Tamoxifen 10 mg 

Name of the medicinal product

Tamoxifen

 Qualitative and quantitative composition

Active substance: Tamoxifen Citrate, corresponding to 10 mg, 20 mg, respectively

 

 Formulation

 

Coated (covered with water film) Tablets 10 mg and 20 mg.

 

 Clinical Data

 Witness

 

Palliative treatment of hormone dependent tumors such as breast cancer.

 

 Posology and method of administration

 

The dose for initiation of therapy is 20 mg daily if neobhosimo, in 2 divided doses of 10 mg. If you do not notice an effect within 1 month, the dose may be increased to 40 mg daily, or as a single dose or in 2 divided doses per day.

 

 Contraindications

 

Tamoxifen is contraindicated in patients with known hypersensitivity to tamoxifen or to any of the excipients of the medicinal product. Tamoxifen is contraindicated in pregnancy.

 

Patients who are post-menopausal, should be carefully evaluated prior to treatment with tamoxifen to exclude pregnancy.

 

 Special warnings and precautions

 

Special warnings:

 

Menstruation can be suppressed in the majority of patients in the menopausal who use tamoxifen to treat breast cancer.

 

Following initiation of therapy may occur in the flare development of breast cancer. This may be accompanied by local pain (especially in bone metastases), tumor enlargement and erythema of the cancer stricken areas. These symptoms may respond best response in this case smptomite will disappear spontaneously.

 

In patients with bone metastases may develop hypercalcemia during treatment. In this case it is necessary to adjust the dose (to reduce or suspension) and side effects can be treated symptomatically. Reported to increase the incidence of endometrial changes associated with long-term treatment with tamoxifen as hyperplasia, polyps and carcinomas. It is assumed that these changes are related to the characteristics of estrogen tamoxifen. If patients treated with tamoxifen complain of abnormal vaginal bleeding, it is necessary to immediately do further research.

 

There have been reports of eye injuries, including corneal changes, cataracts and retinopathy in patients receiving tamoxifen. Ophthalmologic examination should be performed prior to initiation of treatment with tamoxifen and change in vision during treatment.

Is there literature on increased incidence of thromboembolic events, including deep vein thrombosis and pulmonary embolism during treatment with tamoxifen, it is therefore necessary attention and rigorous assessment of the risk / benefit in treating patients with a thromboembolic event.

 

Special precautions:

 

Tamoxifen should be used with caution in patients with leucopenia and thrombocytopenia. Patients receiving this drug should be periodically complete blood cell count, including platelet count.

It should also be periodically monitored for liver function tests.

For receiving messages uncommon for changes in lipoproteins in patients receiving tamoxifen, including severe hiperlipoproteinemiya marked, periodic monitoring of serum triglycerides and cholesterol during tamoxifen therapy in patients with previous hiperlipoproteinemiya.

 

 Interactions

 

When tamoxifen is used in combination with coumarin-type anticoagulants may appear significant increase in anticoagulant effect. When starting this combination is recommended that the patient be monitored very carefully. Co-administration of estrogen can prevent the therapeutic effect of tamoxifen. Concurrent therapy with tamoxifen and allopurinol can lead to increased nachernodrobnata toxicity induced by allopurinol.

The metabolism of the liver can be affected by concurrent use of tamoxifen and other cancer drugs (such aminoglutetemid and medroxyprogesterone acetate).

Is there literature that the use of tamoxifen in combination with cytotoxic agents, there is an increased risk of thromboembolism.

Tamoxifen / bromocriptine: There was an increase in serum concentrations of tamoxifen in patients receiving both tamoxifen and bromocriptine.

 

 Pregnancy and lactation

 

Pregnancy is protivopoazana during treatment with tamoxifen, which means that patients with premenstrual, pregnancy should be ruled out. Women should be advised not to become pregnant while using tamoxifen, if they are sexually active, you should use a barrier type or other non-hormonal contraceptive methods. Women should be informed of the potential risks to the fetus if they become pregnant during or within 2 months after discontinuation of treatment with tamoxifen.

 

 Effects on ability to drive and use machines

 

There is no evidence that the use of tamoxifen causes damage to the ability to drive and operate machinery. However, if you experience side effects such as dizziness and visual disturbances, this can have a negative impact on ability to drive and use machines.

 

The side effects of tamoxifen are lightweight and are associated with anti-estrogen effects, such as vasomotor effects (eg hot flushes, sweats). Vaginal bleeding, itching of the vulva, irregular menstruation or amenorrhea.

Other common adverse reactions such as: gastrointestinal symptoms (eg, nausea and / or vomiting), tumor flare'''', dizziness, skin rash, fluid retention and alopecia.

 

When these side effects are severe, it may be reduced by lowering the dose without losing control of the disease.

 

In patients with bone metastases, the possibility for the development of hypercalcemia.

Been reported thrombocytopenia and leucopenia, rarely - neutropenia.

 

Are sometimes reported cases of visual disturbances such as changes in corneal, cataract and retinopathy.

 

Have been reported rarely ovarian cysts.

 

Are sometimes reported cases of thromboembolic complications during therapy with tamoxifen.

The use of tamoxifen is associated with changes in liver function disorders, sometimes with serious liver disorders such as fatty degeneration of the liver, cholestasis and hepatitis.

Common adverse events were hypertriglyceridemia, sometimes with pancreatitis. In patients with familial hyperlipidemia risk of developing this side effect is higher. Upon treatment with tamoxifen were observed proliferative changes in the endometrium. According to current data, the risk of endometrial cancer is 2 to 4 times higher during prolonged treatment with tamoxifen than in women treated with tamoxifen.

 

Reports are also side effects such as depression, headache, dizziness, fatigue, mild arthralgia or arthritis.

 

 Overdose

 

There have been reported cases of chronic or ostropredozirane. Teoritini reasons why it is expected that an overdose should increase earlier mentioned anti-estrogenic side effects. In experimental studies in animals it was found that the most extreme overdose (100 to 200 times the recommended daily dose) can cause estrogenic effects. There is no specific antidote for overdose. Treatment should be symptomatic.

 

 Pharmacological

 

 Pharmacological properties

 

Pharmacological group: Anti-estrogens

ATC code: L02BA01

 

Tamoxifen is a nonsteroidal triphenylethylene derivative, which usually manifests as estrogen antagonist. In humans, tamoxifen has mainly anti-estrogenic activity. In some tissues or organs, however, (bone and pituitary) tamoxifen also exercise some estrogenic activity.

The mechanism of action is not fully known. In vitro studies suggest a direct connection with the estrogen receptor, which causes abnormal RNA transcription and inhibited cell proliferation. In postmenopausal women, tamoxifen did not affect plasma levels of estrogens.

 

During treatment with tamoxifen in premenopausal women, the concentrations of estrogens and progesterone may increase. After treatment, these levels decreased again to levels at the start of therapy.

 

The affinity of natural estrogens for estrogen receptors is much higher than the affinity of tamoxifen. Positive effect in premenopausal patients observed in several experiments, however, showed that tamoxifen levels and blood obtained at normal dosage sufficient to maintain effective estrogen blockade.

 

Tamoxifen causes an increase of steroid and thyroid proteins. This can affect the concentrations of cortisol and thyroid hormones.

 

 Pharmaceutical Data

 

 Physical incompatibilities

 

 Expiration date

 

10 mg - 5 years

20 mg - 5 years

The drug should not be used after the expiry date stated on the packaging.

 Special precautions for storage

Protect from light. The drug should be stored out of the reach of children.