Single dose pharmacokinetics of atenolol (AT) enantiomers was studied in human volunteers and in rats. After oral administration of 50 mg of racemic AT to humans, the areas under the plasma concentration-time curves (AUCs; mean +/- SD) were 1640 +/- 602 and 1860 +/- 652 (ng/mL)h for the S(-)- and R(+)-enantiomers, respectively (p less than 0.05). The small difference in the AUC was a reflection of a slight, but statistically significant (p less than 0.05) difference in the renal clearance (CLr, mL/min) of the enantiomers [129 +/- 32, S(-)-AT; 120 +/- 29, R(+)-AT]. However, the two enantiomers were not different from each other (p greater than 0.05) with respect to the volume of distribution (V lambda, L/kg) [0.879 +/- 0.342, S(-)-AT; 0.790 +/- 0.255, R(+)-AT] or the terminal elimination rate constant (lambda z, h-1) [0.113 +/- 0.038, S(-)-AT; 0.114 +/- 0.036, R(+)-AT]. After iv administration of 10 mg/kg of the racemic AT to rats, the R(+)-enantiomer achieved higher AUC values [(ng/mL)h] compared with its antipode (p less than 0.05) [3630 +/- 1040, S(-)-AT; 4020 +/- 1080, R(+)-AT]. Similar to the human results, this difference was due to a stereoselective renal clearance (mL/min/kg) in favor of S(-)-AT [14.9 +/- 5.78, S(-)-AT; 13.0 +/- 4.88, R(+)-AT; p less than 0.05].(ABSTRACT TRUNCATED AT 250 WORDS)