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Fluconazole

Fluconazole is an antifungal azole. It is a broad spectrum antifungal, first approved in Europe in 1988 and then in America in 1990.
It was the first single dose treatment approved for vaginal candidiasis. Fluconazole is an effective agent in the treatment and prophylaxis of Candidal infection

Trade Names:

  • Diflucan*   Roerig
  • Diflucan*   Pfizer

Dosage Types

  • Oral: Tablets: Fluconazole 50, 100, 150, 200mg Diflucan*
  • Capsules: Fluconazole 150mg Diflucan*
  • Suspension: Fluconazole for 10mg/mL or 40 mg/mL Diflucan
  • Parenteral: Fluconazole 200mg/100mL and 400mg/200mL Diflucan*

Uses:

Labeled Indications

Off-Label Uses

Dermatologic
  • Candidiasis, vulvo-vaginalCandidiasis,
  • Oropharyngeal
Dermatologic
  • Onychomycosis
  • Candidiasis, cutaneous #
  • Tinea corporis #
  • Tinea cruris #
  • Tinea pedis #

# - not included in Canadian labeling

 

Therapeutic Regimen

Adult

Pediatric

Vulvovaginal candidiasis
  • Fluconazole capsules 150 mg po x1 dose
Oropharyngeal candidiasis
  • Fluconazole capsules 200 mg po x1, followed by 100mg po daily x 2 weeks
Tinea pedis, cruris, corporis, versicolor (off label)
  • Fluconazole capsules 50 mg po daily x2-6
Dosage has not been established for infants < 6 months old

> 6 months
Oropharyngeal candidiasis
  • Fluconazole oral suspension 3mg/kg x2 weeks

 

Patient Monitoring

Hepatic function tests should be monitored periodically during treatment. Transient increases in transaminases have rarely led to hepatotoxicity in patients receiving fluconazole.

Safety Information

Dose adjustment may be required in patients with renal function impairment.

Side Effects

  • Cutaneous effects may include hypersensitivity reactions including exfoliative dermatitis and Stevens-Johnson syndrome
  • Gastrointestinal effects may include nausea, abdominal pain, diarrhea, constipation, loss of appetite and rarely, hepatotoxicity.
  • Hematologic effects may include agranulocytosis or thrombocytopenia.
  • Other effects may include headache, dizziness and drowsiness.
FDA Pregnancy Category C

Animal studies report rare fetal abnormalities. Not recommended during pregnancy or lactation.

Major Drug Interactions

Concurrent use of antidiabetic agents can lead to hypoglycemia; cyclosporine and phenytoin plasma concentrations may be increased; anticoagulant effects may be increased.

Mechanism of Action / Pharmacokinetics

Fluconazole inhibits ergosterol synthesis in the cell wall of yeast and other fungi.
In Candida albicans, fluconazole may also inhibit the transformation of blastospores into the invasive mycelial form. Fluconazole is absorbed quickly after oral administration and is widely distributed

General References

Saag M, Dismukes WE : Azole antifungal agents : emphasis on the new triazoles. Antimicrob. Agents Chemother. 1988 : 32 : 1 - 8

Drake L, Babel D, Stewart DM, et al : Once-Weekly Fluconazole (150, 300, or 450 mg) in the Treatment of Distal Subungual Onychomycosis of the Fingernail. Jour. Am. Acad. Derm. 1998 : 38 : S87 - S94

Hay RJ, Clayton YM : Fluconazole in the management of patients with chronic mucocutaneous candidiasis. Br. Jour. Derm. 1988 : 119 : 683 - 685

Shahid J, Ihoan Z, Khan S : Oral fluconazole in the treatment of pityriasis versicolor. Jour. Derm. Treat. 2000 : 11 : 101 - 103

Shuttleworth D, Philpot CM, Knight AG : Cutaneous Cryptococcus : treatment with oral fluconazole. Br. Jour. Derm. 1989 : 120 : 683 - 687

Solomon BA, Collins R, Sharma R, et al : Fluconazole for the treatment of tinea capitis in children. Jour. Am. Acad. Derm. 1997 : 37 (2, 1) : 274 - 275

Gupta AK, Adam P, Hofstader SLR, et al : Intermittent short duration therapy with fluconazole is effective for tinea capitis. Br. Jour. Derm 1999 : 141 : 304 - 306

Scher RK, Breneman D, Rich P, et al Once-Weekly Fluconazole (150, 300, or 450mg) in the Treatment of Toenail. Jour. Am. Acad. Derm. 1998 : S77 - S86 Gupta AK, Katz HI, Shear NH : Drug interactions with itraconazole, fluconazole, and terbinafine, and their management. Jour. Am. Acad. Derm. 1999 : 41 : 237 - 249