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Back to Infections Drug Index
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
-
Vaginal candidiasis (vaginal yeast infections due to Candida).
- 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.
- Cryptococcal meningitis.
- 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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