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

    1 tablet, film-coated, contains:

    Active substance:

    Anastrozole

    1.0 mg

    Excipients:


    Magnesium Aluminometasilicate

    9.0 mg

    Croscarmellose sodium

    3.0 mg

    Silica colloidal dioxide

    3.0 mg

    Magnesium stearate

    0.5 mg

    Loudipresse

    83.5 mg

    in terms of components:


    - lactose monohydrate

    77.7 mg

    - Povidone

    2.9 mg

    - crospovidone

    2.9 mg

    Sheath: Opadry II white 85F48105

    5.0 mg

    (polyvinyl alcohol from 35.0 to 49.00%, talc from 9.80 to 25.00%, macrogol 3350 from 7.35 to 35.20%, titanium dioxide from 15.15 to 30.00%)

    Description:round biconvex tablets, covered with a white film shell, on the cross section the nucleus is 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. Aromatase is an enzyme by which in women in the postmenopausal period androstenedione in peripheral tissues is converted into estrone and further into estradiol. Anastrozole has antitumor activity against estrogen-dependent breast tumors in postmenopausal women. In the postmenopausal period, the drug in a daily dose of 1 mg causes a decrease in the concentration of estradiol by 80%.

    Anastrozole does not possess progestagenic, androgenic and estrogenic activity. Anastrozole in a daily dose of up to 10 mg does not have an effect on the secretion of cortisol and aldosterone (therefore, the use of the drug does not require the substitution of corticosteroids).

    Pharmacokinetics:

    Suction

    After oral administration anastrozole quickly absorbed from the gastrointestinal tract. The maximum concentration (CmOh) in plasma is achieved within 2 hours (on an empty stomach). 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 the drug in the plasma with a single daily dose.

    Distribution

    Anastrozole binds to plasma proteins by 40%. After a 7-day treatment, approximately 90 to 95% of the equilibrium plasma anastrozole concentration is achieved. There is no information on the dependence of pharmacokinetic parameters on time and dose.

    Metabolism

    Anastrozole is metabolized by N-dealkylation, hydroxylation and glucuronization. Triazole, the main metabolite, determined in plasma, does not inhibit aromatase.

    Excretion

    Anastrozole is slowly excreted, the half-life (T1/2) is 40-50 hours. Anastrozole and its metabolites are excreted mainly with urine. Less than 10% of the dose is excreted unchanged in urine within 72 hours after taking the drug.

    Pharmacokinetics in special clinical cases

    The determined clearance of anastrozole after oral administration in patients with cirrhosis of the liver or renal dysfunction does not differ from the clearance determined in healthy people.

    The pharmacokinetics of anastrozole does not depend on the age of postmenopausal women.
    Indications:

    Adjuvant therapy of early hormone-positive breast cancer in postmenopausal women.

    Treatment of advanced breast cancer in postmenopausal women.

    Adjuvant therapy for early hormone-positive breast cancer in postmenopausal women after tamoxifen therapy for 2-3 years.
    Contraindications:

    - Hypersensitivity to anastrozole and other components of the drug.

    - Severe renal insufficiency (creatinine clearance less than 20 ml / min).

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

    - Concomitant therapy with tamoxifen or preparations containing estrogens.

    - Child age (safety and efficacy not established).

    - The Premenopausal Period.

    - Pregnancy and the period of breastfeeding.

    Carefully:

    Osteoporosis, hypercholesterolemia, lactase deficiency, lactose intolerance, glucose-galactose malabsorption (in the drug form of the drug contains lactose), ischemic heart disease, impaired liver function.

    Pregnancy and lactation:

    Application of the drug during pregnancy and during breastfeeding it is contraindicated.

    Dosing and Administration:

    The tablet should be swallowed whole and washed with water. It is recommended to take the drug at the same time of day.

    Adults, including elderly patients, the drug prescribed 1 mg orally once a day, long. If signs of disease progression appear, the drug should be discontinued. As an adjuvant therapy, the recommended duration of treatment is 5 years.

    Patients with mild to moderate renal insufficiency not required dose adjustment.

    Patients with mild hepatic impairment no dose adjustment is required.

    Side effects:

    Side effects recorded more often than single observations are listed below for organs and systems, indicating the frequency of their occurrence. Determination of the frequency of adverse reactions: very often (> 10%); often (1-10%); infrequently (0.1-1%); rarely (0,01 - 0,1%); very rarely (<0.01%).

    From the cardiovascular system: very often - "hot flashes" of heat, increased blood pressure; often - vasodilation, ischemic cardiovascular diseases.

    From the musculoskeletal system: very often - arthralgia, joint stiffness, arthritis, back pain, decreased bone mineral density, osteoporosis and bone fractures; often - pain in the bones, myalgia; infrequently - "trigger finger" or "snapping finger" (impaired ability to straighten a finger, usually middle or anonymous).

