Tamoxifenum Geksal

General characteristics. Structure:

Active agent: Tamoxifenum citrate of 15,2 mg, either 30,4 mg, or 45,6 mg, or 60,8 mg that 10 mg, 20 mg, 30 mg and 40 mg of Tamoxifenum respectively are equivalent.

Excipients: lactose 1H2O, sodium starch glycollate, povidone, cellulose microcrystallic, magnesium stearate.
Structure of a cover: lactose, titanium dioxide, gipromelloz, polyethyleneglycol 4000.

Pharmacological properties:

Pharmacodynamics. Tamoxifenum is the nonsteroid anti-oestrogenic means having also weak oestrogenic properties. Its action is based on ability to block receptors of estrogen. Tamoxifenum, and also some of its metabolites compete with oestradiol for places of linkng with cytoplasmatic receptors of estrogen in tissues of a mammary gland, uterus, vagina, a front share of a hypophysis and tumors with the high content of receptors of estrogen. Contrary to a receptor complex of estrogen the receptor complex of Tamoxifenum does not stimulate synthesis of DNA in a kernel, and cell division oppresses that leads to regression of tumor cells and their death.

Pharmacokinetics. After intake Tamoxifenum is well soaked up. The maximum concentration in serum is reached ranging from 4 till 7 o'clock after reception of a single dose. Equilibrium concentration of Tamoxifenum in blood serum is usually reached after 3-4 week receptions. Communication with proteins of plasma - 99%
It is metabolized in a liver with formation of several metabolites. Removal of Tamoxifenum from an organism has two-phase character with an initial stage of semi-removal from 7 to 14 hours and with the subsequent slow terminal elimination half-life within 7 days. It is allocated mainly in the form of conjugates, generally with a fecal masses and only its small amounts are distinguished with urine.

Indications to use:

Estrogenozavisimy cancer of mammary glands at women (especially in a menopause) and chest glands at men.
Drug can be used for cancer therapy of ovaries, endometrial cancer, cancer of a kidney, a melanoma, sarcomas of soft tissues in the presence in a tumor of oestrogenic receptors, and also for cancer therapy of a prostate at resistance to other medicines.

Route of administration and doses:

The mode of dosing is usually set individually depending on indications. The daily dose makes 20-40 mg. As a standard dose reception of 20 mg of Tamoxifenum inside is recommended it is daily long. At emergence of signs of progressing of a disease administration of drug is cancelled.
Pill should be taken without chewing, washing down with a small amount of liquid, in one step in the morning, or, dividing a necessary dose into two receptions in the morning and in the evening.

Features of use:

The women receiving Tamoxifenum have to be exposed to regular gynecologic inspection. At emergence of bloody allocations from a vagina or vulval bleedings administration of drug should be stopped.
At patients with metastasises in a bone periodically during an initial stage of treatment it is necessary to define concentration of calcium in blood serum. In case of the expressed disturbances reception of Tamoxifenum should be stopped temporarily.
At emergence of symptoms of a vein thrombosis of the lower extremities (an onychalgia or their puffiness), embolisms of a pulmonary artery (asthma) administration of drug should be stopped.
Tamoxifenum can cause an ovulation that increases risk of pregnancy in this connection to women who are sexually active, in time (and within about 3 months after) treatments Tamoxifenum recommends use of mechanical or non-hormonal contraceptive.
During therapy it is necessary to control periodically blood coagulation indicators, content of calcium in blood, a blood picture (leukocytes, thrombocytes), indicators of function of a liver, arterial pressure, to perform inspection at the oculist.
At patients with a lipidemia in the course of treatment it is necessary to control concentration of cholesterol and TG in blood serum.
During treatment it is necessary to abstain from occupations potentially dangerous types of activity demanding the increased concentration of attention and speed of psychomotor reactions.

Side effects:

At treatment by Tamoxifenum the side reactions connected with its anti-oestrogenic action, which are shown in the form of pristupoobrazny feelings of heat (inflows), vulval bleedings or allocations, an itch in genitals, an alopecia, pains in the field of the center of defeat, an ossalgiya, increase in body weight most often meet.
The following side reactions were less often or seldom observed: a liquid delay, anorexia, nausea, vomiting, a lock, increased fatigue, a depression, confusion of consciousness, a headache, dizziness, drowsiness, fervescence, skin rash, a vision disorder, including changes of a cornea, a cataract, a retinopathy and retrobulbar neuritis.
In an initiation of treatment perhaps local exacerbation of a disease – the increase in the amount of myagkotkanny educations which sometimes is followed by the expressed erythema of affected areas and adjacent areas – which usually passes within 2 weeks.
The probability of developing of thrombophlebitises and thromboembolisms can increase.
The tranzitorny leukopenia and thrombocytopenia, and also the increase in level of liver enzymes which is very seldom followed by more heavy abnormal liver functions, such as fatty infiltration of a liver, cholestasia and hepatitis can sometimes be observed.
At some patients with metastasises in a bone in an initiation of treatment the hypercalcemia was observed.
Tamoxifenum causes an amenorrhea or an irregularity of approach of periods in women in the premenopausal period, and also reversible development of cystous tumors of ovaries.
At prolonged treatment by Tamoxifenum changes of an endometria, including a hyperplasia, polyps and in isolated cases – endometrial cancer, and also development of fibroma of a uterus can be observed.

Interaction with other medicines:

At co-administration of Tamoxifenum and tsitostatik the risk of a thrombogenesis increases.
Antacids, H2 blockers - histamine receptors and other drugs of similar action, increasing PH value in a stomach, can cause premature dissolution and loss of a protective effect of a kishechnorastvorimy tablet. The interval between reception of Tamoxifenum and these drugs has to make 1-2 hours.
There are messages on strengthening by Tamoxifenum of anti-coagulative effect of drugs of a coumarinic row (for example warfarin).
The drugs reducing calcium removal (for example, diuretics of a tiazidovy row), can increase risk of development of a hypercalcemia.
Combined use of Tamoxifenum and Tegafurum can promote development of active chronic hepatitis and cirrhosis.
Simultaneous use of Tamoxifenum with other hormonal drugs (especially, estrogensoderzhashchy contraceptives) leads to weakening of specific effect of both drugs.

Contraindications:

- Hypersensitivity to Tamoxifenum and/or any other ingredient of drug.
- Pregnancy and feeding by a breast.

With care: a renal failure, a diabetes mellitus, diseases of eyes (including a cataract), a deep vein thrombosis and a clotting disease (including in the anamnesis), a lipidemia, a leukopenia, thrombocytopenia, a hypercalcemia, the accompanying therapy by indirect anticoagulants.

Overdose:

The acute overdose by Tamoxifenum at the person was not observed. It is necessary to expect that the overdose can cause strengthening of the above described side reactions. Specific antidotes do not exist, treatment has to be symptomatic.

Storage conditions:

List B. At a temperature not above 25 °C in the place, unavailable to children.

Issue conditions:

According to the recipe

Packaging:

Tablets on 10 mg, 20 mg, 30 mg and 40 mg. On 10 tablets in a blister strip packaging from PVC/PVDH / aluminum foil. On 3 or 10 blister strip packagings together with the application instruction in a cardboard pack.