[PDF] amide anesthetics metabolism

Amide local anesthetics are generally metabolized by microsomal enzymes that are found inside the liver, most notably, the cytochrome P-450 microsomal enzymes. In contrast, ester local anesthetics are metabolized by plasma enzymes known as pseudocholinesterases, in a process called hydrolysis.
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  • How are amides metabolised?

    The amides are mainly metabolized in the liver, by N-dealkylation followed by oxidation by CYP isozymes.
    Metabolism of these drugs occurs more slowly.

  • Which amide anesthetic undergoes the most rapid metabolism?

    Amide local anesthetics undergo varying rates of metabolism by microsomal enzymes located primarily in the liver. Prilocaine undergoes the most rapid metabolism; lidocaine and mepivacaine are intermediate; and etidocaine, bupivacaine, and ropivacaine undergo the slowest metabolism among the amide local anesthetics.

  • How are amino amides metabolized?

    Metabolism of local anesthetics depends on the chemical structure.
    Amino esterases are degraded primarily by plasma pseudocholinesterases.
    Amino amides are cleared primarily by hepatic metabolism with renal excretion.

  • How are amino amides metabolized?

    The amino esters are eliminated by means of enzymatic hydrolysis in blood while the amino amides are metabolized primarily in the liver.

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