    From the reproductive and genitourinary system: often - dryness of the vaginal mucosa, vaginal bleeding (mainly during the first weeks after the abolition or replacement of previous hormonal therapy for anastrozole preparations), vulvovaginitis, vaginitis, pelvic pain; infrequently - mucous discharge from the vagina, urinary tract infection, chest pain; rarely - endometrial cancer, neoplasms in the chest.

    From the side of the blood and lymphatic system: very often - lymphedema; infrequently, anemia.

    From the digestive system: very often - nausea, vomiting; often - diarrhea, constipation, dyspepsia, increased activity of alkaline phosphatase, alanylaminotransferase, aspartate aminotransferase; infrequently - abdominal pain, increased activity of gamma-glutamintransferase and bilirubin concentration, hepatitis, dry mouth.

    From the nervous system: very often - headache, dizziness, sleep disturbances, depression; often - carpal tunnel syndrome (mainly observed in patients with risk factors for this disease), a sense of anxiety, paresthesia.

    From the sense organs: infrequently, cataract.

    From the respiratory system: very often - pharyngitis, coughing, shortness of breath; infrequently - pain in the chest, sinusitis, bronchitis.

    From the side of metabolism: very often peripheral edema; often - anorexia, hypercholesterolemia, hypercalcemia (with or without increased parathyroid hormone concentration), weight gain.

    From the skin and appendages: very often - skin rash; often thinning hair, alopecia; infrequently, erythema multiforme (Stevens-Johnson syndrome), cutaneous vasculitis (including isolated cases of purpura (Shenlaine-Genoch syndrome)). Allergic reactions: often - allergic reactions; infrequently - hives; rarely anaphylactoid reaction; very rarely - angioedema.

    Other: very often - asthenia.

    If you notice any other side effects not listed in the instructions, inform the doctor about it.

    Overdose:

    Single clinical cases of anastrozole overdose are described. A single dose of anastrozole, at which life-threatening symptoms develop, is not established. Treatment: there is no specific antidote. If necessary, conduct symptomatic therapy. Initiate vomiting (if the patient is conscious), conduct general supportive therapy and monitoring the patient, control the functions of vital organs and systems. Dialysis is possible.

    Interaction:

    The drug interaction with phenazone (Antipyrine) and cimetidine indicates that the combined use of anastrozole with other drugs is unlikely to lead to a clinically significant interaction caused by cytochrome P450.

    There are no data on clinically significant drug interaction with simultaneous administration of anastrozole with other commonly used drugs.

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

    Preparations containing estrogens should not be used concomitantly with anastrozole. they reduce the pharmacological action of the latter.

    Do not use tamoxifen simultaneously with anastrozole, since it can weaken the pharmacological action of the latter.

    Special instructions:

    The hormonal status of menopause in a patient should be confirmed by the determination of sex hormones in the blood serum.

    The efficacy of anastrozole in women with a receptor-negative tumor to estrogens has not been noted, except when there was a previous positive clinical response to the use of tamoxifen.

    There is no data on the safety of anastrozole administration in patients with severe hepatic impairment or in patients with severe renal insufficiency (creatinine clearance less than 20 mL / min).

    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.Reducing the concentration of circulating estradiol, anastrozole can cause a decrease in bone mineral density.

    In patients with osteoporosis or a risk of 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 close medical supervision. There is no data on the simultaneous use of anastrozole and preparations of gonadotropin-releasing hormone analogues (GnRH). It is not known whether anastrozole results of treatment when combined with chemotherapy.

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

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

    Care should be taken when driving vehicles and machinery, becauseSome of the side effects of the drug, such as asthenia, headache, dizziness and sleep disorders, can adversely affect the ability to perform work that requires increased concentration and speed of psychomotor reactions. If these side effects occur, you should refrain from performing these activities.

    Form release / dosage:

    Tablets, film-coated, 1 mg.

    Packaging:

    For 7 tablets in a planar cell box made of polymer film and aluminum foil, 4 contour squares, together with instructions for use, are placed in a cardboard box.

    For 10 tablets in a planar cell package of a polymer film and aluminum foil, 3 contour mesh packages along with the instruction for use are placed in a cardboard box.

    For 14 tablets in a contour cell box made of a polymer film and aluminum foil, 2 contoured cell packs along with the instruction for use are placed in a cardboard box.
    Storage conditions:Store in a dark place at a temperature of no higher than 25 ° 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:LP-002194
    Date of registration:22.08.2013
    The owner of the registration certificate:NATIVA, LLC NATIVA, LLC Russia
    Manufacturer: & nbsp
    Information update date: & nbsp29.12.2014
    Illustrated instructions
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