Where are lidocaine, mepivacaine, and bupivacaine metabolized?

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BlackTom AI · Accepted Answer

Question focus: metabolic site for common amide local anesthetics lidocaine, mepivacaine, and bupivacaine.
Option 1: Liver — This is the correct site. Amide local anesthetics are primarily metabolized in the liver by hepatic enzymes (cytochrome P450 system), converting them to inactive metabolites.
Option 2: Plasma — While some drugs can undergo minimal hydrolysis or distribution-related changes in plasma, the major metabolism of lidocaine, mepivacaine, and bupivacaine does not occur in plasma. Their plasma concentrations reflect distribution and clearance, not primary metabolism.
Option 3: Lungs — The lungs are not the main site of hepatic metabolism for these agents. Some anesthetics are cleared by the lungs (e.g., volatile agents), but these amide locals are predominantly hepatically metabolized, not cycled through the lungs for biotransformation.
Option 4: Kidneys — Renal clearance affects excretion of metabolites and unchanged drug, but metabolism itself is hepatic. The kidneys handle elimination of metabolites to some extent, yet the primary biotransformation does not occur there.
Summary: The central theme is that amide local anesthetics are metabolized mainly in the liver via hepatic enzymes, with lesser roles for distribution and renal excretion in overall clearance. The other sites are more aligned with excretion or distribution processes rather than the principal metabolic step.

Where are lidocaine, mepivacaine, and bupivacaine metabolized?

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