Active substanceLetrozoleLetrozole
Similar drugsTo uncover
  • Lestrodex
    pills inwards 
  • Letrosa®
    pills inwards 
    ANSTAR, AG     Switzerland
  • Letrozole
    pills inwards 
    APF-TRADING, CJSC     Russia
  • Letrozole
    pills inwards 
    JODAS EKSPOIM, LLC     Russia
  • Letrozole
    pills inwards 
  • Letrozole
    pills inwards 
    Kern Pharma S.L.     Spain
  • Letrozole
    pills inwards 
  • Letrozole
    pills inwards 
  • Letrozole-Teva
    pills inwards 
    TEVA, LLC     Russia
  • Letrosan
    pills inwards 
  • Letrotera
    pills inwards 
  • Loreta
    pills inwards 
  • Nexazole®
    pills inwards 
    GEDEON RICHTER, OJSC     Hungary
  • Oreta®
    pills inwards 
  • Femara®
    pills inwards 
    Novartis Pharma AG     Switzerland
  • Extrasia
    pills inwards 
    VEROPHARM SA     Russia
  • Estrolet®
    pills inwards 
    NATIVA, LLC     Russia
  • Dosage form: & nbspfilm-coated tablets
    Composition:

    Each film-coated tablet contains:

    active substance: letrozole - 2.5 mg;

    Excipients: lactose monohydrate - 91.5 mg, croscarmellose sodium 2.0 mg, povidone-K30 1.0 mg, silicon dioxide colloid 2.0 mg, magnesium stearate 1.0 mg;

    shell composition: opadray yellow (hypromellose-2910 (6sP) - 60.00%, titanium dioxide (E171) - 14.11%, macrogol-3350 - 10.00%, iron dye oxide yellow (E172) - 10.89%, talc - 5.00%) - 2.5 mg.
    Description:

    Round biconvex tablets, film-coated, dark yellow, tight "LET" on one side and "2.5" on the other.

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

    L.02.B.G.04   Letrozole

    L.02.B.G   Enzyme Inhibitors

    Pharmacodynamics:

    Letrozole selectively inhibits aromatase (an enzyme for the synthesis of estrogens) by highly competitive binding with the subunit of this enzyme - heme cytochrome P450. It blocks the synthesis of estrogens both in the peripheral and in the tumor tissues.

    In postmenopausal women, estrogens are formed, mainly, with the aromatase enzyme that converts androgen synthesized in the adrenal gland (primarily androstenedione and testosterone) into estrone and estradiol.

    Daily intake of letrozole leads to a decrease in the concentration of estradiol,estrone and estrone sulfate in blood plasma at 75-95% of the original content. Failure of synthesis steroid hormones in the adrenal gland are not observed. Suppression of the synthesis of estrogens is maintained throughout the treatment.

    Blockade biosynthesis of estrogens does not lead to the accumulation of androgens, which are precursors of estrogens. Patients who received letrozole, there were no changes in the concentrations of luteinizing and follicle-stimulating hormones in plasma, as well as there was no change in thyroid function.

    Pharmacokinetics:

    Letrozole is quickly and completely absorbed from the gastrointestinal tract (GIT), on average bioavailability is 99.9%. Food slightly reduces the rate of absorption, but it does not have clinical significance, therefore letrozole can be taken regardless of food intake.

    The connection between letrozole and plasma proteins is approximately 60%, (mainly with albumin - 55%). The equilibrium concentration is achieved during 2-6 weeks of daily intake of a daily dose of 2.5 mg. Pharmacokinetics is nonlinear. Cumulation with long-term use is not noted.

    Letrozole is largely metabolized by isozymes CYP3A4 and CYP2A6, with the formation of a pharmacologically inactive carbinol compound.

    It is excreted mainly by kidneys in the form of metabolites, to a lesser extent - through the intestine. Half-life (T1/2) is 48 hours. It is excreted from the plasma by means of hemodialysis.

    The pharmacokinetic parameters of letrozole do not depend on the age of the patient. In renal failure pharmacokinetic parameters do not change.

    With a mild violation of liver function (Child-Pugh B) mean values AUC (area under the pharmacokinetic curve "concentration-time"), although higher by 37%, but remain within the range of values ​​that are observed in individuals without violations of liver function. In patients with cirrhosis of the liver and severe impairment of its function AUC increases by 95% and T1/2 on 187%. However, given the good tolerability of high doses of the drug (5-10 mg / day) at There is no need to change the dose of letrozole in these cases.

    Indications:

    - Early stages of breast cancer, cells of which have receptors for hormones, in postmenopausal women, as adjuvant therapy;

    - early stages of breast cancer in postmenopausal women after completion of standard adjuvant tamoxifen therapy in quality of extended adjuvant therapy;

    - common hormone-dependent forms of cancer breast cancer in postmenopausal women (first-line therapy);

    - common forms of breast cancer in postmenopausal women (natural or induced artificially); who received previous therapy with antiestrogens.

    Contraindications:

    Increased sensitivity to letrozole or any other component of the drug.

    Endocrine status, characteristic of the premenopausal period.

    Pregnancy, the period of breastfeeding.

    Age to 18 years.

