Procaine and Mepivacaine Have Less Toxicity In Vitro Than Other Clinically Used Local Anesthetics

@article{citeulike:2504329, abstract = {The neurotoxicity of local anesthetics can be demonstrated in vitro by the collapse of growth cones and neurites in cultured neurons. We compared the neurotoxicity of procaine, mepivacaine, ropivacaine, bupivacaine, lidocaine, tetracaine, and dibucaine by using cultured neurons from the freshwater snail Lymnaea stagnalis. A solution of local anesthetics was added to the culture dish to make final concentrations ranging from 1 x 10-6 to 2 x 10-2 M. Morphological changes in the growth cones and neurites were observed and graded 1 (moderate) or 2 (severe). The median concentrations yielding a score of 1 were 5 x 10-4 M for procaine, 5 x 10-4 M for mepivacaine, 2 x 10-4 M for ropivacaine, 2 x 10-4 M for bupivacaine, 1 x 10-4 M for lidocaine, 5 x 10-5 M for tetracaine, and 2 x 10-5 M for dibucaine. Statistically significant differences (P < 0.05) were observed between mepivacaine and ropivacaine, bupivacaine and lidocaine, lidocaine and tetracaine, and tetracaine and dibucaine. The order of neurotoxicity was procaine = mepivacaine < ropivacaine = bupivacaine < lidocaine < tetracaine < dibucaine. Although lidocaine is more toxic than bupivacaine and ropivacaine, mepivacaine, which has a similar pharmacological effect to lidocaine, has the least-adverse effects on cone growth among clinically used local anesthetics. IMPLICATIONS: Systematic comparison was assessed morphologically in growth cones and neurites exposed to seven local anesthetics. The order of neurotoxicity was procaine = mepivacaine < ropivacaine = bupivacaine < lidocaine < tetracaine < dibucaine. Although lidocaine is more toxic than bupivacaine and ropivacaine, mepivacaine, which has a similar pharmacological effect to lidocaine, is the safest among clinically used local anesthetics.}, author = {Kasaba, Toshiharu and Onizuka, Shin and Takasaki, Mayumi }, citeulike-article-id = {2504329}, journal = {Anesth. Analg.}, keywords = {bupivacaine, chronic\_pain, drug\_delivery, mepivacaine, neurotoxicity}, month = {July}, number = {1}, pages = {85--90}, posted-at = {2008-03-10 20:06:11}, priority = {3}, title = {Procaine and Mepivacaine Have Less Toxicity In Vitro Than Other Clinically Used Local Anesthetics}, url = {http://www.anesthesia-analgesia.org/cgi/content/abstract/97/1/85}, volume = {97}, year = {2003} }

TY - JOUR ID - citeulike:2504329 L3 - citeulike-article-id:2504329 TI - Procaine and Mepivacaine Have Less Toxicity In Vitro Than Other Clinically Used Local Anesthetics JF - Anesth. Analg. VL - 97 IS - 1 SP - 85 EP - 90 N2 - The neurotoxicity of local anesthetics can be demonstrated in vitro by the collapse of growth cones and neurites in cultured neurons. We compared the neurotoxicity of procaine, mepivacaine, ropivacaine, bupivacaine, lidocaine, tetracaine, and dibucaine by using cultured neurons from the freshwater snail Lymnaea stagnalis. A solution of local anesthetics was added to the culture dish to make final concentrations ranging from 1 x 10-6 to 2 x 10-2 M. Morphological changes in the growth cones and neurites were observed and graded 1 (moderate) or 2 (severe). The median concentrations yielding a score of 1 were 5 x 10-4 M for procaine, 5 x 10-4 M for mepivacaine, 2 x 10-4 M for ropivacaine, 2 x 10-4 M for bupivacaine, 1 x 10-4 M for lidocaine, 5 x 10-5 M for tetracaine, and 2 x 10-5 M for dibucaine. Statistically significant differences (P < 0.05) were observed between mepivacaine and ropivacaine, bupivacaine and lidocaine, lidocaine and tetracaine, and tetracaine and dibucaine. The order of neurotoxicity was procaine = mepivacaine < ropivacaine = bupivacaine < lidocaine < tetracaine < dibucaine. Although lidocaine is more toxic than bupivacaine and ropivacaine, mepivacaine, which has a similar pharmacological effect to lidocaine, has the least-adverse effects on cone growth among clinically used local anesthetics. IMPLICATIONS: Systematic comparison was assessed morphologically in growth cones and neurites exposed to seven local anesthetics. The order of neurotoxicity was procaine = mepivacaine < ropivacaine = bupivacaine < lidocaine < tetracaine < dibucaine. Although lidocaine is more toxic than bupivacaine and ropivacaine, mepivacaine, which has a similar pharmacological effect to lidocaine, is the safest among clinically used local anesthetics. KW - bupivacaine KW - chronic_pain KW - drug_delivery KW - mepivacaine KW - neurotoxicity AU - Kasaba, Toshiharu AU - Onizuka, Shin AU - Takasaki, Mayumi PY - 2003/07/01/ UR - http://www.anesthesia-analgesia.org/cgi/content/abstract/97/1/85 ER -