Active substanceTamoxifenTamoxifen
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  • Dosage form: & nbsppills
    Composition:

    of the active substance: tamoxifen citrate in terms of tamoxifen - 10 mg;

    Excipients: cellulose microcrystalline - 8,4 mg, lactose monohydrate (sugar milk) - 113.4 mg, potato starch - 41.0 mg, povidone (polyvinylpyrrolidone low molecular weight) - 5.4 mg, magnesium stearate - 1.8 mg.

    Description:Tablets from white to white with grayish kremovatym .ototkom colors, round, flat-cylindrical with a bevel.
    Pharmacotherapeutic group:antitumor agent-antiestrogen.
    ATX: & nbsp

    L.02.B.A.01   Tamoxifen

    Pharmacodynamics:

    Tamoxifen is a non-steroidal antiestrogenic agent, possessing also 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 inhibits cell division, which leads to regression of tumor cells as a result of their death.

    Pharmacokinetics:

    When ingestion - tamoxifen well absorbed. The maximum serum concentration is achieved within 4 to 7 hours after taking a single dose. The equilibrium concentration of tamoxifen in the blood serum is usually achieved after 3 to 4 weeks of admission. The connection with plasma proteins is 99%. Metabolized in the liver with the formation of several metabolites, the metabolism involved isoenzyme CYP2C9. By demethylating tamoxifen metabolized in N-desmethyl- tamoxifen, 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 for early breast cancer with estrogen-positive receptors.

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

    - Breast cancer (including in 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; children's age (data on efficacy and safety in children are absent).

    Carefully:

    eye diseases (including cataracts), expressed thrombophlebitis, thromboembolic disease (including 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:

    Contraindicated for use during pregnancy and during breastfeeding.

    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 antiestrogenic 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 center, 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 individual reports of erythema multiforme, 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 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 "hepatic" enzymes, which are very rarely accompanied by more severe impairment of liver function, can rarely be observed; such as fatty liver infiltration, cholestasis and hepatitis.

    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 long-term treatment with tamoxifen, there may be changes in the endometrium, including hyperplasia, polyps, development of uterine fibroids and in single cases - endometrial cancer, uterine sarcoma.

    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 (for example,. 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.Simultaneous use of tamoxifen with other hormones (especially estrogen-containing contraceptives) leads to a weakening of the specific action of both drugs.

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

    Tamoxifen should not be used concurrently with aromatase inhibitors (anastrozole, letrozole).
    Special instructions:

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

    Tamoxifen can cause ovulation, which increases the risk of pregnancy, and therefore, women of childbearing age should use reliable methods of contraception (non-hormonal) during treatment and for 3 months after 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.When . expressed violations (hypercalcemia), tamoxifen should be temporarily discontinued.

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

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

    In patients with hyperlipidemia, it is necessary to control the concentration of cholesterol and triglycerides in the blood serum.
    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 of 10 mg.

    10 tablets in a planar cell package.

    For 30 or 100 tablets in a can of light-protective glass or a can of polymer, or a polymer bottle.

    Each jar or bottle, or 3, or 5 contour squares with instructions for use in a pack of cardboard.

    Packaging:(10) - packings, cellular, outline (3) - packs, cardboard
    (10) - packings, cellular planimetric (5) - packs cardboard
    (100) - polymer cans (1) - packs of cardboard
    (100) - cans of dark glass (1) - packs cardboard
    (100) - polymer bottles (1) - packs of cardboard
    (30) - polymer cans (1) - packs of cardboard
    (30) - cans of dark glass (1) - packs of cardboard
    (30) - polymer bottles (1) - packs cardboard
    Storage conditions:

    In a dry, protected from light place 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 expiration date printed on the package.

    Terms of leave from pharmacies:On prescription
    Registration number:P N003720 / 01
    Date of registration:14.08.2009
    The owner of the registration certificate:NORTH STAR, CJSC NORTH STAR, CJSC Russia
    Manufacturer: & nbsp
    Information update date: & nbsp02.09.2015
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