Inflammation Research

, Volume 45, Issue 1, pp 20–25 | Cite as

Topical anti-inflammatory properties of flutrimazole, a new imidazole antifungal agent

  • M. Merlos
  • M. L. Vericat
  • J. García-Rafanell
  • J. Forn
Original Research Papers

Abstract

The topical anti-inflammatory properties of flutrimazole, a new imidazole antifungal, have been evaluated. Flutrimazole inhibited mouse ear oedema induced by arachidonic acid, tetradecanoylphorbolacetate and dithranol, with IC50 values of 3.32, 0.55 and 2.42 μmols/ear, respectively. Ketoconazole showed similar potency in arachidonic acid and dithranol models (IC50=3.76 and 2.41 μmols/ear) whereas it was less active against tetradecanoylphorbol acetate (IC50=1.96 μmols/ear). The standard anti-inflammatory sodium diclofenac was overall slightly more potent than antifungals (IC50=2.23, 0.57 and 0.57 μmols/ear against arachidonic acid, tetradecanoylphorbol acetate and dithranol, respectively). Both 2% flutrimazole and 2% ketoconazole creams, applied topically, inhibited carrageenan-induced rat paw oedema by about 40%. Under the same conditions, 1% flutrimazole and diclofenac creams inhibited by 26 and 54%, respectively. Flutrimazole may work through the inhibition of 5-lipoxygenase, as it inhibited LTB4 production by human granulocytes with an IC50 value of 11 μM (IC50 value for ketoconazole was 17 μM), whereas ram seminal vesicle cyclooxygenase was only inhibited by 16% at a concentration of 25 μM. Drugs such as flutrimazole, with dual anti-inflammatory/antifungal activity, may be advantageous in the treatment of topical fungal infections with an inflammatory component.

Key words

Flutrimazole Carrageenan oedema Mouse ear oedema 5-lipoxygenase 

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Copyright information

© Birkhäuser Verlag 1996

Authors and Affiliations

  • M. Merlos
    • 1
  • M. L. Vericat
    • 1
  • J. García-Rafanell
    • 1
  • J. Forn
    • 1
  1. 1.Research Center, J. Uriach & Cía.BarcelonaSpain

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