Klin Farmakol Farm. 2018;32(2):28-32 | DOI: 10.36290/far.2018.012

Local anesthetics from the anesthesiologist perspective

Olga Klementová1, Pavel Michálek2,3
1 Klinika anesteziologie, resuscitace a intenzivní medicíny Fakultní nemocnice Olomouc a LF UP v Olomouci
2 Klinika anesteziologie, resuscitace a intenzivní medicíny, 1. LF UK a Všeobecná fakultní nemocnice, Praha
3 Department of Anaesthesia, Antrim Area Hospital, Antrim, United Kingdom

Local anesthetics are drugs that block the transmission of conduction in nerve structures and cause anesthesia or analgesia in thearea supplied by the given nerve. The only natural local anesthetic is cocaine, others are synthetic drugs. They can be divided intoaminoesthers and aminoamides. Estheric local anesthetics have a rapid onset and short duration of action, similar to lidocaine-typeaminoamide anesthetics. Aminoamide local anesthetics of the bupivacaine type have longer onset of action and longer duration.Local anesthetics are most commonly used in perioperative medicine for application to the mucosa, subcutaneous tissue, nervesand plexuses, or into the epidural and subarachnoid space. Increasingly widespread is the administration between the musclefascias in order to provide postoperative analgesia. Lidocaine is also administered intravenously, using its analgesic, anti-inflammatoryand immunomodulatory effects. The most serious complication associated with local anesthetics is their cardiotoxicity andneurotoxicity. The success rate of resuscitation increased significantly after the introduction of the lipid emulsion as an antidoteinto clinical practice. Long-term administration of local anesthetics to the nerves can result in tachyphylaxis, with a reduction intheir effect. The research of new molecules with local anesthetic action is mainly focused on tetrodotoxin derivatives.

Keywords: local anesthetic, cocaine, lidocaine, bupivacaine, toxicity, lipid emulsion, tachyphylaxes, tetrodotoxin

Published: August 13, 2018  Show citation

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Klementová O, Michálek P. Local anesthetics from the anesthesiologist perspective. Klin Farmakol Farm. 2018;32(2):28-32. doi: 10.36290/far.2018.012.
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References

