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Preliminary pharmacokinetics of the new antitussive compound vadocaine hydrochloride in animals.

The absorption and fate of vadocaine hydrochloride (2',4'-dimethyl-6'-methoxy-3-(2-methylpiperidyl)propionanilide+ ++ hydrochloride, OR K-242-HCl; INN: vadocaine) was studied using both unlabelled compound (rabbits, rats and dogs) and tritium-labelled compound (rats). Although vadocaine was orally absorbed in dogs, no oral absorption was found in the rabbits. The elimination of the intravenously given compound was very fast (t1/2 only about 0.6 h in the rabbits). Most of the drug was metabolized both in rats and dogs. In rats, less than 0.2% of the compound was found intact in 24-h urine. In dogs, the 24-h recovery was 1-5% of the dose. After intravenous injection to rats, 43% of the radioactivity given as tritium-labelled vadocaine was recovered in urine and 19% in faeces. After oral dosing, 37% was recovered in urine and 31% in faeces. Hence, the total 7-day recovery of the radioactivity given as tritium-labelled vadocaine was 62-68% of the dose.