Abstract The metabolism of tocainide, an experimental antiarrhythmic drug, was studied in humans. Urinary excretion of unchanged drug was 28-55% in 24 hr after oral dosing. Urine hydrolysis with hydrochloric acid or β-glucuronidase increased tocainide recovery to 55- 79%. Saccharo-1, 4-lactone inhibited the β-glucuronidase-mediated tocainide recovery increase. Adjustment of urine to pH 13 produced a compound identified as 3-(2, 6-xylyl)-5- ...
