Like other imidazole- and triazole-class antifungals, fluconazole inhibits the fungal cytochrome P450 enzyme 14α-demethylase. Mammalian demethylase activity is much less sensitive to fluconazole than fungal demethylase. This inhibition prevents the conversion of lanosterol to ergosterol, an essential component of the fungal cytoplasmic membrane, and subsequent accumulation of 14α-methyl sterols. Fluconazole is primarily fungistatic; however, it may be fungicidal against certain organisms in a dose-dependent manner, specifically Cryptococcus.
Fluconazole is a first-generation triazole antifungal medication. It differs from earlier azole antifungals (such as ketoconazole) in that its structure contains a triazole ring instead of an imidazole ring. While the imidazole antifungals are mainly used topically, fluconazole and certain other triazole antifungals are preferred when systemic treatment is required because of their improved safety and predictable absorption when administered orally.
Fluconazole's spectrum of activity includes most Candida species (but not Candida krusei or Candida glabrata), Cryptococcus neoformans, some dimorphic fungi, and dermatophytes, among others. Common uses include:
Side effects associated with use of Fluconazole, include the following:
Other side effects of fluconazole include:
Dosage Considerations – Should be Given as Follows:
Adult: 200 mg orally on Day 1, THEN 100 mg once/day
Pediatric: 6 mg/kg orally on Day 1, THEN 3 mg/kg once/day; not to exceed 600 mg/day
Adult: 200 mg orally on Day 1, THEN 100 mg once/day; doses up to 400 mg/day may be used based on patient's response
Pediatric: 6 mg/kg orally on Day 1, THEN 3 mg/kg once/day
Doses up to 12 mg/kg/day may be used, based on patient's response
Prophylaxis of Candidiasis with BMT
Prevention of candidiasis incidence in patients undergoing bone marrow transplant
400 mg orally once/day
Uncomplicated: 150 mg orally as a single dose
Complicated: 150 mg orally every 72 hours for 3 doses
Recurrent: 150 mg orally once/day for 10-14 days followed by 150 mg once weekly for 6 months
50-200 mg orally once/day
Systemic Candida Infections, Pediatric
6-12 mg/kg/day orally/intravenously (IV); not to exceed 600 mg/day
26-29 weeks' gestation: 6-12 mg/kg intravenously (IV)/orally
Maintenance: 3-6 mg/kg IV/orally once/day
Maintenance dose interval
Hepatic impairment: Not studied
If your medical doctor is using this medicine to treat your pain, your doctor or pharmacist may already be aware of any possible drug interactions and may be monitoring you for them. Do not start, stop, or change the dosage of any medicine before checking with your doctor, health care provider or pharmacist first.
Severe interactions of fluconazole include:
Fluconazole has serious interactions with at least 84 different drugs.
Fluconazole has moderate interactions with at least 186 different drugs.
Fluconazole has mild interactions with at least 96 different drugs.
This information does not contain all possible interactions or adverse effects. Therefore, before using this product, tell your doctor or pharmacist of all the products you use. Keep a list of all your medications with you, and share this information with your doctor and pharmacist. Check with your health care professional or doctor for additional medical advice, or if you have health questions, concerns or for more information about this medicine.
All other indications:
Effects of Drug Abuse
Pregnancy and Lactation
Single maternal oral dose of 150 mg for vaginal candidiasis: