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

フォーマット:

論文

責任表示:

石崎, 純子 ; 下村, 祥子 ; 福和, 千恵 ; 嶋田, 努 ; 横川, 弘一 ; 宮本, 謙一

言語:

日本語

出版情報:

日本医療薬学会, 2005-06-01

著者名:

石崎, 純子

下村, 祥子

福和, 千恵

嶋田, 努

横川, 弘一

宮本, 謙一

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掲載情報:

医療薬学

ISSN:

1346-342x      

巻:

31

通号:

6

開始ページ:

445

終了ページ:

450

バージョン:

publisher

概要:

金沢大学大学院自然科学研究科分子作用学<br />金沢大学医学部附属病院薬剤部<br />金沢大学大学院医学系研究科<br />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, w … e 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 続きを見る

URL:

http://hdl.handle.net/2297/6253