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Pediatric Pharmacological Considerations

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Pediatric Atlas of Ultrasound- and Nerve Stimulation-Guided Regional Anesthesia

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Abstract

Local anesthesia in clinical practice has existed since 1884, when Carl Koller demonstrated that cocaine could be used locally to anesthetize tissue during eye surgery. Since then, a number of local anesthetic agents have been developed and marketed, each with specific properties and preferred applications. This chapter provides a background on the structure, action, and pharmacokinetics of local anesthetics. Also covered are the toxic effects of local anesthetics and methods to address local anesthetic toxicity. By the end of the chapter, the reader will have a good understanding of the properties of local anesthetics in general and their use in the pediatric population.

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References

  1. Löfgren N, Lundqvist B. Studies on local anaesthetics II. Svensk Kemisk Tidskrift. 1946;58:206–17.

    Google Scholar 

  2. Ekenstam BEB, Petterson G. Local anaesthetics: I. N-alkyl pyrrolidine and N-alkyl piperidine carboxylic acid amides. Acta Chem Scand. 1957;11:1183–90.

    Article  Google Scholar 

  3. Casati A, Putzu M. Bupivacaine, levobupivacaine and ropivacaine: are they clinically different? Best Pract Res Clin Anaesthesiol. 2005;19:247–68.

    Article  CAS  PubMed  Google Scholar 

  4. Mazoit JX. Pharmacology of local anesthetics. In: Bissonnette BJD, editor. Pediatric anesthesia: principles and practice. 1st ed. New York: McGraw-Hill; 2002. p. 302–37.

    Google Scholar 

  5. Mazoit J-X, Lonnqvist P-A. Local anesthetics and their adjuncts. In: Hatch S, editor. Textbook of pediatric anesthesia. 3rd ed. Boca Raton: CRC Press; 2007. p. 211–25.

    Google Scholar 

  6. Schulman JM, Strichartz GR. Local anesthetic pharmacology. In: Golan DE, Tashjian Jr AH, Armstrong EJ, Armstrong AW, editors. Principles of pharmacology. 3rd ed. Philadelphia: Lippincott Williams & Wilkins; 2012. p. 147–60.

    Google Scholar 

  7. Bruhova I, Tikhonov DB, Zhorov BS. Access and binding of local anesthetics in the closed sodium channel. Mol Pharmacol. 2008;74:1033–45.

    Article  CAS  PubMed  Google Scholar 

  8. Amir R, Argoff CE, Bennett GJ, Cummins TR, Durieux ME, Gerner P, et al. The role of sodium channels in chronic inflammatory and neuropathic pain. J Pain. 2006;7:S1–29.

    Article  CAS  PubMed  Google Scholar 

  9. Ramamurthi RJ, Krane EJ. Local anesthetic pharmacology in pediatric anesthesia. Tech Reg Anesth Pain Manag. 2007;11:229–34.

    Article  Google Scholar 

  10. Strichartz GR, Pastijn E, Sugimoto K. Neural physiology and local anesthetic action. In: Cousins MJ, Carr DB, Horlocker TT, Bridenbaugh PO, editors. Neural blockade in clinical anesthesia and pain medicine. 4th ed. Philadelphia: Lippincott Williams & Wilkins; 2009. p. 26–47.

    Google Scholar 

  11. Berde C. Local anesthetics in infants and children: an update. Pediatr Anesth. 2004;14:387–93.

    Article  Google Scholar 

  12. Burm AG, Vermeulen NP, van Kleef JW, de Boer AG, Spierdijk J, Breimer DD. Pharmacokinetics of lignocaine and bupivacaine in surgical patients following epidural administration. Simultaneous investigation of absorption and disposition kinetics using stable isotopes. Clin Pharmacokinet. 1987;13:191–203.

    Article  CAS  PubMed  Google Scholar 

  13. Mazoit JX, Dalens BJ. Pharmacokinetics of local anaesthetics in infants and children. Clin Pharmacokinet. 2004;43:17–32.

    Article  CAS  PubMed  Google Scholar 

  14. Lonnqvist PA, Westrin P, Larsson BA, Olsson GL, Lybeck A, Huledal G, et al. Ropivacaine pharmacokinetics after caudal block in 1-8 year old children. Br J Anaesth. 2000;85:506–11.

    Article  CAS  PubMed  Google Scholar 

  15. Tucker GT. Pharmacokinetics of local anaesthetics. Br J Anaesth. 1986;58:717–31.

    Article  CAS  PubMed  Google Scholar 

  16. Rothstein P, Arthur GR, Feldman HS, Kopf GS, Covino BG. Bupivacaine for intercostal nerve blocks in children: blood concentrations and pharmacokinetics. Anesth Analg. 1986;65:625–32.

