@article{oai:kanazawa-u.repo.nii.ac.jp:00014800,
 author = {石崎, 純子 and 下村, 祥子 and 福和, 千恵 and 嶋田, 努 and 横川, 弘一 and 宮本, 謙一},
 issue = {6},
 journal = {医療薬学},
 month = {Jun},
 note = {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, 金沢大学大学院自然科学研究科分子作用学, 金沢大学医学部附属病院薬剤部, 金沢大学大学院医学系研究科},
 pages = {445--450},
 title = {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},
 volume = {31},
 year = {2005}
}