Fareston (Fareston)

Composition Pharmacodynamics Indications Carefully Contraindications Dosing and Administration Side effects Form release / dosage
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Active substanceToremifeneToremifene
Similar drugsTo uncover
  • Fareston
    pills inwards 
    Orion Corporation     Finland
    • Dosage form: & nbspPills.
    Composition:
    Each tablet contains
    active substance - toremifene (in the form of toremifene citrate) 20 mg or 60 mg;
    auxiliary substances: corn starch, lactose, povidone, sodium starch glycolate (type A), magnesium stearate, microcrystalline cellulose, siliceous colloidal anhydrous.
    Description:

    Tablets of 20 mg: White round, flat with beveled edge tablets with TO20 code on one side.

    Tablets of 60 mg: White round, flat with beveled edge tablets with code T060 on one side.

    Pharmacotherapeutic group:Antitumor agent, antiestrogen.
    ATX: & nbsp

    L.02.B.A   Antiestrogens

    L.02.B.A.02   Toremifene

    Pharmacodynamics:
    Toremifene is a non-steroidal antiestrogenic agent derived from triphenylethylene.
    Toremifene specifically binds to estrogen receptors, competing with estradiol, inhibits estrogen-induced DNA synthesis, and cell replication. At high doses, toremifene can have an antitumor effect that is not associated with an estrogen-dependent effect.
    The antitumor effect of toremifene in patients with breast cancer is mainly associated with its anti-estrogenic activity, although other mechanisms of action can not be ruled out (regulation of oncogene expression, growth factor secretion, induction of apoptosis, effect on the kinetics of the cell cycle).

    Pharmacokinetics:
    Toremifene is completely absorbed when taken orally. The maximum concentration in the blood serum occurs within 3 hours (2-5 hours). Eating does not affect the completeness of absorption, but can delay the time to reach a maximum concentration of 1.5 -2 hours. These changes have no clinical significance.
    After a fast distribution phase with an average half-life of about 4 hours (2-12 hours), a slow elimination phase begins with an average half-life of about 5 days (2-10 days).
    The connection with proteins is 99.5% (mainly with albumin). The equilibrium concentration in plasma is established within 3-4 weeks (at recommended doses of 60 mg per day).
    Toremifene is metabolized in the liver by hydroxylation and demethylation with the participation of cytochrome CYP3A4 with the formation of an active metabolite - N-demethyltoremifene. The average half-life of toremifene half-life is 5 days, N-demethyltoremifene - 11 days (4-20 days). In the blood serum, there were found three more metabolites: deaminohydroxytorrhoefen, 4-hydroxytorhomiphene and N, N -ddemethyltoremiphene. The total ground clearance is 5 l / h.
    It is excreted through the intestines mainly in the form of metabolites; about 10% - by the kidneys within 1 week.
    Indications:Estrogen-dependent breast cancer in postmenopausal women.
    Contraindications:
    - Hypersensitivity to toremifene and / or any other ingredient in the preparation.
    - Available in the anamnesis indications on endometrial hyperplasia, severe hepatic insufficiency, thromboembolism.
    - Pregnancy and lactation.
    - Congenital or acquired documented elongation of the QT interval.
    - Violation of the electrolyte balance, especially with uncorrected hypokalemia.
    - Clinically significant bradycardia.
    - Clinically significant heart failure with a reduced fraction of ejection of the left ventricle.
    Symptomatic arrhythmia in the anamnesis.
    - Simultaneous reception of drugs that extend the QT interval.

    Carefully:
    - leukopenia,
    - thrombocytopenia,
    - Hypercalcemia (including on the background of metastasis in bone tissue),
    - Decompensated heart failure,
    - severe angina,
    - proaritmogenic states (acute myocardial ischemia, prolongation of the QT interval),
    - elderly age,
    - deficiency of lactase, lactose intolerance, glucose-galactose malabsorption syndrome.
    Pregnancy and lactation:
    Torimifen is recommended to patients in the postmenopausal period.
    The drug is contraindicated for use during pregnancy and lactation.
    Dosing and Administration:
    Inside. The dosage regimen is set individually. As a standard dose for the first line of hormone therapy, taking 60 mg orally daily is long. When appointing Phareston as the second line of hormonal treatment, the dose of the drug can be increased to 240 mg per day (120 mg x 2 times a day).
    When there are signs of progression of the disease, taking the drug is canceled.
    Side effects:The most common side effects are paroxysmal sensations of heat ("hot flashes"), excessive sweating, uterine bleeding, or vaginal discharge (whites), increased fatigue, nausea, rash, itching in the genital area, delay fluid, dizziness, depression. These side effects are usually mild and are caused by hormonal action of toremifene.
    The frequency of unwanted reactions is classified in the following way:

    Very frequent (> 1/10)

    Frequent (> 1/100, < 1/10)

    Infrequent (> 1/1000, <1/100)

    Rare (> 1/10000, <1/1000)

    Very rare (<1/10 000)

    Frequency is unknown (can not be estimated from available data).ATPossible adverse events are presented according to organ systems and are distributed according to the frequency of development.

