Active substanceTamoxifenTamoxifen
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  • Dosage form: & nbsppills
    Composition:

    1 tablet of 10 mg contains:

    active substance: tamoxifen citrate - 15.2 mg in terms of tamoxifen - 10 mg.

    Excipients: lactose monohydrate (sugar milk) - 62,, 0 mg, microcrystalline cellulose - 10.0 mg, corn starch - 7.3 mg, sodium carboxymethyl starch 1.0 mg, Povidone (polyvinylpyrrolidone) - 3.5 mg, magnesium stearate 1.0 mg.

    1 tablet of 20 mg of co-content: active substance: tamoxifen citrate - 30.4 mg in terms of tamoxifen - 20 mg.

    Excipients: lactose monohydrate (milk sugar) - 124.0 mg, microcrystalline cellulose - 20.0 mg, corn starch - 14.6 mg, sodium carboxymethyl starch - 2.0 mg, povidone (polyvinylpyrrolidone) - 7.0 mg, magnesium stearate 2.0 mg.

    Description:

    Tablets from white to white with a greyish-creamy hue of color, flat-cylindrical shape, with a facet on both sides and risk from one side.

    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 the receptor complex of estrogen, the receptor complex of tamoxifen does not stimulate 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:

    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 3-4 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. 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; pregnancy and lactation.Child age (data on effectiveness and safety in children are absent).

    Carefully:eye diseases (including cataracts), expressed thrombophlebitis, thromboembolic disease (including history), hyperlipidemia, leukopenia, thrombocytopenia, hypercalcemia; hereditary lactose intolerance, insufficiency of lactase or impaired absorption of glucose and galactose (the preparation contains lactose).
    Pregnancy and lactation:contraindicated
    Dosing and Administration:

    Inside, not liquid, squeezed a small amount of liquid, in one session in the morning, or, dividing the necessary dose into two doses (morning and evening).

    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, syndrome Stevens-Johnson and bullous pemphigoid), visual impairment, including corneal changes, cataracts and retinopathy, retrobulbar neuritis. 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.

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

    Rarely there was an increase in the level of serum triglycerides in some cases combined with pancreatitis.

    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 be observed.

    Overdose:

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

    Interaction:

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

    There have been reports of tamoxifen potentiating the anticoagulant effect of coumarin preparations (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-desmeth tamoxifen in blood plasma. Tamoxifen should not be used concomitantly with aromatase inhibitors (arimidex, letrozole).

    Special instructions:

    Women receiving tamoxifen, should undergo a regular gynecological examination. 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 methods of contraception (non-hormonal) during 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 extremities (pain in the legs or their swelling), embolism of the pulmonary artery (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), liver function indices, blood pressure, and check with the oculist.

    In patients with hyperlipidemia, the concentration of cholesterol and triglycerides (TG) 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 hazardous activities requiring increased concentration of attention and speed of psychomotor reactions.
    Form release / dosage:

    Tablets 10 mg and 20 mg.

    For 10, 30 tablets in a contour cell packaging from

    films polyvinyl chloride and foil aluminum printed varnished.

    By 10, 20, 30, 40, 50 or 100 tablets in polymer cans

    for medicines.

    One bank or 1, 2, 3, 4, 5 or 10 contour cell packings

    together with instructions for use placed in a cardboard box (pack).

    Storage conditions:In a dry place protected from light at a temperature of no higher than 25 ° C.

    Keep out of the reach of children place.

    Shelf life:

    3 years.

    Do not use after the expiration date.

    Terms of leave from pharmacies:On prescription
    Registration number:LSR-010503/09
    Date of registration:23.12.2009
    The owner of the registration certificate:OZONE, LLC OZONE, LLC Russia
    Manufacturer: & nbsp
    Information update date: & nbsp02.09.2015
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