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.
Terhaag
B
B
Institute of Clinical Pharmacology, Medical Academy Carl Gustav Carus, Dresden, GDR.
Gramatté
T
T
Richter
K
K
Voss
J
J
Feller
K
K
D000319:Adrenergic beta-Antagonists / Q000493:pharmacokinetics*; D000328:Adult; D000368:Aged; D001646:Bile / Q000378:metabolism*; D002851:Chromatography, High Pressure Liquid; D005260:Female; D006207:Half-Life; D006801:Humans; D008297:Male; D008875:Middle Aged; D011412:Propanolamines / Q000493:pharmacokinetics*
D000319:Adrenergic beta-Antagonists; D011412:Propanolamines; C011550:talinolol