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

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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
日本医療薬学会の論文
2005-06-10

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

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