Tamoxifen GEKSAL

Active material: Tamoxifen
When ATH: L02BA01
CCF: Anti-estrogen drug with antitumor activity
When CSF: 15.13.01
Manufacturer: Hexal AG (Germany)

Pharmaceutical form, composition and packaging

Pills, coated white or slightly yellowish, round, lenticular, with a uniform smooth surface.

Excipients: lactose monohydrate, sodium starch glycolate, povidone, microcrystalline cellulose, magnesium stearate.

The composition of the shell: lactose, Titanium dioxide, gipromelloza, polyethylene glycol 4000.

10 PC. – packings Valium planimetric (3) – packs cardboard.
10 PC. – packings Valium planimetric (10) – packs cardboard.

Pills, coated white or slightly yellowish, round, lenticular, with a uniform smooth surface and a notch on one side.

Excipients: lactose monohydrate, sodium starch glycolate, povidone, microcrystalline cellulose, magnesium stearate.

The composition of the shell: lactose, Titanium dioxide, gipromelloza, polyethylene glycol 4000.

10 PC. – contour cell package (3) – packs cardboard.
10 PC. – contour cell package (10) – packs cardboard.

Pills, coated white or slightly yellowish, round, lenticular, with a uniform smooth surface.

Excipients: lactose monohydrate, sodium starch glycolate, povidone, microcrystalline cellulose, magnesium stearate.

The composition of the shell: lactose, Titanium dioxide, gipromelloza, polyethylene glycol 4000.

10 PC. – packings Valium planimetric (3) – packs cardboard.
10 PC. – packings Valium planimetric (10) – packs cardboard.

Pills, coated white or slightly yellowish, round, lenticular, with a uniform smooth surface and a notch on one side.

Excipients: lactose, sodium starch glycolate, povidone, microcrystalline cellulose, magnesium stearate.

The composition of the shell: lactose, Titanium dioxide, gipromelloza, polyethylene glycol 4000.

10 PC. – packings Valium planimetric (3) – packs cardboard.
10 PC. – packings Valium planimetric (10) – packs cardboard.

Pharmacological properties
Farmakodinamika

Tamoxifen is a nonsteroidal anti-estrogen agent, having as weak estrogenic properties. Its action is based on the ability to block estrogen receptors. Tamoxifen, as well as some of its metabolites, estradiol compete for binding sites with cytoplasmic estrogen receptors in breast tissue, uterus, vagina, anterior pituitary tumors and high estrogen receptors. In contrast, receptor complex tamoxifen estrogen receptor complex does not stimulate DNA synthesis in the nucleus, and inhibits cell division, which leads to the regression of tumor cells and their death.

Pharmacokinetics

After oral administration, tamoxifen is well absorbed. The maximum serum concentration is achieved in the range of 4 to 7 hours after receiving a single dose of. The equilibrium concentration of tamoxifen in serum is typically achieved after 3-4 week reception. Relationship to plasma proteins – 99%
It is metabolized in the liver with the formation of several metabolites. Withdrawal of tamoxifen from the body is biphasic with an initial half-life of 7 to 14 hours, followed by a slow terminal elimination half-life for 7 days. It provided mainly as conjugates, primarily, with feces and only a small amount excreted in urine.

Indications

Estrogen-dependent breast cancer in women (especially in menopause) and male breasts.
The preparation may be used for the treatment of ovarian cancer, endometrial cancer, Kidney Cancer, Melanoma, sarcomas of soft tissues in the presence of estrogen receptor in the tumor, and for the treatment of prostate cancer with resistance to other drugs.

Contraindications

• Increased sensitivity to tamoxifen and / or any other ingredients of the formulation.
• Pregnancy and breast-feeding.

Carefully: renal failure, diabetes, eye diseases (incl. Cataract), deep vein thrombosis and thromboembolic disease (incl. history), hyperlipidemia, leukopenia, thrombocytopenia, hypercalcemia, soputstvuyushtaya therapy nepryamыmi antikoagulyantami.

