[Pharmacokinetics of DL-norephedrine 14C in the rat]

After i.v. administration of DL-norephedrine 14C to the rat (535 mug/kg), approximately 75% of the radioactivity was eliminated during the first 18 hr in the urine. Beside the unchanged drug (71.5% of the total urinary radioactivity), the main metabolite was alpha-methyloctopamine (18%), a parahydroxylated derivative of which 68% were excreted as glucuronide conjugates. Kinetic studies of DL-norephedrine in different organs showed that the affinity of tissues for the amine did not change with time. Captation was important and rapid in lungs, adrenals, spleen and heart. The brain was marked by a slow increase of drug level during the first 2 hr. However, the terminal semi-exponential kinetic slopes of DL-norephedrine concentration showed that the elimination processes of the drug were the same in each tissue. The affinity of tissues for alpha-methyloctopamine was shown to be much more specific; its uptake was higher in organs which are rich in adrenergic nerve endings (heart, adrenals and spleen). These results confirm the role of this hydroxylated amine as a false neurotransmitter. A whole body autoradiography in the mouse showed an important uptake of DL-norephedrine 14C in salivary glands and periocular structures.