Azoles

General Properties / Mechanism of Action of AZOLES (CLASS)

Azoles block lanosterol 14α demethylase leading to decreased ergosterol synthesis & impairment of fungal cell wall function, thereby arresting fungal growth (fungistatic >> fungicidal)

Spectrum of Activity of Topical Azoles (CLASS)

  • Antifungal: dermatophytes & yeasts
  • Antibacterial: many azoles have some gram-positive coverage
  • Anti-inflammatory properties (some azoles): decrease neutrophil chemotaxis, decrease lymphocyte synthesis, decrease histamine release, inhibition of calmodulin, inhibition of 5-lipoxygenase (which reduces leukotrienes)

General Adverse Effects

  • Burning, erythema, maceration, allergic contact dermatitis (rarely)

Indications of AZOLES (CLASS)

  • Tinea (dermatophyte) infections, candida, as well as pityriasis versicolor; also used for seborrheic dermatitis due to effect on Malassezia spp.

Specific Medications

  • Pregnancy Category B
Formulation
  • 1% cream, 1% lotion, oral troches (lozenge), intravaginal tablet
Spectrum of Activity
  • Antifungal: dermatophytes & yeasts
  • Antibacterial: some gram-positive coverage
  • Anti-inflammatory properties
Adverse Effects
  • Burning, erythema, maceration, allergic contact dermatitis (rarely)
Other
  • Oral troches: slowly dissolve in the mouth, use 4-5x per day for 2 weeks.
    Intravaginal tablet: once daily for 1-2 days
  • Pregnancy Category B
Formulation
  • 2% cream, ointment, spray, powder, solution, gel
Spectrum of Activity
  • Antifungal: dermatophytes & yeasts
  • Antibacterial: some gram-positive coverage
  • Anti-inflammatory properties
Adverse Effects
  • Burning, erythema, maceration, allergic contact dermatitis (rarely)
Other

* For further reading refer to a pharmacology source

  • Pregnancy Category B
Formulation
  • 2% cream, shampoo 1% (over the counter), 2% shampoo, oral solution, foam
Spectrum of Activity
  • Antifungal: dermatophytes & yeasts
  • Antibacterial: minimal
  • Anti-inflammatory properties
Adverse Effects
  • Burning, erythema, maceration, allergic contact dermatitis (rarely) – allergic contact dermatitis in ketoconazole is due to sodium sulfite or propylene glycol
Other
  • Utilized in Seborrheic dermatitis
  • Anti-inflammatory potency similar to HC1%
  • Pregnancy Category B
Formulation
  • 1% cream, lotion
Spectrum of Activity
  • Antifungal: dermatophytes & yeasts
  • Antibacterial: minimal
  • Anti-inflammatory properties
Adverse Effects
  • Burning, erythema, maceration, allergic contact dermatitis (rarely)
Other
  • Once daily administration
  • Pregnancy Category B
Formulation
  • 1% cream, lotion
Spectrum of Activity
  • Antifungal: dermatophytes & yeasts
  • Antibacterial: some gram-positive coverage
  • Anti-inflammatory properties
Adverse Effects
  • Burning, erythema, maceration, allergic contact dermatitis (rarely) – allergic contact dermatitis to vehicle
Other

* For further reading refer to a pharmacology source

  • Pregnancy Category C
Formulation
  • 1% cream, foam
Spectrum of Activity
  • Antifungal: dermatophytes & yeasts
  • Antibacterial: some gram-positive coverage, also some gram-negative properties
  • Anti-inflammatory properties
Adverse Effects
  • Burning, erythema, maceration, allergic contact dermatitis (rarely)
Other

* For further reading refer to a pharmacology source

  • Pregnancy Category C
Formulation
  • 2% cream, powder, gel, solution, intravaginal tab
Spectrum of Activity
  • Antifungal: dermatophytes & yeasts
  • Antibacterial: some gram-positive coverage
  • Anti-inflammatory properties
Adverse Effects
  • Burning, erythema, maceration, allergic contact dermatitis (rarely)
Other

* For further reading refer to a pharmacology source

  • Pregnancy Category C
Formulation
  • 1% cream
Spectrum of Activity
  • Dermatophytes > Candida (weak)
Adverse Effects
  • Burning, erythema, maceration, allergic contact dermatitis (rarely), cellulitis (rare)
Other
  • Tinea corporis: daily for 1 week
  • Tinea pedis: daily for 2 weeks
  • Pregnancy Category C
Formulation
  • 10% solution
Spectrum of Activity
  • Dermatophytes > Candida (weak)
Adverse Effects
  • Burning, erythema, maceration
Other
  • Apply to affected nails once a day for 48 weeks
  • Approved for dermatophyte onychomycosis (mild / moderate without lunula involvement)