Pharmacokinetics of Disopyramide in Japanese Subjects

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The pharmacokinetics of disopyramide and its effects on the electrocardiogram were studied in five healthy male volunteers after intravenous (50 mg) and oral (200 mg) administration. The apparent half-times of the distribution phase and elimination phase after intravenous administration were 3.78 min and 4.75 hr, respectively. The apparent volume of distribution for the central compartment was 11.95 liters with an eli-mination rate of 0.575 hr-1. These pharmacokinetic parameters in intravenous administration were compatible with previous reports which had been obtained using a pharmacokinetic model with a 2-compartmental system, but they were far from the results previously obtained using a single-compartmental system. The peak-time and peak-concentration after oral administration were 2.67 hr and 1.11% dose/liter, respectively, with the bioavailability calculated at 0.67. These values also agreed with previous reports of the pharmacokinetics of diso-pyramide (free base). These results showed that the pharmacokinetics of diso-pyramide in Japanese subjects was not different from that previously reported with subjects in other countries. In these administrations no significant change was observed in the heart rate, the P-R interval, the duration of QRS complex, and the Q-T corrected interval of electrocardiogram. However, a small but significant change in the shape of the T-wave developed in right precordial leads in all series during the phase of high drug concentration in plasma.
一般社団法人日本臨床薬理学会の論文

Pharmacokinetics of Disopyramide in Japanese Subjects

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