QT prolongation Torsades de pointes Alopecia Anaphylactic reactions Angioedema Cholestasis Dizziness Dyspnea Hepatic failure Hepatitis Hypertriglyceridemia Hypokalemia Increased alkaline phosphatase Increased ALT/AST Jaundice Leukopenia Pallor Seizures Stevens-Johnson syndrome Taste perversion Thrombocytopenia Toxic epidermal necrolysis Hypersensitivity to other azoles Use caution in proarrhythmic conditions and renal impairment Use extreme caution or avoid in congenital long-QT patients and patients with conditions that increase QT-prolongation risk Fluconazole inhibits CYP2C9, CYP2C19, and CYP3A4 isoenzymes; coadministration with drugs that are substrates if these isoenzymes may be contraindicated or warrant dosage modifications Capsules contain lactose and should not be given to patients with rare hereditary problems of galactose intolerance, Lapp lactase deficiency, or glucose-galactose malabsorption Powder for oral suspension contains sucrose and should not be used in patients with hereditary fructose, glucose/galactose malabsorption or sucrase-isomaltase deficiency Syrup contains glycerol; may cause headache, stomach upset, and diarrhea Hepatotoxicity reported with use; use with caution in patients with hepatic impairment Rare exfoliative skin disorders reported; monitor closely if rash develops and discontinue if it progresses When driving vehicles or operating machines, it should be taken into account that dizziness or seizures may occasionally occur Candida krusei is inherently resistant Convenience and efficacy of single dose oral tablet of fluconazole regimen for the treatment of vaginal yeast infections should be weighed against acceptability of higher incidence of drug related adverse events with fluconazole (26%) versus intravaginal agents (16%) If drug is used during pregnancy or if patient becomes pregnant while taking the drug, patient should be informed of potential hazard to fetus; effective contraceptive measures should be considered in women of child-bearing potential who are being treated with 400 to 800 mg/day and should continue throughout the treatment period and for approximately 1 week (5 to 6 half-lives) after the final dose Highly selective inhibitor of fungal cytochrome P-450-dependent enzyme lanosterol 14-alpha-demethylase Subsequent loss of normal sterols correlates with accumulation of 14 alpha-methyl sterols in fungi and may be responsible for the fungistatic activity of fluconazole Additive: TMP-SMX Y-site: Amphotericin B, amphotericin B cholesteryl sulfate, ampicillin, calcium gluconate, cefotaxime, ceftazidime(? ), ceftriaxone, cefuroxime, chloramphenicol, clindamycin, co-trimoxazole, diazepam, digoxin, erythromycin lactobionate, furosemide, haloperidol, hydroxyzine, imipenem/cilastatin, pentamidine, piperacillin, ticarcillin, TMP-SMX Solution: D5W, LR Additive: Acyclovir, amikacin, amphotericin B, cefazolin, ceftazidime, ciprofloxacin, clindamycin, gentamicin, heparin, meropenem, metronidazole, morphine, piperacillin, potassium chloride, ranitidine with ondansetron, theophylline Y-site: Acyclovir, aldesleukin, allopurinol, amifostine, amikacin, aminophylline, amiodarone, ampicillin-sulbactam, aztreonam, benztropine, bivalirudin, cefazolin, cefepime, cefotetan, cefoxitin, cefpirome, chlorpromazine, cimetidine, cisatracurium, dexamethasone sodium phosphate, dexmedetomidine, diltiazem, diphenhydramine, dobutamine, docetaxel, dopamine, doxorubicin liposomal, droperidol, etoposide PO4, famotidine, fenoldopam, filgrastim, fludarabine, foscarnet, ganciclovir, gatifloxacin, gemcitabine, gentamicin, granisetron, heparin, hetastarch, hydrocortisone, immune globulin, leucovorin, linezolid, lorazepam, melphalan, meperidine, meropenem, metoclopramide, metronidazole, midazolam, morphine, nafcillin, nitroglycerin, ondansetron, oxacillin, paclitaxel, pancuronium, penicillin G, phenytoin, piperacillin-tazobactam, prochlorperazine, promethazine, propofol, quinupristin-dalfopristin, ranitidine, remifentanil, sargramostim, tacrolimus, teniposide, theophylline, thiotepa, ticarcillin-clavulanate, tobramycin, vancomycin, vecuronium, vinorelbine, zidovudine Tablets: Store below 86° F (30° C) Dry powder: Store below 86° F (30° C); reconstituted suspension should be stored between 86° F (30° C) and 41° F (5° C), and unused portion should be discarded after 2 weeks; protect from freezing Injection (glass bottles): Store between 86° F (30° C) and 41° F (5° C); protect from freezing Injection (Viaflex Plus plastic containers): Store between 77° F (25° C) and 41° F (5° C); protect from freezing The above information is provided for general informational and educational purposes only. Individual plans may vary and formulary information changes. Contact the applicable plan provider for the most current information. Fluconazole is an antifungal medication used in the treatment of several fungal infections. Fluconazole widely distributes into body tissues, nails and fluids including saliva, sputum, vaginal secretions. Fluconazole does not undergo first pass metabolism and is excreted mostly in the urine and some in the feces. This drug can also be used in the pediatric population. Mechanism: Fluconazole works by altering the fungal cell membrane. It exerts its fungistatic effect by selectively inhibiting 14-alpha demethylase. This is a cytochrome P-450 enzyme that is necessary for synthesizing ergosterol, which is an important component of the fungal cell membrane. 14-alpha demethylase converts lanosterol to ergosterol. Without ergosterol, 14 alpha-methyl sterols increase which subsequently causes the fungal cell membrane to exhibit increased cellular permeability.
are responsible for most of the fungal infections in humans. Available since 1990, fluconazole is well established as a leading drug in the setting of prevention and treatment of mucosal and invasive candidiasis. Fluconazole displays predictable pharmacokinetics and an excellent tolerance profile in all groups, including the elderly and children. Fluconazole is a fungistatic drug against yeasts and lacks activity against moulds. Emergence of azole-resistant strains as well as discovery of new antifungal drugs (new triazoles and echinocandins) have raised important questions about its use as a first line drug. The aim of this review is to summarize the main available data on the position of fluconazole in the prophylaxis or curative treatment of invasive spp. Fluconazole is still a major drug for antifungal prophylaxis in the setting of transplantation (solid organ and bone marrow), intensive care unit, and in neutropenic patients. Prophylactic fluconazole still has a place in HIV-positive patients in viro-immunological failure with recurrent mucosal candidiasis. Fluconazole can be used in adult neutropenic patients with systemic candidiasis, as long as the species identified is a priori susceptible. Antifungal, in the same drug family as ketoconazole and itraconazole. Fluconazole has many advantages over the other antifungal drugs including the option of oral administration.
Fluconazole is used to treat serious fungal or yeast infections, such as vaginal candidiasis, oropharyngeal candidiasis thrush, oral thrush, esophageal. Mechanism of Action. Fluconazole is a highly selective inhibitor of fungal cytochrome P450 dependent enzyme lanosterol 14-α-demethylase. This enzyme.