Pharmacokinetic characteristics of amiodarone in long-term oral therapy in Japanese population.
To evaluate the pharmacokinetic properties and an optimum dose schedule of amiodarone in long-term oral therapy, serum concentrations of amiodarone and its metabolite, desethylamiodarone, were monitored from 345 Japanese inpatients who received amiodarone therapy for a variety of cardiac arrhythmias. Serum amiodarone and desethylamiodarone concentrations were determined by high performance liquid chromatography system. It was observed that the amiodarone and desethylamiodarone concentrations gradually increased with time. The frequency distribution in the amiodarone clearance of 245 subjects, who received fixed maintenance amiodarone therapy for at least 6 months, was nearly a unimodal one. The variation in the ratio of desetylamiodarone to amiodarone concentration in serum was very small. Although no differences in age, dose, dose duration, amiodarone or desethyamiodarone concentration or ratio were observed between men and women: however, the mean amiodarone clearance of women was significantly higer than that of men. The laboratory data were mostly within normal values and no significant relations were observed between serum amiodarone concentration and clinical laboratory data. These results suggest that the individual variation in pharmacokinetics of amiodarone is comparatively small, which might be sufficient to decide that the maintenance dose was the same one (200 mg/d) in long-term oral amiodarone therapy.
Kashima
Asami
A
Department of Pharmaceutical Sciences, Niigata University of Pharmacy and Applied Life Sciences; Niigata 950-2081, Japan.
Funahashi
Miho
M
Fukumoto
Kyoko
K
Komamura
Kazuo
K
Kamakura
Shiro
S
Kitakaze
Masafumi
M
Ueno
Kazuyuki
K
D000284:Administration, Oral; D000638:Amiodarone / Q000008:administration & dosage / Q000097:blood / Q000493:pharmacokinetics*; D000889:Anti-Arrhythmia Agents / Q000008:administration & dosage / Q000097:blood / Q000493:pharmacokinetics*; D002851:Chromatography, High Pressure Liquid; D006207:Half-Life; D006801:Humans
D000889:Anti-Arrhythmia Agents; D000638:Amiodarone