Pharmacy Department, Jewish General Hospital, Montreal, Quebec, Canada
Faculté de Pharmacie, Université de Montréal, Montreal, Quebec, Canada.
Eur J Hosp Pharm. 2023 Jul;30(4):e20. doi: 10.1136/ejhpharm-2021-002901. Epub 2021 Nov 16.
Once administered, risperidone is converted into its pharmacologically active form, paliperidone. Thus, their pharmacological effects are expected to be equivalent. We encountered a psychosis induced by the switch from risperidone to paliperidone.This is the case of a schizoaffective patient stabilised on risperidone long-acting injection (LAI) who consented to switch to paliperidone LAI. On day 0, he received his first dose of paliperidone. On day 86, he presented to the emergency department with an acute psychotic episode. On day 92, he committed a violent act. The patient was restarted on risperidone LAI and stabilised.Risperidone is extensively metabolised to paliperidone via CYP450 2D6. Interindividual and ethnic genetic polymorphism cause variability in CYP450 2D6 phenotypes. In this possible case of low-functioning alleles, the patient had a higher risperidone to paliperidone ratio at steady state. Although risperidone is paliperidone's prodrug, this case highlights the interindividual pharmacotherapeutic response to these two antipsychotics.
一旦给予,利培酮会转化为其具有药理活性的形式,帕利哌酮。因此,预计它们的药理作用相当。我们遇到了一种由利培酮转换为帕利哌酮引起的精神病。这是一位稳定服用利培酮长效注射剂(LAI)的精神分裂症患者的情况,他同意转换为帕利哌酮 LAI。在第 0 天,他接受了第一剂帕利哌酮。在第 86 天,他因急性精神病发作到急诊就诊。在第 92 天,他实施了暴力行为。患者重新开始使用利培酮 LAI 并稳定下来。利培酮通过 CYP450 2D6 广泛代谢为帕利哌酮。个体间和种族遗传多态性导致 CYP450 2D6 表型的变异性。在这种可能的低功能等位基因情况下,患者在稳定状态下具有更高的利培酮与帕利哌酮比值。尽管利培酮是帕利哌酮的前体药物,但这种情况突出了这两种抗精神病药物对个体的药物治疗反应。