Articaine – the queen of infiltrative anaesthesia? A peculiar amino-amide local anaesthetic and its use in the dental practice from a pharmacological perspective

Authors

  • Marcin Pasternak a:1:{s:5:"en_US";s:136:"Jagiellonian University, Medical College, Department of Pharmacology, Division of Clinical Pharmacology, Grzegórzecka 16, 31-531 Cracow";}

DOI:

https://doi.org/10.56782/pps.569

Keywords:

articaine, local anaesthetics, dentistry

Abstract

The importance of local anaesthetics in dentistry cannot be overestimated. Being the most commonly used drugs in dental practice, these medicines are simply indispensable, as they allow for intra-operative and partly post-operative pain control in procedures performed. The injectable agents, currently employed in dentistry, belong, almost exclusively, to the amino-amide class. The paper focuses on articaine — a peculiar amino-amide local anaesthetic, which exhibits exceptional features distinguishing it from other drugs in the group and endearing it to dental practitioners all over the world, at the same time. The structure of the drug is presented and characteristics arising from its unique attributes are discussed. The article covers the practical aspects of articaine use in various fields of dentistry and oral surgery and arising prospects for the future. Despite the wide safety margin of the agent, articaine, like any other local anaesthetic, may induce unwanted side-effects, which were also described here, and their management was briefly presented.

Downloads

Download data is not yet available.

References

1. Pasternak, M.; Woroń, J. The Role of Local Anaesthesia in Intra-Operative Pain Management in Dental Practice. BÓL 2021, 22(1), 24–35. DOI: 10.5604/01.3001.0014.9018 DOI: https://doi.org/10.5604/01.3001.0014.9018

2. Aronson, J.K. Articaine. In: Meyler’s Side Effects of Drugs (16th ed.) 2016, 711–712. DOI: 10.1016/b978-0-444-53717-1.00329-2 DOI: https://doi.org/10.1016/B978-0-444-53717-1.00329-2

3. Martin, E.; Lee, A.; Jennings, E. Articaine: Dental Practitioner Use, Basis of Perception and Evidence-Based Dentistry — a Cross-Sectional Study. BDJ Open 2022, 8(1), Art. No: 20. DOI: 10.1038/s41405-022-00113-9 DOI: https://doi.org/10.1038/s41405-022-00113-9

4. Vree, B. T.; Gielen, M. J. M. Clinical Pharmacology and the Use of Articaine for Local and Regional Anaesthesia. Best Pract. Res. Clin. Anaesthesiol. 2005, 19(2), 293–308. DOI: 10.1016/j.bpa.2004.12.006 DOI: https://doi.org/10.1016/j.bpa.2004.12.006

5. Hopman, A. J. G.; Baart, J. A.; Brand, H. S. Articaine and Neurotoxicity – a Review. Br. Dent. J. 2017, 223 (7), 501–506. DOI: 10.1038/sj.bdj.2017.782 DOI: https://doi.org/10.1038/sj.bdj.2017.782

6. Gufaran Ali, D. S.; Mulay, S. Articaine vs Lidocaine: A Review. IOSR-JDMS 2014, 13(9), 40–44. DOI: https://doi.org/10.9790/0853-13954044

7. Brandt, R. G.; Anderson, P. F.; McDonald, N. J.; Sohn, W.; Peters, M. C. The Pulpal Anesthetic Efficacy of Articaine versus Lidocaine in Dentistry : a meta-analysis. J. Am. Dent. Assoc. 2011, 142(5), 493–504. DOI: 10.14219/jada.archive.2011.0219 DOI: https://doi.org/10.14219/jada.archive.2011.0219

8. Kaczmarzyk, T.; Goszcz, A.; Grodzińska, L; et al.: Współczesna Farmakoterapia W Schorzeniach Chirurgicznych Jamy Ustnej I Tkanek Okolicznych. Wydawnictwo Uniwersytetu Jagiellońskiego, Poland, 2006. ISBN: 9788323320647

9. Snoeck, M. Articaine: A Review of Its Use for Local and Regional Anesthesia. Local Reg. Anesth. 2012, 5, 23-33. DOI: 10.2147/lra.s16682 DOI: https://doi.org/10.2147/LRA.S16682

10. Jeske, A. H. Local Anesthetics. Springer eBooks 2024, 9–23. DOI: 10.1007/978-3-031-53954-1_2 DOI: https://doi.org/10.1007/978-3-031-53954-1_2

11. Elheeny, A. A. H. Articaine Efficacy and Safety in Young Children below the Age of Four Years: An Equivalent Parallel Randomized Control Trial. Int. J. Paediatr. Dent. 2020, 30(5), 547-555. DOI: 10.1111/ipd.12640 DOI: https://doi.org/10.1111/ipd.12640

