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タイトル: 局所麻酔薬ropivacaineのα_1-酸性糖タンパク結合動態と薬物間相互作用の検討
その他のタイトル: Binding Disposition of Local Anesthetic Ropivacaine to α_1-acid Glycoprotein and Interactions with Co-administered Drugs
著者: 石崎, 純子 link image link image
下村, 祥子
福和, 千恵
嶋田, 努
横川, 弘一
宮本, 謙一
Ishizaki, Junko
Shimamura, Shoko
Fukuwa, Chie
Shimada, Tsutomu
Yokogawa, Koichi
Miyamoto, Kenichi
発行日: 2005年 6月 1日
出版社(者): 日本医療薬学会
引用: 医療薬学 31(6), pp.445-450
雑誌名: 医療薬学
ISSN: 1346-342X
巻: 31
号: 6
開始ページ: 445
終了ページ: 450
キーワード: ropivacaine α_1-acid glycoprotein protein binding drug interaction
抄録: We examined the influence of basic drugs and protein variants on the binding disposition of ropivacaine to α_1-acid glycoprotein (AGP). On doing this, we found the values of the competitive inhibition constant (K_i) for dipyridamole, verapamil, lidocaine and disopyramide with respect to the binding of ropivacaine to commercial AGP (70mg/dL) to be 2.1, 5.2, 6.0 and 11.0μM, respectively. Also, there was a strong correlation between the f_u value and the AGP concentration when ropivacaine was added to plasma samples from ten healthy volunteers (r=0.861). Among the volunteers, eight showed F_1S variants and two showed F_1 variants without the S variant of AGP. There was no difference in the f_u value of ropivacaine between these two groups. However, when ropivacaine was added together with dipyridamole, the f_u values of ropivacaine in plasma from volunteers with F_1S variants were clearly higher than those from volunteers without the S variant. When ropivacaine was added together with disopyramide or lidocaine, however, there was no difference in f_u values between these variants. Our results indicate that variability in the effectiveness and/or adverse effects of ropivacaine are caused by changes in f_u as a consequence of changes in AGP concentration. They also suggest that in combination therapy, it is also important to consider the AGP variant-dependence of the inhibitory effect of concomitantly administered drugs
URI: http://hdl.handle.net/2297/6253
資料種別: Journal Article
版表示: publisher

このアイテムを引用あるいはリンクする場合は次の識別子を使用してください。 http://hdl.handle.net/2297/6253



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