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Advances in Topical Antifungal Therapy pp 4–20Cite as

Bifonazole, a New Topical Azole Antimycotic with Specific Properties

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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.

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Author information

Authors and Affiliations

  1. Institutes of Chemotherapy, Biochemistry and Clinical Pharmacology, BAYER Pharma Research Centre, 5600, Wuppertal 1, Federal Republic of Germany

    M. Plempel, D. Berg & W. Ritter

Authors
  1. M. Plempel
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  2. D. Berg
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  3. W. Ritter
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Editor information

Editors and Affiliations

  1. Institute of Dermatology, United Medical and Dental Schools of Guy’s and St. Thomas’s Hospitals, 5 Lisle Street, London, WC2H 7BJ, Great Britain

    R. J. Hay MD, MRCP, MRCPath.

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© 1986 Springer-Verlag Berlin Heidelberg

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Plempel, M., Berg, D., Ritter, W. (1986). Bifonazole, a New Topical Azole Antimycotic with Specific Properties. In: Hay, R.J. (eds) Advances in Topical Antifungal Therapy. Springer, Berlin, Heidelberg. https://doi.org/10.1007/978-3-642-71717-8_2

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  • DOI: https://doi.org/10.1007/978-3-642-71717-8_2

  • Publisher Name: Springer, Berlin, Heidelberg

  • Print ISBN: 978-3-540-17302-1

  • Online ISBN: 978-3-642-71717-8

  • eBook Packages: Springer Book Archive

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