Carstairs Shaun D, Williams Saralyn R
Department of Emergency Medicine, Naval Medical Center, San Diego, California.
Division of Medical Toxicology, Department of Emergency Medicine, University of California, San Diego Medical Center, San Diego, California; California Poison Control System, San Diego Division, San Diego, California.
J Emerg Med. 2005 Apr;28(3):311-313. doi: 10.1016/j.jemermed.2004.09.013.
Aripiprazole is the first member of a new class of antipsychotic medications. Unlike other antipsychotics, it acts as a partial agonist at dopamine D(2) and 5-HT(1A) receptors, thereby mitigating most of the adverse reactions such as extrapyramidal side effects and hyperprolactinemia. Additionally, most research to date has suggested a low incidence of QTc prolongation and orthostatic hypotension at therapeutic doses. Experience in the setting of intentional overdose, however, is limited. We present a case of a 27-year-old woman who intentionally ingested 330 mg of aripiprazole in a suicide attempt. Clinical effects were limited to mild sedation. Serum levels performed by the drug's manufacturer confirmed a total level (parent drug and active metabolite) of 716 ng/mL, nearly six times the upper limit of accepted therapeutic levels. This suggests that aripiprazole's therapeutic index is quite high and reinforces the drug's known safety profile.
阿立哌唑是一类新型抗精神病药物中的首个成员。与其他抗精神病药物不同,它在多巴胺D(2)和5-羟色胺(1A)受体上作为部分激动剂发挥作用,从而减轻大多数不良反应,如锥体外系副作用和高催乳素血症。此外,迄今为止的大多数研究表明,治疗剂量下QTc延长和体位性低血压的发生率较低。然而,关于故意过量服用的经验有限。我们报告一例27岁女性,她为自杀故意服用了330毫克阿立哌唑。临床效应仅限于轻度镇静。药物制造商检测的血清水平证实总水平(母体药物和活性代谢物)为716纳克/毫升,几乎是公认治疗水平上限的六倍。这表明阿立哌唑的治疗指数相当高,并强化了该药物已知的安全性。