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Pharmacology of Local Anesthetics

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Essentials of Pharmacology for Anesthesia, Pain Medicine, and Critical Care

Abstract

The development of local anesthetics dates to the first use by the Incas of Peru, using cocaine for its medicinal properties. They treated headaches with trepanation or by burrowing holes in the skull with chewed cocaine as the local anesthetic. Today, the use of local anesthetics by anesthesia providers has gained increasing popularity, traditionally in both obstetric and regional anesthesia. This chapter will focus on the types of local anesthetics, dosing and mechanism of action, indications with clinical pearls, and drug interactions/toxicity profile.

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References

  1. Vandam LD. Some Aspects of the history of local anesthesia. Local anesthetics: handbook of experimental pharmacology. Heidelberg: Springer; 1987. p. 1–19

    Google Scholar 

  2. Wong K, Strichartz GR, Raymond SA. On the mechanisms of potentiation of local anesthetics by bicarbonate buffer: drug structure-activity studies on isolated peripheral nerve. Anesth Analg. 1993;76:131–43.

    Article  CAS  PubMed  Google Scholar 

  3. Johns RA, DiFazio CA, Longnecker DE. Lidocaine constricts or dilates rat arterioles in a dose-dependent manner. Anesthesiology. 1985;62:141–4.

    Article  CAS  PubMed  Google Scholar 

  4. Arcisio-Miranda M, Muroi Y, Chowdhury S, Chanda B. Molecular mechanism of allosteric modification of voltage-dependent sodium channels by local anesthetics. Physiology. 2010;136(5):541–54.

    CAS  Google Scholar 

  5. Scholz A. Mechanisms of (local) anaesthetics on voltage-gated sodium and other ion channels. Br J Anaesth. 2002;89:52–61.

    Article  CAS  PubMed  Google Scholar 

  6. Zahedi S. Retrospective review of dental local anesthetic induced paresthesia in the United Kingdom. Thesis for masters degree. University of Toronto; 2012. https://tspace.library.utoronto.ca/bitstream/1807/33617/1/Zahedi_Sepehr_201211_MSc_thesis.pdf.

  7. Badgwell JM, Heavner JE, Kyttä J, Rosenberg PH. Cardiovascular and central nervous system effects of co-administered lidocaine and bupivacaine in piglets. Reg Anesth. 1991;16:89–94.

    PubMed  Google Scholar 

  8. Davies JAH, Wilkey AD, Hall ID. Bupivacaine leak past inflated tourniquets during intravenous regional analgesia. Anaesthesia. 1984;39:996.

    Article  CAS  PubMed  Google Scholar 

  9. Atanassoff PG, Aouad R, Hartmannsgruber MW, Halaszynski T. Levobupivacaine 0.125% and lidocaine 0.5% for intravenous regional anesthesia in volunteers. Anesthesiology. 2002;97:325.

    Article  CAS  PubMed  Google Scholar 

  10. Littlewood DG, Scott DB, Wilson J, Covino B. Comparative anaesthetic properties of various local anaesthetic agents in extradural block for labour. Br J Anaesth. 1979;49:75–9.

    Article  Google Scholar 

  11. Freedman JM, Li DK, Drasner K, et al. Transient neurologic symptoms after spinal anesthesia: an epidemiologic study of 1,863 patients. Anesthesiology. 1998;89:633–41 [erratum appears in Anesthesiology 1998 Dec;89(6):1614].

    Article  CAS  PubMed  Google Scholar 

  12. Eberhart LH, Morin AM, Kranke P, et al. Transient neurologic symptoms after spinal anesthesia. A quantitative systematic overview (meta-analysis) of randomized controlled studies. Anaesthesist. 2002;51:539–46.

    Article  CAS  PubMed  Google Scholar 

  13. Nordström H, Stånge K. Plasma lidocaine levels and risks after liposuction with tumescent anaesthesia. Acta Anaesthesiol Scand. 2005;49:1487–90.

    Article  PubMed  Google Scholar 

  14. Tetzlaff J. Clinical pharmacology of local anesthetics. Woburn: Butterworth-Heinemann; 2000.

    Google Scholar 

  15. Palkama VJ, Neuvonen PJ, Olkkola KT. Effect of itraconazole on the pharmacokinetics of bupivacaine enantiomers in healthy volunteers. Br J Anaesth. 1999;83:659–61.

