Involvement of phenobarbital and SKF 525A in the hepatotoxicity of antifungal drugs itraconazole and fluconazole in rats

Drug and Chemical Toxicology

Volumn 29, Issue 3, 2006, Pages 237-253

  Somchit, N ^a   Wong, C W ^a   Zuraini, A ^a   Ahmad Bustamam, A ^a   Hasiah, A H ^a   Khairi, H M ^a   Sulaiman, M R ^a   Israf, D A ^a  

^a UNIVERSITY PUTRA MALAYSIA   (Malaysia)

Author keywords

Cytochrome P450; Fluconazole; Hepatotoxicity; Itraconazole; Phenobarbital; SKF 525A

Indexed keywords

ALANINE AMINOTRANSFERASE; ALKALINE PHOSPHATASE; ANTIFUNGAL AGENT; CYTOCHROME P450; FLUCONAZOLE; GAMMA GLUTAMYLTRANSFERASE; ISOENZYME; ITRACONAZOLE; PHENOBARBITAL; PROADIFEN; SODIUM CHLORIDE;

ALANINE AMINOTRANSFERASE BLOOD LEVEL; ALKALINE PHOSPHATASE BLOOD LEVEL; ANIMAL EXPERIMENT; ANIMAL TISSUE; ARTICLE; CONTROLLED STUDY; DRUG POTENCY; ENZYME ACTIVITY; ENZYME INDUCTION; GAMMA GLUTAMYL TRANSFERASE BLOOD LEVEL; HISTOPATHOLOGY; IN VIVO STUDY; LIVER PROTECTION; LIVER TOXICITY; LIVER WEIGHT; MALE; NONHUMAN; RAT;

ANIMALS; ANTIFUNGAL AGENTS; CYTOCHROME P-450 ENZYME SYSTEM; DRUG-INDUCED LIVER INJURY; ENZYME INHIBITORS; FLUCONAZOLE; HEPATITIS, TOXIC; HYPNOTICS AND SEDATIVES; ISOENZYMES; ITRACONAZOLE; LIVER; MALE; MICROSOMES, LIVER; ORGAN SIZE; PHENOBARBITAL; PROADIFEN; RATS; RATS, SPRAGUE-DAWLEY;

EID: 33745685444     PISSN: 01480545     EISSN: 15256014     Source Type: Journal    
DOI: 10.1080/01480540600651535     Document Type: Article

References (32)

