fluconazole(redirected from Apo-Fluconazole)
Also found in: Dictionary.
Pharmacologic class: Synthetic azole
Therapeutic class: Systemic antifungal
Pregnancy risk category C
Alters cellular membrane, increasing permeability and leakage of essential elements needed for fungal growth. At higher concentrations, may be fungicidal.
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
➣ Candidal urinary tract infection; peritonitis
Adults: 50 to 200 mg P.O. or I.V. daily
➣ 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
• Renal impairment
• Elderly patients
• Hypersensitivity to drug or its components
• Concurrent use of terfenadine (not available in U.S.) in patients receiving fluconazole at multiple doses of 400 mg or higher and other drugs known to prolong QT interval and that are metabolized via CYP3A4, such as cisapride, astemizole (not available in U.S.), pimozide, and quinidine
Use cautiously in:
• hypersensitivity to other azole antifungals
• renal impairment or hepatic disease
• potentially proarrhythmic conditions
• concurrent use of erythromycin because of potential for increased risk of prolonged QT interval, torsades de pointes, and consequently sudden death (avoid use)
• pregnant or breastfeeding patients
• children younger than 6 months.
☞ 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.
• Be aware that powder for oral suspension contains sucrose and shouldn't be used in patients with hereditary fructose intolerance, glucose-galactose malabsorption, and sucrase-isomaltase deficiency.
CNS: headache, dizziness
CV: QT interval prolongation, torsades de pointes
GI: nausea, vomiting, diarrhea, dyspepsia, abdominal discomfort
Hematologic: leukopenia, thrombocytopenia
Skin: rash, pruritus, exfoliative skin disorders (including Stevens-Johnson syndrome)
Other: altered taste, anaphylaxis
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
☞ Stay alert for signs and symptoms of anaphylaxis. Stop drug immediately if these occur.
☞ Monitor liver function test results and hematologic studies; discontinue drug if clinical signs and symptoms consistent with liver disease develop that may be attributable to fluconazole.
☞ 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.
☞ 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.