Active substanceAnastrozoleAnastrozole
Similar drugsTo uncover
  • AXASTROL®
    pills inwards 
    GRINDEX, JSC     Latvia
  • ANAMASTEN®
    pills inwards 
  • Anaester
    pills inwards 
  • Anastrozole
    pills inwards 
    ATOLL, LLC     Russia
  • Anastrozole
    pills inwards 
    BIOCAD, CJSC     Russia
  • Anastrozole
    pills inwards 
  • Anastrozole Kabi
    pills inwards 
  • Anastrozole San
    pills inwards 
  • Anastrozole-Teva
    pills inwards 
  • Anastrozole-TL
    pills inwards 
  • Anastrax®
    pills inwards 
    ANSTAR, AG     Switzerland
  • Arimidex®
    pills inwards 
    AstraZeneca UK Ltd     United Kingdom
  • Vero-Anastrozole
    pills inwards 
    VEROPHARM SA     Russia
  • Selana®
    pills inwards 
    NATIVA, LLC     Russia
  • Egistrazole
    pills inwards 
  • Estarizol
    pills inwards 
  • Dosage form: & nbspfilm coated tablets
    Composition:

    1 film coated tablet contains:

    Active substance: anastrozole -1 mg;

    Excipients: lactose monohydrate (Pharmatose 200M) 89.70 mg, povidone (Plasdone K29 / 32) 1.5 mg, sodium carboxymethyl starch 7.0 mg, magnesium stearate 0.8 mg.

    Shell composition: Deficient white (Y-1-7000) - 2.00 mg (hypromellose - 62.50%, titanium dioxide - 31.25%, macrogol 400 - 6.25%).

    Description:

    Round, biconvex tablets covered with a film shell of white or almost white color, engraved "H" on one side of the tablet and "1" on the other. On the cross-section the nucleus is white.

    Pharmacotherapeutic group:Antitumor agent, 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 that, with the help of androstendione in postmenopausal women, transforms into estrone in the peripheral tissues and further at estradiol. 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 oral administration (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 to 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 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 glucuronidation.

    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 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.

    Contraindications:

    - Hypersensitivity to anastrozole or other components of the drug.

    - The Premenopausal Period;

    - Severe hepatic impairment (safety and efficacy not established)

    - Concomitant therapy with tamoxifen or estrogens;

    - Pregnancy and lactation.

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

    Carefully:Osteoporosis, hypercholesterolemia, ischemic heart disease, liver dysfunction, 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 the meal.

    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 impaired renal function is not required

    Dysfunction of the liver: dose adjustment in patients with mild to moderate the degree of impaired 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 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 cardiovascular system: very often - the "tides" of blood to the face.

    From the musculoskeletal system: very often - arthralgia, bone pain, stiffness of joints, arthritis; rarely a trigger finger.

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

    From the skin and skin appendages: very often - skin rash; often thinning hair, alopecia; infrequently - hives, vasculitis, purpura (Shenllein-Genocha), erythema multiforme; very rarely - polymorphic 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 alanine aminotransferase, aspartate aminotransferase and alkaline phosphatase; rarely - increased activity of gamma-glutamyl transferase 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. Admission 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 clinical cases of accidental drug overdose are described. A single dose of anastrozole, which could lead to symptoms threatening life, 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. It is recommended that general supportive therapy, monitoring the patient and monitoring the functions of vital organs and systems.

    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.

    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.

    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, treatment or prevention of osteoporosis should be initiated under close observation of the patient's condition.

    To date, there is insufficient data on the positive effects of bisphosphonates on the loss of mineral bone density caused by anastrozole or their benefits when used for the purpose of prevention.

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

    In women with a receptor-negative tumor to estrogens, the efficacy of anastrozole has not been demonstrated, except in cases where there was a previous positive clinical response to tamoxifen.

    Preparations containing estrogens should not be administered concurrently 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 hormonal receptors are comparable to those of tamoxifen alone.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 dangerous activities requiring elevated attention and speed of psychomotor reactions. In this regard, it is recommended that when these symptoms occur, use caution when operating vehicles and mechanisms.

    Form release / dosage:

    Tablets, film-coated, 1 mg.

    Packaging:

    For 10 tablets in a PVDC / A1 blister.

    For 3 or 6 blisters with instructions for use in a pack of cardboard.

    When packaged at OOO "MAKIZ-PHARMA", Russia

    For 3 or 6 blisters together with instructions for use in a pack of cardboard.

    Storage conditions:

    In dry, 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-001675
    Date of registration:28.04.2012 / 06.10.2016
    Expiration Date:28.04.2017
    The owner of the registration certificate:Heterose Labs LimitedHeterose Labs Limited India
    Manufacturer: & nbsp
    Information update date: & nbsp28.08.2017
    Illustrated instructions
      Instructions
      Up