[Pharmacokinetics of the trichomonacidal agent ZK 25 095 in 6 normal subjects following intravenous and oral administration (author's transl)].
The distribution, absorption and elimination of 5-morpholinomethyl-3-(5-nitro-1-methyl-2-imidazolyl-methylene-amino)-2-oxazolidinone-hydrochloride (test designation ZK 25 095), which proved to be an effective trichomonacidal agent in animal and clinical trials, was determined microbiologically and with the aid of 14C-labelled substance. After i.v. injection of 10 mg ZK 25095 in each of two volunteers the substance was distributed between blood and body tissues within approximately 10 min. The calculated volume of distribution amounted to 70% of the body volume. After oral administration of 250 mg in tablet form to each of three volunteers the substance was almost completely absorbed within a few hours. The maximum blood level was reached 3 to 4 h after administration. It amounted to about 80% of the blood levels (distribution equilibrium) after i.v. administration. ZK 25 095 was eliminated from the body with a half-life of approximately 9 h. 3/4 of the elimination were effected via urine and 1/4 via the faeces. 30-50% of the radioactivity eliminated with urine originated from microbiologically active (trichomonacidal) substance.
D000284:Administration, Oral; D000328:Adult; D000994:Antitrichomonal Agents / Q000008:administration & dosage / Q000032:analysis / Q000378:metabolism*; D001412:Bacillus subtilis; D001681:Biological Assay; D002855:Chromatography, Thin Layer; D006801:Humans; D007275:Injections, Intravenous; D007700:Kinetics; D008297:Male; D008875:Middle Aged; D009593:Nitroimidazoles / Q000008:administration & dosage / Q000032:analysis / Q000378:metabolism*; D023303:Oxazolidinones
D000994:Antitrichomonal Agents; D009593:Nitroimidazoles; D023303:Oxazolidinones; C013139:moxnidazole
Pharmakokinetik des Trichomonazidums ZK 25 095 bei 6 gesunden Probanden nach intravenöser und oraler Applikation