Fluconazole
Fluconazole (Diflucan)
Fluconazole
(flew- KON-ah-zohl)
Pregnancy Category: C Diflucan Difulcan-150 (Rx)

Classification: Antifungal agent

Action/Kinetics: Inhibits the enzyme cytochrome P-450 in the organism, which results in a decrease in cell wall integrity and extrusion of intracellular material, leading to death. Apparently does not affect the cytochrome P-450 enzyme in animals or humans. Peak plasma levels: 1-2 hr. t 1/2: 30 hr, which allows for once daily dosing. Penetrates all body fluids at steady state. Bioavailability is not affected by agents that increase gastric pH. Eighty percent of the drug is excreted unchanged by the kidneys.

Uses: Oropharyngeal and esophageal candidiasis. Serious systemic candidal infection (including UTIs, peritonitis, and pneumonia). Cryptococcal meningitis. Maintenance therapy to prevent cryptococcal meningitis in AIDS clients. Vaginal candidiasis. To decrease the incidence of candidiasis in clients undergoing a bone marrow transplant who receive cytotoxic chemotherapy or radiation therapy. Treatment of cryptococcal meningitis and candidal infections in children.

Contraindications: Hypersensitivity to fluconazole.

Special Concerns: Use with caution during lactation and if client shows hypersensitivity to other azoles. Efficacy has not been adequately assessed in children.

Side Effects: Following single doses. GI: Nausea, abdominal pain, diarrhea, dyspepsia, taste perversion. CNS: Headache, dizziness. Other: Angioedema, anaphylaxis (rare).
Following multiple doses. Side effects are more frequently reported in HIV-infected clients than in non-HIV-infected clients. GI: N&V;, abdominal pain, diarrhea, serious hepatic reactions. CNS: Headache, seizures. Dermatologic: Skin rash, exfoliative skin disorders (including Stevens-Johnson syndrome and toxic epidermal necrolysis), alopecia. Hematologic: Leukopenia, thrombocytopenia. Other: Hypercholesterolemia, hypertriglyceridemia, hypokalemia.

Laboratory Test Alterations: AST, serum transaminase (especially if used with isoniazid, oral hypoglycemic agents, phenytoin, rifampin, valproic acid).

Drug Interactions: Alfentanil / Plasma alfentanil levels Cimetidine / Fluconazole plasma levels Cisapride / Risk of serious cardiac arrhythmias Cyclosporine / Cyclosporine levels in renal transplant clients with or without impaired renal function Glipizide / Plasma glipizide levels R/T liver breakdown Glyburide / Plasma glyburide levels R/T liver breakdown Hydrochlorothiazide / Plasma fluconazole levels R/T renal clearance Phenytoin / Plasma phenytoin levels Rifampin / Plasma fluconazole levels R/T liver breakdown Theophylline / Plasma theophylline levels Tolbutamide / Plasma tolbutamide levels R/T liver breakdown Warfarin / PT Zidovudine / Plasma AZT levels Zolpidem / Zolpidem effects

How Supplied: Injection: 2 mg/mL, 200 mg/100 mL, 400 mg/200 mL; Powder for Reconstitution: 50 mg/5mL, 200 mg/5mL; Tablet: 50 mg, 100 mg, 150 mg, 200 mg

Dosage
?Tablets, Oral Suspension, IV Vaginal candidiasis.
150 mg as a single oral dose.
Oropharyngeal or esophageal candidiasis.
Adults, first day: 200 mg; then, 100 mg/day for a minimum of 14 days (for oropharyngeal candidiasis) or 21 days (for esophageal candidiasis). Up to 400 mg/day may be required for esophageal candidiasis. Children, first day: 6 mg/kg; then 3 mg/kg once daily for a minimum of 14 days (for oropharyngeal candidiasis) or 21 days (for esophageal candidiasis).
Candidal UTI and peritonitis.
50-200 mg/day.
Systemic candidiasis (e.g., candidemia, disseminated candidiasis, and pneumonia).
Optimal dosage and duration in adults have not been determined although doses up to 400 mg/day have been used. Children: 6-12 mg/kg/day.
Acute cryptococcal meningitis.
Adults, first day: 400 mg; then, 200 mg/day (up to 400 mg may be required) for 10 to 12 weeks after CSF culture is negative. Children, first day: 12 mg/kg; then 6 mg/kg once daily for 10 to 12 weeks after CSF culture is negative.
Maintenance to prevent relapse of cryptococcal meningitis in AIDS clients.
Adults: 200 mg once daily. Pediatric: 6 mg/kg once daily.
Prevention of candidiasis in bone marrow transplant.
400 mg once daily. In clients expected to have severe granulocytopenia (less than 500 neutrophils/mm ³), start fluconazole several days before the anticipated onset of neutropenia and continue for 7 days after the neutrophil count rises about 1,000 cells/mm ³. In clients with renal impairment, an initial loading dose of 50-400 mg can be given; daily dose is based then on C _CR.