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Ketoconazole

Ketoconazole is a synthetic acetylchichlorophenyl imidazole.

Mechanism of action:

Azoles are predominantly fungistatic. Azoles act by inhibiting the enzyme demethylase (Lanosterol 14 alpha-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. Ketoconazole is available for oral administration and well absorbed from the gastrointestinal tract.
  2. The drug is well bound to albumin, and high therapeutic blood levels are maintained.
  3. 90% of the drug is excreted by the liver and the remainder 10% by the kidneys.
  4. Ketoconazole is available in 200-mg tablets for oral administration. Recommended daily dose is 200–400mg.
  5. A topical preparation is available as 1% Suspension.

Topical

Subconjunctival

Intravitreal

Intravenous

Oral

1% Suspension

NA

NA

NA

200–400 mg/day

 

Spectrum of  susceptible organisms :

Candida, Cladosporium, Fusarium, Penicillium

Side effects:

In addition to blocking fungal ergosterol synthesis, ketoconazole also inhibits human gonadal and adrenal steroid synthesis and cytochrome P450 dependent hepatic drug-metabolizing enzymes.

Common systemic side effects are pruritus, nausea, vomiting, diarrhea, cramps, gynecomastia and elevations in liver enzyme levels .

Drug Interaction:

Ketoconazole can affect the efficacy and concentration of cyclosporine, warfarin, phenytoin, and theophylline. It has been shown that oral ketoconazole may augment topical natamycin therapy

Caution:

Ketoconazole should not be given in the first 3 months of pregnancy or to patients with a history of hypersensitivity

Statutory Warning

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