The active substance group:
Tamoxifen (Tamoxifen), antitumor agent, an anti-estrogen
Dosage Form:
tablets, coated tablets
Contraindications:
Hypersensitivity, pregnancy, lactation. Eye diseases (including cataracts), hyperlipidemia, leukopenia, thrombocytopenia, hypercalcemia, expressed thrombophlebitis, thromboembolic disease (including history).
Dosage and administration:
Usually set individually depending on the evidence.
Inside, breast cancer, kidney – 20-40 mg 1-2 times a day (morning and evening), endometrial – 20-30 mg 1-2 times a day. On course – 2.4-9.6, the treatment is carried out for a long time (until evidence of disease progression), as the effect lasts only against the background of constant use; If necessary, use in combination with radiotherapy and cytostatic therapy.
Tablets should be taken with liquid, squeezed small amounts of liquid in one go in the morning or sharing the required dose into 2 doses, morning and evening.
Pharmachologic effect:
The anti-tumor anti-estrogen agent. Competitively inhibits estrogen receptors in the target organs and tumors originating from these bodies. The result is a complex (drug-receptor-cofactor transport), which, after translocation into the nucleus of cells prevents hypertrophy, estrogen dependent regulation. Has antigonadotropnym properties, it inhibits the synthesis of Pg in the tumor tissue. It stops the progression of the tumor process, stimulated by estrogen.
The ability to block estrogen can persist for several weeks after a single dose. Read more
In addition, tamoxifen may cause ovulation in women in its absence, by stimulating the release of GnRH from the hypothalamus, which stimulates the release of pituitary gonadotropins. In men with oligospermia it increases the concentration of LH and FSH, testosterone and estrogen in the blood serum. Tamoxifen and some of its metabolites (N-dezmetiltamoksifen, 4-hydroxy tamoxifen) are potent inhibitors of mixed function oxidases of the cytochrome P450 liver, but the clinical significance of these effects is not defined.
Side effects:
Ossalgia, sore lesions, fever; loss of appetite, nausea, vomiting, constipation or diarrhea, and in rare cases – fatty liver, cholestasis, hepatitis; flushing of the skin with a sensation of heat; leukopenia, thrombocytopenia, thrombosis, thromboembolism, thrombophlebitis; skin rash, dry skin, increasing the size of soft tissue structures, sometimes accompanied by severe erythema lesions and surrounding areas (usually goes away within 2 weeks); hypercalcemia, peripheral edema (fluid retention associated with), alopecia, weight gain; depression, headache, dizziness, myasthenia gravis, fatigue, drowsiness, confusion; loss of visual acuity, corneal opacities, cataracts, retinopathy, optic neuritis.
Women – endometrial hyperplasia, a reversible development of cystic tumors, vaginal discharge, metrorrhagia, dysmenorrhea, genital itching, amenorrhea.
The men – reduced potency and / or libido. Peredozirovka. Symptoms: increased side effects.
Treatment: symptomatic. No specific antidote.
Special instructions:
Prior to treatment, women should undergo a thorough gynecological (except pregnancy), and physical examination.
Tamoxifen induces ovulation, which increases the risk of pregnancy, so women of childbearing age should use reliable methods of contraception (hormonal) during treatment and for 3 months after treatment.
During the period of treatment is necessary to periodically monitor the performance of blood clotting, Ca2 + concentration in the blood, blood count (leukocytes and platelets), liver function tests, blood pressure, inspect an ophthalmologist – every 3 months, gynecological examination (when a bloody vaginal discharge or vaginal bleeding the drug should be discontinued).
In patients with bone metastases periodically during the initial period of treatment should be to determine the concentration of Ca2 + in the blood serum (in the case of severe hypercalcemia tamoxifen should be suspended). Is ineffective in the treatment of patients with metastatic disease (especially in liver).
If signs of deep vein thrombosis of the lower limbs (leg pain or swelling), thromboembolism, pulmonary artery branches (dyspnea) receiving the drug should be discontinued.
Patients with hyperlipidemia in the treatment process to control the concentration of cholesterol and triglycerides in the blood serum. see more
During the period of treatment must be careful when driving and other lesson. Potentially hazardous activities that require high concentration and speed of psychomotor reactions.
Interaction:
- It enhances the effect of indirect anticoagulants (requires careful monitoring for dose adjustment of anticoagulants).
- Cytostatics increase the risk of thrombosis.
- Allopurinol promotes hepatotoxic effects.
- The combined use of tamoxifen and tegafur can cause chronic active hepatitis and cirrhosis.
- Concomitant use of tamoxifen with others. Hormonal drugs (contraceptives, especially estrogensoderjath) leads to a weakening of the specific effects of both drugs.
- Drugs that reduce the excretion of Ca2 + (for example thiazide diuretics number) may increase the risk of hypercalcemia.
Antacids, H2-blockers of histamine receptors and dr.LS reducing gastric acidity, can cause premature dissolution and loss of the protective effect of Valium pills. The interval between tamoxifen and these drugs should be 1-2 hours.