fluconazole

fluconazole

(floo kon' a zole)

Diflucan

Pregnancy Category C

Drug class

Antifungal

Therapeutic actions

Binds to sterols in the fungal cell membrane, changing membrane permeability; fungicidal or fungistatic depending on concentration and organism.

Indications

·        Treatment of oropharyngeal, esophageal, vaginal, and systemic candidiasis

·        Treatment of cryptococcal meningitis

·        Prophylaxis of candidiasis in bone marrow transplants

Contraindications and cautions

·        Contraindicated with hypersensitivity to fluconazole, lactation.

·        Use cautiously with renal or hepatic impairment.

Available forms

Tablets—50, 100, 150, 200 mg; powder for oral suspension—10, 40 mg/mL; injection—2 mg/mL

Dosages

Individualize dosage; same for oral or IV routes because of rapid and almost complete absorption.

ADULTS

·        Oropharyngeal candidiasis: 200 mg PO or IV on the first day, followed by 100 mg daily. Continue treatment for at least 2 wk to decrease likelihood of relapse.

·        Esophageal candidiasis: 200 mg PO or IV on the first day, followed by 100 mg daily. Dosage up to 400 mg/day may be used in severe cases. Treat for a minimum of 3 wk; at least 2 wk after resolution.

·        Systemic candidiasis: 400 mg PO or IV on the first day, followed by 200 mg daily. Treat for a minimum of 4 wk; at least 2 wk after resolution.

·        Vaginal candidiasis: 150 mg PO as a single dose.

·        Cryptococcal meningitis: 400 mg PO or IV on the first day, followed by 200 mg daily. 400 mg daily may be needed. Continue treatment for 10–12 wk after cultures of CSF become negative.

·        Suppression of cryptococcal meningitis in AIDS patients: 200 mg daily PO or IV.

·        Prevention of candidiasis in bone marrow transplants: 400 mg PO daily for several days before and 7 days after neutropenia.

PEDIATRIC PATIENTS

·        Oropharyngeal candidiasis: 6 mg/kg PO or IV on the first day, followed by 3 mg/kg once daily for at least 2 wk.

·        Esophageal candidiasis: 6 mg/kg PO or IV on the first day, followed by 3 mg/kg once daily. Treat for a minimum of 3 wk; at least 2 wk after resolution.

·        Systemic Candida infections: Daily doses of 6–12 mg/kg/day PO or IV.

·        Cryptococcal meningitis: 12 mg/kg PO or IV on the first day, followed by 6 mg/kg once daily. Continue treatment for 10–12 wk after cultures of CSF become negative.

·        Suppression of cryptococcal meningitis in children with AIDS: 6 mg/kg daily PO or IV.

PATIENTS WITH RENAL IMPAIRMENT

Initial dose of 50–400 mg PO or IV. If creatinine clearance > 50 mL/min, use 100% recommended dose; for creatinine clearance 21–50 mL/min, use 50% of the recommended dose; for creatinine clearance 11–20 mL/min, use 25% of recommended dose; for patients on hemodialysis, use one dose after each dialysis.

Pharmacokinetics

Route	Onset	Peak	Duration
Oral	Slow	1–2 hr	2–4 days
IV	Rapid	1 hr	2–4 days

Metabolism: Hepatic; T_1/2: 30 hr

Distribution: Crosses placenta; may enter breast milk

Excretion: Urine

IV facts

Preparation: Do not remove overwrap until ready for use. Inner bag maintains sterility of product. Do not use plastic containers in series connections. Tearoverwrap down side at slit, and remove solution container. Some opacity of plastic may occur; check for minute leaks, squeezing bag firmly. Discard solution if any leaks are found.

Infusion: Infuse at a maximum rate of 200 mg/hr given as a continuous infusion.

Incompatibilities: Do not add any supplementary medications.

Adverse effects

·        CNS: Headache

·        GI: Nausea, vomiting, diarrhea, abdominal pain; AST/ALT elevations

·        Other: Rash

Interactions

Drug-drug

·        Increased serum levels and therefore therapeutic and toxic effects of cyclosporine, phenytoin, benzodiazepines, oral hypoglycemics, warfarin anticoagulants,zidovudine

·        Decreased serum levels with rifampin, theophylline, tacrolimus

Nursing considerations

Assessment

·        History: Hypersensitivity to fluconazole, renal impairment, lactation, pregnancy

·        Physical: Skin color, lesions; T; injection site; orientation, reflexes, affect; bowel sounds; LFTs, renal function tests; CBC and differential; culture of area involved

Interventions

·        Culture infection before therapy; begin treatment before lab results are returned.

·        Decrease dosage in cases of renal failure.

·        Infuse IV only; not intended for IM or subcutaneous use.

·        Do not add supplement medication to fluconazole.

·        Administer through sterile equipment at a maximum rate of 200 mg/hr given as a continuous infusion.

·        WARNING: Monitor renal function tests weekly, discontinue or decrease dosage of drug at any sign of increased renal toxicity. Monitor LFTs monthly during therapy.

Teaching points

·        Drug may be given orally or IV as needed. The drug will need to be taken for the full course and may need to be taken long term.

·        Use hygiene measures to prevent reinfection or spread of infection.

·        Arrange for frequent follow-up while you are taking this drug. Be sure to keep all appointments, including those for blood tests.

·        You may experience these side effects: Nausea, vomiting, diarrhea (frequent small meals may help); headache (analgesics may be ordered).

·        Report rash, changes in stool or urine color, difficulty breathing, increased tears or salivation.

Adverse effects in Italic are most common; those in Bold are life-threatening.