Advertisement

Pharmacy World and Science

, Volume 20, Issue 2, pp 88–92 | Cite as

Comparison of the effects and disposition kinetics of articaine and lidocaine in 20 patients undergoing intravenous regional anaesthesia during day case surgery.

  • Marc A.M. Simon
  • Tom B. Vree
  • Mathieu J.M. Gielen
  • Leo H.D.J. Booij
Article

Abstract

The aim of this investigation was to assess the effects and dispostion kinetics of the local anaesthetic drugs (±)articaine and lidocaine during intravenous regional anaesthesia (IVRA). The mean onset time of surgical analgesia of articaine was 2.5±1.1 min and that of lidocaine 11.2 ± 5.1 min (p = 0.0006). None of the patients exhibited objective symptoms of toxicity, either local or systemic, during injection of articaine or lidocaine, nor were there any subjective complaints. No changes in blood pressure, heart rate or oxygen saturation were observed with these local anesthetics at any time during the procedure, nor after deflation of the tourniquet. After releasing the tourniquet, articaine appears in the blood and is rapidly eliminated with a t1/2a of 5±3 min and a t1/2β of 59±39 min due to hydrolysis. Lidocaine is rapidly and biexponentially eliminated with similar half‐lives of t1/2a of 4±2 min and a t1/2β of 79±31 min. Total body clearance of articaine (8.9±3.5 L/min) is ten times greater than that of lidocaine (0.9±0.4 L/min; p = 0.0005). We concluded that both (±)articaine and lidocaine are suitable and safe agents for IVRA with rapid onset of good surgical anaesthesia. Articaine is a racemic mixture, which is nowadays considered as less favourable. After releasing the tourniquet, articaine is eliminated with a t1/2β of 60 min and lidocaine with a t1/2β of 80 min. Quicker onset and shorter elimination time favours (±)articaine over lidocaine for IVRA in day case settings so that patients treated with articaine will be ‘drug free’ more quickly than those who receive lidocaine. Faster elimination and more rapid onset are important advantages for articaine in IVRA for day‐case procedures.

Articaine Lidocaine Intravenous regional analgesia Elimination kinetics Disposition 

Preview

Unable to display preview. Download preview PDF.

Unable to display preview. Download preview PDF.

