Active substanceTamoxifenTamoxifen
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  • Dosage form: & nbsppills
    Composition:

    1 tablet contains

    Active substance: tamoxifen citrate 15.2 mg, 30.4 mg, 45.6 mg or 60.8 mg, which is equivalent to 10 mg, 20 mg, 30 mg or 40 mg tamoxifen, respectively. Excipients: lactose, cellulose, starch, silicon dioxide colloid, magnesium stearate.

    Description:

    Tablets of 10 mg

    Round tablets are almost white, with a cross-shaped dividing groove on one side Tablets of 20 mg and 30 mg

    Round tablets of almost white color, with a separating groove on one side Tablets of 40 mg

    Tablets of oblong form, almost white, with a dividing groove on both sides.

    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 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 week admission.

    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 mammary 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.
    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 there are signs of 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, dividing the necessary dose into two doses, in the morning and in the evening.

    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 (tides), 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, 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 a pronounced erythema of the 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 impairment of liver function, such as fatty liver, cholestasis, and hepapp.

    In some patients with metastases at bones at the beginning of the treatment there was hypercalcemia.

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

    With long-term treatment with tamoxifen, changes in the 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 an increase in the above-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.

    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.

    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 indicators, 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 dangerous activities that require a high concentration of attention and speed of psychomotor reactions.
    Form release / dosage:

    Tablets of 10 mg, 20 mg, 30 mg and 40 mg mg.

    Packaging:For 10 tablets in a planar cell pack of aluminum foil; 3 packs in a cardboard box with the attached instruction for use.
    Storage conditions:

    List B. In dry the dark place at a temperature of no higher than 25 ° C

    Shelf life:3 years
    Terms of leave from pharmacies:On prescription
    Registration number:P N015178 / 01-2003
    Date of registration:16.06.2008
    Date of cancellation:2016-11-17
    The owner of the registration certificate:Ebewe Pharma Gesmb.b. Nfg. KGEbewe Pharma Gesmb.b. Nfg. KG Austria
    Manufacturer: & nbsp
    Representation: & nbspSANDOZ SANDOZ Switzerland
    Information update date: & nbsp17.11.2016
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