Skip to main content
SpringerLink
Log in

Clinical Pharmacokinetics of Articaine

  • Review Article
  • Drug Disposition
  • Published:
Clinical Pharmacokinetics Aims and scope Submit manuscript

Summary

Articaine is the most widely used local anaesthetic agent in dentistry in a number of European countries. The amide structure of articaine is similar to that of other local anaesthetics, but it contains an additional ester group which is quickly hydrolysed by esterases.

High performance liquid chromatography has been used to determine the concentrations of articaine and its metabolite articainic acid in serum. Rapid sample preparation is critical in the accurate determination of articaine serum concentrations, since blood and serum are the sites of metabolism. The time to maximum drug concentrations of articaine occurs about 10 to 15 minutes after submucosal injection of articaine 4% 80mg, irrespective of epinephrine (adrenaline). The mean maximum plasma drug concentration is about 400 μg/L for articaine with epinephrine 1: 200 000 and 580 μg/L for articaine without epinephrine. The elimination half-time of articaine is about 20 minutes.

The rapid breakdown of articaine to the inactive metabolite articainic acid is related to a very low systemic toxicity and consequently to the possibility of repeated injections. Equal analgesic efficacy along with lower systemic toxicity (i.e. a wide therapeutic range) permits the use of articaine in higher concentrations than other amide-type local anaesthetics. Complete anaesthesia can be observed in nearly 90% of all cases, using articaine 4% 60 to 80mg with epinephrine 1: 200 000. Articaine is better able to diffuse through soft tissue and bone than other local anaesthetics.

The concentration of articaine in the alveolus of a tooth in the upper jaw after extraction was about 100 times higher than that in systemic circulation. The plasma protein binding rate of articaine and articainic acid is 70%. It has been concluded that an unintentional intravascular injection of articaine 80mg does not cause toxic effects in healthy individuals.

This is a preview of subscription content, log in via an institution to check access.

Access this article

Log in via an institution

Price excludes VAT (USA)
Tax calculation will be finalised during checkout.

Instant access to the full article PDF.

Institutional subscriptions

Similar content being viewed by others

References

  1. Boaro G, Mayer G. Clinical trials of a new local anaesthetic (Carticain) in orthopaedic and traumatologic surgery. Minerva Anestesiol 1979; 45: 299–308

    PubMed  CAS  Google Scholar 

  2. Glatzl A. Regionalanästhesie des Plexus supraclavicularis mit Carticain. Prakt Anaesth 1974; 9: 165–7

    PubMed  CAS  Google Scholar 

  3. Schobel H. Erfahrungen mit Carticain in der Mikrochirurgie des Ohrs. Prakt Anaesth 1974; 9: 183–7

    PubMed  CAS  Google Scholar 

  4. van Oss GE, Vree TB, Baars A, et al. Pharmacokinetics, metabolism and renal excretion of articaine and its metabolite articainic acid in patients after epidural administration. Eur J Anaesthesiol 1989; 6: 49–56

    PubMed  Google Scholar 

  5. Vree TB, van Oss GE, Gielen MJ, et al. Epidural metabolism of articaine and its metabolite articainic acid in five patients after epidural administration of 600mg articaine. J Pharm Pharmacol 1997; 49: 158–63

    Article  PubMed  CAS  Google Scholar 

  6. Eerola R. A comparative study of carticaine and prilocaine in regional intravenous analgesia. Prakt Anaesth 1974; 9: 171–5

    PubMed  CAS  Google Scholar 

  7. Simon MA, Gielen MJ, Alberink N, et al. Intravenous regional anesthesia with 0.5% articaine, 0.5% lidocaine, or 0.5% prilocaine: a double-blind randomized clinical study. Reg Anesth 1997; 22: 29–34

    Article  PubMed  CAS  Google Scholar 

  8. Müller WPE, Weiser P, Scholler KL. Pharmakokinetik von - Articain bei der Nervus-mandibularis- Blockade. Reg Anesth 1991; 14: 52–5

    Google Scholar 

  9. Oertel R, Richter K, Weile K, et al. A simple method for the determination of articaine and its metabolite articainic acid in dentistry. Methods Find Exp Clin Pharmacol 1993; 15: 541–7

