Abstract
Itraconazole is a widely used antifungal drug. In situations such as managing patients with gastrointestinal basidiobolomycosis, third of which cases world-wide occur in the southwestern region of Saudi Arabia, prolonged treatment with this drug is required. Thus, this is study was designed to investigate the hepatotoxicity of long term administration of itraconazolein in Wistar rats. Two groups of rats were treated with itraconazole at doses of 5 and 10 mg kg-1, for 30 and 60 days, respectively. At the end of each period sera of rats were tested for liver enzymes (including ALT, ALP and γGTT, albumin and protein). Animals were sacrificed and livers were processed for histological examination. Compared to controls, all rats treated for 30 and 60 days showed significant elevation in the levels of liver enzymes. Histologically there was severe liver injury. Although itraconazole is a safe antifungal drug, prolonged treatment with this drug may lead to severe hepatitis and liver cell injury. Patients who require treatment with this drug for long periods (12 to 18 months) should have their liver functions periodically monitored.
Highlights
Itraconazole is a synthetic triazole fungicidal agent, was approved for use in 1992 in the USA and continues to be used widely as antifungal
Itraconazole is a widely used antifungal drug. In situations such as managing patients with gastrointestinal basidiobolomycosis, third of which cases world-wide occur in the southwestern region of Saudi Arabia, prolonged treatment with this drug is required
Itraconazole is a safe antifungal drug, prolonged treatment with this drug may lead to severe hepatitis and liver cell injury
Summary
Itraconazole is a synthetic triazole fungicidal agent, was approved for use in 1992 in the USA and continues to be used widely as antifungal. The drugs bind to fungal cytochrome P450, preventing the conversion of lanosteroltoergosterol, which leads to abnormalities in cellmembrane activity and membrane-bound enzymeactivities causing fungal cell death (Bailey et al, 1990). The level of serum transaminases increases in 1 to 5% of patients who receive continuous therapy (Persat et al, 2000; Gupta et al, 2002). Itraconazole has been used for 15 years in more than 50 million patients; serum enzymes elevations occurred in 1 to 5% of patients on continuous itraconazole therapy and 1.7 to 2% on pulse therapy; systematic hepatotoxicity is rare (Gupta et al, 2001). Peak bilirubin level of 32 mg dL−1 was documented approximately after two months after discontinuation of itraconazole therapy
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