Clinical pharmacology of dilevalol (i.v.). Influence of hepatic and renal functions on the disposition of dilevalol and atenolol in hypertensive subjects

Dilevalol (100 mg) or atenolol (50 mg) was given orally in 13 subjects with essential hypertension. Two trials were done by a single-blind, crossover design with an interval of 6 days. Blood samples for drug concentrations were taken for a period of 24 hours after dosage. A retained percentage of indocyanine green dye at 15 minute (ICG R15) reflecting hepatic function and a creatinine clearance (CLCR) reflecting renal function were determined in each subject during observation period. A significant correlation was observed between the ICG R15 and the area under the plasma concentration-time curve (AUC) of dilevalol, while there was no significant correlation between the CLCR and any pharmacokinetic parameter of the agent. In contrast to dilevalol, significant correlations were observed between the CLCR and AUC or elimination half-life of atenolol. However, there was no significant correlation between the ICG R15 and any pharmacokinetic parameter of atenolol. These data indicate that the disposition of dilevalol is influenced by hepatic rather than by renal function while that of atenolol is altered by renal function.