    Article  CAS  PubMed  Google Scholar 

  17. Rochette A, Dadure C, Raux O, Capdevila X. Changing trends in paediatric regional anaesthetic practice in recent years. Curr Opin Anaesthesiol. 2009;22:374–7.

    Article  PubMed  Google Scholar 

  18. Ala-Kokko TI, Karinen J, Raiha E, Kiviluoma K, Alahuhta S. Pharmacokinetics of 0.75% ropivacaine and 0.5% bupivacaine after ilioinguinal-iliohypogastric nerve block in children. Br J Anaesth. 2002;89:438–41.

    CAS  PubMed  Google Scholar 

  19. Stoelting RK, Hillier SC. Pharmacokinetics and pharmacodynamics of injected and inhaled drugs. In: Stoelting RK, Hillier SC, editors. Pharmacology and physiology in anesthetic practice. 4th ed. Philadelphia: Lippincott Williams & Wilkins; 2006. p. 3–41.

    Google Scholar 

  20. Mazoit JX, Denson DD, Samii K. Pharmacokinetics of bupivacaine following caudal anesthesia in infants. Anesthesiology. 1988;68:387–91.

    Article  CAS  PubMed  Google Scholar 

  21. Emanuelsson BM, Zaric D, Nydahl PA, Axelsson KH. Pharmacokinetics of ropivacaine and bupivacaine during 21 hours of continuous epidural infusion in healthy male volunteers. Anesth Analg. 1995;81:1163–8.

    CAS  PubMed  Google Scholar 

  22. Morrison LM, Emanuelsson BM, McClure JH, Pollok AJ, McKeown DW, Brockway M, et al. Efficacy and kinetics of extradural ropivacaine: comparison with bupivacaine. Br J Anaesth. 1994;72:164–9.

    Article  CAS  PubMed  Google Scholar 

  23. Luz G, Innerhofer P, Haussler B, Oswald E, Salner E, Sparr H. Comparison of ropivacaine 0.1% and 0.2% with bupivacaine 0.2% for single-shot caudal anaesthesia in children. Pediatr Anesth. 2000;10:499–504.

    Article  CAS  Google Scholar 

  24. Hansen TG, Ilett KF, Reid C, Lim SI, Hackett LP, Bergesio R. Caudal ropivacaine in infants: population pharmacokinetics and plasma concentrations. Anesthesiology. 2001;94:579–84.

    Article  CAS  PubMed  Google Scholar 

  25. Aberg G. Toxicological and local anaesthetic effects of optically active isomers of two local anaesthetic compounds. Acta Pharmacol Toxicol (Copenh). 1972;31:273–86.

    Article  CAS  Google Scholar 

  26. Dalens BJ, Truchon R. Neural blockade for pediatric surgery. In: Cousins MJ, Carr DB, Horlocker TT, Bridenbaugh PO, editors. Neural blockade in clinical anesthesia and pain medicine. 4th ed. Philadelphia: Lippincott Williams & Wilkins; 2009. p. 595–629.

    Google Scholar 

  27. Dalens BJ, Mazoit JX. Adverse effects of regional anaesthesia in children. Drug Saf. 1998;19:251–68.

    Article  CAS  PubMed  Google Scholar 

  28. Luz G, Innerhofer P, Bachmann B, Frischhut B, Menardi G, Benzer A. Bupivacaine plasma concentrations during continuous epidural anesthesia in infants and children. Anesth Analg. 1996;82:231–4.

    CAS  PubMed  Google Scholar 

  29. Mazoit JX, Baujard C. Paediatric caudal and epidural analgesia. Curr Opin Anaesthesiol. 2002;15:533–6.

    Article  PubMed  Google Scholar 

  30. Berde CB. Convulsions associated with pediatric regional anesthesia. Anesth Analg. 1992;75:164–6.

    Article  CAS  PubMed  Google Scholar 

  31. Giaufre E, Dalens B, Gombert A. Epidemiology and morbidity of regional anesthesia in children: a one-year prospective survey of the French-Language Society of Pediatric Anesthesiologists. Anesth Analg. 1996;83:904–12.

    CAS  PubMed  Google Scholar 

  32. Bosenberg AT. Epidural analgesia for major neonatal surgery. Pediatr Anesth. 1998;8:479–83.

    Article  CAS  Google Scholar 

  33. Agarwal R, Gutlove DP, Lockhart CH. Seizures occurring in pediatric patients receiving continuous infusion of bupivacaine. Anesth Analg. 1992;75:284–6.

