[Present status and perspectives on antimycotics with systemic effects].
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 beta-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.
Haber
J
J
I. interní klinika 1. LF UK a VFN, Praha. haber@mbox.cesnet.cz
D000935:Antifungal Agents / Q000009:adverse effects / Q000737:chemistry / Q000627:therapeutic use; D006801:Humans; D009181:Mycoses / Q000188:drug therapy
D000935:Antifungal Agents