Ketoconazole Drug Profile

General
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Ketoconazole (Drug Profile)

  • Chemical Formula: C₂₆H₂₈Cl₂N₄O₄

  • Mechanism of Action: Ketoconazole interacts with 14-α-sterol demethylase, a cytochrome P-450 enzyme necessary for the conversion of lanosterol to ergosterol. This increases the cellular permeability and accumulation of 14α-methyl-3,6-diol, a toxic metabolite that increases the fluidity of the membrane. drugbank

  • Protein binding: Ketoconazole is approximately 84% bound to plasma albumin, with another 15% associated with blood cells for a total of 99% binding within the plasma.

  • Half-life: The first phase having a half-life of 2 hours and a terminal half-life of 8 hours.

  • Toxicity: Overdosing may include

        • Acute liver injury
        • anorexia, fatigue, nausea, and jaundice.
        • hepatocellular and cholestatic injury.

  • Interactions

  • Food Interaction:

  • Drinking alcohol during ketoconazole treatment may cause liver injury.

  • Multivalent ions may decrease ketoconazole concentration.

  • Consumption after food decreases gastrointestinal irritation caused by ketoconazole.

  • Drug Interaction:

  • Benzodiazepine: The metabolism of benzodiazepine may decrease when combined with ketoconazole.

  • Abatacept: The risk or severity of liver damage can be increased when ketoconazole is combined with abatacept.

  • Abacavir: The metabolism of Abacavir can be decreased when combined with Ketoconazole.

Source of information: DrugBank Ketoconazole (DrugBank ID: DB 01026)

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