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.