12. Leith, R.; Lynch, K.; O’Connell, A. C. Articaine Use in Children: A Review. Eur. Arch. Paediatr. Dent. 2012, 13(6), 293–296. DOI: 10.1007/bf03320829 DOI: https://doi.org/10.1007/BF03320829

13. Luo, W.; Zheng, K.; Kuang, H.; Li, Z.; Wang, J.; Mei, J. The Potential of Articaine as New Generation of Local Anesthesia in Dental Clinics: A Review. Medicine 2022, 101(48), Art. No: e32089. DOI: 10.1097/MD.0000000000032089 DOI: https://doi.org/10.1097/MD.0000000000032089

14. Pasternak, M.; Woroń, J. The Injectable Local Anaesthetics in the Prevention of Intraoperative Pain in Paediatric Dentistry – Practical Remarks on Agent Choice and Methods. Possible Complications of Local Anaesthetic Administration in Paedodontics. BÓL 2022, 23(4), 37–46. DOI: 10.5604/01.3001.0016.2231 DOI: https://doi.org/10.5604/01.3001.0016.2231

15. Winther, J. E.; Patirupanusara, B. Evaluation of Carticaine—a New Local Analgesic. Int. J. Oral Surg. 1974, 3(6), 422–427. DOI: 10.1016/s0300-9785(74)80007-4 DOI: https://doi.org/10.1016/S0300-9785(74)80007-4

16. Amorim, K. S.; Fontes, V. T. S.; Gercina, A. C.; Groppo, F. C.; Souza, L. M. A. Buffered 2% Articaine versus Non-Buffered 4% Articaine in Maxillary Infiltration: Randomized Clinical Trial. Clin. Oral Investig. 2020, 25(6), 3527–3533. DOI: 10.1007/s00784-020-03674-x DOI: https://doi.org/10.1007/s00784-020-03674-x

17. Paxton, K.; Thome, D. E. Efficacy of Articaine Formulations: Quantitative Reviews. Dent. Clin. North Am. 2010, 54(4), 643–653. DOI: 10.1016/j.cden.2010.06.005 DOI: https://doi.org/10.1016/j.cden.2010.06.005

18. Ramadurai, N.; Gurunathan, D.; Samuel, A. V.; Subramanian, E.; Rodrigues, S. J. L. Effectiveness of 2% Articaine as an Anesthetic Agent in Children: Randomized Controlled Trial. Clin. Oral Investig. 2018, 23(9), 3543–3550. DOI: 10.1007/s00784-018-2775-5 DOI: https://doi.org/10.1007/s00784-018-2775-5

19. Thiem, D.L.; Blatt, S.; Römer, P.; Heimes, D.; Bilal Al-Nawas; Kämmerer, P. W. Hyperspectral Imaging to Study Dynamic Skin Perfusion after Injection of Articaine-4% with and without Epinephrine—Clinical Implications on Local Vasoconstriction. J. Clin. Med. 2021, 10(15), 3411–3411. DOI: 10.3390/jcm10153411 DOI: https://doi.org/10.3390/jcm10153411

20. Yamamoto, T.; Inoue, T.; Yoshida, M.; Seki, S.; Kishimoto, N. Articaine as a Potential Alternative to Lidocaine in Japanese Dental Practice. J. Dent. Anesth. Pain Med. 2025, 25(3), 219–219. DOI: 10.17245/jdapm.2025.25.3.219 DOI: https://doi.org/10.17245/jdapm.2025.25.3.219

21. Lygre, H.; Moe, G.; Nerdal, W.; Holmsen, H. Interaction of Articaine Hydrochloride with Prokaryotic Membrane Lipids. Acta Odontol. Scand. 2009, 67(1), 1–7. DOI: 10.1080/00016350802443466 DOI: https://doi.org/10.1080/00016350802443466

22. Pelz, K.; Wiedmann-Al-Ahmad, M.; Bogdan, C.; Otten, J.-E. Analysis of the Antimicrobial Activity of Local Anaesthetics Used for Dental Analgesia. J. Med. Microbiol. 2008, 57(1), 88–94. DOI: 10.1099/jmm.0.47339-0 DOI: https://doi.org/10.1099/jmm.0.47339-0

23. Kaewjiaranai, T.; Srisatjaluk, R. L.; Sakdajeyont, W.; Pairuchvej, V.; Wongsirichat, N. The Efficiency of Topical Anesthetics as Antimicrobial Agents: A Review of Use in Dentistry. J. Dent. Anesth. Pain Med. 2018, 18(4), 223–233. DOI: 10.17245/jdapm.2018.18.4.223 DOI: https://doi.org/10.17245/jdapm.2018.18.4.223

