Fluconazole (Diflucan®): a review

Zervos, M. J.; Meunier, Françoise

doi:10.1016/0924-8579(93)90009-t

Cited by 56 publications

(24 citation statements)

References 102 publications

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“…Amphotericin B is fungicidal for C. albicans and is currently the treatment of choice for life-threatening candidiasis, although nephrotoxicity, fever, chills, and rigors are frequent complications (3). Fluconazole is fungistatic for C. albicans but has significant advantages over amphotericin B in terms of safety, predictable pharmacokinetics, and the flexibility of oral and intravenous dosage forms (27). In addition, a recently completed multicenter comparative study has shown that the efficacy of fluconazole is comparable to that of amphotericin B in the treatment of candidemia (19).…”

Section: Discussionmentioning

confidence: 99%

Combination therapy of murine invasive candidiasis with fluconazole and amphotericin B

Sugar

Hitchcock

Troke

et al. 1995

Antimicrob Agents Chemother

110

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A study was performed to assess the in vivo relevance of the in vitro antagonism between fluconazole and amphotericin B against Candida albicans. Combinations of fluconazole and amphotericin B were explored for their efficacies against acute (100% mortality in 2 to 5 days) or less acute (100% mortality in 30 days) invasive candidiasis infections in mice with healthy immune systems and immunocompromised mice. Treatment efficacy was assessed by protection from mortality and/or a reduction in the fungal burden in tissue. In models of acute infection in mice with healthy immune systems or less acute infection in immunocompromised mice, combinations of fluconazole and amphotericin B were superior to fluconazole alone, and the effects were at least additive. Combination therapy was at least as efficacious as amphotericin B alone. In a different model of less acute infection in mice with healthy immune systems, combinations of fluconazole and amphotericin B showed no interactions and were no better than either drug alone. We conclude that combination therapy with fluconazole and amphotericin B is not antagonistic in vivo, in contrast to published in vitro studies, and, consequently, suggest that combination therapy should be considered in the management of clinical candidiasis.

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Section: Discussionmentioning

confidence: 99%

Combination therapy of murine invasive candidiasis with fluconazole and amphotericin B

Sugar

Hitchcock

Troke

et al. 1995

Antimicrob Agents Chemother

110

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“…In this regard, the efficacy of these compounds, which are listed as azole derivatives, were reported to have an antifungal effect against human infectious diseases. In this regard, the newer azole class of antifungal agents (fluconazole, itraconazole, ketoconazole and stevia) has also proven to be effective in treating invasive mycoses (Zervos and Meunier 1993;Espinel-Ingroff et al 2001;Rambali et al 2001;Diekema et al 2003;Clausen and Yang 2005;Tadhani and Subhash 2006). Hitchcock (1991) reported that the azole antifungal agents work by inhibiting cytochrome P-450-dependent 14 ά-sterol demethylase of ergosterol biosynthesis (P-450DM).…”

Section: In Vitro Testsmentioning

confidence: 99%

Effect of a New Chemical Formula on Postharvest Decay Incidence in Citrus Fruit

El-Mougy¹,

Abdel-Kader²,

Aly³

2012

Journal of Plant Protection Research

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Postharvest diseases caused by Geotricum candidum (sour rot), Penicillium digitatum (green mould), and P. italicum (blue mould) are the most important negative factors affecting handling and marketing of citrus fruits in Egypt. A new formula containing stevia leaf powder and a mixture of the three commercial chemical active ingredients: ketoconazole, fluconazole, and itraconazole has been successfully applied. Either chitosan or water wax were used as carriers, against fruit mould pathogenic fungi under laboratory and storage conditions. Results of the in vitro test showed that a complete reduction in linear fugal growth was observed when the ingredients of the new formula were used individually at a concentration of 400 μg/ml each, while a mixture of all the tested chemicals had a superior effect with all fungal growth completely inhibited with the use of the mixture at a concentration of 100 μg/ml. Similar results were recorded on citrus fruits which were coated with the suggested formula of chitosan or wax containing chemical compounds as a semi applicable technique using navel orange peel discs. Furthermore, the obtained results were confirmed using in vivo testing on navel orange and lime fruits, under artificial inoculation conditions of the pathogenic fungi within a storage period extended for four weeks. The proposed approach provides the treated agricultural products with long acting protection against microbial invasion and even association. This formula could be used as a fungicide alternative for protecting the agricultural products which have high moisture contents. The formula can be used against mould pathogens to prolong the healthy shelf life of the agricultural products. Such a treatment is safe, cheap, easily applied, and without residues which are harmful to people and the environment.

