Fluconazole

A to Z Drug Facts

 Action Interferes with the formation of fungal cell membrane, causing leakage of cellular contents and cell death.

 Indications Oropharyngeal and esophageal candidiasis; vaginal candidiasis; prevention of candidiasis in bone marrow transplant; cryptococcal meningitis.

 Contraindications Standard considerations.

 Route/Dosage

Oropharyngeal or esophageal candidiasis

ADULTS: PO/IV 200 mg first day, followed by 100 mg qd thereafter for minimum of 2 wk for oropharyngeal candidiasis or 3 wk for esophageal candidiasis. CHILDREN: PO/IV 6 mg/kg on first day, followed by 3 mg/kg qd thereafter for minimum of 2 wk for oropharyngeal candidiasis or 3 wk (at least 2 weeks after symptom resolution) for esophageal candidiasis.

Vaginal candidiasis

ADULTS: PO 150 mg single dose.

Prevention of candidiasis in bone marrow transplant

ADULTS: PO/IV 400 mg once daily; in patients with anticipated severe granulocytopenia (< 500 neutrophils/mm³) start fluconazole several days before anticipated onset and continue 7 days after neutrophil count rises > 1000 cells/mm³.

Cryptococcal meningitis

ADULTS: PO/IV 400 mg first day, followed by 200 mg qd thereafter (400 mg may be used) for 10 to 12 wk after CSF culture is negative for initial meningitis; 200 mg qd for suppression of relapse of cryptococcal meningitis.

Candidemia and disseminated candida infections

CHILDREN: PO/IV 6 to 12 mg/kg/day.

Cryptococcal 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 weeks after CSF becomes culture negative.

Suppression of relapse in AIDS patients– 6 mg/kg/day. NEONATES: Experience is limited to pharmacokinetic studies in premature newborns. Prolonged half-life 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 hr. After the first 2 wk, dose once daily.

 Interactions

Anticoagulants (eg, warfarin): Anticoagulant effect may be increased. Alfentanil, benzodiazepines (eg, midazolam), buspirone, corticosteroids (eg, prednisone), nisoldipine, tacrolimus, vinca alkaloids (eg, vincristine): Levels may be elevated by fluconazole, increasing the risk of side effects and toxicity. Cyclosporine: Increased cyclosporine concentrations. Hydantoins (eg, phenytoin): Increased hydantoin levels. Rifamycins (eg, rifampin): Fluconazole plasma levels may be reduced, decreasing therapeutic effects.

 Lab Test Interferences Elevated transaminase levels. Coumadin: Increased PT may occur in patient receiving warfarin.

 Adverse Reactions

CNS: Headache; seizures. DERM: Rash, exfoliative skin disorder. GI: Nausea; vomiting; abdominal pain; diarrhea. HEMA: Leukopenia; thrombocytopenia. HEPA: Hepatic reactions, including abnormal liver function test results, hepatitis, cholestasis, hepatic failure.

 Precautions

Pregnancy: Category C. Lactation: Excreted in breast milk. Children: Efficacy not established; some patients 3 to 13 yr have been treated safely with 3 to 6 mg/kg/day. Anaphylaxis: Has occurred rarely. Dermatologic changes: Exfoliative skin disorders have been reported. Hepatic injury: Patients with abnormal liver function test results should be monitored for development of more severe hepatic injury. Immunocompromised patients: To prevent relapse, patients with AIDS and cryptococcal meningitis usually require maintenance therapy. Renal impairment: Dosage reduction based on creatinine clearance may be necessary.

 Administration/Storage

• Do not administer if solution is cloudy or if precipitate is present.
• Do not add supplemental medications to IV infusion.
• Administer IV infusion at maximum rate of 200 mg/hr.

 Assessment/Interventions

• Obtain patient history, including drug history and any known allergies. Note renal impairment and sensitivity to fluconazole or other azoles.
• Obtain baseline BUN and creatinine levels.
• Ensure that baseline liver function tests have been obtained and monitor at regular intervals during treatment.
• Assess skin for rashes before beginning therapy and q 8 hr during treatment.
• If patient is receiving anticoagulants, assess for bleeding. Monitor coagulation studies closely.
• For patients also receiving coumadin, monitor PT for possible increased levels.
• If patient develops signs and symptoms of liver disease or new rash during therapy, notify physician.

 Patient/Family Education

• Emphasize importance of taking drug for full course of therapy, which may be several weeks.
• Tell patient that if dose is missed, it should be taken as soon as possible. If close to next dose, do not double up; take next dose as scheduled.
• Instruct patient to report the following symptoms to physician: Nausea, vomiting, right upper quadrant abdominal pain, diarrhea, headache, rash.

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Copyright © 2003 Facts and Comparisons
David S. Tatro
A to Z Drug Facts