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慢性精神分裂症患者血浆和红细胞中氟哌啶醇及其代谢产物浓度降低。

Haloperidol and reduced haloperidol concentrations in plasma and red blood cells from chronic schizophrenic patients.

作者信息

Ko G N, Korpi E R, Kirch D G

机构信息

Psychiatry Service, Bronx Veterans Administration Medical Center, New York 10468.

出版信息

J Clin Psychopharmacol. 1989 Jun;9(3):186-90.

PMID:2661607
Abstract

In a double-blind, placebo-controlled study, 15 drug-free chronic schizophrenic inpatients were treated with a fixed dose of haloperidol for 6 weeks. Haloperidol and its metabolite, reduced haloperidol, were measured in plasma and red blood cells after 2, 4, and 6 weeks of treatment. Behavioral change was rated using the Brief Psychiatric Rating Scale (BPRS). Not only the raw concentrations, but also blood compartment sums and ratios of these four drug measurements were tested for their strength of association with behavioral improvement. Positive associations with some BPRS subscales at some time points emerged; however, no significant correlations were found to extend across all time points measured. There was a trend in this cohort for negative symptom improvement to be associated with the ratio of haloperidol to reduced haloperidol in red blood cells. The ratio of haloperidol to reduced haloperidol in plasma was always greater than that in the red blood cells for all patients, reflecting an accumulation of the metabolite in red blood cells.

摘要

在一项双盲、安慰剂对照研究中,15名未服用药物的慢性精神分裂症住院患者接受了固定剂量的氟哌啶醇治疗,为期6周。在治疗2周、4周和6周后,测定血浆和红细胞中的氟哌啶醇及其代谢产物去氢氟哌啶醇。使用简明精神病评定量表(BPRS)对行为变化进行评分。不仅对这四种药物测量的原始浓度,而且对血室总和及比率,都测试了它们与行为改善的关联强度。在某些时间点出现了与一些BPRS分量表的正相关;然而,在所有测量的时间点上均未发现显著相关性。在该队列中存在一种趋势,即阴性症状的改善与红细胞中氟哌啶醇与去氢氟哌啶醇的比率相关。对于所有患者,血浆中氟哌啶醇与去氢氟哌啶醇的比率始终高于红细胞中的比率,这反映了代谢产物在红细胞中的积累。

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Haloperidol and reduced haloperidol concentrations in plasma and red blood cells from chronic schizophrenic patients.慢性精神分裂症患者血浆和红细胞中氟哌啶醇及其代谢产物浓度降低。
J Clin Psychopharmacol. 1989 Jun;9(3):186-90.
2
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引用本文的文献

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Haloperidol versus placebo for schizophrenia.氟哌啶醇与安慰剂治疗精神分裂症的对比
Cochrane Database Syst Rev. 2013 Nov 15;2013(11):CD003082. doi: 10.1002/14651858.CD003082.pub3.
2
Potent inhibition of CYP2D6 by haloperidol metabolites: stereoselective inhibition by reduced haloperidol.氟哌啶醇代谢物对CYP2D6的强效抑制作用:还原型氟哌啶醇的立体选择性抑制
Br J Clin Pharmacol. 2001 Jan;51(1):45-52. doi: 10.1046/j.1365-2125.2001.01313.x.
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The relationship between serum concentration and therapeutic effect of haloperidol in patients with acute schizophrenia.
急性精神分裂症患者中氟哌啶醇血清浓度与治疗效果的关系。
Clin Pharmacokinet. 1998 Mar;34(3):227-63. doi: 10.2165/00003088-199834030-00005.
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A method to estimate in vivo D2 receptor occupancy by antipsychotic drugs.一种估计抗精神病药物体内D2受体占有率的方法。
J Psychiatry Neurosci. 1996 Nov;21(5):325-33.
5
Clinically significant interactions of psychotropic agents with antipsychotic drugs.精神药物与抗精神病药物的临床显著相互作用。
Drug Saf. 1996 Nov;15(5):333-46. doi: 10.2165/00002018-199615050-00004.
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Nonlinear relationship between circulating concentrations of reduced haloperidol and haloperidol: evaluation of possible mechanisms.还原型氟哌啶醇与氟哌啶醇循环浓度之间的非线性关系:可能机制的评估
Psychopharmacology (Berl). 1994 Oct;116(2):161-6. doi: 10.1007/BF02245058.
7
Reduced haloperidol plasma concentration and clinical response in acute exacerbations of schizophrenia.精神分裂症急性加重期氟哌啶醇血浆浓度降低与临床反应
Psychopharmacology (Berl). 1990;102(4):514-20. doi: 10.1007/BF02247134.
8
Reduced haloperidol: a factor in determining the therapeutic benefit of haloperidol treatment?氟哌啶醇用量减少:决定氟哌啶醇治疗疗效的一个因素?
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Determination of haloperidol and reduced haloperidol in the plasma and blood of patients on depot haloperidol.
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