Open AccessBupivacaine and Other Amide Local Anesthetics Inhibit the Hydrolysis of Chloroprocaine by Human Serum
Author(s) -
David Lalka,
N Vicuna,
S R Burrow,
D. D. Jones,
Thomas M. Ludden,
K. D. Haegele,
J. L. McNay
Publication year - 1978
Publication title -
anesthesia and analgesia/anesthesia and analgesia
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 1.404
H-Index - 201
eISSN - 1526-7598
pISSN - 0003-2999
DOI - 10.1213/00000539-197809000-00004
Subject(s) - mepivacaine , medicine , local anesthetic , bupivacaine , lidocaine , anesthesia , hydrolysis , pharmacology , biochemistry , chemistry
The rate of hydrolysis of chloroprocaine by human serum was studied in the presence and absence of a number of aminde local anesthetics and their metabolites. Bupivacaine (2.4 microgram/ml) and etidocaine (2.3 microgram/ml) caused 38% and 21% inhibition respectively of the rate of chloroprocaine hydrolysis. Circulating concentrations of these drugs have been reported in this range by several investigators following epidural doses of 150 to 400 mg of either drug. Mepivacaine, lidocaine, and two lidocaine metabolites (glycine xylidide and monoethylglycine xylidide) were only inhibitory at levels much greater than those seen in blood following the usual local anesthetic doses of the parent compounds. Since serum is an important site of chloroprocaine metabolism in man, the probability of chloroprocaine intoxication may be increased when it is administered with local anesthetics such as bupivacaine and etidocaine.