The antitumor agent. Antiestrogen. Blocks estrogen receptors and thereby inhibits the progression of neoplastic disease stimulated by estrogens.
Tamoxifen is metabolized in the liver and undergoes enterohepatic recycling. Excreted in the bile as metabolites.
1 tablet contains:
Active ingredients: 10 mg of tamoxifen
Excipients: corn starch, lactose, povidone, magnesium stearate, sodium starch glycolate, purified water
In a blister pack of 10 tablets. The carton 3 blisters.
- Breast cancer in postmenopausal women;
- breast cancer in men after castration;
- kidney cancer;
- melanoma (containing estrogen receptors);
- ovarian cancer;
- prostate cancer with resistance to other drugs.
- increased sensitivity to tamoxifen.
From the digestive system: nausea, vomiting, increase in liver transaminases; in some cases – fatty liver, cholestasis, hepatitis
From the CNS: rarely – depression, dizziness, headache, optic neuritis
From a sight organ: rare – retinopathy, keratopathy, cataract
From the hematopoietic system: rarely – thrombocytopenia, leukopenia
From the endocrine system: in women – endometrial hyperplasia, vaginal bleeding, hot flashes, weight gain; men – impotence, decreased libido
Since the cardiovascular system: edema, thrombosis, phlebitis
Dermatological reactions: alopecia, rash, itching,
Other: bone pain and lesions, fever
How to accept, acceptance rate and dosage
The mode set individually, depending on the evidence, the state of the patient and the applied scheme anticancer therapy.
In a dry place, protected from light at a temperature not higher than 25 ° C
In an application with anticoagulant coumarin derivatives increases the risk of increased anticoagulant effect; cytostatics – may increase the risk of thrombotic events
While the use of allopurinol may hepatotoxicity; with aminoglutethimide – decrease in the concentration of tamoxifen in plasma, apparently due to increasing its metabolism
In patients receiving tamoxifen may prolongation of neuromuscular blockade induced by atracurium.
With the simultaneous use of bromocriptine may increase the dopaminergic action of bromocriptine. In patients receiving tamoxifen, when warfarin is a risk of threatening clinical situations: possible prolongation of the prothrombin time, haematuria, hematoma
While the use of mitomycin C increases the risk of hemolytic-uremic syndrome.
Perhaps the decrease in the concentration of tamoxifen in plasma, which appears to be due to induction of CYP3A4 by rifampicin action.
Estrogen may reduce the therapeutic effect of tamoxifen.
Be wary of leukopenia, thrombocytopenia, hypercalcemia in patients with cataracts, hyperlipidemia.
In the course of treatment should be regularly monitored picture peripheral blood (especially platelet count); calcium, and glucose in the blood; long-term use indicated observation oculist (every 3 months).
It should not be combined with drugs, containing hormones, especially estrogen.
While the use of drugs that affect blood clotting, necessary dose adjustment tamoxifen.
In experimental studies have found a carcinogenic effect of tamoxifen.
Pregnancy and lactation
Tamoxifen is contraindicated during pregnancy. If necessary, use during lactation should stop breastfeeding.
In experimental studies established teratogenic effect of tamoxifen.
Acute overdose of tamoxifen in humans has not been observed.
Symptoms: it is expected that an overdose can cause amplification of the above adverse reactions.
Treatment: There is no specific antidote, treatment should be symptomatic