Dosing and Administration

The dosage regimen is generally determined individually depending on indications. The daily dose is 20-40 mg. As a standard dose recommended intake 20 mg of tamoxifen daily for a long time inside. If signs of disease progression the drug overturned.
Tablets should be taken with liquid, drinking a small amount of liquid, at one time in the morning, or, separating the required dose into two doses in the morning and evening.

Side effect

When tamoxifen most common adverse reactions, associated with its anti-estrogenic action, manifested in the form of hot flashes (tides), vaginal bleeding or discharge, pruritus genitals, Alopecia, pain in lesion area, ossalgia, weight gain.
Less common or rare side effects observed following: fluid retention, anorexia, nausea, vomiting, constipation, fatigue, depression, confusion, headache, dizziness, drowsiness, fever, skin rash, blurred vision, including changes in the cornea, cataracts, retinopathy and optic neuritis.
At the beginning of the treatment capacity of local exacerbation - Increase the size of the soft tissue structures, sometimes accompanied by severe erythema lesions and surrounding areas - which usually goes away within 2 weeks.
It may increase the risk of thromboembolism and thrombophlebitis.
Sometimes there may be transient leukopenia and thrombocytopenia, and an increase in liver enzymes, very rarely accompanied by a severely impaired liver function, such as fatty liver, cholestasis and hepatitis.
In some patients with bone metastases at the beginning of the treatment of hypercalcemia observed.
Tamoxifen causes amenorrhea or irregular menstruation in women premenopausal, as well as the development of reversible cystic ovarian tumors.
Prolonged treatment with tamoxifen may experience changes in the endometrium, hyperplasia comprising, polyps, and in rare cases - endometrial cancer, and the development of uterine fibroids.

Overdose

Acute overdose of tamoxifen was not observed in humans. It is expected, overdose can cause increased adverse reactions described above. There is no specific antidote, treatment should be symptomatic.

Interaction with other drugs

When concomitant administration of tamoxifen and cytotoxic drugs increase the risk of thrombosis.
Antacids, H2-blockers of histamine receptors and other drugs of similar action, raising pH in the stomach, can cause premature dissolution and loss of the protective effect of Valium tablets. The interval between tamoxifen and these drugs should be 1-2 o'clock.
There are reports on the strengthening effects of the drug tamoxifen anticoagulant coumarin (such as warfarin).
Preparations, reduce the excretion of calcium (eg, thiazide diuretics series), may increase the risk of hypercalcemia.
The combined use of tamoxifen and tegafur can contribute to chronic active hepatitis and cirrhosis.
Concomitant use of tamoxifen with other hormonal drugs (especially, estrogensoderjath contraceptives) It leads to a weakening of the specific actions of both drugs.

Cautions

Women, receiving tamoxifen should undergo regular gynecological examination. When bleeding from the vagina, or vaginal bleeding should stop taking the drug.
In patients with bone metastases periodically during the initial period of treatment should determine the concentration of calcium in blood serum. In cases where violations tamoxifen should be suspended.
If signs of venous thrombosis of lower extremities (leg pain or swelling), pulmonary embolism (breathlessness) the drug should be discontinued.
Tamoxifen can cause ovulation, which increases the risk of pregnancy, in connection with which women, who are sexually active, during (and for about 3 months) tamoxifen is recommended to use mechanical or non-hormonal contraceptive.
During therapy should periodically monitor the performance of blood clotting, blood calcium, blood picture (leukocytes, platelets), liver function tests, blood pressure, be inspected by an ophthalmologist.
Patients with hyperlipidemia in the treatment process to control the concentration of cholesterol and triglycerides in blood serum.
In the period of treatment should refrain from activities potentially hazardous activities, require high concentration and speed of psychomotor reactions.

Product form

The tablets of 10 mg, 20 mg, 30 mg 40 mg. By 10 tablets in blisters made of PVC / PVDC / aluminum foil. By 3 or 10 contour cell package together with instructions for use in carton pack.

Storage conditions

List B. The temperature is not above 25 ° C away from children.

Shelf life

5 years.
Do not use beyond the expiration date, on the package.

Conditions of supply of pharmacies

On prescription.