Tamoksimed

General characteristics. Structure:

Active ingredient: 10 mg or 20 mg of Tamoxifenum in the form of citrate Tamoxifenum.

Excipients: magnesium stearate, лудипрессо (lactose, povidone, кросповидон).

Pharmacological properties:

Pharmacodynamics. Tamoxifenum is an antimetabolite (anti-estrogen) competitively contacting receptors of estrogen in cytoplasm of estrogenozavisimy tumor cells. Together with them gets into a kernel where blocks interaction of estrogen with the receptors.

Pharmacokinetics. After oral administration drug is quickly absorbed and the maximum concentration in serum are reached within 4-7 hours.

Steady concentration (about 300 ng/ml) are reached after four-week treatment with a daily dose of reception of 40 mg. Tamoxifenum well contacts a seralbumin (> 99%).

As a result of metabolism, in the course of a hydroxylation, demethylation and conjugation, there is a formation of a number of the metabolites having indicators of a pharmacological profile, similar to initial chemical compound that, thus, promotes achievement of therapeutic effect. The elimination half-life makes 7 days. Allocation happens mainly through fecal masses.

Indications to use:

Metastatic breast cancer, especially at the patients who are in a menopause, endometrial cancer, kidneys, sarcoma of soft tissues, anovulatory infertility, a puerperal agalaxia, an oligospermatism, hypophysis tumors. It is noticed that preventive introduction of Tamoxifenum to women with risk of a breast cancer reduces their incidence by 45% in comparison with women of the same risk, but not accepting drug.

Route of administration and doses:

At a breast cancer, an endometria or kidneys on 10-20 mg 2-3 times a day. The course dose makes 2,4-9,6 g; treatment continues before regression of process and within the next 1-2 months.

At anovulatory infertility on 10 mg 2 times a day for 4 days, since 2nd day of periods, then on 20 mg 2 times a day, and if necessary on 40 mg 2 times a day.

At a puerperal agalaxia on 10 mg 4 times a day for 5 days.

At an oligospermatism on 10 mg 2 times a day.

Features of use:

In the course of treatment control of number of leukocytes, thrombocytes, level of calcium, indicators of coagulant system of blood is necessary.

It is a little effective in treatment of patients with metastasises (especially in a liver).

At a number of the women accepting Tamoxifenum for cancer therapy of a mammary gland in the premenopausal period lack of periods is observed.

it is recommended to exercise careful control of patients at simultaneous use of anticoagulants of coumarinic type.

Lactation: Data on allocation of Tamoxifenum in breast milk at women are absent therefore its use during a lactation is not recommended.

Side effects:

Lack of appetite, nausea, vomiting. Feeling of fatigue, drowsiness, dizziness, erythema, hypercalcemia, moderate metrorrhagias. Pulmonary embolisms, fibrinferments. A hyperplasia of an endometria, polyposes or an endometrial carcinoma, uterus fibroma, cystous swelling of ovaries at women, a retinopathy, opacification of a cornea, heat attacks, a weight increase, an itch of generative organs, changes of a menstrual cycle. Headaches. Seldom fever, a leukopenia, sometimes with anemia and/or thrombocytopenia, a nytropeniya. Change of levels of enzymes of a liver, and in rare instances, with more serious violations, including fatty infiltration of a liver, a cholestasia and hepatitis.

Interaction with other medicines:

Antacids and sekretolitik should not be appointed along with Tamoxifenum, and with an interval at 2 o'clock.

Estrogen weakens effect of Tamoxifenum, and progestogens strengthen.

Cytostatics increase risk of thromboses.

Use of drug in a combination with anticoagulants of coumarinic type can cause considerable strengthening of anti-coagulating action.

Contraindications:

Absolute – pregnancy, thrombophlebitis, hypersensitivity to Tamoxifenum.

Relative – a leukopenia, thrombocytopenia, a lipidemia, a hypercalcemia, a cataract.

Overdose:

Strengthening of anti-oestrogenic by-effects. The specific antidote is not available, and treatment has to be symptomatic.

Storage conditions:

To store at a temperature of 15-25 °C, in dry, protected from light and the place, unavailable to children. Period of validity 2 years. Not to use after the expiry date specified on packaging.

Issue conditions:

According to the recipe

Packaging:

Tablets of 10 mg and 20 mg. On 10 or 20 tablets in a blister strip packaging. On 5, 15, 25, 50, 100, 500 tablets in packages. On 5, 15, 25, 50, 100 tablets in bottles.