No

Antifungal Agent, Oral; Antifungal Agent, Parenteral

Indications for use in adult patients: Oral or vaginal candidiasis unresponsive to nystatin or clotrimazole; nonlife-threatening Candida infections (eg, cystitis, esophagitis); treatment of hepatosplenic candidiasis and other Candida infections in persons unable to tolerate amphotericin B; treatment of cryptococcal infections; secondary prophylaxis for cryptococcal meningitis in persons with AIDS; antifungal prophylaxis in allogeneic bone marrow transplant recipients

C

Known hypersensitivity to fluconazole or other azoles; concomitant administration with terfenadine

Should be used with caution in patients with renal and hepatic dysfunction or previous hepatotoxicity from other azole derivatives. Patients who develop abnormal liver function tests during fluconazole therapy should be monitored closely and discontinued if symptoms consistent with liver disease develop. Should be used with caution in patients receiving cisapride or astemizole.

1% to 10%:

Central nervous system: Headache

Dermatologic: Rash

Gastrointestinal: Nausea, vomiting, abdominal pain, diarrhea

<1%: Pallor, dizziness, hypokalemia, increased AST/ALT, or alkaline phosphatase

Symptoms of overdose include decreased lacrimation, salivation, respiration and motility, urinary incontinence, cyanosis

Treatment includes supportive measures, a 3-hour hemodialysis will remove 50%

CYP2C9 enzyme inducer; CYP2C9, 2C18, and 2C19 enzyme inhibitor and CYP3A3/4 enzyme inhibitor (weak)

Increased effect/toxicity:

Coadministration with terfenadine or cisapride is contraindicated; use with caution with astemizole due to increased risk of significant cardiotoxicity

Hydrochlorothiazide may decrease fluconazole clearance

Fluconazole may also inhibit warfarin, phenytoin, cyclosporine, and theophylline, zidovudine, sulfonylureas, rifabutin, and warfarin clearance

Nephrotoxicity of tacrolimus may be increased

Parenteral admixture at room temperature (25°C): Manufacturer expiration dating; do not refrigerate

Interferes with cytochrome P-450 activity, decreasing ergosterol synthesis (principal sterol in fungal cell membrane) and inhibiting cell membrane formation

Distribution: Widely distributed throughout body with good penetration into CSF, eye, peritoneal fluid, sputum, skin, and urine; relative diffusion of antimicrobial agents from blood into CSF: Adequate with or without inflammation (exceeds usual MICs)

Ratio of CSF to blood level (%): Normal meninges: 70-80; Inflamed meninges: >70-80

Protein binding, plasma: 11% to 12%

Bioavailability: Oral: >90%

Half-life: 25-30 hours with normal renal function

Time to peak serum concentration: Oral: Within 2-4 hours

Elimination: 80% of a dose excreted unchanged in the urine

The daily dose of fluconazole is the same for oral and I.V. administration

Children: Once-daily dosing by indication:

Oropharyngeal candidiasis:

Day 1: 6 mg/kg; then 3 mg/kg for at least 14 days

Esophageal candidiasis:

Day 1: 6 mg/kg; then 3-12 mg/kg for a minimum of 21 days and for at least 2 weeks following resolution of symptoms

Systemic candidiasis:

6-12 mg/kg/day for at least 28 days

Cryptococcal meningitis:

Day 1: 12 mg/kg; then 6-12 mg/kg for at least 10-12 weeks after CSF culture becomes negative

Cryptococcal meningitis, relapse:

Day 1: 6 mg/kg; then 6 mg/kg for at least 10-12 weeks after CSF culture becomes negative

Adults: Oral, I.V.: Once-daily dosing by indication:

Oropharyngeal candidiasis:

Day 1: 200 mg; then 100 mg/day for at least 14 days

Esophageal candidiasis:

Day 1: 200 mg; then 100 mg/day for a minimum of 21 days and for at least 14 days following resolution of symptoms

Prevention of candidiasis in bone marrow transplant:

Day 1: 400 mg; then 400 mg/day for a minimum of 3 days before neutropenia, 7 days after neutrophils >1000 cells/mm³

Candidiasis UTIs, peritonitis:

50-200 mg/day

Systemic candidiasis:

Day 1: 400 mg; then 200 mg/day for at least 28 days

Cryptococcal meningitis, acute:

Day 1: 400 mg; then 200 mg/day for at least 10-12 weeks after CSF culture becomes negative

Cryptococcal meningitis, relapse:

Day 1: 200 mg; then 200 mg/day for at least 10-12 weeks after CSF culture becomes negative

Vaginal candidiasis:

Day 1: 150 mg single dose

Dosing adjustment/interval in renal impairment:

No adjustment for vaginal candidiasis single-dose therapy

For multiple dosing, administer usual load then adjust daily doses

Cl_cr 11-50 mL/minute: Administer 50% of recommended dose or administer every 48 hours

Hemodialysis: One dose after each dialysis

Continuous arteriovenous or venovenous hemodiafiltration (CAVH) effects: Dose as for Cl_cr 10-50 mL/minute

No data reported

Periodic liver function tests (AST, ALT, alkaline phosphatase) and renal function tests, potassium

May cause dizziness

None reported; CYP3A4 inhibitor; use caution with triazolam and alprazolam

No information available to require special precautions

No effects or complications reported

Take as directed, around-the-clock. Take full course of medication as ordered. Follow good hygiene measures to prevent reinfection. Frequent blood tests may be required. Maintain adequate hydration (2-3 L/day of fluids unless instructed to restrict fluid intake). You may experience headache, dizziness, drowsiness (use caution when driving or engaging in tasks that require alertness until response to drug is known); nausea, vomiting, or diarrhea (small frequent meals, frequent mouth care, sucking lozenges, or chewing gum may help). Report skin rash, redness, or irritation; persistent GI upset; urinary pattern changes; excessively dry eyes or mouth; changes in color of stool or urine. Pregnancy/breast-feeding precautions: Inform prescriber if you are or intend to be pregnant. Consult prescriber if breast-feeding.

Parenteral fluconazole must be administered by I.V. infusion over ~1-2 hours; do not exceed 200 mg/hour when administering I.V. infusion; final concentration for administration of 2 mg/mL; do not unwrap unit until ready for use; do not use if cloudy or precipitated

Injection: 2 mg/mL (100 mL, 200 mL)

Powder for oral suspension: 10 mg/mL (35 mL); 40 mg/mL (35 mL)

Tablet: 50 mg, 100 mg, 150 mg, 200 mg

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