Clinical pharmacology of dilevalol (III). A pharmacokinetic study of dilevalol in elderly subjects with essential hypertension.
Dilevalol (100 mg) was given once daily for 8 days in eight elderly subjects with essential hypertension. Blood samples for plasma dilevalol concentrations were taken during an 8-hour post-drug period following the first and eighth dosages, and the time to maximum concentration (tmax), maximum plasma concentration (Cmax), distribution half-life (t1/2 alpha), elimination half-life (t1/2 beta) and area under the plasma concentration-time curve (AUC) were determined. A wide intra-subject variability was observed in tmax during the repeated administration. A high inter-subject variability was also demonstrated in tmax, Cmax, t1/2 beta and AUC during both observation periods. No significant difference was observed, however, in these pharmacokinetic parameters between the first and eighth dosages. These data indicate that the pharmacokinetic profiles of dilevalol are not altered during 8 days of therapy in elderly subjects with essential hypertension. Since elderly subjects are potentially heterogenous in capacities for handling the drug, the observed variability in pharmacokinetic parameters may reflect the heterogeneity in the sample chosen for examination in the current study.
Fujimura
A
A
Department of Clinical Pharmacology, Medical College of Oita, Japan.
Sugimoto
K
K
Kumagai
Y
Y
Nakashima
H
H
Ebihara
A
A
D000319:Adrenergic beta-Antagonists / Q000097:blood / Q000493:pharmacokinetics* / Q000627:therapeutic use; D000368:Aged; D000369:Aged, 80 and over; D001794:Blood Pressure / Q000187:drug effects; D005260:Female; D006801:Humans; D006973:Hypertension / Q000188:drug therapy* / Q000503:physiopathology; D007700:Kinetics; D007741:Labetalol / Q000097:blood / Q000493:pharmacokinetics* / Q000627:therapeutic use; D008297:Male
D000319:Adrenergic beta-Antagonists; D007741:Labetalol