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Chemical Compound Review

Tiberal     1-chloro-3-(2-methyl-5-nitro- imidazol-1...

Synonyms: Madelen, Ornidazol, Ornidazole, Ornidazolum, Prestwick_584, ...
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Disease relevance of Ornidazole


High impact information on Ornidazole


Chemical compound and disease context of Ornidazole


Biological context of Ornidazole

  • Pharmacokinetics of ornidazole in patients with severe liver cirrhosis [3].
  • Restoration of fertility and normal sperm motility and velocity were observed in the group of recovery rats assessed 2 weeks after the cessation of ornidazole treatment [14].
  • The effects of the male antifertility agent ornidazole on glycolysis as a prerequisite for fertilization were investigated in rats [13].
  • DJ-1 was identified as an activated ras-dependent oncogene product, and was also found to be an infertility-related protein (contraception-associated protein 1; CAP 1) that was reduced in rat spermatozoa treated with ornidazole, one of the endocrine disrupting substances that causes reversible infertility in rats [15].
  • Male rats were treated for 61 days prior to mating and female rats were treated for 2 weeks prior to mating and throughout gestation and lactation at doses of 0 (control), 25, 100, and 400 mg of ornidazole/kg/day [16].

Anatomical context of Ornidazole


Associations of Ornidazole with other chemical compounds


Gene context of Ornidazole

  • Epididymal fluid from rats rendered infertile by oral administration of ornidazole contains a protein CAP1 (contraception-associated protein 1) that is absent from epididymal fluid, but present on epididymal sperm, from fertile vehicle-treated rats [22].
  • DJ-1 was first identified as an activated ras-dependent oncogene product and was later also found to be an infertility-related protein affected by sperm toxicants such as ornidazole (OR) and epichlorohydrin [23].
  • Flow cytometric analysis of sperm from ornidazole-fed rats revealed a significant decline (of 22%-24%) in the amount of sperm surface CAP1 compared with controls, which is associated with an altered location on the sperm head [24].
  • OBJECTIVE: To review the literature on novel immunomodulators such as tumor necrosis factor alpha (TNF-alpha)- and interleukin (IL)-related agents, 6-thioguanine (6-TG), tacrolimus, and leflunomide, and antibiotics such as ornidazole, rifaximin, and ciprofloxacin for the treatment of Crohn's disease [25].
  • Mean-maximal (15 min) and last-determined (24 h) ornidazole levels in serum were 24 +/- 5.2 and 6.3 +/- 1.4 mg/liter, respectively. beta-Phase elimination half-life was 14.1 +/- 2.7 h, and clearance and apparent volume of distribution were 47 +/- 12 ml/min and 0.9 +/- 0.13 liters/kg, respectively [9].

Analytical, diagnostic and therapeutic context of Ornidazole

  • Plasma concentrations of ornidazole and its two major hydroxylated metabolites, M1 [alpha-(chloromethyl)-2-hydroxymethyl-5-nitroimidazole-1-ethanol] and M4 [3-(2-methyl-5-nitroimidazole 1-yl)-1,2-propane diol] were measured by HPLC assay [4].
  • During the operation the concentration in serum was 7.90 +/- 0.57 microgram/ml, and in appendix tissue, 5.26 +/- 0.60 microgram/g. In the series of 200 patients undergoing appendectomy, six patients treated with ornidazole and 12 patients treated with placebo developed a wound infection [17].
  • Ceftriaxone and ornidazole concentrations were determined by high-performance liquid chromatography [7].
  • Concentrations in serum and tissue were determined after intravenous infusion of 500 mg of ornidazole 15 min prior to appendectomy [17].
  • Plasma and epiploic fat drug concentrations and fat penetration of ceftriaxone and ornidazole given for antimicrobial prophylaxis were studied in 11 patients scheduled for liver transplantation [7].


