Pharmacodynamic and Pharmacokinetic Comparisons to Evaluate Bioequtvalence of Atenolol

AbstractFor some drugs, particularly chiral compounds, differential potencies of the enantiomers may lead to variable pharmacologic effects which cannot be identified just by comparing pharmacokinetics of the racemic mixture. Therefore true “bioequivalence” may be established by measuring pharmacologic response along with the pharmacokinetics. Atenolol was used as a model compound because only (S)-atenolol contributes to the β-blocking effect. Bioequivalency of atenolol, was studied in 31 healthy volunteers as a randomized, two treatment single dose crossover study. Following oral administration of Mylan (Trt A) and Reference (Trt B) atenolol tablets (100mg), 15 serial blood samples were drawn up to 24 hours, including a predose sample and plasma atenolol was analyzed by HPLC. Resting Systolic (SBP) and Diastolic (DBP) blood pressures and heart rates (HR) were measured at each blood sampling time. The Cpeak, Tpeak, AUC(0-tlast), AUC(O-inf), Kel and half-life were not statistically different and within 80%...