Macroautoradiographic study of the distribution and excretion of 14C-pentobarbitone in rats pretreated with phenobarbitone.

The distribution and excretion of pentobarbitone were studied, using macroautoradiography, in two groups of rats at times ranging from 1 min to 70 min after the i.v. injection of 100 muCi given as 30 mg/kg of 14C-pentobarbitone. In a control group, the carbon-14 concentration (concentration of pentobarbitone) in the brain remained always greater than that in heart blood (unchanged pentobarbitone and metabolites). In a group subjected to enzyme induction (pretreated with phenobarbitone), however, the carbon-14 concentration in the brain exceeded that in the heart blood initially and then decreased rapidly. In the induced group, the carbon-14 concentration in the urine and small intestine (almost all of which was metabolites) increased with time. In particular, 70 min after the injection, the carbon-14 concentration in the small intestine of the induction group was twice that of the control group. It was concluded that in the induction group the rapid decrease in carbon-14 concentration in the brain was mainly a result of an increase in the metabolic breakdown of pentobarbitone in the liver.