Active substanceTamoxifenTamoxifen
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  • Dosage form: & nbsppills
    Composition:

    1 tablet contains:

    Active substance: tamoxifen citrate 15.2 mg and 30.4 mg, equivalent to 10 mg and 20 mg tamoxifen

    Excipients: corn starch 40.0 mg (100.0 mg), lactose 40.0 mg (103.1 mg), povidone 7.0 mg (14.0 mg), magnesium stearate 1.0 mg (2.5 mg) , sodium starch glycolate 10.0 mg (20.0 mg), purified water (q.s.).

    Description:

    Round, biconvex tablets from white with yellowish to white with a cream-yellowish shade of color.

    On 10 mg tablets on one side - the figure "10"; on 20 mg tablets on one side - the figure "20".

    Pharmacotherapeutic group:antitumor agent - antiestrogen.
    ATX: & nbsp

    L.02.B.A.01   Tamoxifen

    Pharmacodynamics:

    Tamoxifen is a non-steroidal antiestrogenic agent that also has a non-weak estrogenic properties.Its action is based on the ability to block estrogen receptors. Tamoxifen, and also some of its metabolites compete with estradiol for binding sites with cytoplasmic estrogen receptors in the tissues of the breast, uterus, vagina, anterior pituitary gland and tumors with high the content of estrogen receptors. 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 and their death.

    Pharmacokinetics:

    After oral administration 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 administration. Connection with plasma proteins - 99%

    Metabolized in the liver with the formation of several metabolites. 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 allocated mainly in the form of conjugates, mainly with fecal masses and only small amounts are excreted in the urine.

    Indications:

    Estrogen-dependent breast cancer in women (especially menopause) and pectoral glands in men.

    The drug can be used for the treatment of ovarian cancer, endometrial cancer, kidney cancer, melanoma, soft tissue sarcomas in the presence of estrogen receptors in the tumor, as well as for the treatment of prostate cancer in the resistance to other medicines.

    Contraindications:

    - Hypersensitivity to tamoxifen and / or any other ingredient in the drug.

    - Pregnancy and lactation.

    Carefully:renal failure, diabetes, eye diseases (including cataracts), deep vein thrombosis and thromboembolic disease (including history), hyperlipidemia, leukopenia, thrombocytopenia, hypercalcemia, concomitant therapy with indirect anticoagulants.
    Pregnancy and lactation:contraindicated
    Dosing and Administration:

    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. the appearance of signs. progression of the disease taking the drug is canceled.

    Tablets should be taken without chewing, squeezed a small amount of liquid, in one dose in the morning, or, sharing the necessary dose for two meals in the morning and evening.
    Side effects:

    In the treatment with Tamoxifen, the most frequent adverse reactions associated with its anti-estrogenic effect, manifested in the form of paroxysmal sensations of heat (tides), vaginal bleeding or discharge, itching in the genital area, alopecia, pain in the area of ​​the lesion; ossaly, increase in body weight.

    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, visual impairment, including corneal changes, cataracts , retinopathy and, retrobulbar neuritis.

    At the beginning of treatment, local exacerbation of the disease is possible - an increase in the size of soft tissue formations,sometimes accompanied by severe erythema of affected areas and adjacent areas - which usually occurs within 2 weeks.

    The likelihood of thrombophlebitis and thromboembolism may increase.

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

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

    Tamoxifen causes amenorrhea or irregularity of menstrual periods in premenopausal women, as well as reversible development of cystic ovarian tumors.

    With long-term treatment with Tamoxifen, changes, endometrium, including hyperplasia, polyps and in some cases - endometrial cancer, as well as the development of uterine fibroids, can be observed.

    Overdose:An acute overdose of tamoxifen in humans was not observed. It should be expected that an overdose can cause.wof the described adverse reactions. Specific antidotes do not exist, treatment should be symptomatic.
    Interaction:

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

    Antacids, H2 blockers, histamine receptors and other drugs of similar action by increasing the value of pH in the stomach can cause premature dissolution and loss of protective effect of enteric tablets. The interval between taking tamoxifen and these drugs should be 1-2 hours.

    There are reports of increased Tamoxifen anticoagulant effect of coumarin drugs (eg warfarin).

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

    The combined use of tamoxifen and tegafur can contribute. the development of active chronic hepatitis and cirrhosis of the liver.

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

    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, 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. Tamoxifen can cause ovulation, which increases the risk of pregnancy, so that women who have an active sex life during (and within about 3 months after) treatment with tamoxifen recommended the use of a mechanical or non-hormonal contraceptive.

    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 TG in serum should be monitored during treatment.

    Effect on the ability to drive transp. cf. and fur:During the treatment period it is necessary to refrain from 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 30 or 100 tablets in polymer bottles with the control of the first opening. 1 bottle with instructions for use in cardboard pack
    Packaging:(100) - vial (1) - Cardboard tutu
    (10000) - container (1)
    (30) - vial (1) - Cardboard tutu
    (5000) - container (1)
    Storage conditions:

    At a temperature of 15 to 25 ° C.

    Keep out of the reach of children!

    Shelf life:

    5 years.

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

    Terms of leave from pharmacies:On prescription
    Registration number:P N008975
    Date of registration:28.09.2011
    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: & nbsp02.09.2015
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