TY - JOUR
T1 - Pharmacokinetics of Disopyramide in Japanese Subjects
AU - Kusuoka, Hideo
AU - Inoue, Michitoshi
AU - Hori, Masatsugu
AU - Takeda, Hiroshi
AU - Abe, Hiroshi
AU - Kajiya, Fumihiko
PY - 1980
Y1 - 1980
N2 - 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 elimination 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 disopyramide (free base). These results showed that the pharmacokinetics of disopyramide 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.
AB - 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 elimination 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 disopyramide (free base). These results showed that the pharmacokinetics of disopyramide 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.
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U2 - 10.3999/jscpt.11.49
DO - 10.3999/jscpt.11.49
M3 - Article
AN - SCOPUS:85008028691
SN - 0388-1601
VL - 11
SP - 49
EP - 57
JO - Rinsho yakuri/Japanese Journal of Clinical Pharmacology and Therapeutics
JF - Rinsho yakuri/Japanese Journal of Clinical Pharmacology and Therapeutics
IS - 1
ER -