Biotransformation

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.
#000040; color: #000040; font-family: Verdana, Arial; background-color: #e4eaff;" />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.