Tamoxifen Citrate

pharmachologic effect

The antitumor agent. Antiestrogen. Blocks estrogen receptors and thereby inhibits the progression of neoplastic disease stimulated by estrogens.

testimony

Breast cancer in postmenopausal women, breast cancer in men after castration, renal cancer, melanoma (containing estrogen receptors), ovarian cancer; prostate cancer with resistance to other drugs.

dosage

The mode set individually depending on the indication, patient and tumor therapy scheme used.

Side effect

From the digestive system: nausea, vomiting, increase in liver transaminases; in some cases – fatty liver, cholestasis, hepatitis.

CNS: rarely – depression, dizziness, headache, optic neuritis.

From a sight organ: rare – retinopathy, keratopathy, cataract.

Hematopoietic system: rarely – thrombocytopenia, leukopenia.

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

Cardio-vascular system: edema, thrombosis, phlebitis.

Dermatological reactions: alopecia, rash, pruritus.

Other: pain in the bones and lesions, fever.

Contraindications

Thrombophlebitis, pregnancy, increased sensitivity to 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.

special instructions

To use caution when leukopenia, thrombocytopenia, hypercalcemia in patients with cataract, hyperlipidemia.

In the course of treatment should be regularly monitored picture peripheral blood (especially platelet count); and the level of calcium in the blood glucose; long-term use is shown watching ophthalmologist (every 3 months).

Should not be combined with preparations containing hormones, especially estrogen.

In an application with drugs that affect blood clotting, dosage adjustment is necessary tamoxifen.

In experimental studies have found a carcinogenic effect of tamoxifen.

Drug interactions

In an application with anticoagulant coumarin derivatives increases the risk of increasing the anticoagulant action; cytostatics – may increase the risk of thrombosis.

In an application with allopurinol possible hepatotoxic effects; with aminoglutethimide – reduction in the plasma concentration of tamoxifen, apparently due to increasing its metabolism.

In patients receiving tamoxifen may prolongation of neuromuscular blockade induced by atracurium.

With 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.

Tamoxifen may reduce the plasma concentration that is apparently due to induction of isoenzyme CYP3A4 by rifampicin action.

Estrogens may reduce the therapeutic effect of tamoxifen.

Drug interactions

In an application with anticoagulant coumarin derivatives increases the risk of increasing the anticoagulant action; cytostatics – may increase the risk of thrombosis.

In an application with allopurinol possible hepatotoxic effects; with aminoglutethimide – reduction in the plasma concentration of tamoxifen, apparently due to increasing its metabolism.

In patients receiving tamoxifen may prolongation of neuromuscular blockade induced by atracurium.

With 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.

Tamoxifen may reduce the plasma concentration that is apparently due to induction of isoenzyme CYP3A4 by rifampicin action.

Estrogens may reduce the therapeutic effect of tamoxifen.

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