Table of Contents Author Guidelines Submit a Manuscript
Journal of Toxicology
Volume 2017 (2017), Article ID 6746989, 9 pages
https://doi.org/10.1155/2017/6746989
Research Article

Comparative Hepatotoxicity of Fluconazole, Ketoconazole, Itraconazole, Terbinafine, and Griseofulvin in Rats

1Department of Clinical Pharmacology, College of Health Sciences, University of Zimbabwe, Harare, Zimbabwe
2Department of Anatomy, College of Health Sciences, University of Zimbabwe, Harare, Zimbabwe

Correspondence should be addressed to Star Khoza; wz.ca.zu.hcsdem@azohks

Received 7 October 2016; Revised 19 December 2016; Accepted 18 January 2017; Published 5 February 2017

Academic Editor: Brad Upham

Copyright © 2017 Star Khoza et al. This is an open access article distributed under the Creative Commons Attribution License, which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited.

Linked References

  1. Food and Drug Administration Drug Safety Communication, FDA Limits Usage of Nizoral (ketoconazole) Oral Tablets Due to Potentially Fatal Liver Injury and Risk of Drug Interactions and Adrenal Gland Problems, FDA, Silver Spring, Md, USA, 2013, http://www.fda.gov/drugs/drugsafety/ucm362415.htm.
  2. European Medicines Agency's Committee on Medicinal Products for Human Use (EMA-CHMP), European Medicines Agency Recommends Suspension of Marketing Authorisations for Oral Ketoconazole, EMA July 2013, http://www.ema.europa.eu/ema/index.jsp?curl=pages/news_and_events/news/2013/07/news_detail_001855.jsp&mid=WC0b01ac058004d5c1.
  3. Food and Drug Administration Drug Safety Communication, FDA Advises Against Using Oral Ketoconazole in Drug Interaction Studies Due to Serious Potential Side Effects, FDA, Silver Spring, Md, USA, 2013, http://www.fda.gov/Drugs/DrugSafety/ucm371017.htm.
  4. B. Han, J. Mao, J. Y. Chien, and S. D. Hall, “Optimization of drug-drug interaction study design: comparison of minimal physiologically based pharmacokinetic models on prediction of CYP3A inhibition by ketoconazole,” Drug Metabolism and Disposition, vol. 41, no. 7, pp. 1329–1338, 2013. View at Publisher · View at Google Scholar · View at Scopus
  5. I. Fuchs, V. Hafner-Blumenstiel, C. Markert et al., “Effect of the CYP3A inhibitor ketoconazole on the PXR-mediated induction of CYP3A activity,” European Journal of Clinical Pharmacology, vol. 69, no. 3, pp. 507–513, 2013. View at Publisher · View at Google Scholar · View at Scopus
  6. Z. Yang, B. Vakkalagadda, G. Shen et al., “Inhibitory effect of ketoconazole on the pharmacokinetics of a multireceptor tyrosine kinase inhibitor BMS-690514 in healthy participants: assessing the mechanism of the interaction with physiologically-based pharmacokinetic simulations,” Journal of Clinical Pharmacology, vol. 53, no. 2, pp. 217–227, 2013. View at Publisher · View at Google Scholar · View at Scopus
  7. J. H. Lewis, H. J. Zimmerman, G. D. Benson, and K. G. Ishak, “Hepatic injury associated with ketoconazole therapy. Analysis of 33 cases,” Gastroenterology, vol. 86, no. 3, pp. 503–513, 1984. View at Google Scholar · View at Scopus
  8. B. H. C. Stricker, A. P. R. Blok, F. B. Bronkhorst, G. E. Van Parys, and V. J. Desmet, “Ketoconazole-associated hepatic injury. A clinicopathological study of 55 cases,” Journal of Hepatology, vol. 3, no. 3, pp. 399–406, 1986. View at Publisher · View at Google Scholar · View at Scopus
  9. K. N. Buchi, P. D. Gray, and K. G. Tolman, “Ketoconazole hepatotoxicity: an in vitro model,” Biochemical Pharmacology, vol. 35, no. 16, pp. 2845–2847, 1986. View at Publisher · View at Google Scholar · View at Scopus
