Pharmacokinetics and metabolism of taglutimide (K-2004) in the rat.

Absorption, blood level course, renal, fecal, and biliary elimination and the metabolisation of 2-(bicyclo[2,2,1]-heptane-2-endo-3-endo-dicarboximido)-glutarimide (taglutimide, K-2004), a new hypnotic-sedative substance, were studied in the rat, and the pharmacokinetic constants were calculated. After oral administration of 10 mg per animal, which corresponds to the 7- to 10-fold human dose, a fast and practically total absorption and a quick and complete excretion was observed. Within 1 h 82% of the dose given were absorbed, and 12 h after the dosing 88% had been excreted again. The elimination was effected nearly exclusively (over 95%) via the urine. Besides 10 defined metabolites only 10% of the drug appeared unchanged.