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Back to Infections Drug Index

Back to Antifungals

Name: Fluconazole

Pregnancy Category C

Drug classes of Fluconazole

Therapeutic actions of Fluconazole

Fluconazole is a highly selective inhibitor of fungal cytochrome P-450 sterol C-14
alpha-demethylation. This decreases ergosterol synthesis which is the principal sterol in fungal cell membranes, thus inhibiting cell membrane formation.

Indications of Fluconazole

  1. Vaginal candidiasis (vaginal yeast infections due to Candida).
  2. Oropharyngeal and esophageal candidiasis. In open noncomparative studies of relatively
    small numbers of patients, fluconazole was also effective for the treatment of Candida
    urinary tract infections, peritonitis, and systemic Candida infections including candidemia,
    disseminated candidiasis, and pneumonia.
  3. Cryptococcal meningitis.
  4. Prophylaxis. fluconazole is also indicated to decrease the incidence of candidiasis in patients undergoing bone marrow transplantation who receive cytotoxic chemotherapy and/or radiation therapy.

Specimens for fungal culture and other relevant laboratory studies (serology, histopathology) should be obtained prior to therapy to isolate and identify causative organisms. Therapy may be instituted before the results of the cultures and other laboratory studies are known; however, once these results become available, anti-infective therapy should be adjusted accordingly.

Contraindications/cautions of Fluconazole

  • hypersensitivity to fluconazole or to any of its excipients. Caution should be used in prescribing fluconazole to patients with hypersensitivity to other azoles.
  • Concomitant adminstration with terfanidine, cisapride or astemizole.
  • Patients with liver failure.
  • Fluconazole should be administered with caution to patients with these potentially proarrhythmic conditions.
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Adverse effects of Fluconazole

  • hypersensitivity to fluconazole or to any of its excipients. Caution should be used in prescribing fluconazole to patients with hypersensitivity to other azoles.
  • Hepatic injury: Fluconazole has been associated with rare cases of serious hepatic
    toxicity, including fatalities primarily in patients with serious underlying medical
    conditions. Fluconazole hepatotoxicity has usually, but not always, been reversible on discontinuation of therapy.
  • Anaphylaxis: In rare cases, anaphylaxis has been reported.
  • Dermatologic: Patients have rarely developed exfoliative skin disorders during treatment with fluconazole. In patients with serious underlying diseases (predominantly AIDS and
    malignancy), these have rarely resulted in a fatal outcome. Patients who develop rashes during treatment with fluconazole should be monitored closely and the drug discontinued if lesions progress.
  • Some azoles, including fluconazole, have been associated with prolongation of the QT interval torsade de pointes on the electrocardiogram. Most of these reports
    involved seriously ill patients with multiple confounding risk factors, such as structural heart disease, electrolyte abnormalities and concomitant medications that may have been contributory. Fluconazole should be administered with caution to patients with these potentially proarrhythmic conditions.
 

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