Pharmacokinetics of the enantiomers of terbutaline after repeated oral dosing with racemic terbutaline

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Abstract
Terbutaline is a β2‐agonist and administered as the racemic mixture. The pharmacokinetics of the separate enantiomers differ with respect to degree of absorption and clearance. In the present study, repeated doses of racemic terbutaline were given to six healthy volunteers. Plasma was analyzed for the concentrations of the two enantiomers. The observed plasma concentrations at steady state differed from those predicted from the values observed after single dose administration of the separate enantiomers. The difference between the observed and predicted values can be tentatively explained by a combined influence of (−)‐terbutaline on the absorption of (+)‐terbutaline and the influence of (+)‐terbutaline on the elimination of (−)‐terbutaline. The results have implications for the interpretation of effect/concentration studies with terbutaline, but do not affect the doses used in clinical practice.