Ciszowski Krzysztof, Szpak Dorota, Wilimowska Jolanta
Klinika Toksykologii i Chorób Srodowiskowych, Katedry Toksykologii Kliniczne i Srodowiskowej UJ CM w Krakowie.
Przegl Lek. 2010;67(8):602-5.
Risperidone (RIS) is a benzisoxazole derivative, an atypical neuroleptic used in the treatment of schizophrenia and other psychoses. The therapeutic action of RIS depends not only on the parent compound but also its major active metabolite, 9-hydroxyrisperidone (9-OH-RIS), and the pharmacokinetics is modified by the genetic polymorphism of CYP2D6, the main site o RIS metabolism. Diverse symptoms of an acute RIS poisoning result from its interaction with multiple receptors, i.e. serotoninergic 5-HT2A and 5-HT7, dopaminergic D2, adrenergic alpha1 and alpha2, as well as histamine H1. The clinical picture of acute RIS poisoning consists predominantly of central nervous system and cardiovascular effects and the most severe symptoms are: hypotension, dysrrhythmias, consciousness disturbances, seizures and respiratory failure. No specific antidote for RIS poisoning is known and the treatment is only symptomatic and supportive. Quantitative determination of RIS blood concentration seems to be helpful in confirmation and monitoring of acute poisoning, nevertheless further investigations are needed to evaluate the relation between drug concentration and clinical symptoms.
利培酮（RIS）是一种苯并异恶唑衍生物，是一种用于治疗精神分裂症和其他精神病的非典型抗精神病药物。利培酮的治疗作用不仅取决于母体化合物，还取决于其主要活性代谢物9-羟基利培酮（9-OH-RIS），并且药代动力学因CYP2D6的基因多态性而改变，CYP2D6是利培酮代谢的主要部位。急性利培酮中毒的各种症状源于其与多种受体的相互作用，即5-羟色胺能5-HT2A和5-HT7、多巴胺能D2、肾上腺素能α1和α2以及组胺H1。急性利培酮中毒的临床表现主要包括中枢神经系统和心血管系统效应，最严重的症状是：低血压、心律失常、意识障碍、癫痫发作和呼吸衰竭。目前尚无已知的利培酮中毒特效解毒剂，治疗仅为对症和支持治疗。利培酮血药浓度的定量测定似乎有助于急性中毒的确诊和监测，然而，需要进一步研究以评估药物浓度与临床症状之间的关系。
