flu·con·a·zole (fl -k n  -z l , -kn-)n. A broad-spectrum antifungal agent used especially to treat candidiasis and infections caused by Cryptococcus neoformans. |
fluconazole [floo-kon´ah-zōl]
fluconazole
zōl), n brand name: Diflucan;
drug class: antifungal;
action: inhibits ergosterol biosynthesis;
uses: oropharyngeal candidiasis, urinary candidiasis, cryptococcal meningitis, vaginal candidiasis.
fluconazole
Canesten Oral (UK), Diflucan
Pharmacologic class: Synthetic azole
Therapeutic class: Systemic antifungal
Pregnancy risk category C
Action
Alters cellular membrane, increasing permeability and leakage of essential elements needed for fungal growth. At higher concentrations, may be fungicidal.
Availability
Injection: 2 mg/ml in 100- or 200-ml bottles or containers
Powder for oral suspension: 50 mg/5 ml in 35-ml bottle, 200 mg/5 ml in 35-ml bottle
Tablets: 50 mg, 100 mg, 150 mg, 200 mg
⊘Indications and dosages
➣ Oropharyngeal candidiasis
Adults: 200 mg P.O. or I.V. on first day, followed by 100 mg/day for at least 2 weeks
Children: 6 mg/kg P.O. or I.V. on first day, followed by 3 mg/kg/day for at least 2 weeks
➣ Esophageal candidiasis
Adults: 200 mg P.O. or I.V. on first day, followed by 100 mg/day for 3 weeks and then for 2 weeks after symptom resolution. Up to 400 mg/day may be used in severe cases.
Children: 6 mg/kg P.O. or I.V. on first day, followed by 3 mg/kg/day for 3 weeks and for at least 2 weeks after symptom resolution
➣ Systemic candidiasis
Adults: 400 mg P.O. or I.V. on first day, followed by 200 mg/day for 4 weeks and for at least 2 weeks after symptom resolution
Children: 6 to 12 mg/kg/day P.O. or I.V.
➣ Vaginal candidiasis
Adults: 150 mg P.O. as a single dose
➣ Cryptococcal meningitis
Adults: 400 mg P.O. or I.V. on first day, followed by 200 or 400 mg/day for 10 to 12 weeks after cerebrospinal fluid (CSF) is negative
Children: 12 mg/kg P.O. or I.V. on first day, followed by 6 mg/kg/day for 10 to 12 weeks after CSF is negative
➣ Suppression of cryptococcal meningitis in patients with AIDS
Adults: 200 mg/day P.O. or I.V.
➣ To prevent candidiasis after bone marrow transplantation
Adults: 400 mg/day P.O. or I.V. for several days before and 7 days after neutrophil count rises above 1,000 cells/mm3
Dosage adjustment
• Renal impairment
• Elderly patients
Contraindications
• Hypersensitivity to drug or its components
Precautions
Use cautiously in:
• hypersensitivity to other azole antifungals
• renal impairment or hepatic disease
• pregnant or breastfeeding patients
• children younger than 6 months.
Administration
☞ Limit single I.V. infusion to 200 mg/hour or less, using infusion pump.
• Don't piggyback with other I.V. infusions.
• Keep overwrap on I.V. bag until just before use.
• Know that plastic container may be opaque (from moisture absorbed during sterilization). This doesn't affect drug and will decrease over time.
| Route | Onset | Peak | Duration |
| P.O. | Slow | 1-2 hr | 2-4 days |
| I.V. | Rapid | 1 hr | 2-4 days |
Adverse reactions
CNS: headache, dizziness
GI: nausea, vomiting, diarrhea, dyspepsia, abdominal discomfort
Hematologic: leukopenia, thrombocytopenia
Hepatic: hepatotoxicity
Skin: rash, pruritus, exfoliative skin disorders (including Stevens-Johnson syndrome )
Other: altered taste, anaphylaxis
Interactions
Drug-drug. Alfentanil, cyclosporine, phenytoin, rifabutin, tacrolimus, theophylline, zidovudine: increased blood levels of these drugs, greater risk of toxicity
Benzodiazepines, buspirone, losartan, nisoldipine, tricyclic antidepressants, zolpidem: increased blood levels and effects of these drugs
CYP3A4 inducers: inhibited CYP3A4 enzyme system, altered actions of CYP3A4 inducers (with fluconazole dosages above 200 mg/day)
Glipizide, glyburide, tolbutamide: increased hypoglycemic effect of these drugs
Rifampin: increased rifampin blood level, decreased fluconazole blood level
Thiazide diuretics: increased fluconazole blood level
Warfarin: increased warfarin activity
Drug-diagnostic tests. Alanine aminotransferase, alkaline phosphatase, bilirubin, gamma-glutamyltransferase, hepatic enzymes: increased levels
Platelets, white blood cells: decreased counts
Patient monitoring
☞ Stay alert for signs and symptoms of anaphylaxis. Stop drug immediately if these occur.
• Monitor liver function test results and hematologic studies.
☞ Assess for rash; if lesions develop, monitor patient. Stop drug and notify prescriber if lesions progress (may signal Stevens-Johnson syndrome).
• Be aware that patients with human immunodeficiency virus have greater risk of adverse reactions.
Patient teaching
☞ Teach patient how to recognize and immediately report signs and symptoms of allergic response.
• Urge patient to contact prescriber if rash occurs, to determine whether Stevens-Johnson syndrome is developing.
• Caution patient to avoid driving and other hazardous activities until he knows how drug affects concentration and alertness.
• Advise patient to minimize GI upset by eating frequent, small servings of food and drinking adequate fluids.
• Tell female patient to inform prescriber if she is pregnant or breastfeeding.
• As appropriate, review all other significant and life-threatening adverse reactions and interactions, especially those related to the drugs and tests mentioned above.
fluconazole
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