Trade Names:Diflucan- Tablets 50 mg- Tablets 100 mg- Tablets 150 mg- Tablets 200 mg- Powder for Oral Suspension 10 mg/mL when reconstituted- Powder for Oral Suspension 40 mg/mL when reconstituted- Injection 2 mg/mLApo-Fluconazole (Canada)Apo-Fluconazole-150 (Canada)Diflucan-150 (Canada)Gen-Fluconazole (Canada)PMS-Fluconazole (Canada)
Interferes with the formation of fungal cell membrane, causing leakage of cellular contents and cell death.
Bioavailability is more than 90%. T max is 1 to 2 h.
Apparent Vd is 0.65 L/kg, and it is 11% to 12% protein bound. Ratio of tissue (fluid) concentrations to concurrent plasma concentrations is as follows: CSF, 0.5 to 0.9; saliva, 1; sputum, 1; blister fluid, 1; urine, 10; normal skin, 10; nails, 1; blister skin, 2; vaginal tissue, 1; and vaginal fluid, 0.4 to 0.7.
Mean body Cl is 0.23 mL/min/kg; t ½ is 20 to 50 h. The drug is cleared primarily by renal excretion, about 80% in urine as unchanged drug and 11% excreted in urine as metabolites.Hemodialysis
A 3-h session decreases plasma concentrations about 50%.
Pharmacokinetics are markedly affected; there is an inverse relationship between t ½ and CrCl.Children9 mo to 15 yr of age
Mean Cl is 0.4 to 0.66 mL/min/kg; t ½ is 15.2 to 25 h. C max is 2.9 to 14.1 mcg/mL; Vd ss is 0.722 to 1.069.Neonates (gestational age 26 to 29 wk)
Mean Cl is 0.18 to 0.333 mL/min/kg (increases with time after birth); t ½ is 73.6 to 46.6 h (decreases with time after birth).
Oropharyngeal and esophageal candidiasis; vaginal candidiasis; prevention of candidiasis in bone marrow transplant; Cryptococcal meningitis .
Coadministration of cisapride; hypersensitivity to any component of the product.
PO / IV 6 to 12 mg/kg/day.C. meningitis
12 mg/kg on first day, followed by 6 mg/kg/day (or 12 mg/kg/day based on medical judgment of patient's response). Recommended duration is 10 to 12 wk after CSF becomes culture negative.Newborns
Experience is limited to pharmacokinetic studies in premature newborns. Prolonged t ½ has been noted. These children, in the first 2 wk of life, should receive the same mg/kg dosage as other children, but administered every 72 h. After the first 2 wk, dose every day.Cryptococcal MeningitisAdults
PO / IV 400 mg first day, followed by 200 mg every day thereafter (400 mg may be used) for 10 to 12 wk after CSF culture is negative for initial meningitis; 200 mg ever day for suppression of relapse of cryptococcal meningitis.Oropharyngeal or Esophageal CandidiasisAdults
PO / IV 200 mg first day, followed by 100 mg every day thereafter for minimum of 2 wk for oropharyngeal candidiasis, or for 3 wk and at least 2 wk following resolution of symptoms for esophageal candidiasis.Children
PO / IV 6 mg/kg on first day, followed by 3 mg/kg every day thereafter for minimum of 2 wk for oropharyngeal candidiasis or 3 wk (at least 2 wk after symptom resolution) for esophageal candidiasis.Prevention of Candidiasis in Bone Marrow TransplantAdults
PO / IV 400 mg every day; in patients with anticipated severe granulocytopenia (less than 500 neutrophils/mm 3 ), start fluconazole several days before anticipated onset and continue 7 days after neutrophil count rises more than 1,000 cells/mm 3 .Systemic Candida InfectionsAdults
Optimal therapeutic dosage and duration not established; however, in noncomparative studies of small numbers of patients, doses up to 400 mg/day have been used.UTIs and PeritonitisAdults
Daily doses of 50 to 200 mg have been used in open, noncomparative studies of small numbers of patients.Vaginal CandidiasisAdults
PO 150 mg single dose.
Levels may be elevated by fluconazole, increasing the risk of adverse reactions and toxicity.Anticoagulants (eg, warfarin)
Anticoagulant effect may be increased.Cimetidine, rifamycins (eg, rifampin)
Fluconazole plasma levels may be reduced, decreasing therapeutic effects.Cisapride
Contraindicated; increased cisapride plasma levels with cardiotoxicity may occur.Cyclosporine
Increased cyclosporine concentrations.Hydantoins (eg, phenytoin)
Increased hydantoin levels.Hydrochlorothiazide
May increase fluconazole levels, increasing adverse reactions.
None well documented.
QT prolongation (including torsades de pointes).
Skin rash (2%); exfoliative skin disorders (including Stevens-Johnson syndrome and toxic epidermal necrolysis).
Nausea (4% [children 2%]); vomiting (2% [children 5%]); abdominal pain (2% [children 3%]); diarrhea (2%).
Leukopenia (including neutropenia and agranulocytosis); thrombocytopenia.
Hepatitis; cholestasis; fulminant hepatitis.
Category C .
Excreted in breast milk.
An open-label, randomized, controlled trial has shown fluconazole to be effective in children 6 mo to 13 yr of age. Efficacy has not been established in infants younger than 6 mo of age.
Dosage reduction based on CrCl may be necessary.
Anaphylaxis occurred rarely.
Exfoliative skin disorders reported.
Monitor patients with abnormal LFT results for development of more severe hepatic injury.
To prevent relapse, patients with AIDS and cryptococcal meningitis usually require maintenance therapy.
Hallucinations, paranoid behavior.
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