Tamoxifen, tablets 10 mg 30 pcs

Pharmacodynamics

Antitumor agent. Anti-estrogen. Blocks estrogen receptors and thus inhibits the progression of estrogen-stimulated tumor disease.

Pharmacokinetics

Tamoxifen is metabolized in the liver, undergoing intestinal-hepatic recirculation. It is excreted with the bile as metabolites.

Indications

Active ingredient

Composition

1 tablet contains:

Active substances:

Tamoxifen 10 mg.

Associates:

Corn starch,

lactose,

povidone,

magnesium stearate,

sodium starch glycolate,

purified water.

There are 10 tablets in the blister.

There are 3 blisters in the carton.

How to take, the dosage

The dosing regimen is established individually, depending on the indication, the patient’s condition, and the antitumor therapy regimen used.

Interaction

Concomitant use with anticoagulants coumarin derivatives increases the risk of increased anticoagulant effect; with cytostatics – possible increased risk of thrombosis.

In concomitant use with allopurinol hepatotoxic effect is possible; with aminoglutethimide – decrease of plasma concentration of tamoxifen, probably due to its increased metabolism.

In patients receiving tamoxifen, atracurium-induced neuromuscular blockade may be prolonged.

The concomitant use of bromocriptine may increase the dopaminergic effect of bromocriptine. In patients receiving tamoxifen, when using warfarin, there is a risk of developing a threatening clinical situation: prolongation of prothrombin time, hematuria, hematoma are possible.

Concomitant use with mitomycin increases the risk of hemolytic-uremic syndrome.

The concentration of tamoxifen in plasma may decrease, which appears to be due to induction of CYP3A4 isoenzyme by rifampicin.

Estrogens may decrease the therapeutic effect of tamoxifen.

Special Instructions

With caution, use in leukopenia, thrombocytopenia, hypercalcemia, patients with cataracts, hyperlipidemia.

The peripheral blood count (especially the platelet count); calcium and blood glucose levels should be monitored regularly during treatment; with long-term use an ophthalmologist should be seen (every 3 months).

Do not combine with drugs containing hormones, especially estrogens.

In case of concomitant use with drugs that affect the clotting system, correction of the dose of tamoxifen is necessary.

In experimental studies the carcinogenic effect of tamoxifen has been established.

Contraindications

Side effects

Digestive system disorders: nausea, vomiting, increased liver transaminase activity; in some cases – fatty liver infiltration, cholestasis, hepatitis.

CNS disorders: rarely – depression, dizziness, headache, retrobulbar neuritis.

An organ of vision: rarely – retinopathy, keratopathy, cataracts.

Hematopoietic system: rare – thrombocytopenia, leukopenia.

Endocrine system disorders: in women – endometrial hyperplasia, vaginal bleeding, hot flashes, weight gain; in men – impotence, decreased libido.

Cardiovascular system: edema, thromboembolism, phlebitis.

Dermatological reactions: alopecia, rash, itching.

Others: pain in the bones and lesions, increased body temperature.

Overdose

Acute overdose with tamoxifen has not been observed in humans.

Symptoms: an overdose can be expected to cause an increase in the adverse reactions described above.

Treatment: there are no specific antidotes, treatment should be symptomatic.

Pregnancy use

Tamoxifen is contraindicated in pregnancy. If it is necessary to use during lactation, breastfeeding should be stopped.

The teratogenic effect of tamoxifen has been established in experimental studies.