Bifonazole, a New Topical Azole Antimycotic with Specific Properties

  • M. Plempel
  • D. Berg
  • W. Ritter

Abstract

Bifonazole, a recently developed imidazole derivative, exhibits under conventional in vitro test conditions the well-known and classical (antifungal) properties of the azoles:
  • 1. A broad antimycotic spectrum comprising dermatophytes, yeasts, molds, and biphasic fungi

  • 2. A high intensity of antimycotic activity

  • 3. A satisfactory resistance situation with a low incidence of primary resistance, and secondary resistance which could not be detected up to now

  • 4. Excellent in vivo effects following topical application using the trichophytosis model in the guinea pig

  • 5. Effects after oral administration in the murine candidiasis model

In addition, bifonazole is characterized by a long retention time on the skin, as demonstrated with the infection prophylaxis model, and by an increased fungicidal activity on filamentous fungal elements, in particular of dermatophytes, owing to a twofold inhibition on the ergosterol biosynthesis in fungal cells

The uptake of bifonazole into the fungal cells reaches a maximum after only 20-30 min, and the drug remains there for about 120 h, continuously inhibiting the ergosterol biosynthesis. Thus in bifonazole-contaminated fungal cells a pronounced loss of virulence is observed, which finally influences the various steps from contamination to infection in macroorganisms and the conversion from the saprophytic to the parasitic stage in fungi. Based on these experimental properties in vitro and in vivo, bifonazole allows for a once daily application and a shorter duration of treatment.

Keywords

Agar Mold Chitin Aspergillus Candida 

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Copyright information

© Springer-Verlag Berlin Heidelberg 1986

Authors and Affiliations

  • M. Plempel
    • 1
  • D. Berg
    • 1
  • W. Ritter
    • 1
  1. 1.Institutes of ChemotherapyBiochemistry and Clinical Pharmacology, BAYER Pharma Research CentreWuppertal 1Federal Republic of Germany

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