Active substanceTamoxifenTamoxifen
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  • Dosage form: & nbsppills
    Composition:

    1 tablet contains:

    active substance: tamoxifen citrate, equivisovalent 10 mg or 20 mg of tamoxifen - 15.2 mg or 30.4 mg

    Excipients: lactose monohydrate - 117.2 mg or 234.4 mg, starch cartoffee - 39.7 mg or 79.4 mg, povidone - 6.1 mg or 12.2 mg, magnesium stearate - 1.8 mg or 3.6 mg.

    Description:

    Tablets from white to white with a grayish or creamy hue of a flat-cylindrical shape with a bevel for a dosage of 10 mg, with a facet and a risk for a dosage of 20 mg.

    Pharmacotherapeutic group:antitumor agent-antiestrogen
    ATX: & nbsp

    L.02.B.A.01   Tamoxifen

    Pharmacodynamics:Tamoxifen is a non-steroidal antiestrogenic agent that also has weak estrogenic properties. Its action is based on the ability to block estrogen receptors. Tamoxifen, as well as some of its metabolites, compete with estradiol for binding sites with cytoplasmic estrogen receptors in the tissues of the mammary gland, uterus, vagina, anterior lobe of the pituitary gland, and tumors with a high estrogen receptor content. In contrast to estrogen tamoxifen, binding to estrogen receptors, does not affect the synthesis of DNA in the nucleus, but depresses the division of the cell, which leads to regression of tumor cells as a result of their death.
    Pharmacokinetics:

    Ingestion tamoxifen well absorbed. The maximum concentration in the serum is reached within 4 to 7 hours after taking a single dose. The equilibrium concentration of tamoxifen in the blood serum is usually achieved after 3-4 weeks of administration. Connection with plasma proteins - 99 %. Metabolized in the liver with the formation of several metabolites, the metabolism involved isoenzyme CYP2C9. By demethylating tamoxifen metabolized in N-desmethyltamoxifen, which, in turn, N-detylation is transformed into N-decimethyl metabolite. Excretion of tamoxifen from the body has a two-phase character with an initial half-life of 7 to 14 hours and with a subsequent slow terminal elimination half-life within 7 days.It is excreted primarily through the intestine, mainly in the form of metabolites; a small amount - by the kidneys.

    Indications:

    -Adjuvant therapy early cancer mammary gland with estrogen-

    positive receptors.

    Treatment of locally advanced or metastatic cancer dairy glands with estrogen-positive receptors.

    Breast cancer (including men after castration).

    Tamoxifen can also be used in other solid tumors that are resistant to standard treatments, with overexpression of estrogen receptors.

    Contraindications:

    Hypersensitivity to tamoxifen and / or any other component of the drug; pregnancy and the period of breastfeeding; children's age (data on efficacy and safety in children are absent).

    Carefully:

    eye diseases (including cataracts), expressed thrombophlebitis,

    thromboembolic disease (including in the anamnesis), hyperlipidemia, leukopenia, thrombocytopenia, hypercalcemia, liver disease; hereditary lactose intolerance, insufficiency of lactase or impaired absorption of glucose and galactose (the preparation contains lactose).

    Pregnancy and lactation:Is a contraindication for the use of the drug.
    Dosing and Administration:

    Inside, not liquid, squeezed a small amount of liquid, once in the morning or in the morning and in the evening (with a two-time intake).

    The dosage regimen is usually set individually, depending on the indications. The daily dose is 20-40 mg. As a standard dose, taking 20 mg of tamoxifen inside daily for a long time is recommended. When there are signs of progression of the disease, taking the drug is canceled.

    Side effects:

    In the treatment of tamoxifen, the most frequent adverse reactions associated with its anti-estrogenic effect, manifested in the form of paroxysmal sensations of heat ("hot flashes"), vaginal bleeding or discharge, itching in the genital area, alopecia, pain in the area of ​​the lesion, ossalgia, weight gain .

    Less frequently or rarely, the following adverse reactions were observed: fluid retention, anorexia, nausea, vomiting, constipation, fatigue, depression, confusion, headache, dizziness, drowsiness, fever, skin rash (including occasional reports of multiform erythema,Stevens-Johnson syndrome and bullous pemphigoid), visual impairment, including corneal changes, cataract and retinopathy, retrobulbar neuritis, allergic reactions, including angioedema; decreased libido in men, impotence. Interstitial pneumonitis was rarely observed. At the beginning of treatment, local exacerbation of the disease is possible - an increase in the size of soft tissue formations, sometimes accompanied by a pronounced erythema of the affected areas and adjacent areas, which usually occurs within 2 weeks.

