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Clotrimazole

Azole: a broad spectrum antifungal developed in 1967. It was one of the first azoles to be developed. Formulations are now generic in a number of countries.

It is effective against Candida albicans and the dermatophytes. Its action is fungistatic or fungicidal, depending upon the concentration used.
This azole drug is available in a variety of dosage forms, including oral lozenges and vaginal formulations. It is also available in a variety of combinations with antibiotics and corticosteroids.

Trade Name:

  • Canesten* Bayer
  • Mycelex* Bayer
  • Desenex* Novartis

Oral:

  • Lozenges: Clotrimazole 10 mg Mycelex*
  • Topical: Cream: Clotrimazole 1% Desenex* Lotrimin*
            - Lotion: Clotrimazole 1% Desenex* Lotrimin*
            - Solution: Clotrimazole 1% Desenex*

Used for

  • Tinea corporis
  • Tinea cruris
  • Tinea pedis
  • Pityriasis versicolor
  • Cutaneous candidiasis
  • Nail and skin infections, fungal or gram positive

Therapeutic Regimen

Adult

Pediatric

Dermatomycoses

Clotrimazole 1% cream, solution, or lotion bid x14-28d, apply in a thin layer to the affected area and surrounding skin.

  • Topical preparations should not be used in children < 2 years old
  • Vaginal preparations are not recommended for children < 12 years old
  • Lozenges should not be used in children < 5 years old


Safety Information

  • Avoid applying dressings that seal the area
  • Elevated liver function tests have been observed in patients using Clotrimazole lozenges.

Side Effects

Local cutaneous effects may include irritation, hypersensitivity, burning, pruritus, erythema, fissuring, or swelling.

FDA Pregnancy Category C
Oral formulation shows toxicity in animal trials. Use is not recommended during pregnancy or lactation.

Mechanism of Action / Pharmacokinetics

Clotrimazole damages the fungal cell wall and alters the permeability. It also inhibits the activity of intracellular enzymes, leading to a buildup of toxic concentrations of hydrogen peroxide within the fungal cell, causing death of the cell. Systemic absorption is minimal.

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