24. Potočnik, I.; Tomšič, M.; Sketelj, J.; Bajrović, F. F. Articaine Is More Effective than Lidocaine or Mepivacaine in Rat Sensory Nerve Conduction Block in Vitro. J. Dent. Res. 2006, 85(2), 162–166. DOI: 10.1177/154405910608500209 DOI: https://doi.org/10.1177/154405910608500209

25. Borchard, U.; Drouin, H. Carticaine: Action of the Local Anesthetic on Myelinated Nerve Fibres. Eur. J. Pharmacol. 1980, 62(1), 73–79. DOI: 10.1016/0014-2999(80)90482-3 DOI: https://doi.org/10.1016/0014-2999(80)90482-3

26. Kanaa, M. D.; Whitworth, J. M.; Corbett, I. P.; Meechan, J. G. Articaine Buccal Infiltration Enhances the Effectiveness of Lidocaine Inferior Alveolar Nerve Block. Int. Endod. J. 2009, 42(3), 238–246. DOI: 10.1111/j.1365-2591.2008.01507.x DOI: https://doi.org/10.1111/j.1365-2591.2008.01507.x

27. Fowler, S.; Drum, M.; Reader, A.; Beck, M. Anesthetic Success of an Inferior Alveolar Nerve Block and Supplemental Articaine Buccal Infiltration for Molars and Premolars in Patients with Symptomatic Irreversible Pulpitis. J. Endod. 2016, 42(3), 390–392. DOI: 10.1016/j.joen.2015.12.025 DOI: https://doi.org/10.1016/j.joen.2015.12.025

28. Goutham, P. A. J.; Rajakumaran, A.; Kuzhanchinathan, M.; Balaji, L. Anesthetic Efficacy of Articaine versus Lignocaine as Supplementary Buccal Infiltration after Failed Inferior Alveolar Nerve Block – a Systematic Review of Randomized Clinical Trials. Endodontology 2023, 35(4), 297–303. DOI: 10.4103/endo.endo_9_23 DOI: https://doi.org/10.4103/endo.endo_9_23

29. Komsic, J.; Vujkov, S.; Neskovic, I.; Blagojevic, D.; Tadic, A.; Petrovic, B.; Bajkin, B. Comparative Evaluation of Alveolar Nerve Block with 2% Lidocaine–Epinephrine and 4% Articaine–Epinephrine Buccal Infiltration in Mandibular Premolar and Molar Region in Children: A Double-Blind, Randomized Trial. Children 2025, 12(2), Art. No: 215. DOI: 10.3390/children12020215 DOI: https://doi.org/10.3390/children12020215

30. Nogueira, E.; Almeida, R.; B. de Souza; Aguiar, P.; Vasconcellos, R. Why Choose Articaine over Lidocaine for the Removal of Third Molars? Systematic Review and Meta-Analysis. J. Clin. Exp. Dent. 2023, 15(11), e963–e977. DOI: 10.4317/jced.60682 DOI: https://doi.org/10.4317/jced.60682

31. Pasternak, M.; Woroń, J. Buffering of Injectable Local Anaesthesia Solution in Dentistry –Theory and Practice. Chair-Side Methods of Alkalinization. BÓL 2025, 26(1), 42–49. DOI: 10.5604/01.3001.0055.1224 DOI: https://doi.org/10.5604/01.3001.0055.1224

32. Pasternak, M.; Woroń, J. Pain Management and Discomfort Alleviation during Administration of Local Anaesthetic Solution – Methods Useful in Paediatric Dentistry. BÓL 2022, 23(2), 22–28. DOI: 10.5604/01.3001.0016.0381 DOI: https://doi.org/10.5604/01.3001.0016.0381

33. Mutlu, V.; Kaya, Z. Comparison of the Effect of the Lidocaine, Tetracaine, and Articaine Application into Nasal Packs on Pain and Hemorrhage after Septoplasty. Eur. Arch. Otorhinolaryngol. 2018, 275(10), 2481–2485. DOI: 10.1007/s00405-018-5084-3 DOI: https://doi.org/10.1007/s00405-018-5084-3

34. Mutlu, V.; Kaya, Z. Comparative Efficacy of Topical Lidocaine, Tetracaine, and Articaine for Post-Tonsillectomy Pain Management in Children: A Prospective, Placebo-Controlled Study. Acta Octolaryngol. 2024, 144(4), 320–324. DOI: 10.1080/00016489.2024.2372298 DOI: https://doi.org/10.1080/00016489.2024.2372298

