Active substanceTamoxifenTamoxifen
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  • Dosage form: & nbsppills
    Composition:

    for 1 tablet

    active substance: tamoxifen citrate equivalent to 0.01 g (10 mg) or 0.02 g (20 mg) tamoxifen 0.0152 g (15.2 mg) or 0.0304 g (30.4 mg)

    Excipients: potato starch, lactose, microcrystalline cellulose, povidone low molecular weight, magnesium stearate.

    Description:Tablets from white to white with a greyish-creamy hue of color, round, flat-cylindrical shape with a bevel (for a dosage of 10 mg), with a facet and a risk on one side of the tablet (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 metabolitesyou compete with estradiolaboutm for binding sites with cytoplasmIchetheestrogen receptors in the tissues of the mammary gland, uterus, vagina, anterior 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:

    Ingestion tamoxifen well absorbed. The maximum concentrationSerum 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 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-desmethyltamoxifen, which, in turn, N- demethylation is transformed into N-decimethyl metabolite. The excretion of tamoxifen from the body has a two-phase character with an initiala half-life of 7 to 14 hours and a subsequent slow terminal half-life for 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, resistant to standard methods of treatment, in the presence of 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, oncerum or morning and evening (with a two-time reception).

    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 are 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: lagtand, schyrexia, nausea, vomitingbut, constipation, upetiredebridge, deetcessia, 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 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 "hepatic" enzymes, 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.

    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 bloody discharge from the vagina or vaginal bleeding occurs, the drug should be discontinued. Tamoxifen can cause ovulation, which increases the risk of pregnancy, so that 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 the case of severe disorders (hypercalcemia), tamoxifen should be administered temporarilyto steal.

    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 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 during treatment, 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 10 mg and 20 mg.

    For 10 tablets in a contour mesh package made of a polyvinyl chloride film and foil of aluminum printed lacquered.

    By 3, 5, 6 or 10 contour mesh packages together with instructions for usein a pack of cardboard.

    Packaging:
    Storage conditions:

    In dry, dark 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:LSR-008845/10
    Date of registration:30.08.2010
    The owner of the registration certificate:OBOLENSKOE PHARMACEUTICAL ENTERPRISE, CJSC OBOLENSKOE PHARMACEUTICAL ENTERPRISE, CJSC Russia
    Manufacturer: & nbsp
    Information update date: & nbsp02.08.2015
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