    Highly

    Frequent

    Infrequent

    Rare

    Highly

    Frequency


    frequent




    rare

    unknown

    Goodwillat





    cancer

    endometrria


    ence,

    malignant and

    unspecified

    neoplasms (including cysts and polyps)




    Violations of the bloodand

    lmnfatichessystem






    Thrombocytopenia,

    anemia and

    leukopenia

    Disorders of nutrition and metabolism



    loss of appetite




    Disorders of the psyche


    Deprezthis

    insomnia




    Disturbances from the nervous system


    Headcircling

    headache




    Vision disorders





    Pomutnethe

    cornea


    Hearing impairments




    vertigo



    Vascular disorders

    "tides"


    Thrombotembolic






    state of




    Disturbances from the respiratory, thoracic and mediastinal organs



    dyspnea





    Disorders from the gastrointestinal tract


    sickeninglyta, vomiting

    constipation





    Disturbances from the liver and biliary tractother ways




    rise

    activity

    hepatictranceaminase

    jaundice



    Disturbances from the skin and subcutaneous fat

    Potleycognition

    rash, itching



    alopecia



    Disorders from the reproductive sidesystem and mammary glands


    Matoobleedingcurrents or whites

    hypertrophyendometrium

    polyps of the endometrium

    hyperplasticendometrial glandria



    General disorders and disorders at the site of administration


    Mouthswelling, swelling

    Increasebody weight




















    Thromboembolic complications include deep venous thrombosis, thrombophlebitis and pulmonary embolism.
    Therapy with toremifene is accompanied by changes in the level of hepatic enzymes (an increase in the level of transaminases) and in very rare cases with more severe impairment of liver function (jaundice). In some cases, patients with bone metastases at the beginning of treatment with toremifene noted hypercalcemia.
    Hypertrophy of the endometrium may develop during treatment due to the partial estrogenic effect of toremifene. There is a risk of increased changes in the endometrium such as hyperplasia, polyposis and cancer. This can be caused by the main pharmacological property of toremifene - estrogen stimulation.
    Overdose:Symptoms: vertigo, dizziness, headache nausea and / or vomiting were noted at daily doses of 680 mg. Theoretically, an overdose may be manifested by increased anti-estrogenic effects ("hot flashes") or estrogenic effects (vaginal bleeding).The possibility of a dose-dependent prolongation of the QT interval should be taken into account.
    Treatment: symptomatic therapy.
    Interaction:
    Drugs that reduce renal calcium excretion (including thiazide diuretics) may increase the risk of hypercalcemia.
    Drugs that stimulate the intensity of microsomal oxidation (for example, phenobarbital, phenytoin or carbamazepine), can accelerate the metabolism of toremifene, thereby reducing its concentration in the serum. In such cases, the daily dose should be doubled.
    Interaction between antiestrogens and warfarin can lead to a marked increase in bleeding time (simultaneous use of toremifene and drugs of this group should be avoided).
    Inhibitors isoenzymes of cytochrome CYP3A (erythromycin, oleandomycine; ketoconazole and others antifungal drugs) reduce the metabolic rate toremifene (caution should be exercised while using these drugs with toremifene at the same time). It is impossible to exclude the additive effect on the prolongation of the QT interval between intertormifen and the following preparations,which can lead to an increased risk of ventricular arrhythmia, including ventricular arrhythmia such as "pirouette":
    - antiarrhythmic drugs IA class (for example, quinidine, hydroquinidine, disopyramide);
    - antiarrhythmic drugs of III class (for example, amiodarone, sotalol, dofetilide, ibutilide);
    neuroleptics (for example, phenothiazine, pimozide, sertindole, haloperidol, sultopride);
    - certain antimicrobial agents (moxifloxacin, erythromycin, pentamidine, antimalarials, in particular halofantrine);
    - certain antihistamines (terfenadine, astemizole, misolastine);
    - other (cisapride, wincamine intravenously, bepridil, difemanyl).
    Simultaneous reception of toremifene with data drugs is contraindicated.

    Special instructions:
    Before starting treatment, the patient must undergo a checkup with a gynecologist. Particular attention should be paid to the condition of the endometrium. Then gynecological examinations should be repeated at least once a year. Patients with diseases such as hypertension, diabetes mellitus having a high level of body mass index (> 30) or receiving long-term hormone replacement therapy,are at risk for endometrial cancer, and therefore need careful monitoring.
    Toremifene is not recommended for patients who have a history of severe thromboembolic complications.
    Patients with decompensated heart failure or severe angina pendant need careful monitoring.
    Since in patients with metastases in the treatment of drugs can develop hypercalcemia, these patients need careful monitoring. On electrocardiograms of some patients, when taking toremifene, a dose-dependent prolongation of the QT interval was observed.
    Toremifene should be used with caution in patients with proarrhythmogenic conditions (especially in elderly patients) such as acute myocardial ischemia or prolonged QT interval, as this may lead to an increased risk of ventricular arrhythmia (including ventricular arrhythmia of the pirouette type) and cardiac arrest .
    If, during treatment with toremifene, symptoms or signs that may indicate arrhythmias occur, therapy should be withdrawn and an ECG done. If the interval QT> 500 msec, do not take toremifene.
    Tablets of Fareston contain lactose.
    Anemia, leukopenia and thrombocytopenia were noted. When taking toremifene, the number of erythrocytes, leukocytes or platelets should be monitored.
    Effect on the ability to drive transp. cf. and fur:Toremifene does not affect the ability to drive and other machinery.
    Form release / dosage:
    Tablets of 20 mg or 60 mg.
    Packaging:
    Tablets of 20 mg or 60 mg:
    - 10 tablets in a contour pack of PVC film and aluminum foil (3 or 10 packs per carton pack with instructions for use).
    - for 30, 60 or 100 tablets in a vial of HDPE with a polypropylene lid (1 bottle per carton with instructions for use).

    Storage conditions:List B. In a dry place, at a temperature of 15 - 25 ° C, out of reach of children.
    Shelf life:Do not use after the expiration date printed on the package!
    Terms of leave from pharmacies:On prescription
    Registration number:П N014925 / 01-2003
    Date of registration:18.07.2008
    The owner of the registration certificate:Orion CorporationOrion Corporation Finland
    Manufacturer: & nbsp
    Representation: & nbspORION CORPORATION ORION PHARMA ORION CORPORATION ORION PHARMA Finland
    Information update date: & nbsp12.09.2015
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