1. Back, D. J., Tjia, J. F. (1991). Comparative effects of the antimycotic drugs ketoconazole, fluconazole, itraconazole and terbinafine on the metabolism of cyclosporin by human liver microsomes. Br. J. Clin. Pharmacol. 32:624-626.
2. Biswas, S. J., Pathak, S., Khuda-Bukhsh, A.R. (2004). Assessment of the genotoxic and cytotoxic potential of an anti-epileptic drug, phenobarbital, in mice: a time course study. Mutat. Res. 563:1-11.
3. Burgess, D. S., Hastings, R. W. (2000). A comparison of dynamic characteristics of fluconazole, itraconazole, and amphotericin B against Cryptococcus neoformans using time-kill methodology. Diagn. Microbiol. Infect. Dis. 38:87-93.
4. Collazos, J., Mayo, J., Martinez, E., Diaz, F. (1995). Unusual liver toxicity due to the new antifungal agents fluconazole and itraconazole. Int. Hepatol. Comm. 3:112-115.
5. Feldman, D. (1986). Ketoconazole and other imidazole derivatives as inhibitors of steroidogenesis. Endocr. Rev. 7:409-420.
6. Fry, J. R., Wiebkin, P., Bridges, J. W. (1980). 7-Ethoxycoumarin O-deethylase induction by phenobarbitone and 1,2-benzanthracene in primary maintenance cultures of adult rat hepatocytes. Biochem. Pharmacol. 29:(4):577-581.
7. Grant, S. M., Clissold, S. P. (1990). Fluconazole. A review of its pharmacodynamics and pharmacokinetic properties, and therapeutic potential in superficial and systematic. Mycoses 39:877-916.
8. Gunawan, B., Kaplowitz, N. (2004). Clinical perspectives on xenobiotic-induced hepatotoxicity. Drug Metab. Rev. 36(2):301-12.
9. Haria, M., Bryson, H. M., Goa, K. L. (1996). Itraconazole: a reappraisal of its pharmacological properties and therapeutic use in the management of superficial fungal infection. Drugs 51:586-620.
10. Kaliste-Korhonen, K., Tuovinen, K., Hanninen, O. (1998). Effect of phenobarbital and B-naphthoflavone on activities of different rat esterases after paraoxon exposure. Gen. Pharmacol. 31:307-312.
11. Koop, D. R., Tierney, D. J. (1990). Multiple mechanisms in the regulation of ethanol-inducible cytochrome P450IIE1. Bioessays 12(9):429-435.
12. Kraemer, F. B., Spilman, S. D. (1986). Effects of ketoconazole on cholesterol synthesis. J. Pharmacol. Exp. Ther. 238:905-911.
13. Labib, R., Turkall, R., Abdel-Rahman, M. S. (2002). Inhibition of cocaine oxidative metabolism attenuates endotoxin potentiation of cocaine mediated hepatotoxicity. Toxicology 179:9-19.
14. Lamb, D. C., Kelly, D. E., Baldwin, B. C., Kelly, S. L. (2000). Differential inhibition of human CYP3A4 and Candida albicans CYP51 with azole antifungal agents. Chem. Biol. Interact. 125:165-175.
15. Lavrijsen, K., van Houdt, J., van Dyck, D. M., Meuldermans, W., Heykants, J. (1990). Induction potential of fluconazole towards drug-metabolising enzymes in rats. Antimicrob. Agents Chemother. 34:402-408.
16. Lavrijsen, A. P. M., Balmus, K. J., Nugteren-Huying, W. M., Roldaan, A. C., VantWout, J. W., Stricker, B. H. C. (1992). Hepatic injury associated with itraconazole. Lancet 340:251-252.
17. Pekarthy, J., Albert, J. S., Lansing, A., Lieberman, I. (1972). Function and control of liver alkaline phosphatase. J. Biol. Chem. 247:1767-1774.
18. Lewis, J. H., Zimmerman, H. J., Benson, G. D., Ishak, K. G. (1984). Hepatic injury associated with ketoconazole therapy. Gastroenterology 86:503-513.
19. Martin, M. V. (1999). The use of fluconazole and itraconazole in the treatment of Candida albicans infections: a review. J. Antimicrob. Chemother. 44(4):42-37.
20. Menon, T., Umamaheswari, K., Kumarasamy, N., Solomon, S., Thyagarajah, S. P. (2001). Efficacy of fluconazole and itraconazole in the treatment of oral candidiasis in HIV patients. Acta Trop. 80:151-154.
21. Restrepo, A., Roobledo, J., Gomez, I. (1986). Itraconazole therapy in lymphagenic and cutaneous sporotrichosis. Arch. Dermatol. 122:413-417.
22. Robertson, P., DeCory, H. H., Madan, A., Parkinson, A. (2000). In vitro inhibition and induction of human hepatic cytochrome P450 enzymes by modafinil. Drug Metab. Dispos. 28(6):664-671.
23. Rodrigues, A. D., Waddell, P. R., Ah-Sing, B., Morris, B. A., Wolf, C. R., Ioannides, C. (1988). Induction of the rat hepatic microsomal mixed-function oxidases by 3 imidazole-containing antifungal agents: selectivity for the cytochrome P450IIB and P450III families. Toxicology 50:283-301.
24. Rodriguez, J., Acosta, D., Jr. (1995). Comparison of ketoconazole and fluconazole-induced hepatotoxicity in a primary culture system of rat hepatocytes. Toxicology 96:83-92.
25. Rodriguez, R. J., Acosta, D., Jr. (1997). N-deacetyl ketoconazole induced hepatoxicity in a primary culture system of rat hepatocytes. Toxicology 117:123-131.
26. Saag, M. S., Dismukes, W. E. (1988). Azole antifungal agents: emphasis on new triazoles. Antimicrob. Agents Chemother. 32:1-8.
27. Somchit, N., Hassim, S. M., Samsudin, H. (2002). Itraconazole and fluconazole-induced toxicity in rat hepatocytes: a comparative in vitro study. Hum. Exp. Toxicol. 21(1):43-48.
28. Somchit, N., Norshahida, A. R., Hasiah, A. H., Zuraini, A., Sulaiman, M. R., Noordin, M. M. (2004). Hepatotoxicity induced by antifungal drugs itraconazole and fluconazole in rats: a comparative in vivo study. Hum. Exp. Toxicol. 23:519-525.
29. Swales, N. J., Johnson, T., Caldwell, J. (1996). Cryopreservation of rat and mouse hepatocytes. II Assessment of metabolic capacity using testosterone metabolism. Drug Metab. Dispos. 24:1224-1230.
30. Terrell, C. L. (1999). Antifungal agents: part II. The azoles. Mayo Clin. Proc. 74:78-100.
31. Wade, L. T., Kenna, J. G., Caldwell, J. (1997). Immunochemical identification of mouse hepatic protein adducts derived from the nonsteroidal anti-inflammatory drugs diclofenac, sulindac, and ibuprofen. Chem. Res. Toxicol. 10(5):546-555.
32. Waxman, D. J., Azaroff, L. (1992). Phenobarbital induction of cytochrome P450 gene expression. Biochem. J. 28:577-592.