Overview of medically important antifungal azole derivatives.

Fromtling, Robert A.

doi:10.1128/cmr.1.2.187-217.1988

Cited by 27 publications

(39 citation statements)

References 124 publications

(149 reference statements)

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“…Fluconazole is effectively distributed throughout all tissues, including a high penetration into cerebrospinal fluid, 13,14 and has also been shown to be nonmutagenic and less toxic than the other azoles. 29 The application of corticosteroids to reduce the nonspecific inflammatory processes remains controversial in the treatment of fungal keratitis. Many studies have shown a more pronounced recultivation rate of remaining pathogens after additional treatment with corticosteroids in fungal infections.…”

Section: Discussionmentioning

confidence: 99%

Combined Topical Fluconazole and Corticosteroid Treatment for ExperimentalCandida albicansKeratomycosis

Schreiber¹,

Olbrisch²,

Vorwerk³

et al. 2003

Invest. Ophthalmol. Vis. Sci.

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Section: Discussionmentioning

confidence: 99%

Combined Topical Fluconazole and Corticosteroid Treatment for ExperimentalCandida albicansKeratomycosis

Schreiber¹,

Olbrisch²,

Vorwerk³

et al. 2003

Invest. Ophthalmol. Vis. Sci.

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“…Troke and colleagues (22) showed that fluconazole has significantly more potent activity than ketoconazole against A. fumigatus in a murine model. The evaluation of fluconazole in a murine model of aspergillosis may be limited by the relatively rapid clearance of fluconazole in mice, because sustained levels are not readily achieved in the sera and tissues of mice (5). The t 1/2 s of fluconazole in serum are 22 h for humans, 8.9 h for rabbits, but only 4.8 h for mice after p.o.…”

Section: Discussionmentioning

confidence: 99%

T-8581, a new orally and parenterally active triazole antifungal agent: in vitro and in vivo evaluations

Yotsuji

Shimizu

Araki

et al. 1997

Antimicrob Agents Chemother

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T-8581 is a new water-soluble triazole antifungal agent. The geometric mean IC80s (GM-IC80S; where the IC80 is the lowest drug concentration which reduced the optical density at 630 nm by 80% compared with the optical density at 630 nm of the drug-free control) for Candida albicans were as follows: T-8581, 0.218 microgram/ml; fluconazole; 0.148 microgram/ml; and itraconazole, 0.0170 microgram/ml. For Cryptococcus neoformans the GM-IC80s were as follows: T-8581, 9.28 micrograms/ml; fluconazole, 4.00 micrograms/ml; and itraconazole, 0.119 microgram/ml. For Aspergillus fumigatus the GM-IC80s were as follows: T-8581, 71.0 micrograms/ml; fluconazole, 239 micrograms/ml; and itraconazole, 0.379 microgram/ml. Against systemic candidiasis in mice, the 50% effective doses (ED50s) of T-8581, fluconazole, and itraconazole (given orally) were 0.412, 0.392, and > 320 mg/kg of body weight, respectively. Against systemic aspergillosis in mice, the ED50s of T-8581, fluconazole, and itraconazole (given orally) were 50.5, 138, > 320 mg/kg, respectively. T-8581 was also efficacious when it was given parenterally (ED50, 59.2 mg/kg), while the ED50 of fluconazole given parenterally was > 20 mg/kg. Against systemic aspergillosis in rabbits, T-8581 was more effective than fluconazole and itraconazole in prolonging the life span. The high concentrations of T-8581 were observed in the sera of mice, rats, rabbits and dogs. Species differences in half-lives and areas under the concentration-time curves were observed, with the values for mice, rats, rabbits, and dogs increasing in that order. These results suggest that T-8581 would be a potentially effective antifungal drug for oral and parenteral use.

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“…The increase in the variety of pathogens associated with serious fungal infections has not been matched by a corresponding increase in the number of antifungal agents available for their treatment. Amphotericin B and azole derivatives, most notably fluconazole and itraconazole, are the primary drugs used for treatment of serious fungal infections (13,15). However, limitations in the efficacy and/or tolerability of these agents have prompted a search for new drugs that may be effective in the management of patients with mycoses due to a wide range of filamentous fungi and yeast pathogens.…”

mentioning

confidence: 99%

“…However, limitations in the efficacy and/or tolerability of these agents have prompted a search for new drugs that may be effective in the management of patients with mycoses due to a wide range of filamentous fungi and yeast pathogens. Much of this search has centered on azole derivatives (13,15).…”

mentioning

confidence: 99%

In Vitro Activity of the New Triazole Voriconazole (UK-109,496) against Opportunistic Filamentous and Dimorphic Fungi and Common and Emerging Yeast Pathogens

Espinel-Ingroff

1998

J Clin Microbiol

326

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The in vitro antifungal activity of a new triazole derivative, voriconazole, was compared with those of itraconazole and amphotericin B against 67 isolates of Aspergillus flavus,Aspergillus fumigatus, Bipolaris spp.,Fusarium oxysporum, Fusarium solani,Pseudallescheria boydii, Rhizopus arrhizus,Blastomyces dermatitidis, Histoplasma capsulatum, and Sporothrix schenckii. The in vitro activities of voriconazole were also compared with those of amphotericin B, fluconazole, and itraconazole against 189 isolates of emerging and common yeast pathogens of Blastoschizomyces capitatus, Candida (13 species), Cryptococcus neoformans, Hansenula anomala, Rhodotorula rubra, Saccharomyces cerevisiae, Sporobolomyces salmonicolor, and Trichosporon beigelii. MICs were determined according to a procedure under evaluation by the National Committee for Clinical Laboratory Standards (NCCLS) for broth microdilution testing of filamentous fungi and by the NCCLS M27-A broth microdilution method for yeasts. The in vitro activities of voriconazole were similar to or better than those of itraconazole and amphotericin B against Aspergillus spp.,Fusarium spp., and P. boydii as well as againstB. dermatitidis and H. capsulatum. The activities of voriconazole were also comparable to or better than those of amphotericin B, fluconazole, and itraconazole against most species of yeasts tested. Exceptions were certain isolates of R. rubra and S. salmonicolor. These results suggest that voriconazole has a wide spectrum of activity in vitro; its effectiveness in the treatment of human mycoses is under evaluation in clinical trials.

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Overview of medically important antifungal azole derivatives.

Cited by 27 publications

References 124 publications

Combined Topical Fluconazole and Corticosteroid Treatment for ExperimentalCandida albicansKeratomycosis

Combined Topical Fluconazole and Corticosteroid Treatment for ExperimentalCandida albicansKeratomycosis

T-8581, a new orally and parenterally active triazole antifungal agent: in vitro and in vivo evaluations

In Vitro Activity of the New Triazole Voriconazole (UK-109,496) against Opportunistic Filamentous and Dimorphic Fungi and Common and Emerging Yeast Pathogens

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