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  Česky / Czech version Čas. Lék. čes., 140, 2001, No. 19, p. 596-604
 
Present Situation and Perspectives of Antimycotics with Systemic Effect 
Haber J. 

I. interní klinika 1. LF UK a VFN, Praha
 


Summary:

       Spectrum of antimycotics used in treatment of systemic mycoses is comparatively poor. The oldest and till present received „golden standard“ is polyen amphotericin B (AmB). It has the widest spectrum of effects and has the lowest incidence of resistances. However, the therapy can be accompanied by manifestations of toxicity, namely that of nephrotoxicity. „Lipoid“ form of AmB (Abelcet, Amphocil, AmBisome) with only 20% risk of nephrotoxicity partly solved the problem. Wider use of these drugs is hindered by their high price. The azoles group (ketoconazole, fluconazole, itraconazole) today represents the most frequently used group of antimycotics; triazols of the 3rd generation (variconazole, posaconazole, ravuconazole) broaden the spectrum of effects namely to aspergil infections. In the future substances with a different target structure will be used. According the mechanism of effect they can be classified as echinocandins (inhibition of b-glucane synthesis), echinocandins (inhibition of chitin synthesis), sordarines (selective inhibitors of proteosynthesis), pradimicines (cell lysis by binding on manoproteins). The rising occurrence of resistance should be coped with inhibitors of the efflux pump (milbemycine). Clinical testing of all these substances is already in progress, in some of them already in phase III.

        Key words: amphotericin B, nystatine, azoles, fluconazole, ketoconazole, itraconazole, variconazole, ravucona - zole, posaconazole, echinocandins, sordarines, pradimicines, efflux pump inhibitors.
       

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