Ciszowski Krzysztof, Szpak Dorota, Wilimowska Jolanta
Klinika Toksykologii i Chorób Srodowiskowych, Katedry Toksykologii Klinicznej i Srodowiskowej UJ CM w Krakowie.
Przegl Lek. 2010;67(8):606-9.
Sulpiride is a benzamide neuroleptic used in the treatment of some psychiatric and gastroenterological disorders. Its antipsychotic, antiautistic, activizing and antidepressive properties result from antagonistic action to dopaminergic D2, D3 and D4 receptors in the central nervous system (CNS). The oral bioavailability of sulpiride is poor and it does not appear to have an extensive first-pass metabolism, nor is it extensively protein-bound. Elimination of sulpiride appears to depend primarily on the kidneys. The acute sulpiride poisoning includes mainly neuropsychiatric (i.e., agitation, hallucinations, and CNS depression) as well as cardiac effects (i.e., hypotension, dysrhythmias, and sinus tachycardia). The life-threatening conditions with sometimes fatal outcome after sulpiride poisoning are prolongation of QTc interval with consequent torsade de pointes (TdP) and neuroleptic malignant syndrome (NMS). The quantitative methods for the measurement of sulpiride blood concentration are not routinely available and the toxic blood concentration is probably higher than 2 mg/L. Treatment of acute sulpiride poisoning includes standard protocols of gastrointestinal decontamination and further symptomatic and supportive measures, among them TdP (magnesium sulphate, isoproterenol, electrotherapy) and NMS treatment (benzodiazepines, bromocriptine, dantrolene, physical cooling).
舒必利是一种苯甲酰胺类抗精神病药，用于治疗某些精神和胃肠疾病。其抗精神病、抗自闭症、激活和抗抑郁特性源于对中枢神经系统（CNS）中多巴胺能D2、D3和D4受体的拮抗作用。舒必利的口服生物利用度较差，似乎没有广泛的首过代谢，也没有广泛的蛋白结合。舒必利的消除似乎主要依赖于肾脏。舒必利急性中毒主要包括神经精神症状（如躁动、幻觉和中枢神经系统抑制）以及心脏效应（如低血压、心律失常和窦性心动过速）。舒必利中毒后有时会导致致命后果的危及生命情况是QTc间期延长，继而发生尖端扭转型室速（TdP）和抗精神病药恶性综合征（NMS）。测量舒必利血药浓度的定量方法并非常规可用，中毒血药浓度可能高于2mg/L。急性舒必利中毒的治疗包括胃肠道去污的标准方案以及进一步的对症和支持措施，其中包括TdP（硫酸镁、异丙肾上腺素、电疗法）和NMS治疗（苯二氮䓬类、溴隐亭、丹曲林、物理降温）。
