In this case, risperidone did not have to tropic holinoretseptory. Antipsychotic drug action due to the blockade of dopamine D2-receptors and mezokortikalnoy mesolimbic system. In addition, he has quite pronounced sedative, antiemetic and hypothermic action. Sedative effects due to blockade of adrenergic receptors of the reticular formation of the brainstem, antiemetic action - blockade of dopamine D2-receptor trigger zone of the vomiting center, and hypothermic action - blockade of dopamine receptors of the hypothalamus. According to numerous clinical trials conducted both in Russia and abroad, risperidone is not less effective than previous "gold standard" treatment of schizophrenia - haloperidol, reduces the productive (positive) disorder (delusions, hallucinations, symptoms of mental automatism, psychotic affect and psychomotor agitation). In strength as its influence on negative symptoms with risperidone was significantly superior to haloperidol at all stages of therapy. As for portability, then compared risperidone with haloperidol significantly less common and inhibits motor activity of patients in therapeutic doses rarely stimulates the development of extrapyramidal side effects, the risk of which is further reduced thanks to a balanced central antagonism of serotonin and dopamine. Risperidone may cause a dose-dependent increase in prolactin concentrations in blood plasma, which on the one hand, it is more common in women, but on the other - does not always lead to some clinically negative consequences. Thus, the aggregate performance of efficacy and tolerability of risperidone has a distinct premuschestvom before haloperidol, claiming the title of "the new gold standard of treatment of schizophrenia and other psychotic disorders level. Pharmacokinetic data indicate that risperidone, when taken orally is absorbed rapidly and completely, and the food does not affect the completeness and rate of absorption. Maximum drug concentration in plasma is achieved in 1-2 hours. He is a 90% bound to plasma proteins and rapidly penetrates the central nervous system. The main metabolite of risperidone - 9-hydroxy-risperidone - an active substance with a longer half-life. As a result of antipsychotic fraction of the drug (risperidone + 9-hydroxy-risperidone) is excreted within 21 hours, in most cases allows you to assign his patients once a day. Excretion of risperidone from the body by 70% through the kidneys. In this regard, patients with renal insufficiency and in elderly patients may show delayed elimination of the drug and sometimes jumps in the level of its concentration in blood plasma. The main indications for the use of risperidone include: acute and chronic schizophrenia and other delusional and affective-delusional psychosis, psychomotor agitation and other behavioral disorders in patients with dementia, manic excitement in bipolar affective disorder.
No comments:
Post a Comment