    Carefully:

    In severe violations of the liver and kidneys (creatinine clearance less than 10 ml / min) before the appointment of letrozole should carefully weigh the ratio between the potential risk and the expected effect of treatment.

    Deficiency of lactase, lactose intolerance, glucose-galactose malabsorption (dosage form contains lactose).

    Dosing and Administration:

    Inside, regardless of food intake.

    The recommended dose of letrozole is 2.5 mg once daily, daily, and for a long time.If signs of disease progression appear, letrozole should be discontinued.

    In elderly patients, dosage correction of letrozole is not required.

    Patients with impaired hepatic and / or renal function. In patients with impaired hepatic or renal function (creatinine clearance 10 ml / min) dose adjustment is not required. Nevertheless, patients with severe impairment of liver function should be under constant supervision.

    Side effects:

    The frequency of side effects: very often - ≥10%, often - ≥1-10%, sometimes - ≥0.1% - <1%, rarely - ≥0.01-0.1%, very rarely - <0.01%, including individual messages.

    On the part of the digestive system: often - nausea, vomiting, indigestion, constipation, diarrhea; sometimes - pain in the abdominal region, stomatitis, dry mouth, increased activity of "liver" enzymes; very rarely - hepatitis.

    From the central and peripheral nervous system: often - headache, weakness, depression, irritability; sometimes - nervousness, hypoesthesia, anxiety, drowsiness, insomnia, memory impairment, dysesthesia; rarely - hyperesthesia.

    From the hemopoietic system and lymphatic system: sometimes - a leukopenia.

    From the cardiovascular system: sometimes - a feeling of palpitations, tachycardia, deep and superficial venous thrombophlebitis, increased blood pressure (BP), angina pectoris, myocardial infarction, heart failure; rarely - pulmonary embolism, thrombosis of the arteries, cerebral circulation disorders.

    From the respiratory system: sometimes - shortness of breath, cough.

    From the skin and skin appendages: often - alopecia, increased sweating, skin rash (erythematous, maculopapular, vesicular, psoriasis-like); sometimes - itchy skin, dry skin, urticaria; rarely - angioedema, anaphylactic reactions, Lyell's syndrome, Stephen-Johnson syndrome.

    From the musculoskeletal system: very often - arthralgia; often - myalgia, ossalgia, osteoporosis, fractures of bones; sometimes - arthritis.

    From the sense organs: sometimes - cataract, eye irritation, "misting" sight, a violation of taste.

    From the side of the urinary system: sometimes - frequent urination.

    On the part of the reproductive system: sometimes - pain in the mammary glands, vaginal bleeding, vaginal discharge, dryness of the vagina.

    Other: very often - paroxysmal sensations of heat ("hot flashes"), often - increased fatigue, asthenia, general malaise, peripheral edema, weight gain, hypercholesterolemia, increased appetite; sometimes - thirst, weight loss, pain in the tumor nodes, urinary tract infection; rarely - a febrile state.

    Overdose:

    When Oreta overdoses, it may develop symptoms similar to the side effect of the drug. Specific treatments for overdose are unknown.

    Symptomatic and supportive therapy is indicated.

    Interaction:

    Clinical Application Experience letrozole in combinations with other antitumour agents are not currently available.

    According to the research results in vitro, letrozole suppresses activity of cytochrome P450 isoenzymes - CYP2A6 and CYP2C19 (the latter is moderately). When deciding the importance of this data for clinics it is necessary to take into account that isoenzyme CYP2A6 does not play a significant role in the metabolism of drugs. In experiments in vitro it was shown that letrozole, in concentrations 100 times higher than equilibrium plasma, does not have the ability to significantly inhibit the metabolism of diazepam (a substrate for CYP2C19). Thus, clinically significant interactions from isoenzyme CYP2C19 unlikely. Nevertheless, caution should be exercised in the joint use of letrozole and drugs metabolized, mainly, with the participation of the aforementioned isoenzymes and with a narrow therapeutic index.
    Special instructions:

    Patients with severe impairment of liver function should be under constant supervision.

    Effect on the ability to drive transp. cf. and fur:Some of the side effects of the drug, such as general weakness and dizziness, can affect the ability to perform potentially dangerous activities requiring concentration and quick reactions. In this regard, care should be taken when driving vehicles and machinery.
    Form release / dosage:Tablets, film-coated, 2.5 mg.
    Packaging:

    For 10 tablets in PVC / PVDC / aluminum blister. 3 blisters per pack of cardboard with instructions for use.

    Storage conditions:

    At a temperature of no higher than 25 ° C.

    Keep out of the reach of children!

    Shelf life:

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

    Terms of leave from pharmacies:On prescription
    Registration number:LP-001062
    Date of registration:27.10.2011 / 20.12.2012
    Expiration Date:27.10.2016
    Date of cancellation:2016-10-27
    The owner of the registration certificate:Dr. Reddy's Laboratories Ltd.Dr. Reddy's Laboratories Ltd. India
    Manufacturer: & nbsp
    Representation: & nbspDR REDDY'S LABORATORIS LTD. DR REDDY'S LABORATORIS LTD. India
    Information update date: & nbsp11.06.2017
    Illustrated instructions
      Instructions
      Up