    The likelihood of thrombophlebitis and thromboembolism may increase.

    Often leg cramps are noted.

    Transient leukopenia and thrombocytopenia, as well as an increase in the activity of "liver" enzymes, very rarely accompanied by more severe impairments of liver function, such as fatty liver infiltration, cholestasis and hepatitis, can rarely occur.

    An increase in serum triglyceride concentrations in some cases combined with pancreatitis was rarely observed.

    In some patients with bone metastases, hypercalcaemia was observed at the beginning of treatment.

    Tamoxifen causes amenorrhea or irregularity of menstrual periods in premenopausal women, as well as the reversible occurrence of cystic ovarian tumors. With prolonged treatment with tamoxifen, changes in the endometrium, including hyperplasia, polyps, development of uterine fibroids and in isolated cases - endometrial cancer, uterine sarcoma, can occur.

    Overdose:

    An acute overdose of tamoxifen in humans was not observed. In case of an overdose it is possible to develop neurotoxicity (tremor, hyperreflexia, unsteadiness of gait, dizziness). The specific antidote is not known. Treatment is symptomatic.

    Interaction:

    With the simultaneous use of tamoxifen and cytostatics, the risk of thrombosis increases.

    There have been reports of an increase in tamoxifen anticoagulant effect of indirect anticoagulants - coumarin derivatives (eg, warfarin).

    Drugs that reduce the excretion of calcium (eg, thiazide diuretics) may increase the risk of hypercalcemia.

    Joint use of tamoxifen and tegafur can promote the development of active chronic hepatitis and cirrhosis of the liver.

    The simultaneous use of tamoxifen with other hormonal drugs (especially estrogen-containing contraceptives) leads to a weakening of the specific effects of both drugs.

    With the simultaneous use of tamoxifen and bromocriptine, tamoxifen concentrations increase and N-desmethyltamoxifen in blood plasma.

    Special instructions:

    Women receiving tamoxifen, it is necessary to conduct regular gynecological examinations (1 time in 3 months). When bloody discharge from the vagina or vaginal bleeding occurs, the drug should be discontinued.

    Tamoxifen can cause ovulation, which increases the risk of pregnancy, therefore, women of reproductive age need to use reliable contraceptive methods (non-hormonal) during the treatment and within 3 months after the end of treatment.

    In patients with metastases in the bone, periodically during the initial period of treatment should determine the concentration of calcium in the blood serum. In case of severe disorders (hypercalcemia), tamoxifen should be temporarily discontinued. .

    When signs of thrombosis of the veins of the lower limbs (pain in the legs or their swelling), pulmonary embolism (dyspnea), the drug should be stopped.

    During the period of therapy, it is necessary to periodically monitor the blood clotting parameters, the calcium content in the blood, the blood picture (leukocytes, platelets), the liver function indices, blood pressure, and every 3 months for an ophthalmologist.

    In patients with hyperlipidemia, the concentration of cholesterol and triglycerides in serum should be monitored during treatment.

    Effect on the ability to drive transp. cf. and fur:During the treatment period, care must be taken when driving vehicles and engaging in potentially dangerous activities that require a high concentration of attention and speed of psychomotor reactions.
    Form release / dosage:

    Tablets 10 mg and 20 mg.

    For 10 tablets in a planar cell packaging made of polyvinylchloride film and aluminum foil printed lacquered.

    For 100 tablets with a dosage of 10 mg in polymer cans complete with lids.

    Each jar, 3 contiguous cell packs with tablets of 20 mg or.. 10 contour cell packs with 10 mg tablets together with instructions for use in a pack of cardboard.

    Packaging:(10) - packings cellular planimetric (10) - packs cardboard
    (100) - polymer cans (1) - packs of cardboard
    Storage conditions:

    In the dark place at a pacenot higher than 25 ° С.

    Keep out of the reach of children.

    Shelf life:

    2 years.

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

    Terms of leave from pharmacies:On prescription
    Registration number:P N002325 / 01
    Date of registration:04.04.2008
    The owner of the registration certificate:VALENTA PHARM, PAO VALENTA PHARM, PAO Russia
    Manufacturer: & nbsp
    Information update date: & nbsp03.09.2015
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