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題 名 | 葡萄柚汁對Clozapine代謝的影響=Effects of Grapefruit Juice on Clozapine Metabolism |
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作 者 | 黃名琪; 劉宗憲; 陳喬琪; 劉慧卿; 藍先元; 張文和; 胡維恆; | 書刊名 | 臺灣精神醫學 |
卷 期 | 15:2 2001.06[民90.06] |
頁 次 | 頁59-67 |
分類號 | 418.1 |
關鍵詞 | 藥物動力學; 葡萄柚汁; Pharmacokinetics; Clozapine; Grapefruit juice; |
語 文 | 中文(Chinese) |
中文摘要 | 目的:本研究欲探討服用葡萄柚汁對於clozapine代謝的影響。葡萄柚汁會抑制細胞色素P450 3A4 (CYP3A4)的活性,而其對於CYP1A2的作用則尚無定論;clozapine則是這兩種isozymes-CYP3A4和CYP1A2的受質。過去文獻上指出單一劑量的葡萄柚汁即會改變單一劑量CYP3A4受質的藥物動力學,故本研究欲探討單一劑量的葡萄柚汁,對於單一劑量的clozapine和其兩個主要代謝物norclozapine及clozapine N-oxide在藥物動力學上的影響。方法:6位精神分裂症男性住院病患以隨機交叉試驗(相隔兩週)接受250毫升的水或一般強度 (regular-strength) 葡萄汁,併用50毫克的clozapine。以高效液相層析法 (HPLC) 在0.5、1、1.5、2、2.5、3、4、5、6、8、10、12、24、36、48小時後檢測clozapine及其主要代謝物norclozapine和clozapine N-oxide的血漿濃度,並且比較它們藥物動力學各項參數的變化。結果:單一劑量葡萄柚汁或水,併用單一劑量clozapine時,clozapine及其主要代謝物,在藥物動力學的指標上如達鋒時間 (Tmax)、尖峰藥物濃度 (Cmax)、血漿濃度-時間曲線下面積 (AUC) 等結果相類似。結論:單一劑量的葡萄柚汁對單一劑量的clozapine的代謝並無影響。原因之一是葡萄柚汁可能只抑制了腸道CYP3A的活性,而另一解釋是clozapine的代謝涉及了多種酵素,非僅限於CYP3A。 |
英文摘要 | Objective: Grapefruit juice increases the bioavailability of several drugs metabolized by CYP3A4, however, its effect on CYP1A2 remains controversial. Since clozapine is the substrate for both of these isozymes, this study was designed to investigate the pharmacokinetic impact of single-dose clozapine, taken with 250 ml of either grapefruit juice or water as control, with respect to its two main metabolites, norclozapine and clozapine N-oxide. Methods: In a randomized crossover trial, six male schizophrenic inpatients received a single 50-mg dose of clozapine, taken with 250 ml of either water or regular-strength grapefruit juice. Plasma concentrations for clozapine and its two metabolites, norclozapine and clozapine N-oxide, as well as a number of other parameters, were measured over 48 hours post dose by HPLC/UV. The pharmacokinetics of clozapine and the two metabolites were compared for the two treatments using paired t-test. Results: No statistically significant difference for pharmacokinetic interactions was observed comparing single-dose clozapine taken either with grapefruit juice or water. Results for pharmacokinetic parameters for clozapine and its metabolites, including Tmax、Cmax、and AUC, were similar comparing the two treatments. Conclusion: No statistically verifiable effects were demonstrated for grapefruit juice on the principal markers of clozapine metabolism. One of the possible reasons for this lack of effect may simply be that grapefruit juice's inhibition of CYP3A activity is restricted to the gut, and does not affect metabolism occurring in the liver. Another possible explanation is that multiple enzymes are involved in clozapine metabolism. |
本系統中英文摘要資訊取自各篇刊載內容。