Cited by 661Antifungal resistance and susceptibilityFungal Infections and StudiesFungal Plant Pathogen Control

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Fluconazole: A Review of its Pharmacodynamic and Pharmacokinetic Properties, and Therapeutic Potential in Superficial and Systemic Mycoses

Grant, Susan M., Clissold, Stephen P.·1990·Drugs

DOI 10.2165/00003495-199039060-00006

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Abstract

Fluconazole is a bis-triazole antifungal drug with novel pharmacokinetic properties (metabolic stability, relatively high water solubility) which contribute to its therapeutic activity. Clinical experience is limited to a relatively small number of mycoses and, as might be expected at this early stage of development, optimal dosage and duration of treatment for some serious mycoses is not yet established. Further study to evaluate higher dosages and to establish the efficacy of fluconazole relative to more established antifungal agents is required. In patients with oropharyngeal or oesophageal candidiasis, fluconazole produces rapid relief and eradicates the yeast in 50 to 90% of patients. Relapse of oral infection is common in chronically immunocompromised patients regardless of the antifungal used, and adequate primary therapy plus long term prophylaxis appears necessary in patients with AIDS. A single oral dose of fluconazole was comparable to standard topical azole therapy in women with acute vaginal candidiasis. Preliminary reports of success against deep-seated candidiasis are encouraging; moreover, experience in noncomparative clinical trials suggests that fluconazole 200 to 400mg once daily resolves infection in the majority of seriously ill patients. Clinical improvement has been reported in a few cases of pulmonary Aspergillus infection but the overall efficacy of conventional dosages of fluconazole in this mycosis has not been as impressive. Early experience in coccidioidosis, predominantly meningitis, suggests a beneficial clinical effect with oral fluconazole in this difficult to treat mycosis but relapse remains a problem. Fluconazole is a promising treatment of cryptococcal meningitis. The rate of clinical resolution and eradication of Cryptococcus neoformans from cerebrospinal fluid has been similar between fluconazole and amphotericin B treatment groups in comparative trials. Comparative trials of maintenance therapy indicate a similar low rate of relapse among patients given oral fluconazole once daily and intravenous amphotericin B once weekly. However, these results are preliminary and further study is required. Fluconazole has been well tolerated to date but wider clinical experience is needed, especially with regard to the rate occurrence of hepatotoxicity and exfoliative skin reactions. The promising clinical response of patients with various forms of candidiasis or cryptococcosis--together with convenient administration regimens--recommends fluconazole as a useful addition to currently available systemic antifungal therapies, in particular for the treatment of mycoses in patients with AIDS.

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Authors: Grant, S. M., & Clissold, S. P.
ORCID: Grant, Susan M.
Venue: Drugs
Publisher: Springer Science and Business Media LLC
Published: 1990-06
Volume: 39
Issue: 6
Pages: 877-916
ISSN: 0012-6667 (ISSN-L)
DOI: 10.2165/00003495-199039060-00006
OpenAlex: W1971920484
Cited by: 661
References: 160
Citations by year: 2026: 6 · 2025: 7 · 2024: 6 · 2023: 8 · 2022: 8 · 2021: 11 · 2020: 9 · 2019: 10 · 2018: 8 · 2017: 9 · 2016: 12 · 2015: 12 · 2014: 13 · 2013: 14 · 2012: 12
FWCI: 25.31
Type: journal article
Language: en
Open access: closed
Locations: Drugs (publishedVersion)
PubMed (publishedVersion)
Topics: Health Sciences › Medicine › Infectious Diseases › Antifungal resistance and susceptibility
Health Sciences › Medicine › Infectious Diseases › Fungal Infections and Studies
Life Sciences › Agricultural and Biological Sciences › Plant Science › Fungal Plant Pathogen Control
Keywords: antifungal agents, candidiasis, cryptococcosis, cryptococcal meningitis, AIDS, pulmonary aspergillosis, coccidioidomycosis, vaginal candidiasis, oropharyngeal candidiasis, drug metabolism, pharmacokinetics, hepatotoxicity, drug interactions, adverse drug reactions
MeSH terms: Animals, Fungi, Humans, Mycoses, Fluconazole

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Fluconazole: A Review of its Pharmacodynamic and Pharmacokinetic Properties, and Therapeutic Potential in Superficial and Systemic Mycoses

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