    Article  CAS  PubMed  Google Scholar 

  16. Boren E, Teuber SS, Naguwa SM, Gershwin ME. A critical review of local anesthetic sensitivity. Clin Rev Allergy Immunol. 2007;32(1):119–28.

    Article  CAS  PubMed  Google Scholar 

  17. Lund P, Cwik J. Propitocaine (Citanest) and methemoglobinemia. Anesthesiology. 1980;53:259.

    Article  Google Scholar 

  18. Zink W, Graf BM. Local anesthetic myotoxicity. Reg Anesth Pain Med. 2004;29(4):333–40.

    Article  CAS  PubMed  Google Scholar 

  19. Reisner LS, Hochman BN, Plumer MH. Persistent neurologic deficit and adhesive arachnoiditis following intrathecal 2-chloroprocaine injection. Anesth Analg. 1980;59:452–4.

    Article  CAS  PubMed  Google Scholar 

  20. Pollock JE. Transient neurologic symptoms: etiology, risk factors, and management. Reg Anesth Pain Med. 2002;27(6):581–6.

    PubMed  Google Scholar 

  21. De Jong RH, Ronfeld RA, DeRosa RA. Cardiovascular effects of convulsant and supraconvulsant doses of amide local anesthetics. Anesth Analg. 1982;61(1):3–9.

    PubMed  Google Scholar 

  22. Clarkson CW, Hondeghem LM. Mechanism for bupivacaine depression of cardiac conduction: fast block of sodium channels during the action potential with slow recovery from block during diastole. Anesthesiology. 1985;62:396–405.

    Article  CAS  PubMed  Google Scholar 

  23. Tsen LC, Tarshis J, Denson DD, Osanthanondh R. Measurements of maternal protein binding of bupivacaine throughout pregnancy. Anesth Analg. 1999;89(4):965–8.

    CAS  PubMed  Google Scholar 

  24. Neal JM, Bernards CM, Butterworth JF, Di Gregorio G, Drasner K, Hejtmanck MR, Mulroy MF, Rosenquist RW, Weinberg GL. Checklist for treatment of local anesthetic systemic toxicity. Reg Anesth Pain Med. 2010;35:152–61.

    Article  PubMed  Google Scholar 

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Author information

Authors and Affiliations

  1. Department of Anesthesiology, UCLA- Santa Monica Medical Center and Orthopedic Hospital, Santa Monica, CA, USA

    Neesa Patel MD & Alireza Sadoughi MD

  2. Department of Anesthesiology, Ronald Reagan UCLA Medical Center, Los Angeles, CA, USA

    Neesa Patel MD

  3. Department of Anesthesiology, David Geffen School of Medicine, University of California, Los Angeles, CA, USA

    Neesa Patel MD & Alireza Sadoughi MD

Authors
  1. Neesa Patel MD
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  2. Alireza Sadoughi MD
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Corresponding author

Correspondence to Neesa Patel MD .

Editor information

Editors and Affiliations

  1. Departments of Anesthesiology and Pharmacology, LSU Health Sciences Center, New Orleans, Louisiana, USA

    Alan David Kaye

  2. Department of Pharmacy Practice, Thomas J. Long School of Pharmacy and Health Sciences, Stockton, California, USA

    Adam M. Kaye

  3. Center for Perioperative Management and Medical Informatics, Brigham and Women’s Hospital, Boston, Massachusetts, USA

    Richard D. Urman

Chemical Structures

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Patel, N., Sadoughi, A. (2015). Pharmacology of Local Anesthetics. In: Kaye, A., Kaye, A., Urman, R. (eds) Essentials of Pharmacology for Anesthesia, Pain Medicine, and Critical Care. Springer, New York, NY. https://doi.org/10.1007/978-1-4614-8948-1_11

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  • DOI: https://doi.org/10.1007/978-1-4614-8948-1_11

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  • Publisher Name: Springer, New York, NY

  • Print ISBN: 978-1-4614-8947-4

  • Online ISBN: 978-1-4614-8948-1

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