Activity of Orally, Topically, and Parenterally Administered Itraconazole in the Treatment of Superficial and Deep Mycoses: Animal Models

Cutsem, J. Van; Gerven, F. Van; Janßen, Paul

doi:10.1093/clinids/9.supplement_1.s15

Cited by 202 publications

(96 citation statements)

References 24 publications

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“…The wider spectrum of activity and greater potency are advantages over ketoconazole (3,7,32,36,37). Itraconazole therapy has been effective in some patients who have experienced failures of prior therapy with either ketoconazole or AMB (8).…”

Section: Discussionmentioning

confidence: 99%

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High-dose itraconazole in the treatment of severe mycoses

Sharkey

Rinaldi

Dunn

et al. 1991

Antimicrob Agents Chemother

138

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Eight patients with systemic mycoses and with prior treatment failures were treated with itraconazole (600 mg/day) for a mean duration of 5.5 months. All six patients without AIDS experienced improvement or stabilization of their fungal infections while receiving high-dose itraconazole, although two patients later experienced treatment failures, one by relapse and one by progression, on lower doses. Treatment failures also occurred in the two patients with AIDS and cryptococcal meningitis. The failures were associated with low serum itraconazole concentrations (<2.5 ,ug/ml) in both patients. All other patients had mean trough levels in serum above 5 ,ug/ml. One patient who was improving on 600 mg/day developed a progressive infection after reduction of the dose to 400 mg/day. Side effects included reversible adrenal insufficiency in one patient; severe hypokalemia, mild diastolic hypertension, and rhabdomyolysis in one patient; mild hypokalemia and hypertension in four other patients; and breast tenderness in one patient. The mean decrease in serum potassium during treatment was statistically significant (P = 0.05). Selected patients with severe systemic mycoses may benefit from prolonged high-dose itraconazole treatment. However, 600 mg/day may be approaching the upper limits of acceptable dosing for long-term treatment.

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Section: Discussionmentioning

confidence: 99%

“…It is more potent and has a wider spectrum of activity than ketoconazole in vitro and in vivo (3,7,32,36,37). Clinical responses have been reported in patients with systemic mycoses, including coccidioidomycosis, sporotrichosis, chromoblastomycosis, and aspergillosis.…”

mentioning

confidence: 99%

High-dose itraconazole in the treatment of severe mycoses

Sharkey

Rinaldi

Dunn

et al. 1991

Antimicrob Agents Chemother

138

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“…Itraconazole is a potent agent for the oral and parenteral treatment of a wide variety of experimental systemic and superficial fungal infections. Van Cutsem et al (319,320) summarized several "in house" studies of the efficacy of itraconazole in animal models of fungal infections. Overall, it was more active than ketoconazole in treating most of the experimental infections.…”

Section: Antifungal Imidazoles Under Developmentmentioning

confidence: 99%

Overview of medically important antifungal azole derivatives

1988

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Fungal infections are a major burden to the health and welfare of modern humans. They range from simply cosmetic, non-life-threatening skin infections to severe, systemic infections that may lead to significant debilitation or death. The selection of chemotherapeutic agents useful for the treatment of fungal infections is small. In this overview, a major chemical group with antifungal activity, the azole derivatives, is examined. Included are historical and state of the art information on the in vitro activity, experimental in vivo activity, mode of action, pharmacokinetics, clinical studies, and uses and adverse reactions of imidazoles currently marketed (clotrimazole, miconazole, econazole, ketoconazole, bifonazole, butoconazole, croconazole, fenticonazole, isoconazole, oxiconazole, sulconazole, and tioconazole) and under development (aliconazole and omoconazole), as well as triazoles currently marketed (terconazole) and under development (fluconazole, itraconazole, vibunazole, alteconazole, and ICI 195,739).

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“…Itraconazole, a nitrogen-substituted triazole, has been found to be active in vitro against several species of Aspergillus [36,37]. In vivo evaluation with use of a murine model revealed greater activity than that achieved by ketoconazole, but no comparison was made with the activity of amphotericin B [37,38]. It is unfortunate that only a limited number of case repons have described the use of itraconazole for the treatment of aspeg illosis in humans, with variable results [39][40][41].…”

Section: Discussionmentioning

confidence: 99%