Pharmacokinetic and Metabolic Studies with Ornidazole in Man. Comparison with Metronidazole

  • D. E. Schwartz
  • F. Jeunet
Part of the Chemotherapy book series (CT, volume 6)


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.


Minimum Inhibitory Concentration Metabolic Study Total Radioactivity Unchanged Drug Entamoeba Histolytica 
These keywords were added by machine and not by the authors. This process is experimental and the keywords may be updated as the learning algorithm improves.


Unable to display preview. Download preview PDF.

Unable to display preview. Download preview PDF.


  1. (1).
    Hoffer, M. and Grunberg, E.: Synthesis and antiprotozoal activity of l-(3-Chloro-2-hydroxypropyl)-substituted nitroimidazoles. J. Med. Chem. 17: 1019–1020 (1974).PubMedCrossRefGoogle Scholar
  2. (2).
    Fernex, M., Jeunet, P. and Richie, R.: Development of a nitro-imidazole derivative (Ro 7–0207) for the treatment of amoebiasis, lambliasis and trichomoniasis. 8th Int. Congr. Chemotherapy, Athens, September 1975.Google Scholar
  3. (3).
    Richie, R. and Surbek, B.: Entwicklung neuer Nitroimidazol-Deri-vate als Protozoenmittel. Kongr. Deutschsprachiger Tropenmed. Ges., Montreux, Juni 1972.Google Scholar
  4. (4).
    Kee-Mok Cho, Hai-Young Cha and Chin-Thack Soh: Clinical trials of Ro 7–0207 against Entamoeba histolytica infections (Double blind trials versus metronidazole). Yonsei Rep. Trop. Med. 3: 123–133 (1972).Google Scholar
  5. (5).
    Powell, S.J. and Elsdon-Dew, R.: Some new nitroimidazole derivatives. Clinical trials in amoebic liver abscess. Amer. J. trop. Med. Hyg. 21: 518–520 (1972).Google Scholar
  6. (6).
    Ruas, A., Ramalho Correia, M.H., Correia do Valle, J. and Ataide Ribeiro, J.: Ro 7–0207 in amoebic liver abscess. Comparative study of the effects of Ro 7–0207 and metronidazole. Centr. Afr. J. Med. 19: 128–132 (1973).Google Scholar
  7. (7).
    Wolfensberger, H.R.: Results of double-blind comparative trials in amoebiasis and giardiasis with a new nitroimidazole derivative (Ro 7–0207) versus metronidazole. 9th Int. Congr. Trop. Med. and Malaria, Athens, October 1973.Google Scholar
  8. (8).
    Lean, T.H. and Vengadasalam, D.: Treatment of vaginal trichomoniasis with a new anti-protozoal compound, α-(chloromethyl)-2-methyl-5-nitro-1-imidazole-ethanol. Brit. J. vener. Dis. 49: 69–71 (1973).Google Scholar
  9. (9).
    Sandront, M.A. and Lambotte, R.: Conception nouvelle de la thérapeutique des vaginites à trichomonas vaginalis. Traitement minute. Revue Française de Gynecologie 69: 623–625 (1974).Google Scholar
  10. (10).
    Schwartz, D.E. and Jeunet, F.: Comparative Pharmacokinetic Studies of Ornidazole and Metronidazole in Man. Submitted for publication. Chemotherapy, in press, 1976.Google Scholar

Copyright information

© Springer Science+Business Media New York 1976

Authors and Affiliations

  • D. E. Schwartz
    • 1
  • F. Jeunet
    • 1
  1. 1.F. Hoffmann-La Roche & Co. Ltd.Departments of Experimental Medicine/Clinical ResearchBasleSwitzerland

Personalised recommendations