    PubMed  CAS  Google Scholar 

  10. Uihlein M. Analytische Untersuchungen mit dem Lokalanästhetikum Ultracain (Hoe 045). Prakt Anaesth 1974; 9: 152–6

    PubMed  CAS  Google Scholar 

  11. Vree TB, Baars AM, van Oss GE, et al. High performance liquid chromatography and preliminary pharmacokinetics of articaine and its 2-carboxy metabolite in human serum and urine. J Chromatogr 1988; 424: 440–4

    Article  PubMed  CAS  Google Scholar 

  12. Hofer H, Eberl R, Altmann H. Pharmakokinetische Untersuchungen mit 35S-markiertem Carticaine. Prakt Anaesth 1974; 9: 157–61

    PubMed  CAS  Google Scholar 

  13. Rahn R, Vogt R, Hellenbrecht D, et al. Serum-Spiegel von Articain nach intraoraler Lokalanästhesie mit Ultracain D-S bzw. Ultracain 2 % o.V. Dtsch Zahnarztl Z 1992; 47: 126–9

    Google Scholar 

  14. Rahn R, Hofmann R, Minner E. Lokalanästhetische Wirksamkeit unterschiedlicher Adrenalin-freier Articain-Lösungen. Zahnaerztl Welt 1994; 103: 745–49

    Google Scholar 

  15. Hornke I, Eckert HG, Rupp W. Pharmakokinetik und Metabolismus von Articain nach intramuskulärer Injektion am männlichen Probanden. Dtsch Z Mund Kiefer Gesichts Chir 1984; 8: 67–71

    CAS  Google Scholar 

  16. Kirch W, Kitteringham N, Lambers G, et al. Die klinische Pharmakokinetik von Articain nach intraoraler und intramuskulärer Applikation. Schweiz Monatsschr Zahnheilkd 1983; 93: 713–9

    Google Scholar 

  17. Jakobs W, Ladwig B, Cichon P, et al. Serum levels of articaine 2% and 4% in children. Anesth Prog 1995 42: 113–5

    PubMed  CAS  Google Scholar 

  18. Vree TB, Simon MA, Gielen MJ, et al. Regional metabolism of articaine in 10 patients undergoing intravenous regional anaesthesia during day case surgery. Br J Clin Pharmacol 1997; 44: 29–34

    Article  PubMed  CAS  Google Scholar 

  19. Rahn R, Oertel R, Richter K, et al. Serum-Konzentration von Articain bei wiederholter submuköser Injektion einer 4 %igen Vasokonstriktor-freien Lösung. Dtsch Zahnarztl Z 1996; 51: 399–401

    Google Scholar 

  20. Oertel R, Oertel A, Weile K, et al. Die Konzentration von Lokalanästhetika in der Zahnalveole — vergleichende Untersuchungen von Lidocain und Articain im Unter- und Oberkiefer. Schweiz Monatsschr Zahnmed 1994; 104: 952–5

    PubMed  CAS  Google Scholar 

  21. Oertel R, Oertel A, Feller K. A new method of blood sampling and determination of the local anesthetic agent lidocaine in dentistry. Methods Find Exp Clin Pharmacol 1993; 15: 131–6

    PubMed  CAS  Google Scholar 

  22. Wright JD, Boudinot FD, Ujhelyi MR. Measurement and Analysis of unbound Drug Concentrations. Clin Pharmacokinet 1996; 30: 445–62

    Article  PubMed  CAS  Google Scholar 

  23. van Oss GE, Vree TB, Baars AM, et al. Clinical effects and pharmacokinetics of articainic acid in one volunteer after intravenous administration. Pharm Weekbl Sci 1989; 10: 284–6

    Article  Google Scholar 

  24. Borchard U. Vergleichende Pharmakologie der Lokalanästhetika und spezielle Pharmakologie von Carticain. Anaesthesiol Intensivmed 1978; 113: 7–11

    Google Scholar 

  25. Malamed SF. Handbook of local anesthesia. 2nd ed. St Louis: C.V. Mosby Co., 1986

    Google Scholar 

  26. Oertel R, Berndt A, Kirch W. Saturable in vitro metabolism of articaine by serum esterases — does it contribute to the persistence of the local anaesthetic effect? Reg Anesth 1996; 21: 576–81

