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Clotrimazole

Clotrimazole is an azole antifungal agent with a broad antifungal spectrum.

Mechanism of action:

Azoles are predominantly fungistatic. Azoles act by inhibiting the enzyme demethylase (Lanosterol 14 α-demethylase is a cytochrome P450 enzyme that converts lanosterol to cholesterol.) This blocks the demethylation of lanosterol to ergosterol, the principal sterol of fungal membranes . This leads to disruption of fungal cell membrane and inhibition of  fungal cell growth.

Pharmacokinetics:

  1. Most fungal strains are inhibited at concentrations of 2–4mg/mL, which can be readily achieved with topical and oral administration.
  2. Clotrimazole  is poorly absorbed parenterally.
  3. The topical preparation of clotrimazole is available as 1% solution. Recommended dosage is hourly for 2–3 days,which is then tapered over 8–12 weeks.
  4. Oral administration in a dosage range of 60–150mg/kg/day can be given with an achievable serum concentration of 0.4–5.5mg/mL.

Topical

Subconjunctival

Intravitreal

Intravenous

Oral

1% Suspension, 1% Solution

NA

NA

NA

60–150mg/ kg/day

 

Spectrum of  susceptible organisms :

Alternaria , Aspergillus , Candida, Cladosporium, Curvularia,  Paecilomyces Penicillium. Thus clotrimazole has a wide spectrum of activity against numerous fungi, but poor activity with Fusarium. Many studies had proposed clotrimazole as the drug of choice for Aspergillus infections of the eye.

Side effects:

Side effects of the systemic administration include anorexia, nausea, hallucinations, confusion, and epigastric pain.

Statutory Warning

Materials / Informations provided here are for educational purpose only ; and not to be used for medical advice, diagnosis or treatment