  10. G. Lake-Bakaar, P. J. Scheuer, and D. S. Sherlock, “Hepatic reactions associated with ketoconazole in the United Kingdom,” British Medical Journal, vol. 294, no. 6569, pp. 419–422, 1987. View at Publisher · View at Google Scholar · View at Scopus
  11. R.-N. Chien, L.-J. Yang, P.-Y. Lin, and Y.-F. Liaw, “Hepatic injury during ketoconazole therapy in patients with onychomycosis: a controlled cohort study,” Hepatology, vol. 25, no. 1, pp. 103–107, 1997. View at Publisher · View at Google Scholar · View at Scopus
  12. J. Y. Yan, X. L. Nie, Q. M. Tao, S. Y. Zhan, and Y. D. Zhang, “Ketoconazole associated hepatotoxicity: a systematic review and meta-analysis,” Biomedical and Environmental Sciences, vol. 26, no. 7, pp. 605–610, 2013. View at Publisher · View at Google Scholar · View at Scopus
  13. A. Srebrnik, S. Levtov, R. Ben-Ami, and S. Brenner, “Liver failure and transplantation after itraconazole treatment for toenail onychomycosis,” Journal of the European Academy of Dermatology and Venereology, vol. 19, no. 2, pp. 205–207, 2005. View at Publisher · View at Google Scholar · View at Scopus
  14. Z. Perveze, M. W. Johnson, R. A. Rubin et al., “Terbinafine-induced hepatic failure requiring liver transplantation,” Liver Transplantation, vol. 13, no. 1, pp. 162–164, 2007. View at Publisher · View at Google Scholar · View at Scopus
  15. K. R. Reddy and E. R. Schiff, “Hepatotoxicity of antimicrobial, antifungal, and antiparasitic agents,” Gastroenterology Clinics of North America, vol. 24, no. 4, pp. 923–936, 1995. View at Google Scholar · View at Scopus
  16. R. O. Chiprut, A. Viteri, C. Jamroz, and W. P. Dyck, “Intrahepatic cholestasis after griseofulvin administration,” Gastroenterology, vol. 70, no. 6, pp. 1141–1143, 1976. View at Google Scholar · View at Scopus
  17. S. A. Linnebur and B. L. Parnes, “Pulmonary and hepatic toxicity due to nitrofurantoin and fluconazole treatment,” Annals of Pharmacotherapy, vol. 38, no. 4, pp. 612–616, 2004. View at Publisher · View at Google Scholar · View at Scopus
  18. M. Thiim and L. S. Friedman, “Hepatotoxicity of antibiotics and antifungals,” Clinics in Liver Disease, vol. 7, no. 2, pp. 381–399, 2003. View at Publisher · View at Google Scholar · View at Scopus
  19. J.-L. Wang, C.-H. Chang, Y. Young-Xu, and K. A. Chan, “Systematic review and meta-analysis of the tolerability and hepatotoxicity of antifungals in empirical and definitive therapy for invasive fungal infection,” Antimicrobial Agents and Chemotherapy, vol. 54, no. 6, pp. 2409–2419, 2010. View at Publisher · View at Google Scholar · View at Scopus
  20. C.-H. Chang, Y. Young-Xu, T. Kurth, J. E. Orav, and A. K. Chan, “The safety of oral antifungal treatments for superficial dermatophytosis and onychomycosis: a meta-analysis,” The American Journal of Medicine, vol. 120, no. 9, pp. 791–798.e3, 2007. View at Publisher · View at Google Scholar · View at Scopus
  21. L. A. García Rodrǐguez, A. Duque, J. Castellsague, S. Pérez-Gutthann, and B. H. C. Stricker, “A cohort study on the risk of acute liver injury among users of ketoconazole and other antifungal drugs,” British Journal of Clinical Pharmacology, vol. 48, no. 6, pp. 847–852, 1999. View at Publisher · View at Google Scholar · View at Scopus
  22. W.-Y. Kao, C.-W. Su, Y.-S. Huang et al., “Risk of oral antifungal agent-induced liver injury in Taiwanese,” British Journal of Clinical Pharmacology, vol. 77, no. 1, pp. 180–189, 2014. View at Publisher · View at Google Scholar · View at Scopus
