• Widescreen
    Biotransformation

    Biotransformation into inactive product

    • Bio-inactivation

    Example: procaine is used for dental procedures and is metabolized locally by the enzyme pseudo-cholinesterase (hydrolysis). The result is two inactive compounds.

    • Preparation for elimination

    Example: paracetamol is metabolized primarily in the liver, where it undergoes conjugation with sulphate and glucuronide. The result is two inactive polar compounds ready for renal elimination.

     

    Biotransformation into active product

    • Pro-drugs

    Example: sulindac is an inactive compound that converted by liver enzymes to a sulphide. The result is an active NSAID.

    • Active metabolites

    Example: imipramine is a tricyclic antidepressant that is oxidized by microsomal enzymes in the liver to desipramine. The result is an equally effective tricyclic antidepressant.

    Search