  1. Ornidazole for prophylaxis of postoperative Crohn's disease recurrence: a randomized, double-blind, placebo-controlled trial. Rutgeerts, P., Van Assche, G., Vermeire, S., D'Haens, G., Baert, F., Noman, M., Aerden, I., De Hertogh, G., Geboes, K., Hiele, M., D'Hoore, A., Penninckx, F. Gastroenterology (2005) [Pubmed]
  2. Single-dose treatment of giardiasis with ornidazole in children. Werkman, H.P., Meuwissen, J.H. Lancet (1979) [Pubmed]
  3. Pharmacokinetics of ornidazole in patients with severe liver cirrhosis. Taburet, A.M., Delion, F., Attali, P., Thebault, J.J., Singlas, E. Clin. Pharmacol. Ther. (1986) [Pubmed]
  4. Pharmacokinetics of ornidazole in patients with acute viral hepatitis, alcoholic cirrhosis, and extrahepatic cholestasis. Taburet, A.M., Attali, P., Bourget, P., Etienne, J.P., Singlas, E. Clin. Pharmacol. Ther. (1989) [Pubmed]
  5. Treatment of giardiasis: comparative evaluation of ornidazole and tinidazole as a single oral dose. Jokipii, L., Jokipii, A.M. Gastroenterology (1982) [Pubmed]
  6. Investigation of the potential role of Enterococcus faecalis in the pathophysiology of experimental peritonitis. Montravers, P., Andremont, A., Massias, L., Carbon, C. J. Infect. Dis. (1994) [Pubmed]
  7. Concentrations in plasma and tissue penetration of ceftriaxone and ornidazole during liver transplantation. Steib, A., Jacoberger, B., Von Bandel, M., Beck, F., Beller, J.P., Boudjema, K., Koffel, J.C., Otteni, J.C. Antimicrob. Agents Chemother. (1993) [Pubmed]
  8. Pharmacokinetics and protein binding of ceftriaxone during pregnancy. Bourget, P., Fernandez, H., Quinquis, V., Delouis, C. Antimicrob. Agents Chemother. (1993) [Pubmed]
  9. Pharmacokinetics and tissue penetration of a single dose of ornidazole (1,000 milligrams intravenously) for antibiotic prophylaxis in colorectal surgery. Martin, C., Bruguerolle, B., Mallet, M.N., Condomines, M., Sastre, B., Gouin, F. Antimicrob. Agents Chemother. (1990) [Pubmed]
  10. Effect of ornidazole and clarithromycin resistance on eradication of Helicobacter pylori in peptic ulcer disease. Lehmann, F.S., Drewe, J., Terracciano, L., Beglinger, C. Aliment. Pharmacol. Ther. (2000) [Pubmed]
  11. Shedding of a rat epididymal sperm protein associated with infertility induced by ornidazole and alpha-chlorohydrin. Wagenfeld, A., Yeung, C.H., Strupat, K., Cooper, T.G. Biol. Reprod. (1998) [Pubmed]
  12. A comparison of the in vitro activity of rosamicin, erythromycin, clindamycin, metroidazole and ornidazole against Haemophilus ducreyi, including beta-lactamase producing strains. Feltham, S., Ronald, A.R., Albritton, W.L. J. Antimicrob. Chemother. (1979) [Pubmed]
  13. Effect of ornidazole on fertility of male rats: inhibition of a glycolysis-related motility pattern and zona binding required for fertilization in vitro. Bone, W., Jones, N.G., Kamp, G., Yeung, C.H., Cooper, T.G. J. Reprod. Fertil. (2000) [Pubmed]
  14. The effect of ornidazole on fertility and epididymal sperm function in rats. McClain, R.M., Downing, J.C. Toxicol. Appl. Pharmacol. (1988) [Pubmed]
  15. Immunocytochemical localization of DJ-1 in human male reproductive tissue. Yoshida, K., Sato, Y., Yoshiike, M., Nozawa, S., Ariga, H., Iwamoto, T. Mol. Reprod. Dev. (2003) [Pubmed]
  16. Reproduction studies in rats treated with ornidazole. McClain, R.M., Downing, J.C. Toxicol. Appl. Pharmacol. (1988) [Pubmed]
  17. Ornidazole and anaerobic bacteria: in vitro sensitivity and effects on wound infections after appendectomy. Palmu, A., Renkonen, O.V., Aromaa, U. J. Infect. Dis. (1979) [Pubmed]
  18. The in vitro effect of some nitroimidazoles on microtubule formation. Bendahmane, M., Chauvet Monges, A.M., Braguer, D., Peyrot, V., Crevat, A. Biochem. Pharmacol. (1984) [Pubmed]
  19. Influence of oral administration of ornidazole on capacitation and the activity of some glycolytic enzymes of rat spermatozoa. Oberländer, G., Yeung, C.H., Cooper, T.G. J. Reprod. Fertil. (1996) [Pubmed]
  20. In vivo evaluation of guar gum-based colon-targeted drug delivery systems of ornidazole in healthy human volunteers. Krishnaiah, Y.S., Indira Muzib, Y., Bhaskar, P. Journal of drug targeting. (2003) [Pubmed]
  21. Typhoid enteric perforation. Akgun, Y., Bac, B., Boylu, S., Aban, N., Tacyildiz, I. The British journal of surgery. (1995) [Pubmed]
  22. Molecular cloning and expression of rat contraception associated protein 1 (CAP1), a protein putatively involved in fertilization. Wagenfeld, A., Gromoll, J., Cooper, T.G. Biochem. Biophys. Res. Commun. (1998) [Pubmed]
  23. DJ-1, a target protein for an endocrine disrupter, participates in the fertilization in mice. Okada, M., Matsumoto, K., Niki, T., Taira, T., Iguchi-Ariga, S.M., Ariga, H. Biol. Pharm. Bull. (2002) [Pubmed]
  24. Expression and cellular localization of contraception-associated protein. Wagenfeld, A., Yeung, C.H., Shivaji, S., Sundareswaran, V.R., Ariga, H., Cooper, T.G. J. Androl. (2000) [Pubmed]
  25. Novel therapies for Crohn's disease: focus on immunomodulators and antibiotics. Wilhelm, S.M., Taylor, J.D., Osiecki, L.L., Kale-Pradhan, P.B. The Annals of pharmacotherapy. (2006) [Pubmed]
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