    Article  CAS  PubMed  Google Scholar 

  34. Peutrell JM, Hughes DG. A grand mal convulsion in a child in association with a continuous epidural infusion of bupivacaine. Anaesthesia. 1995;50:563–4.

    Article  CAS  PubMed  Google Scholar 

  35. Wood CE, Goresky GV, Klassen KA, Kuwahara B, Neil SG. Complications of continuous epidural infusions for postoperative analgesia in children. Can J Anesth. 1994;41:613–20.

    Article  CAS  PubMed  Google Scholar 

  36. Dalens B, Hasnaoui A. Caudal anesthesia in pediatric surgery: success rate and adverse effects in 750 consecutive patients. Anesth Analg. 1989;68:83–9.

    Article  CAS  PubMed  Google Scholar 

  37. Veyckemans F, Van Obbergh LJ, Gouverneur JM. Lessons from 1100 pediatric caudal blocks in a teaching hospital. Reg Anesth. 1992;17:119–25.

    CAS  PubMed  Google Scholar 

  38. McGown RG. Caudal analgesia in children. Five hundred cases for procedures below the diaphragm. Anaesthesia. 1982;37:806–18.

    Article  CAS  PubMed  Google Scholar 

  39. Matsumiya N, Dohi S, Takahashi H, Kondo Y, Naito H. Cardiovascular collapse in an infant after caudal anesthesia with a lidocaine-epinephrine solution. Anesth Analg. 1986;65:1074–6.

    Article  CAS  PubMed  Google Scholar 

  40. Ved SA, Pinosky M, Nicodemus H. Ventricular tachycardia and brief cardiovascular collapse in two infants after caudal anesthesia using a bupivacaine-epinephrine solution. Anesthesiology. 1993;79:1121–3.

    Article  CAS  PubMed  Google Scholar 

  41. Freid EB, Bailey AG, Valley RD. Electrocardiographic and hemodynamic changes associated with unintentional intravascular injection of bupivacaine with epinephrine in infants. Anesthesiology. 1993;79:394–8.

    Article  CAS  PubMed  Google Scholar 

  42. 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 

  43. Veering BT. Complications and local anaesthetic toxicity in regional anaesthesia. Curr Opin Anaesthesiol. 2003;16:455–9.

    Article  PubMed  Google Scholar 

  44. Heavner JE. Cardiac toxicity of local anesthetics in the intact isolated heart model: a review. Reg Anesth Pain Med. 2002;27:545–55.

    CAS  PubMed  Google Scholar 

  45. Reiz S, Haggmark S, Johansson G, Nath S. Cardiotoxicity of ropivacaine–a new amide local anaesthetic agent. Acta Anaesthesiol Scand. 1989;33:93–8.

    Article  CAS  PubMed  Google Scholar 

  46. Carpenter TC, Stenmark KR. High-dose epinephrine is not superior to standard-dose epinephrine in pediatric in-hospital cardiopulmonary arrest. Pediatrics. 1997;99:403–8.

    Article  CAS  PubMed  Google Scholar 

  47. Weinberg GL, VadeBoncouer T, Ramaraju GA, Garcia-Amaro MF, Cwik MJ. Pretreatment or resuscitation with a lipid infusion shifts the dose-response to bupivacaine-induced asystole in rats. Anesthesiology. 1998;88:1071–5.

    Article  CAS  PubMed  Google Scholar 

  48. Rosenblatt MA, Abel M, Fischer GW, Itzkovich CJ, Eisenkraft JB. Successful use of a 20% lipid emulsion to resuscitate a patient after a presumed bupivacaine-related cardiac arrest. Anesthesiology. 2006;105:217–8.

    Article  PubMed  Google Scholar 

  49. Weinberg G. LipidRescue. 2012. Available from: www.lipidrescue.org.

  50. Weinberg G, Ripper R, Feinstein DL, Hoffman W. Lipid emulsion infusion rescues dogs from bupivacaine-induced cardiac toxicity. Reg Anesth Pain Med. 2003;28:198–202.

    Article  CAS  PubMed  Google Scholar 

  51. Picard J, Meek T. Lipid emulsion to treat overdose of local anaesthetic: the gift of the glob. Anaesthesia. 2006;61:107–9.

    Article  PubMed  Google Scholar 

  52. Ozcan MS, Weinberg G. Intravenous lipid emulsion for the treatment of drug toxicity. J Intensive Care Med. 2014;29:59–70.

