Tamoxifen Hexal, 20 mg 30 pcs

Tamoxifen is a non-steroidal anti-estrogenic drug that also has weak estrogenic properties. Its action is based on the ability to block estrogen receptors.

Tamoxifen and some of its metabolites compete with estradiol for binding sites with cytoplasmic estrogen receptors in breast, uterine, vaginal, anterior pituitary lobe tissues and tumors with high estrogen receptor content.

In contrast to the estrogen receptor complex, the tamoxifen receptor complex does not stimulate DNA synthesis in the nucleus but inhibits cell division, which leads to regression of tumor cells and their death.

Indications

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

The drug can be used to treat:

ovarian cancer:
endometrial cancer;
kidney cancer;
melanoma;
soft tissue sarcomas in the presence of estrogen receptors in the tumor;
prostate cancer with resistance to other drugs.

Pharmacological effect

Tamoxifen is a nonsteroidal antiestrogenic agent that also has weak estrogenic properties. Its action is based on its 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 breast, uterus, vagina, anterior pituitary gland and tumors with a high content of estrogen receptors.

In contrast to the estrogen receptor complex, the tamoxifen receptor complex does not stimulate DNA synthesis in the nucleus, but inhibits cell division, which leads to regression of tumor cells and their death.

Special instructions

Women receiving tamoxifen should undergo regular gynecological examinations. If bloody vaginal discharge or vaginal bleeding occurs, the drug should be discontinued.

In patients with bone metastases, serum calcium concentrations should be determined periodically during the initial treatment period. In case of severe disturbances, tamoxifen should be temporarily discontinued.

If signs of thrombosis of the veins of the lower extremities appear (pain in the legs or swelling), pulmonary embolism (shortness of breath), the drug should be discontinued. Tamoxifen can cause ovulation, which increases the risk of pregnancy, and therefore in women who are sexually active, the use of mechanical or non-hormonal contraception is recommended during (and for approximately 3 months after) treatment with tamoxifen. During the period of therapy, it is necessary to periodically monitor blood coagulation indicators, calcium levels in the blood, blood picture (leukocytes, platelets), liver function indicators, blood pressure, and an examination by an ophthalmologist.

In patients with hyperlipidemia, during treatment it is necessary to monitor the concentration of cholesterol and triglycerides in the blood serum.

Impact on the ability to drive vehicles and other mechanisms that require increased concentration

During the treatment period, it is necessary to refrain from engaging in potentially hazardous activities that require increased concentration and speed of psychomotor reactions.

Active ingredient

Tamoxifen

Composition

1 tablet contains:

Active substances:

tamoxifen citrate 30.4 mg, which corresponds to the content of tamoxifen 20 mg.

Excipients:

lactose monohydrate – 142.6 mg,

sodium starch glycolate – 20 mg,

povidone – 5 mg,

microcrystalline cellulose – 49.6 mg,

magnesium stearate – 2.4 mg.

Shell composition:

white opadry dye – 5 mg (lactose – 1.8 mg, titanium dioxide – 1.3 mg, hypromellose – 1.4 mg, polyethylene glycol 4000 – 0.5 mg).

Contraindications

Pregnancy;
lactation period (breastfeeding);
hypersensitivity to tamoxifen and/or any other ingredient of the drug.

With caution: renal failure, diabetes mellitus, eye diseases (including cataracts), deep vein thrombosis and thromboembolic disease (including a history), hyperlipidemia, leukopenia, thrombocytoenia, hypercalcemia, concomitant therapy with indirect anticoagulants.

Side Effects

When treating with tamoxifen, the most common side effects associated with its antiestrogenic effect are manifested in the form of paroxysmal sensations of heat (hot flashes), vaginal bleeding or discharge, itching in the genital area, alopecia, pain in the affected area, ossalgia, and weight gain.

The following adverse reactions were observed less frequently or rarely: fluid retention, anorexia, nausea, vomiting, constipation, fatigue, depression, confusion, headache, dizziness, drowsiness, fever, skin rash, visual disturbances including corneal changes, cataracts, retinopathy and retrobulbar neuritis. At the beginning of treatment, a local exacerbation of the disease is possible – an increase in the size of soft tissue formations, sometimes accompanied by severe erythema of the affected areas and adjacent areas – which usually resolves within 2 weeks.

The likelihood of thrombophlebitis and thromboembolism may increase.

Transient leukopenia and thrombocytopenia, as well as increased liver enzyme levels, may occasionally occur, very rarely accompanied by more severe liver dysfunction such as fatty liver, cholestasis and hepatitis.

Some patients with bone metastases experienced hypercalcemia at the start of treatment.

Tamoxifen causes amenorrhea, or irregular menstruation, in premenopausal women, as well as the reversible development of cystic ovarian tumors.

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

Interaction

When tamoxifen and cytostatics are prescribed simultaneously, the risk of thrombosis increases.

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

There are reports of tamoxifen enhancing the anticoagulant effect of coumarin drugs (for example, warfarin).

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

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

The simultaneous use of tamoxifen with other hormonal drugs (especially estrogen-containing contraceptives) leads to a weakening of the specific effect of both drugs.

Overdose

Acute overdose with tamoxifen has not been observed in humans. It should be expected that an overdose may cause an increase in the above-described adverse reactions.

There are no specific antidotes; treatment should be symptomatic.

Storage conditions

Store out of the reach of children at a temperature not exceeding 25°C.

Shelf life

5 years.

Manufacturer

Salutas Pharma GmbH, Germany