacotherapeutic group:Antitumor agent, estrogen synthesis inhibitor
    ATX: & nbsp

    L.02.B.G   Enzyme Inhibitors

    L.02.B.G.03   Anastrozole

    Pharmacodynamics:

    Arimidex® is a highly selective, non-steroidal aromatase inhibitor, an enzyme used to treat androstanedione in postmenopausal women peripheral tissues is converted into estrone and further into estradiol. Decrease of the level circulating estradiol in patients with breast cancer has a therapeutic effect. In postmenopausal women, Arimidex® at a daily dose of 1 mg causes a decrease in the level of estradiol by 80%.

    Arimidex® does not possess progestogen, androgenic and estrogenic activity. Arimidex® in daily doses up to 10 mg does not have an effect on the secretion of cortisol and aldosterone, therefore, when using Arimidex®, no substitution corticosteroids are required.

    Effect on bone mineral density

    It was shown that in patients with hormone-positive early breast cancer in postmenopause, who take Arimidex ®, changes in the bone system may be warned in accordance with standards established to treat patients with a certain risk of fractures. Thus, the advantage of Arimidex ® in combination with bisphosphonates (in comparison with Arimidex ® only) in patients with an average and high risk of fracture was demonstrated after 12 months in terms of bone mineral density, structural changes in bone tissue and markers of bone resorption. Moreover, in the low-risk group, there was no change in the mineral bone density index against the background of therapy with a single preparation of Arimidex® and maintenance treatment with vitamin D and calcium.

    Lipids

    When therapy with Arimidex®, including when taken in combination with bisphosphonates, no changes in the level of lipids in the plasma were detected.
    Pharmacokinetics:

    Absorption of anastrozole is fast, the maximum concentration in the plasma is reached 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 plasma with a single daily dose of Arimidex®. After a 7-day treatment, approximately 90-95% of the equilibrium concentration of anastrozole in plasma is achieved. Information about there is no 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 withdrawn slowly, the half-life from the plasma is 40-50 hours. Extensively metabolized in postmenopausal women. Less than 10% of the dose is excreted unchanged in urine within 72 hours after taking the drug. Anastrozole metabolism is carried out N-dealkylation, hydroxylation and glucuronization. Metabolites are excreted mainly with urine. Triazole, the main metabolite, determined in plasma, does not inhibit aromatase.

    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, 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 constituents of the drug
    • Pregnancy and lactation
    • In premenopausal women
    • Severe renal insufficiency (creatinine clearance less than 20 ml / min)
    • Moderate or severe hepatic insufficiency (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 liver function, lactase deficiency, glucose-galactose malabsorption.

    Dosing and Administration:

    Inside. Swallow the whole tablet with water. It is recommended to take the drug at the same time.

    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.

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

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

    Side effects:

    Frequency of occurrence was calculated from the number of undesirable phenomena, observed in the phase III study in 9,366 women with operable breast cancer in postmenopausal women who received treatment for 5 years, while the frequency of adverse events in the comparison groups and the opinion of the researcher as to the dependence of the undesirable phenomenon on the study drug are not taken into account.

    Determination of the frequency of adverse reactions: very often (more than or equal to 10%); often (from 1 to less than 10%); infrequently (from 0.1 to less than 1%); rarely (from 0.01 to less than 0.1%); very rarely (less than 0.01%).

    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 breast: often - dryness of the mucosa the vagina; vaginal bleeding (mainly during the first weeks after the abolition or change of previous hormonal therapy for Arimidex®).

    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 (Shenllein-Genoch syndrome)), very rarely Stevens syndrome -Johnson, angioedema.

    From the gastrointestinal tract: very often - nausea, often - diarrhea, vomiting.

    From the liver and biliary tract: 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 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 that are not related to taking Arimidex®: 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 Arimidex®, which could lead to life-threatening symptoms, has not been established.

    Specific antidote does not exist, in case of an overdose, treatment should be symptomatic. You can induce vomiting if the patient is conscious. Can be done, dialysis. General supportive therapy, patient monitoring and monitoring of the function of vital organs and systems are recommended.

    Interaction:

    Studies on the drug interaction with phenazone (antipyrine) and cimetidine indicate that the combined use of Arimidex® with other drugs is unlikely to result in a clinically significant drug interaction mediated by cytochrome P450.

    Clinically significant drug interaction with taking Arimidex® simultaneously with other commonly prescribed drugs is not available.

    At the moment there is no information on the use of the drug Arimidex ® in combination with other antitumor drugs.

    Preparations containing estrogens reduce the pharmacological action of the drug Arimidex®, and therefore they should not be administered concomitantly with the preparation of Arimidex®.

    Do not assign tamoxifen at the same time as Arimidex®, because it can weaken the pharmacological action of the latter.
    Special instructions:

    Safety and efficacy in children is not established.

    In women with a receptor-negative tumor to estrogens, the efficacy of Arimidex® has not been demonstrated, except in cases where there was a previous positive clinical response to tamoxifen. In case of doubt, the patient's hormonal status of menopause should be confirmed by the determination of sex hormones in the blood serum.

    No data on the use of the drug. Arimidex® in patients with moderate or severe hepatic impairment and in patients with severe renal insufficiency (creatinine clearance less than 20 mL / min).

    In the case of persisting uterine bleeding against the background of taking Arimidex®, consultation and supervision of the gynecologist is necessary.

    Preparations containing estrogens should not be given concomitantly with the preparation of Arimidex®, since these drugs will neutralize its pharmacological action.

    Reducing the level of circulating estradiol, Arimidex® can cause a decrease in bone mineral density, followed by an increased risk of fracture.Patients with such a high risk should be treated according to the guidelines for the therapy of these complications.

    In patients suffering from osteoporosis or who are at risk for developing osteoporosis, bone mineral density should be assessed by densitometry, for example, DEXA scanning (Dual-Energy, X-ray Absorptiometry - dual-energy X-ray absorptiometry), at the beginning of treatment and in dynamics. If necessary, treatment should be initiated or prevention, osteoporosis, under the careful supervision of a doctor.

    There is no data on the simultaneous use of anastrozole and LHRH analogues. It is not known whether anastrozole results of treatment when used in conjunction with chemotherapy.

    Safety data for prolonged treatment with anastrozole have not yet been obtained.

    When using the drug Arimidex ® more often than with tamoxifen, there were ischemic diseases, but no statistical significance was noted.

    The efficacy and safety of Arimidex® 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.

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

    Some of the side effects of Arimidex®, such as asthenia and drowsiness, can adversely affect the ability to perform potentially dangerous activities that require increased concentration, attention 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 each.

    Packaging:14 tablets in a blister of Al / PVC; 2 blisters with instructions for use in a cardboard bundle with the control of the first autopsy.
    Storage conditions:

    At temperatures not higher than 30 ° C, out of reach of children.

    Shelf life:

    5 years.

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

    Terms of leave from pharmacies:On prescription
    Registration number:П N013285 / 01
    Date of registration:19.02.2010 / 14.08.2017
    Expiration Date:Unlimited
    The owner of the registration certificate:AstraZeneca UK LtdAstraZeneca UK Ltd United Kingdom
    Manufacturer: & nbsp
    Information update date: & nbsp12.09.2017
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