References

  1. 1.
    Bier A. Ñber einen neuen Weg Lokal anästhesie an der Gliedmaassen zu erzeugen. Arch Klin Chir 1908; 86: 1007–16.Google Scholar
  2. 2.
    Davies JAH, Gill SS, Weber JCP. Intravenous regional anaesthesia using bupivacaine. Anesthesia 1981; 36: 1059–60.Google Scholar
  3. 3.
    Albright GA. Cardiac arrest following regional anesthesia with etidocaine or bupivacaine. Anesthesiology 1979; 51: 285–6.PubMedGoogle Scholar
  4. 4.
    Heath ML. Bupivacaine toxicity and Bier blocks. Anesthesiology 1983; 59: 481.PubMedGoogle Scholar
  5. 5.
    Heath ML. Deaths after intravenous regional anaesthesia. Br Med J 1982; 285: 913–4.Google Scholar
  6. 6.
    Van Oss GECJM, Vree TB, Baars AM, Termond EFS, Booij LHDJ. Pharmacokinetics, metabolism, and renal excretion of articaine and its metabolite articainic acid in patients after epidural administration. Eur J Anaesthesiol 1989; 6: 49–56.PubMedGoogle Scholar
  7. 7.
    Eerola R. A comparative study of carticaine and prilocaine in regional intravenous analgesia. Prakt Anästh 1974; 9: 171–5.Google Scholar
  8. 8.
    Adams JP, Dealy EJ, Kenmore PI. Intravenous regional anesthesia in hand surgery. J Bone Jt Surg 1964; 46A; 811–6.Google Scholar
  9. 9.
    Bell HM, Slater EM, Harris WH. Regional anesthesia with intravenous lidocaine. J Am Med Assoc 1963;186: 544–9.Google Scholar
  10. 10.
    Biscoping J. Die intravenöse Regionalanästhesie des Armes (IVRA). Wiener Medizinische Wochenschrift 1993; 143: 179–83.PubMedGoogle Scholar
  11. 11.
    Eriksson E, Persson A, Örtengren B. Intravenous regional anaesthesia-an attempt to determine the safety of the method and a comparsion between prilocaine and lidocaine. Acta Chirurg Scand 1966; Suppl 358: 47–54.Google Scholar
  12. 12.
    Miles DW, James JL, Clark DE, Whitwam JG. Site of action of intravenous regional anaesthesia. J Neurol Neurosurg Psychiat 1964; 27: 574–6.PubMedGoogle Scholar
  13. 13.
    Moller RA, Covino BG. Cardiac electrophysiologic effects of articaine compared with bupivacaine and lidocaine. Anesth Analg 1993; 76: 1266–73.PubMedGoogle Scholar
  14. 14.
    Schüle H. Klinisch-experimentelle Untersuchungen über die Verkerhrstüchtigkeit nach zahnärztlichen Eingriffen. Dtsch Zahnärzt Z 1980; 35: 183–9.Google Scholar
  15. 15.
    Wörner H, Frank S, Stumpf H. Lokalanästhesie und Verkehrstüchtigkeit. Dtsch Zahnärztl Z 1980; 35: 377–84.Google Scholar
  16. 16.
    Tam YK, Tawfik SR, Ke J, Coutts RT, Gray MR, Wyse DG. Highperformance liquid chromatography of lidocaine and nine of its metabolites in human plasma and urine. J Chromatogr 1987; 423: 199–206.PubMedGoogle Scholar
  17. 17.
    Vree TB, Baars AM, van Oss GECJM, Booij LHDJ. High performance liquid chromatography and preliminary pharmacokinetics of articaine and its 2-carboxy metabolite in humans in serum and urine. J Chromatogr 1988; 424: 440–4.PubMedGoogle Scholar
  18. 18.
    Proost JH, Meijer DKW. MW/Pharm, an integrated software package for drug dosage regimen calculation and therapeutic drug monitoring. Comput Biol Med 1992; 22: 155–63.PubMedGoogle Scholar
  19. 19.
    Holmes CMcK. Intravenous regional analgesia. A useful method of producing analgesia of the limbs. Lancet 1963; A: 245–7.CrossRefGoogle Scholar
  20. 20.
    Lofgren N, Tegner C. Studies on local anesthetics. XX. Synthesis of some α-monoalkylamino-2-methyl propionanilides. Acta Chem Scand 1960; 14: 486–9.Google Scholar
  21. 21.
    Bonica JJ. Regional anesthetica with tetracaine. Anesthesiology 1950; 11: 716–29.PubMedGoogle Scholar
  22. 22.
    Merrifield AJ, Carter SJ. Intravenous regional analgesia: lignocaine blood levels. Anaesthesia 1965; 20: 287–303Google Scholar
  23. 23.
    Hargrove RL, Hoyle JR, Parker JBR, Beckett AH, Boyes RN. Blood lignocaine levels following intravenous regional analgesia. Anaesthesia 1966; 21: 37–41.PubMedGoogle Scholar
  24. 24.
    Dickler DJ, Friedman PL, Susman IC. Intravenous regional anesthesia with chloroprocaine. Anesthesiology 1965; 26: 244–5.Google Scholar
  25. 25.
    Pitkänen MT, Suzuki N, Rosenberg PH. Intravenous regional anaesthesia with 0.5% prilocaine or 0.5% chloroprocaine. A double blind comparison in volunteers. Anaesthesia 1992; 47: 618–9.PubMedGoogle Scholar
  26. 26.
    Borchard U, Niesel HC. Grundlagen der Pharmakologie der Lokalanästhetika. In: Niesel HC, ed. Regionalanästhesie Lokalanästhesie Regionale Schmerztherapie. Stuttgart, New York: Georg Thieme Verlag, 1994: 35–68.Google Scholar
  27. 27.
    Niesel HC. Klinische Pharmakologie und Toxikologie. Anwendung der Lokalanästhetika. In: Niesel HC, ed. Regionalanästhesie Lokalanästhesie Regionale Schmerztherapie. Stuttgart, New York: Georg Thieme Verlag, 1994; 69–165.Google Scholar
  28. 28.
    Thorn-Alquist AM. Blood concentrations of local anaesthetics after intravenous regional anaesthesia. Acta Anaesth Scand 1969; 13: 229–40.PubMedGoogle Scholar
  29. 29.
    Covino BG. Pharmacokinetics of local anaesthetic drugs: In: Prys-Robert C, Hug CG, eds. Pharmacokinetics of Anaesthesia. Oxford: Blackwell Sci Publishers, 1984; 270–92.Google Scholar
  30. 30.
    Akerman B, Aström A, Ross S, Telc A. Studies on absorption, distribution and metabolism of labelled prilocaine and lidocaine in some animals. Acta Pharmacol Toxicol 1966; 24: 389–403.Google Scholar
  31. 31.
    Sorbie C, Chacha P. Regional anaesthesia by the intravenous route. Br Med J 1965; 1: 957–60.Google Scholar
  32. 32.
    Deacock ARC, Simpson WT. Fatal reactions to lignocaine. Anaesthesia 1964; 19: 217–21.PubMedGoogle Scholar
  33. 33.
    Pieper JA, Rodman JH. Lidocaine. In: Evans WE, Schentag JJ, Jusko WJ, Harrison H, eds. Applied Pharmacokinetics. Principles of Therapeutic Monitoring (Second Edition). Spokane, USA: Applied Therapeutics Inc, 1986: 639–81.Google Scholar
  34. 34.
    Van Oss GECJM, Vree TB, Baars AM, Termond EFS, Booij LHDJ. Clinical effects and pharmacokinetics of articainic acid in one volunteer after intravenous administration. Pharm Weekbl [Sci] 1988; 10: 284–7.Google Scholar
  35. 35.
    De Jong R. Biotransformation of local anesthetics: general concepts. Int Anesthesiol Clin 1975; 13: 1–20.Google Scholar
  36. 36.
    Boyes RN. A review of the metabolism of amide local anaesthetic agents. Br J Anaesth 1975; 47: 225–30.PubMedGoogle Scholar
  37. 37.
    Tucker GT, Mather LE. Clinical pharmacokinetics of local anaesthetics. Clin Pharmacokin 1979; 4: 241–78.Google Scholar

Copyright information

© Kluwer Academic Publishers 1998

Authors and Affiliations

  • Marc A.M. Simon
    • 1
  • Tom B. Vree
    • 2
  • Mathieu J.M. Gielen
    • 3
  • Leo H.D.J. Booij
    • 3
  1. 1.Department of AnesthesiologyMedisch Spectrum TwenteEnschedeThe Netherlands
  2. 2.Department of Clinical PharmacyAcademic Hospital Nijmegen Sint RadboudNijmegenThe Netherlands
  3. 3.Institute for AnesthesiologyAcademic Hospital Nijmegen Sint RadboudNijmegenThe Netherlands

Personalised recommendations