The biliary elimination of the selective beta-receptor blocking drug talinolol in man.

The biliary elimination of the beta-1-receptor blocking agent talinolol was investigated after intravenous administration of 30 mg in 6 patients with a T-tube drain after cholecystectomy. Serum concentration decreased in a biexponential manner with a median terminal half-life time of 4.4 h (range: 3.0-6.2 h). In some patients a second peak of the serum level was found. Concentration-time curves in bile paralleled serum profiles. The bile:serum concentration ratio (b:s-ratio) ranged from 24 to 98. The biliary clearance amounted to 43 ml/h.kg (range: 13-212 ml/h.kg). The median of the amount of talinolol eliminated by bile was 2.8 mg (range: 1.1-7.4 mg). It is concluded that talinolol undergoes an enterohepatic circulation. However, the amount eliminated cannot provide a sufficient explanation for the second peak, observed in some patients.