Reference

Pharmacokinetic and metabolic studies with ornidazole in man

Pharmacokinetic and metabolic studies with ornidazole in man. Comparison with metronidazole. Schwartz, D. E.; Jeunet, F. (Dep. Exp. Med., F. Hoffmann-La Roche und Co. Ltd., Basel, Switz.). Chemother., Proc. Int. Congr. Chemother., 9th, Meeting Date 1975, Volume 6, 49-59. Edited by: Williams, John David; Geddes, Alexander M. Plenum: New York, N. Y. (English) 1976. 62580-80-7 and 62580-79-4 which are cas registry numbers are also used here. CODEN: 35DFA6. DOCUMENT TYPE: Conference CA Section: 1 (Pharmacodynamics) The pharmacokinetics and the metab. of 2-14C-labeled ornidazole (I) [16773-42-5] and metronidazole [443-48-1] have been compared in human subjects. I reached peak concn. in the plasma 2 to 3 h after administration (metronidazole 1/2 to 1 h). I was eliminated from plasma with a mean half-life of 14.4 h (metronidazole 8.4 h). I excreted unaltered in the urine amounted to 4% of the dose (metronidazole 7.7%). The bioavailability of I tested in two dogs amounted to 94 and 99% resp. In man, unaltered I and 6 radioactive metabolites were detected in free form as well as conjugated in the urine. Two of these could be identified to the 2-oxymethyl- [62580-79-4] and .alpha.-oxymethyl- [62580-80-7] derivs. They were less active against Trichomonas vaginalis than the parent compd. Small amts. of I could be detected in the faeces of man. Vaginal administration of I will ensure high initial concn. of the drug in this organ. Subsequently, as it gradually reaches the circulatory system, it will sustain the plasma levels and consequently also prolong the time during which it will flow back into the vagina. .

Electron-capture gas chromatographic assays of 5-nitroimidazole class of antimicrobials in blood

Electron-capture gas chromatographic assays of 5-nitroimidazole class of antimicrobials in blood. Bhatia, S. C.; Shanbhag, V. D. (Res. Cent.Chemicals with cas numbers 89422-94-6 and 3366-95-8 also play role., Hindustan Ciba-Geigy Ltd., Bombay 400 063, India). J. Chromatogr., 305(2), 325-34 (English) 1984. CODEN: JOCRAM. ISSN: 0021-9673. DOCUMENT TYPE: Journal CA Section: 1 (Pharmacology) Sensitive and selective electron-capture gas chromatog. methods for the detn. of N-1-substituted 5-nitroimidazole (I; R1 = Me, chlorinated or hydroxylated alkyl, SO2-contg. alkyl; R2 = Me or heterocycle) antiprotozoals in blood are described. Metronidazole [443-48-1], secnidazole [3366-95-8] and ornidazole [16773-42-5] having a hydroxyl function in the N-1 substitution, were converted to their resp. trimethylsiiyl derivs. before chromatog. on an OV-11 column. Tinidazole [19387-91-8] and satranidazole (II) [56302-13-7], devoid of the hydroxy group but contg. a sulfur atom in the mol., were chromatographed as such on the same stationary phase. Blood levels as low as 50 ng/mL for all the 5-nitroimidazoles have been measured with good precision. The method can be readily utilized for pharmacokinetic studies. .