    PubMed  CAS  Google Scholar 

  27. Khoury F, Hinterthan A, Schürmann J, et al. Klinische Vergleichsuntersuchung von Lokalanästhetika. Dtsch Zahnarztl Z 1991; 46: 822–4

    PubMed  CAS  Google Scholar 

  28. Raab WHM, Müller R, Müller HF. Vergleichende Untersuchungen zum anästhetischen Wirkpotential von 2- und 4%igem Articain. Quintessenz 1990; 41: 1207–16

    PubMed  CAS  Google Scholar 

  29. Rahn R, Hauzeneder W, Flanze L. Wirksamkeit einer zweiprozentigen, adrenalinfreien Articain-Lösung (Ultracain 2 %) zur zahnärztlichen Lokalanästhesie. Dtsch Stomatol 1991; 41: 379–82

    PubMed  CAS  Google Scholar 

  30. Rahn R, Mohr A. Vergleichende Untersuchungen der lokalanästhetischen Wirksamkeit und Wirkdauer einer 4%igen Articainlösung mit unterschiedlichen konzentriertem Adrenalin-Zusatz. Dtsch Zahnarztl Z 1997; 52: 335–7

    Google Scholar 

  31. Bartlett SZ. Clinical observation on the effect of injections of local anaesthetics preceded by aspiration. Oral Surg 1972; 33: 520–5

    Article  PubMed  CAS  Google Scholar 

  32. Knoll-Köhler E. Mögliche Ursachen von Zwischenfällen während dentaler Lokalanästhesie. Zahnaerztl Welt 1991; 100: 780–6

    Google Scholar 

  33. Rupprecht S, Knoll-Köhler E. Vergleichende Untersuchung äquimolarer Lösungen von Lidocain und Articain zur Anästhesie. Schweiz Monatsschr Zahnmed 1991; 101: 1286–90

    Google Scholar 

  34. Scott DB. Evaluation of the toxicity of local anaesthetic agents in man. Br J Anaesth 1975 47: 56–62

    Article  PubMed  CAS  Google Scholar 

  35. Sonnabend E, Maschinski G. Tierexperimentelle Untersuchungen zur Toxizität von Carticain und Lidocain. Dtsch Zahnarztl Z 1976; 31: 126–7

    PubMed  CAS  Google Scholar 

  36. Szabo G, Gaspar L, Divinyi T. Klinische Erfahrungen mit Ultra-cain-Zubereitungen im Vergleich zu verschiedenen Lidocain-Präparaten. Z Stomatol 1988; 85: 235–8

    PubMed  CAS  Google Scholar 

  37. Rahn R, Offenloch K, Hellenbrecht D, et al. Verträglichkeit von niedrigdosiertem Articain und Lidocain bei intravenöser Applikation. Dtsch Zahnarztl Z 1994; 49: 691–7

    Google Scholar 

Download references

Author information

Authors and Affiliations

  1. Institute of Clinical Pharmacology, Medical Faculty Carl Gustav Carus, Technical University Dresden, Fiedlerstr. 27, 01307, Dresden, Germany

    Reinhard Oertel & Wilhelm Kirch

  2. Clinic of Dentistry, J. W. Goethe University, Frankfurt/Main, Germany

    Rainer Rahn

Authors
  1. Reinhard Oertel
    View author publications

    You can also search for this author in PubMed Google Scholar

  2. Rainer Rahn
    View author publications

    You can also search for this author in PubMed Google Scholar

  3. Wilhelm Kirch
    View author publications

    You can also search for this author in PubMed Google Scholar

Corresponding author

Correspondence to Reinhard Oertel.

Rights and permissions

Reprints and permissions

About this article

Cite this article

Oertel, R., Rahn, R. & Kirch, W. Clinical Pharmacokinetics of Articaine. Clin Pharmacokinet 33, 417–425 (1997). https://doi.org/10.2165/00003088-199733060-00002

Download citation

  • Published:

  • Issue Date:

  • DOI: https://doi.org/10.2165/00003088-199733060-00002

Keywords

Search

Navigation