Pharmacokinetics and biotransformation of the anxiolytic abecarnil in healthy volunteers.
1. The pharmacokinetics of abecarnil were studied in eight healthy male volunteers using 14C-abecarnil and an h.p.l.c. method for determination of unchanged drug. 2. Abecarnil was rapidly and nearly completely absorbed after an oral dose of 10 mg; bioavailability was 40%. Plasma levels of the unchanged drug declined with a terminal half-life of 4 h. The total clearance of abecarnil was 11 ml/min per kg. 14C-Abecarnil was excreted rapidly and completely. The main route of elimination was in the faeces. 3. Abecarnil was extensively metabolized resulting in ether cleavage at position 6 with subsequent glucuronidation or sulphation and, to a minor extent, in ester cleavage.
Krause
W
W
Research Laboratories of Schering AG, Berlin, Germany.
Duka
T
T
Matthes
H
H
D000284:Administration, Oral; D014151:Anti-Anxiety Agents / Q000378:metabolism*; D001711:Biotransformation; D002243:Carbolines / Q000008:administration & dosage / Q000378:metabolism* / Q000493:pharmacokinetics; D002250:Carbon Radioisotopes; D005243:Feces / Q000737:chemistry; D006207:Half-Life; D006801:Humans; D007275:Injections, Intravenous; D007408:Intestinal Absorption; D008297:Male; D008657:Metabolic Clearance Rate; D008875:Middle Aged; D011865:Radioisotope Dilution Technique
D014151:Anti-Anxiety Agents; D002243:Carbolines; D002250:Carbon Radioisotopes; C062769:abecarnil