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Pharmaceutisch Weekblad

, Volume 13, Issue 2, pp 45–57 | Cite as

Fluconazole

Review and situation among antifungal drugs in the treatment of opportunistic mycoses of human immuno-deficiency virus infections
  • Françoise N. Vincent-Ballereau
  • Olivier N. Patey
  • Christian Lafaix
Reviews

Abstract

Fluconazole is a novel triazole antifungal drug chiefly used in the treatment of opportunistic mycoses in immuno-compromised patients, particularly those with the acquired immuno-deficiency syndrome (AIDS). In comparison with other antifungal drugs, fluconazole has outstanding physical and pharmacokinetic properties, such as an excellent aqueous solubility allowing a parenteral formulation, high bioavailability by the oral route, even distribution throughout the tissues, including the central nervous system and the cerebro-spinal fluid, a long half-life (permitting once daily administration), and low binding to plasma proteins. It is excreted mainly as unchanged drug in the urine. Fluconazole is a broad-spectrum antifungal agent, especially effective againstCandida spp.,Cryptococcus neoformans and dermatophytes. Its antifungal efficacy was mainly proved by testing in animal models, since there is no relationship betweenin vitro andin vivo activities. It possesses a low toxicity and it is well-tolerated. Fluconazole is currently marketed for the treatment of oropharyngeal candidiasis in immuno-compromised patients and of atrophic oral candidiasis. Its place in the treatment of opportunistic mycoses in human immuno-deficiency virus-positive patients, in particular cryptococcal meningitis, is still under investigation but is promising.

Keywords

AIDS Candidiasis Cryptococcosis Fluconazole Myeoses Pharmacokinetics 

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Copyright information

© Royal Dutch Association for Advancement of Pharmacy 1991

Authors and Affiliations

  • Françoise N. Vincent-Ballereau
    • 1
  • Olivier N. Patey
    • 2
  • Christian Lafaix
    • 2
  1. 1.Pharmacie CHRUHôtel DieuNantes, cédex 01France
  2. 2.Department of Infectious DiseasesCHGVilleneuve St. GeorgesFrance

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