  1. Koller C. On the use of cocaine for producing anaesthesia on the eye. Lancet 1884; 124: 990-992. Go to original source...
  2. Schott H. Kronika medicíny. Fortuna Print, 1994.
  3. Lassner J. Bupivacaine: a delayed action local anesthetic. Preliminary note. Cah Anesthesiol 1968; 16: 39-43. Go to PubMed...
  4. Butterworth JF. Models and mechanisms of local anesthetic cardiac toxicity: a review. Reg Anesth Pain Med 2010; 35: 167-176. Go to original source...
  5. Borgeat A, Aguirre J. Update on local anesthetics. Curr Opin Anesthesiol 2010; 23: 466-4671. Go to original source... Go to PubMed...
  6. Becker DE, Reed KL. Local anesthetics: review of pharmacological considerations. Anesth Progress 2012; 59: 90-102. Go to original source... Go to PubMed...
  7. Rosenberg PH, Veering BT, Urmey WF. Maximum recommended doses of local anesthetics: a multifactorial concept. Reg Anesth Pain Med 2004; 29: 564-575. Go to original source...
  8. Dunn LK, Durieux ME. Perioperative use of intravenous lidocaine. Anesthesiology 2017; 126: 729-737. Go to original source... Go to PubMed...
  9. Weibel S, Jokinen J, Pace NL, Schnabel A, Hollmann MW, Hahnenkamp K, Eberhart LH, Poepping DM, Afshari A, Kranke P. Efficacy and safety of intravenous lidocaine for postoperative analgesia and recovery after surgery: a systematic review with trial sequential analysis. Br J Anaesth 2016; 116: 770-783. Go to original source...
  10. Chowdhury A, Fernandes B, Melhuish TM, White LD. Antiarrhythmics in cardiac arrest: a systematic review and meta-analysis. Heart Lung Circ 2018; 27: 280-290. Go to original source... Go to PubMed...
  11. Knezevic NN, Tverdohleb T, Nikibin F, Knezevic I, Candido KD. Management of chronic neuropathic pain with single and compounded topical analgesics. Pain Manage 2017; 7: 537-558. Go to original source... Go to PubMed...
  12. Rickard JP, Kish T. Systemic intravenous lidocaine for the treatment of complex regional pain syndrome: a case report and literature review. Am J Ther 2016; 23: e1266-9. Go to original source...
  13. Shulman M, Harris JE, Lubenow TR, Nath HA, Ivankovich AD. Comparison of epidural butamben to celiac plexus neurolytic block for the treatment of the pain of pancreatic cancer. Clin J Pain 2000; 16: 304-309. Go to original source...
  14. Christie LE, Picard J, Weinberg GL. Local anaesthetic systemic toxicity. BJA Education 2014, 15: 136-142. Go to original source...
  15. Mercado P, Weinberg GL. Local anesthetic systemic toxicity: prevention and treatment. Anesthesiol Clin 2011; 29: 233-242. Go to original source...
  16. Weinberg GL. Lipid emulsion infusion resuscitation for local anesthetic and other drug overdose. Anesthesiology 2012; 117: 180-187. Go to original source... Go to PubMed...
  17. 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: 1572-1574. Go to original source...
  18. Weinberg GL. Lipid rescue resuscitation from local anaesthetic cardiac toxicity. Toxicol Rev 2006; 25: 139-145. Go to original source... Go to PubMed...
  19. Coleman MD, Coleman NA. Drug induced methaemoglobinaemia. Treatment issues. Drug Saf 1996; 14: 394-405. Go to original source...
  20. Kongsgaard UE, Werner MU. Tachyphylaxis to local anaesthetics. What is the clinical evidence? A systematic review. Acta Anaesthesiol Scand 2016; 60: 6-14. Go to original source... Go to PubMed...
  21. Prasanna Vadhanan C, Adhinarayanan S. Future local anesthetics: neurotoxins? Anaesth Pain Intensive Care 2014; 18: 308-312.
  22. Kohane DS, Lu NT, Gokgol-Kline AC, Shubina M, Kuang Y, Hall S, Strichartz GR, Berde CB: The local anesthetic properties and toxicity of saxitonin homologues for rat sciatic nerve block in vivo. Reg Anesth Pain Med 2000; 25: 52-59. Go to original source...
  23. Alberto J, Rodriguez-Navarro AJ, Lagos N,Lagos M, Braghetto I, Csendes A. Neo saxitoxin as a local anesthetic. Anesthesiology 2007; 106: 339-345. Go to original source... Go to PubMed...
  24. Rodríguez-Navarro AJ, Berde CB, Wiedmaier G, Mercado A, Garcia C, Iglesias V, Zurakowski D. Comparison of neosaxitoxin versus bupivacaine via port infiltration for postoperative analgesia following laparoscopic cholecystectomy. A randomized double-blind controlled trial. Reg Anesth Pain Med 2011; 36: 103-109. Go to original source...
  25. Wallace MS, Rauck R, Fisher R, et al. Intrathecal ziconotide for severe chronic pain: safety and tolerability results of an open-label, long-term trial. Anesth Analg 2008; 106: 628-637. Go to original source...
  26. Beiranvand S, Eatemadi A, Karimi A. New updates pertaining to drug delivery of local anesthetics in particular bupivacaine using lipid nanoparticles. Nanoscale Res Lett 2016; 11: 307. Go to original source... Go to PubMed...
  27. Ginosar Y, Haroutounian Kagan L, Naveh M, Aharon A, Davidson EM. Proliposomal ropivacaine oil: pharmacokinetic and pharmacodynamic data after subcutaneous administration in volunteers. Anesth Analg 2016; 122: 1673-1680. Go to original source...




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