    Article  PubMed  Google Scholar 

  53. Litz RJ, Popp M, Stehr SN, Koch T. Successful resuscitation of a patient with ropivacaine-induced asystole after axillary plexus block using lipid infusion. Anaesthesia. 2006;61:800–1.

    Article  CAS  PubMed  Google Scholar 

  54. Foxall G, McCahon R, Lamb J, Hardman JG, Bedforth NM. Levobupivacaine-induced seizures and cardiovascular collapse treated with intralipid. Anaesthesia. 2007;62:516–8.

    Article  CAS  PubMed  Google Scholar 

  55. Litz RJ, Roessel T, Heller AR, Stehr SN. Reversal of central nervous system and cardiac toxicity after local anesthetic intoxication by lipid emulsion injection. Anesth Analg. 2008;106:1575–7.

    Article  PubMed  Google Scholar 

  56. Warren JA, Thoma RB, Georgescu A, Shah SJ. Intravenous lipid infusion in the successful resuscitation of local anesthetic-induced cardiovascular collapse after supraclavicular brachial plexus block. Anesth Analg. 2008;106:1578–80.

    Article  PubMed  Google Scholar 

  57. Ludot H, Tharin JY, Belouadah M, Mazoit JX, Malinovsky JM. Successful resuscitation after ropivacaine and lidocaine-induced ventricular arrhythmia following posterior lumbar plexus block in a child. Anesth Analg. 2008;106:1572–4.

    Article  CAS  PubMed  Google Scholar 

  58. Barrington MJ, Kluger R. Ultrasound guidance reduces the risk of local anesthetic systemic toxicity following peripheral nerve blockade. Reg Anesth Pain Med. 2013;38:289–97.

    Article  PubMed  Google Scholar 

  59. de Jong RH, editor. Local anesthetics. St. Louis: Mosby-Year Book; 1994. p. 165.

    Google Scholar 

Suggested Reading

  • Ecoffey C. Narcotics and non-narcotic analgesics. In: Dalens BJ, editor. Pediatric regional anesthesia. Boca Raton: CRC Press Inc.; 1990. p. 127–41.

    Google Scholar 

  • Haberer JP, Dalens BJ. Local anesthetics and additives. In: Dalens BJ, editor. Pediatric regional anesthesia. Boca Raton: CRC Press Inc.; 1990. p. 91–126.

    Google Scholar 

  • Mather SJ. Biology and pharmacology: some differences. In: Peutrell JM, Mather SJ, editors. Regional anaesthesia for babies and children. Oxford: Oxford University Press; 1997. p. 33–48.

    Google Scholar 

  • Murat I. Pharmacology. In: Dalens B, editor. Regional anesthesia in infants, children, and adolescents. Philadelphia: Lippincott Williams & Wilkins; 1995. p. 67–125.

    Google Scholar 

  • Suresh S, Polaner DM, Cote CJ. Regional Anesthesia. In: Cote CJ, Lerman J, Anderson BJ, Eds. 5th ed. Philadelphia: WB Saunders; 2013. p. 835–879.

    Google Scholar 

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Authors and Affiliations

  1. Department of Anesthesiology and Pain Medicine, University of Alberta, 2-150 Clinical Sciences Building, Edmonton, AB, Canada

    Derek Dillane MB BCh BAO, MMedSci, FCARCSI

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  1. Derek Dillane MB BCh BAO, MMedSci, FCARCSI
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Correspondence to Derek Dillane MB BCh BAO, MMedSci, FCARCSI .

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Editors and Affiliations

  1. Stollery Children's Hospital/University of Alberta Hospital, Cross Cancer Institute, Department of Anesthesiology and Pain Medicine, University of Albertra, Edmonton, Alberta, Canada

    Ban C.H. Tsui

  2. Department of Pediatric Anesthesiology and Feinberg School of Medicine, Ann and Robert H. Lurie Children's Hospital of Chicago and Northwestern University, Chicago, Illinois, USA

    Santhanam Suresh

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Dillane, D. (2016). Pediatric Pharmacological Considerations. In: Tsui, B., Suresh, S. (eds) Pediatric Atlas of Ultrasound- and Nerve Stimulation-Guided Regional Anesthesia. Springer, New York, NY. https://doi.org/10.1007/978-0-387-79964-3_7

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  • DOI: https://doi.org/10.1007/978-0-387-79964-3_7

  • Publisher Name: Springer, New York, NY

  • Print ISBN: 978-0-387-79963-6

  • Online ISBN: 978-0-387-79964-3

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