The broad-spectrum oral triazole antifungal, itraconazole, has been sh
own to be effective in the treatment of superficial and systemic infec
tions with fungi including Candida albicans, C. krusei and C. glabrata
, Cryptococcus, Aspergillus, Histoplasma, Blastomyces and others. Its
broad spectrum of activity, high and persistent tissue levels and favo
urable safety profile suggest that it may be appropriate for the preve
ntion of opportunistic fungal infections in at-risk patients. In this
study, itraconazole's prophylactic efficacy was tested against experim
ental models of Candida and Aspergillus infection. A single dose of 1.
25 mg kg(-1) or 2.5 mg kg(-1), given Ih before vaginal infection with
C. albicans, protected 50% of treated rats. In systemic and disseminat
ed candidosis, prophylaxis with itraconazole reduced both folliculitis
and organ Candida content in guinea pigs. Amphotericin B was also use
d in this study and was found to be less efficacious than itraconazole
. Itraconazole prolonged survival when administered to guinea pigs bef
ore experimental induction of systemic and invasive aspergillosis. In
all cases, increasing the itraconazole dosage increased its prophylact
ic efficacy. Therefore, as the clinical efficacy of itraconazole is ac
curately reflected by the results of animal models, this study shows i
traconazole to be a potential prophylactic therapy for patients at ris
k of opportunistic fungal infection.