Well absorbed and rapidly after the / m and by ingestion. Bioavailability after oral administration – 50%. Cmax in plasma achieved in 1-2 hours – after the / m and 2-4 hours after ingestion. Relationship to plasma proteins – 90-99%. Nonuniformly accumulated in various organs. Easily penetrate the while its concentration in the brain than in plasma concentration. There is no direct correlation between plasma concentration and therapeutic effect. Has the effect of “first pass” through the liver where the drug is extensively metabolized by oxidation (30%), hydroxylation (30%) and dezametilirovaniya (20%). Possess pharmacological activity oxidized hydroxylated metabolites that are inactivated by binding with glucuronic acid, either by further oxidation to form sulfoxides inactive. Excreted by the kidneys and the bile. Side effects of tamoxifenper day output of about 20% of the dose, 1-6% of the dose excreted by the kidneys unchanged. Traces of metabolites found in the urine after 12 months or more after stopping treatment. Due to the high protein binding is not substantially subjected to dialysis.
Indications : In psychiatry, – psychomotor agitation (including patients with schizophrenia); acute delirium, manic and hypomanic excitement in manic-depressive psychosis, chronic psychosis; mental diseases of various origins, accompanied by fear, anxiety, agitation, insomnia; psychopathy (including in patients with epilepsy and organic diseases of the central nervous system), alcoholic psychosis. Severe nausea and vomiting, persistent hiccups. To enhance the analgesic action for persistent pain. Diseases accompanied by increased muscle tone: after cerebrovascular, tetanus , and others.
- increased individual sensitivity;
- depression and coma function of any etiology;
- brain injury;
- liver disease, kidney and blood-forming organs in violation of the functions;
- progressive system of the brain and spinal cord diseases;
- gastric ulcer and 12 duodenal ulcer during the exacerbation;
- heart disease in the stage of decompensation (heart disease, myocardial dystrophy, rheumatic heart disease, etc.), severe hypotension, diseases accompanied by the risk of thromboembolic complications;
- bronchiectasis in the stage of decompensation;
- angle-closure glaucoma side effects of tamoxifen (risk of increased intraocular pressure);
- prostatic hyperplasia;
- pregnancy, breast-feeding;
- children up to 3 years.With caution :
Parkinson’s disease, active side effects of tamoxifen alcoholism (the risk of hepatotoxic effects), breast cancer, epilepsy, chronic diseases accompanied by respiratory failure (especially in children), Reye’s syndrome, cachexia, old age, vomiting (antiemetic effect of phenothiazines may mask vomiting, associated with overdose al. drugs).