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題 名 | Clozapine及其代謝物於精神分裂症患者之藥物動力學=Pharmacokinetics of Clozapine, Desmethylclozapine and Clozapine-N-OXide in Taiwanese Schizophrenic Patients |
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作 者 | 邱智強; 藍先元; 劉慧卿; 陳錦宏; 鄭平石; 張文和; | 書刊名 | 臺灣精神醫學 |
卷 期 | 12:1 1998.03[民87.03] |
頁 次 | 頁27-35 |
分類號 | 418.21 |
關鍵詞 | 藥物動力學; Pharmacokinetics; Clozapine; Clozapine-N-oxide; Desmethylclozapine; |
語 文 | 中文(Chinese) |
中文摘要 | Clozapine此種非典型的抗精神病藥物,在人體經肝臟代謝成多種代謝物,其中以 desmethylclozapine(DCLOZ)及clozapine-N-oxide(CLOZNO)為主。本研究即以單一劑量 clozapine投予11名精神分裂症病患後,分析clozapine及其兩種主要代謝物的藥物動力學之 各個參數。方法:病患於服用單一劑量50 mg clozapine之後的48小時內定時接受靜脈血之採 樣,再以高效液相層析法分析血漿中三種化合物的濃度。結果:clozapine的平均清除率及半衰 期分別為64.3(標準差=6.4)L/hr及15.1(2.8)hours。Clozapine、DCLOZ及CLOZNO的平均尖 鋒濃度分別為75.1(7.7),22.8(1.8)及26.7(2.5)ng/ml;平均達鋒時間為2.5(0.6),2.5(0.7)及 l.7(0.4)hours;平均AUC為748.3(75.1),362.2(43.7)及146.5(15.2)ng.hr/ml。此外,DCLOZ的 平均AUC與clozapine的平均AUC比值為0.478(0.031),而CLOZNO與clozapine的平均AUC 比值則為0.212(0.021)。結論:本研究顯示clozapine與其兩個主要代謝物的單一劑量藥物動力 學參數,皆存在著極顯著的個體差異。本國的精神分裂症患者clozapine的擬似分布體積,明 顯地高於高加索人,而clozapine其他的藥物動力學參數上則無明顯的差異。 |
英文摘要 | Objective: Clozapine is metabolizaed via the hepatic microsomal enzyme system into two major metablites: desmethylclozapine (DCLOZ) and clozapine N-oxide (CLOZNO). Moreover, CLOZNO can be converted back to its parent compound. However, no studies have simultaneously determined the single-dose pharmacokinetics of these three compounds following clozapine administration. This study investigated the single-dose pharmacokinetics of clozapine and its two major metabolites in schizophrenic patients. Methods: eleven schizophrenic male patients participated in this study (age 37±12.4 yr; BW 56±12.3 kg). Pattients were prohibited from taking medications which are known to be metabolized by, or able to induce or to inhibit cytochrome P450 1A2 or 3A for a least 2 months before the study and throughout the course of the study. A single dose of 50 mg clozapine was administered and venous blood samples were obtained over the next 48 hours. Clozapine and its two metabolites were assayed by high-performance liquid chromatography with ultraviolet detection. The pharmacokinetic parameters for clozapine, DCLOZ and CLOZNO were determined by a modal-independent method with nonlinear least-square regression analysis. Results: The mean clearance and half-life of clozapine were 64.3 (SD, 6.4) L/hr and 15.1 (2.8) hours, respectively. The mean Cmax for clozapine, DCLOZ and CLOZNO were 75.1 (7.7), 22.8 (1.8) and 26.7 (2.5) ng/ml, respectively. The mean Tmax for these three compounds were 2.5 (0.6), 2.5 (0.7) and 1.7 (0.4). The mean AUC were 748.3 (75.1), 362.2 (43.7) and 146.5 (15.2) ng.hr ml. The mean AUC ratio of DCLOZ/clozapine and that of CLOZNO/clozapine were 0.478 (0.031) and 0.212 (0.021), respectively. Conclusions: This study found a wide interpatient variability in the pharmacokinetics of clozapine and its metabolites was observed. Except for the greater apparent volume of distribution, the single-dose pharmacokinetic parameters of clozapine found in the Taiwanese patients of this study were quite similar to those reported in Caucasian populations. Further investigation of the factors influencing these parameters is needed. (Full text in Chinese) |
本系統中英文摘要資訊取自各篇刊載內容。