Fluconazole

3
Fluconazole
Brands

DEA Class; Rx

Common Brand Names; Diflucan

  • Antifungals, Systemic; 

First triazole synthetic antifungal agent
Used for treatment of various Candida infections, cryptococcal meningitis, and prophylaxis in BMT patients
Associated with increased incidence of Candida krusei when used for prophylaxis

Indicated for treatment of
  • Oropharyngeal Candidiasis
  • Esophageal Candidiasis
  • Cryptococcal Meningitis
  • Vaginal Candidiasis
  • Candida UTI/Peritonitis

Prevention of candidiasis incidence in patients undergoing bone marrow transplant

Hypersensitivity

Pregnancy

Concurrent QT-prolonging drugs that are metabolized via the enzyme CYP3A4 (cisapride, erythromycin, pimozide, and quinidine)

  • Headache (2-13%)
  • Nausea (2-7%)
  • Abdominal pain (2-6%)
  • Diarrhea (2-3%)
  • Rash (2%)
  • Vomiting (2-5%)
  • 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%)

Secreted in human milk at concentrations similar to maternal plasma concentrations; use caution (AAP Committee states “compatible with nursing”)

Adults

400 mg/day PO/IV is FDA-approved; however, up to 1,200 mg/day PO/IV has been used off-label.

Geriatric

400 mg/day PO/IV is FDA-approved; however, up to 1,200 mg/day PO/IV has been used off-label.

Adolescents

12 mg/kg/day (Max: 600 mg/day) PO/IV is FDA-approved; however, up to 1,200 mg/day PO/IV has been used off-label.

Children

12 mg/kg/day (Max: 600 mg/day) PO/IV is FDA-approved; however, up to 800 mg/day PO/IV has been used off-label.

Infants

6 to 12 months: 12 mg/kg/day PO/IV.
1 to 5 months: Safety and efficacy have not been established; however, up to 12 mg/kg/day PO/IV has been used off-label.

Neonates

Safety and efficacy have not been established; however, 25 mg/kg PO/IV loading dose, then up to 12 mg/kg/day PO/IV has been used off-label.

Fluconazole

injection solution

  • 2mg/mL

oral suspension

  • 10mg/mL
  • 40mg/mL

tablet

  • 50mg
  • 100mg
  • 150mg
  • 200mg
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