FLUCONAZOLE

FLUCONAZOLE
(flu-con'a-zole)
Diflucan
Classifications: antibiotic; azole antifungal;
Therapeutic: azole antifungal antibiotic

Pregnancy Category: C

Availability

50 mg, 100 mg, 150 mg, 200 mg tablets; 10 mg/mL, 40 mg/mL suspension; 2 mg/mL injection

Action

Fungistatic, but may also be fungicidal depending on concentration. Interferes with formation of ergosterol, the principal sterol in the fungal cell membrane leading to cell death.

Therapeutic Effect

Antifungal properties are related to the drug effect on the functioning of fungal cell membrane.

Uses

Cryptococcal meningitis and oropharyngeal and systemic candidiasis, both commonly found in AIDS and other immunocompromised patients; vaginal candidiasis.

Contraindications

Hypersensitivity to fluconazole or other azole antifungals; pregnancy (category C).

Cautious Use

AIDS or malignancy; hepatic impairment; structural cardiac disease; history of torsades de pointes; renal impairment or failure; lactation.

Route & Dosage

Oropharyngeal Candidiasis
Adult: PO/IV 200 mg day 1, then 100 mg/d x 14 d
Child: PO/IV 3–6 mg/kg/d x 14 d

Esophageal Candidiasis
Adult: PO/IV 200 mg day 1, then 100 mg q.d. x 3 wk
Child/Infant: PO/IV 3–6 mg/kg/d x 21 d

Systemic Candidemia
Adult: PO/IV 400 mg day 1, then 200 mg q.d. x 4 wk
Child/Infant/Nenonate (>14 d): PO/IV 6 mg/kg q12h x 28 d
Neonate (0–14 d): IV 6 mg/kg q72h

Vaginal Candidiasis
Adult: PO 150 mg x 1 dose

Cryptococcal Meningitis
Adult: PO/IV 400 mg day 1, then 200 mg q.d. x 10–12 wk
Child/Infant/Neonate (>14 d): PO/IV 12 mg/kg day 1, then 6–12 mg/kg/d x 10–12 wk
Neonate (0–14 d): IV 6–12 mg/kg day 1, then 6–12 mg/kg q48h
Premature Neonates (0–14 d): IV 5–6 mg/kg q72h

Renal Impairment
Clcr ≤50 mL/min (without concurrent dialysis): give 50% of maintenance dose
Dialysis: Administer full dose post-dialysis

Administration

Oral
  • Take this medication for the full course of therapy, which may take weeks or months.
  • Take next dose as soon as possible if you miss a dose; however, do not take a dose if it is almost time for next dose. Do not double dose.
Intravenous

PREPARE: Continuous: Packaged ready for use as a 2 mg/mL solution. Remove wrapper just prior to use.  

ADMINISTER: Continuous: Give at a maximum rate of approximately 200 mg/h. Give after hemodialysis is completed.  

  • Do not use IV admixtures of fluconazole and other medications.

INCOMPATIBILITIES Solution/additive: Trimethoprim-sulfamethoxazole. Y-site: Amphotericin B, amphotericin B cholesteryl, ampicillin, calcium gluconate, cefotaxime, ceftazidime, ceftriaxone, cefuroxime, chloramphenicol, clindamycin, diazepam, digoxin, erythromycin, furosemide, haloperidol, hydroxyzine, imipenem-cilastatin, pentamidine, piperacillin, ticarcillin, trimethoprim-sulfamethoxazole.

Adverse Effects (≥1%)

CNS: Headache. GI: Nausea, vomiting, abdominal pain, diarrhea, increase in AST in patients with cryptococcal meningitis and AIDS. Skin: Rash.

Interactions

Drug: Increased PT in patients on warfarin; may increase alosetron, bexarotene, phenytoin, cevimeline, cilostazol, cyclosporine, dihydroergotamine, ergotamine, dofetilide, haloperidol, levobupivacaine, modafinil, zonisamide levels and toxicity; hypoglycemic reactions with oral sulfonylureas; decreased fluconazole levels with rifampin, cimetidine; may prolong the effects of fentanyl, alfentanil, methadone.

Pharmacokinetics

Absorption: 90% from GI tract. Peak: 1–2 h. Distribution: Widely distributed, including CSF. Metabolism: 11% of dose metabolized in liver. Elimination: In urine. Half-Life: 20–50 h.

Nursing Implications

Assessment & Drug Effects

  • Monitor for allergic response. Patients allergic to other azole antifungals may be allergic to fluconazole.
  • Lab tests: Monitor BUN, serum creatinine, and liver function.
  • Note: Drug may cause elevations of the following laboratory serum values: ALT, AST, alkaline phosphatase, bilirubin.
  • Monitor for S&S of hepatotoxicity.

Patient & Family Education

  • Monitor carefully for loss of glycemic control if diabetic.
  • Inform physician of all medications being taken.

Common adverse effects in italic, life-threatening effects underlined; generic names in bold; classifications in SMALL CAPS; Canadian drug name; Prototype drug

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