  23. R. J. Rodriguez and D. Acosta Jr., “Comparison of ketoconazole- and fluconazole-induced hepatotoxicity in a primary culture system of rat hepatocytes,” Toxicology, vol. 96, no. 2, pp. 83–92, 1995. View at Publisher · View at Google Scholar · View at Scopus
  24. N. Somchit, A. R. Norshahida, A. H. Hasiah, A. Zuraini, M. R. Sulaiman, and M. M. Noordin, “Hepatotoxicity induced by antifungal drugs itraconazole and fluconazole in rats: a comparative in vivo study,” Human and Experimental Toxicology, vol. 23, no. 11, pp. 519–525, 2004. View at Publisher · View at Google Scholar · View at Scopus
  25. M. S. Zakaria, “Comparative study between Griseofulvin and Fluconazole hepatotoxic effects and the protective role of Silymarin,” El-Minia Medical Bulletin, vol. 16, no. 1, pp. 274–285, 2005. View at Google Scholar
  26. Center for Drug Evaluation and Research (CDER), Guidance for Industry Estimating the Maximum Safe Starting Dose in Initial Clinical Trials for Therapeutics in Adult Healthy Volunteer, U.S. Department of Health and Human Services Food and Drug Administration, 2005, http://www.fda.gov/downloads/Drugs/.../Guidances/UCM078932.pdf.
  27. F. Wróblewski and J. S. Ladue, “Serum glutamic pyruvic transaminase in cardiac and hepatic disease,” Proceedings of the Society for Experimental Biology and Medicine, vol. 91, no. 4, pp. 569–571, 1956. View at Publisher · View at Google Scholar · View at Scopus
  28. A. Karmen, F. Wroblewski, and J. S. Ladue, “Transaminase activity in human blood,” The Journal of clinical investigation, vol. 34, no. 1, pp. 126–131, 1955. View at Publisher · View at Google Scholar · View at Scopus
  29. H. U. Bergmeyer and M. Horder, “International federation of clinical chemistry. Scientific committee. Expert panel on enzymes. IFCC document stage 2, draft 1; 1979-11-19 with a view to an IFCC recommendation. IFCC methods for the measurement of catalytic concentration of enzymes. Part 3. IFCC method for alanine aminotransferase,” Journal of Clinical Chemistry and Clinical Biochemistry, vol. 18, no. 8, pp. 521–534, 1980. View at Google Scholar
  30. G. N. Bowers Jr. and R. B. McComb, “Measurement of total alkaline phosphatase activity in human serum,” Clinical Chemistry, vol. 21, no. 13, pp. 1988–1995, 1975. View at Google Scholar · View at Scopus
  31. M. E.-H. A. Kemeir, “Hepatotoxic effect of itraconazole in experimental rats,” American Journal of Animal and Veterinary Sciences, vol. 9, no. 1, pp. 46–52, 2014. View at Publisher · View at Google Scholar
  32. R. J. Rodriguez and D. Acosta Jr, “Metabolism of ketoconazole and deacetylated ketoconazole by rat hepatic microsomes and flavin-containing monooxygenases,” Drug Metabolism and Disposition, vol. 25, no. 6, pp. 772–777, 1997. View at Google Scholar · View at Scopus
  33. R. J. Rodriguez and D. Acosta Jr., “N-Deacetyl ketoconazole-induced hepatotoxicity in a primary culture system of rat hepatocytes,” Toxicology, vol. 117, no. 2-3, pp. 123–131, 1997. View at Publisher · View at Google Scholar · View at Scopus
  34. N. Somchit, S. M. Hassim, and S. H. Samsudin, “Itraconazole and fluconazole-induced toxicity in rat hepatocytes: a comparativein vitro study,” Human and Experimental Toxicology, vol. 21, no. 1, pp. 43–48, 2002. View at Publisher · View at Google Scholar · View at Scopus
  35. D. E. Amacher, “A toxicologist's guide to biomarkers of hepatic response,” Human and Experimental Toxicology, vol. 21, no. 5, pp. 253–262, 2002. View at Publisher · View at Google Scholar · View at Scopus