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“…Amphotericin B has been the mainstay of therapy for patients with life-threatening mycoses, although nephrotoxicity and administration by slow intravenous infusion are frequent complications (2). The newer azole class of antifungal agents (fluconazole, itraconazole, and ketoconazole) has also proven to be effective in treating invasive mycoses and represents an important alternative to amphotericin B for some indications (for a review, see reference 28).…”

mentioning

confidence: 99%

Fluconazole resistance due to energy-dependent drug efflux in Candida glabrata

Parkinson

Falconer

Hitchcock

1995

Antimicrob Agents Chemother

113

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We report on the mechanism of fluconazole resistance in Candida glabrata from a case of infection in which pre-and posttreatment isolates were available for comparison. The resistant, posttreatment isolate was cross-resistant to ketoconazole and itraconazole, in common with other azole-resistant yeasts. Resistance was due to reduced levels of accumulation of [ 3 H]fluconazole rather than to changes at the level of ergosterol biosynthesis. Studies with metabolic or respiratory inhibitors showed that this phenomenon was a consequence of energy-dependent drug efflux, as opposed to a barrier to influx. Since energy-dependent efflux is a characteristic of multidrug resistance in bacteria, yeasts, and mammalian cells, we investigated the possibility that fluconazole resistance is mediated by a multidrug resistance-type mechanism. Benomyl, a substrate for the Candida albicans multidrug resistance protein, showed competition with fluconazole for efflux from resistant C. glabrata isolates, consistent with a common efflux mechanism for these compounds. By contrast, other standard substrates or inhibitors of multidrug resistance proteins had no effect on fluconazole efflux. In conclusion, we have identified energy-dependent efflux of fluconazole, possibly via a multidrug resistance-type transporter, as the mechanism of resistance to fluconazole in C. glabrata.A growing number of debilitated and immunocompromised patients are at risk of serious fungal infections. These include patients receiving cancer therapies and organ transplants and those infected with the virus that causes AIDS. The latter are particularly susceptible to fungal infections because they are permanently immunocompromised, unlike other groups, in whom immunosuppression is transient. Amphotericin B has been the mainstay of therapy for patients with life-threatening mycoses, although nephrotoxicity and administration by slow intravenous infusion are frequent complications (2). The newer azole class of antifungal agents (fluconazole, itraconazole, and ketoconazole) has also proven to be effective in treating invasive mycoses and represents an important alternative to amphotericin B for some indications (for a review, see reference 28).The azole antifungal agents work by inhibiting cytochrome P-450-dependent 14␣-sterol demethylase of ergosterol biosynthesis (P-450 DM ) (for a review, see reference 10). Azoletreated fungi are depleted of ergosterol and accumulate 14␣-methylated sterols which inhibit fungal growth. All of the azoles are fungistatic, as opposed to fungicidal, against Candida spp., underlining the importance of the host's immune system for eradicating the infecting organism and achieving a clinical cure. A corollary of this situation is that AIDS patients require indefinite suppressive therapy, and given the widespread use of fluconazole in end-stage AIDS (including patients who have failed ketoconazole or itraconazole therapy), it is not unexpected that fluconazole-resistant Candida strains have been isolated from this group of patients (22).Stu...

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Fluconazole (Diflucan®): a review

Cited by 56 publications

References 102 publications

Combination therapy of murine invasive candidiasis with fluconazole and amphotericin B

Combination therapy of murine invasive candidiasis with fluconazole and amphotericin B

Effect of a New Chemical Formula on Postharvest Decay Incidence in Citrus Fruit

Fluconazole resistance due to energy-dependent drug efflux in Candida glabrata

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