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題名 | 氟哌啶醇與還原型氟哌啶醇在天竺鼠體內之交互代謝=Reversible Metabolism of Haloperidol and Reduced Haloperidol in Guinea Pigs |
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作者 | 莊東憬; 張素貞; 吳曉恬; 藍先元; 胡維恆; 張文和; | 書刊名 | 臺灣精神醫學 |
卷期 | 11:1 1997.03[民86.03] |
頁次 | 頁48-60 |
分類號 | 418.21 |
關鍵詞 | 佛哌啶醇; 還原型佛哌啶醇; 天竺鼠; 交互代謝; Haloperidol; Reduced haloperidol; Guinea pigs; Reversible netabolism; |
語文 | 中文(Chinese) |
中文摘要 | 目的:氟�珆r醇(haloperidol,HL)是臨床常用之抗精神病藥物(antipsychotics)。HL的主要代謝途徑之一為HL經酮基還原�t(ketone reductase)代謝為還原型HL代謝物(reduced HL,RH)。RH在人及天竺鼠體內可被逆向代謝而氧化回HL,但RH在大白鼠體內則無此逆向代謝過程。本研究以天竺鼠為實驗動物模型探討單一劑量 HL 與 RH 間的交互逆向代謝的各項參數,以為臨床用藥之參考。方法:每6隻天竺鼠為一組,分別經由腹腔內注射投予 HL 或 RH,其劑量為0.1、0.5、0.75、1、2.5及5 mg/kg。在麻醉狀態下,經由頸動脈插管採集投藥前和投藥後1、2、3、4、6、8及12小心等之血液樣本各0.5ml。 血漿中HL及RH之濃度則經由高效液相層析儀結合電化學偵測器分析。動力學參數計算則仿prednisone/prednisolone模式。結果:投予HL後血中RH的濃度遠大於HL濃度。但投予RH後血中HL的濃度則持續為低濃度,且即使劑量上升,HL的濃度仍維持在恆定。HL與RH的藥物濃度-時間曲線下面積(AUC)間存在非線性關係。結論:交互逆向代謝轉換反應參數計算結果顯示交互逆向代謝徑路在不同劑量投予時呈現飽和濃度代謝狀態,提示臨床使用過高劑量HL時,只有極少部分RH將被逆向代謝回原型藥物,從而造成大量RH之聚積。 |
英文摘要 | Objective: Haloperidol (HL) is an antipsychotic drug used in the treatment of schizophrenia. One of the major metabolites of HL is reduced HL (RH). The reversible metabolism of HL and its reduced metabolite was examined in guinea pigs. this study may aid further understanding of HL metabolism in psychiatric patients. Method: Guinea pigs (N=6, per dose-group) received intraperitoneal HL and RH at dosages 0.1 mg/kg, 0.5 mg/kg, 0.75 mg/kg, 1.0 mg/kg, 2.5 mg/kg or 5.0 mg/kg. Blood samples were collected at baseline and 1,2,3,4,6,8, and 12 hours after drug administration. HL and RH were assayed using HPLC with electrochemical detection. Calculations used for the reversible metabolic parameters were similar to those of the prednisone/prednisolone model. Results: The levels of plasma RH formed from HL administration greatly exceeded plasma HL concentrations. However, the formation of plasma HL from RH administration remained very low and constant despite increasing RH dosages. A nonlinear relationship between HL and RH was found in the area under the plasma concentration time curve (AUC). Conclusions: Reversible metabolic clearance calculations showed that two differeent metabolic pathways became saturated at different drug doses for the two compounds. The back conversion of RH of HL appears to be less prominent than the reduction pathway. High concertrations of RH could accumulate in tissues during high-dose HL treatment. |
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