Pharmacokinetic and Metabolic Studies with Ornidazole in Man. Comparison with Metronidazole
Ornidazole *) (1) is a new compound belonging to the group of the 5-nitro-imidazoles (Fig. 1). It showed marked antiprotozoal activity in vitro and in laboratory animals (2, 3). This activity was further confirmed by clinical studies in patients with intestinal and liver amoebiasis (4, 5, 6), lambliasis (7) and vaginal trichomoniasis (8,9). The compound has no basic nor acidic properties, however, due to its secondary alcohol group it is fairly soluble in water. Remarkable also is its high solubility in ether and chloroform which in turn allows us to anticipate a good solubility in lipids. Our aim was to compare the pharmacokinetics and the metabolism of ornidazole to that of metronidazole (FLAGYL) in man (10). For this purpose both drugs were labelled with 14C in position 2 of the imidazole ring. They were administered orally at a dose of 750 mg and at an interval of 2 to 4 weeks to the same 4 adult volunteers. Additional pharmacokinetic studies of ornidazole with single high doses of the drug were carried out with cold material.
KeywordsChloroform CHCl3 Malaria Metronidazole Trop
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