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翻訳と辞書　辞書検索 [ 開発暫定版 ] スポンサード リンク Perhexiline ： ウィキペディア英語版 Perhexiline Perhexiline ''(Pexsig)'' is a prophylactic antianginal agent used primarily in Australia and New Zealand. Perhexiline is thought to act by inhibiting mitochondrial carnitine palmitoyltransferase-1. This shifts myocardial metabolism from fatty acid to glucose utilisation which results in increased ATP production for the same O2 consumption and consequently increases myocardial efficiency. Its clinical use has been limited by its narrow therapeutic index and high inter- and intra-individual pharmacokinetic variability. It was outlawed in many countries due to its adverse effects on poor metabolisers (PM). The product has been reintroduced for patients who have contraindications, or have not responded to other treatments for angina. ==Perhexiline metabolism== The major route of perhexiline metabolism in humans is hydroxylation by microsomal CYP2D6.〔Sørensen, L. B., Sørensen, R. N., Miners, J. O., ''et al.'', Polymorphic hydroxylation of perhexiline ''in vitro''. ''British Journal of Clinical Pharmacology''. 55:635–8, (2003).〕 The two main metabolites of perhexiline are the cis and trans isomers of hydroxyperhexiline.〔 CYP2D6 accounts for only a small percentage of total hepatic CYP450s but it is one of the main pathways for phase one metabolism of xenobiotics.〔Zanger, U.M., Raimundo, S., Eichelbaum, M., Cytochrome P450 2D6: overview and update on pharmacology, genetics, biochemistry. ''Naunyn-Schmiedeberg's Archives of Pharmacology''. 369: 23–37, (2003).〕 The limited availability of CYP2D6 means perhexiline metabolism is a saturable process.〔Morris, R.G., Sallustio, B.C., Saccoia, N.C., ''et al.'' Application of an improved HPLC perhexiline assay to human plasma specimens. ''Journal of Liquid Chromatography''.15:3219–32, (1992).〕 抄文引用元・出典: フリー百科事典『 ウィキペディア（Wikipedia）』 ■ウィキペディアで「Perhexiline」の詳細全文を読む スポンサード リンク 翻訳と辞書 : 翻訳のためのインターネットリソース Copyright(C) kotoba.ne.jp 1997-2016. All Rights Reserved.