カルシウム拮抗薬のもつ局所麻酔様作用

概要

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The local anesthetic effects of calcium antagonists (diltiazem, verapamil, and nicardipine) on extracted rabbit vagus nerve (Fig. 1) and their binding ability to the phospholipid membrane model were examined by ^1H-NMR spectroscopy. Effective concentrations of these drugs for vagus nerve blockage were examined with 12〜14V electrical stimuli. The minimum effective concentration of calcium antagonist which completely blocked the compound action potential was 0.5mM for diltiazem, and 0.2mM for verapamil. Nicardipine did not show any conduction blocking effect at 1.0mM. Local anesthetic effects of ditiazem and verapamil were characterized by a slower onset (over 20 min) and longer duration (over 30 min) compared with lidocaine (Table 1). The local anesthetic effects of dilitiazem and verapamil may be due to the SA and AV nodal blocking effect and reductions in the ventricular rate by these drugs. However, in the SA and AV nodes, depolarization is largely dependent on the movement of Ca^<2+> through the slow channel. The results of ^1H-NMR spectroscopy indicated that poor electrostatic binding with the phospholipid membrane occured only with diltiazem (Fig. 2). Local anesthetic effects of calcium antagonists may not be based on electrostatic binding with the nerve membrane as in the case of local anesthetics.
北海道医療大学の論文
1999-06-30