35. Pasternak, M.; Woroń, J. Enhancing the Effectivity of Topical Anaesthesia – New Approaches, Formulations and Agents with the Possible Application in Dentistry. BÓL 2024, 25(4), 30–41. DOI: 10.5604/01.3001.0054.9765 DOI: https://doi.org/10.5604/01.3001.0054.9765

36. De Grado Gabriel, F.; Clément, B.; Florence, F.; Anne-Marie, M.; Damien, O. Efficacy of Articaine or Eugenol for Pain Relief after Emergency Coronal Pulpotomy in Teeth with Irreversible Pulpitis: A Randomized Clinical Trial. Dent. J. 2023, 11(7), Art. No: 167. DOI: 10.3390/dj11070167 DOI: https://doi.org/10.3390/dj11070167

37. Abdelraziq, M., Joachim, M. V., Resnick, C. M., Winocur, E., Laviv, A., & Abu El-Naaj, I. Controlling Postoperative Pain after Third Molar Extraction with a Dexamethasone and Articaine Injection: A Double-Blind Randomized Controlled Trial. Quintessence Int. 2023, 54(1), 24–32. DOI: 10.3290/j.qi.b3479957

38. Rodrigues da Silva, G. H., Paes Lemes, J. B., Geronimo, G., de Carvalho, F. V., Mendonça, T. C., Malange, K. F., de Lima, F.F.; Breitkreitz, M.C.; Parada, C.A.; Dalla Costa, T.; de Paula, E. Improved Local Anesthesia at Inflamed Tissue Using the Association of Articaine and Copaiba Oil in Avocado Butter Nanostructured Lipid Carriers. Pharmaceuticals 2023, 16(4), Art. No: 546. DOI: 10.3390/ph16040546 DOI: https://doi.org/10.3390/ph16040546

39. Batista, C.; Volpato, M. C.; Muniz, B. V.; Santos; Serpe, L.; Nunes, E.; Ferreira, N.; Fraceto, L. F.; Groppo, F. C.; Franz-Montan, M. Promising Potential of Articaine-Loaded Poly(Epsilon-Caprolactone) Nanocapules for Intraoral Topical Anesthesia. PLoS ONE 2021, 16(2), e0246760–e0246760. DOI: 10.1371/journal.pone.0246760 DOI: https://doi.org/10.1371/journal.pone.0246760

40. Malamed, S. F.; Gagnon, S.; Leblanc, D. Efficacy of Articaine: A New Amide Local Anesthetic. J. Am. Dent. Assoc. 2000, 131(5), 635–642. DOI: 10.14219/jada.archive.2000.0237 DOI: https://doi.org/10.14219/jada.archive.2000.0237

41. von Arx, T.; Lozanoff, S.; Zinkernagel, M. Ophthalmologic Complications after Intraoral Local Anesthesia. Swiss Dent. J. 2014, 124(7/8), 784–806. DOI: 10.61872/sdj-2014-07-08-02 DOI: https://doi.org/10.61872/sdj-2014-07-08-02

42. Steenen, S. A.; Dubois, L.; Saeed, P.; de Lange, J. Ophthalmologic Complications after Intraoral Local Anesthesia: Case Report and Review of Literature. Oral. Surg. Oral Med. Oral Pathol. Oral Radiol. 2012, 113(6), e1-5. DOI: 10.1016/j.tripleo.2011.07.032 DOI: https://doi.org/10.1016/j.tripleo.2011.07.032

43. de Oliveira, B.L.; Aparecida, M.; Hochuli-Vieira, E.; Pereira, A. Transient Diplopia Secondary to Dental Anesthesia. A Case Report. Rev. Port. Estomatol. M. 2016, 57(1), 51–54. DOI: 10.1016/j.rpemd.2015.11.011 DOI: https://doi.org/10.1016/j.rpemd.2015.11.011

44. Alamanos, C.; Raab, P.; Gamulescu, A.; Behr, M. Ophthalmologic Complications after Administration of Local Anesthesia in Dentistry: A Systematic Review. Oral. Surg. Oral Med. Oral Pathol. Oral Radiol. 2016, 121(3), e39–e50. DOI: 10.1016/j.oooo.2015.10.023 DOI: https://doi.org/10.1016/j.oooo.2015.10.023

45. Piccinni, C.; Gissi, D. B.; Gabusi, A.; Montebugnoli, L.; Poluzzi, E. Paraesthesia after Local Anaesthetics: An Analysis of Reports to the FDA Adverse Event Reporting System. Basic Clin. Pharmacol. Toxicol. 2014, 117(1), 52–56. DOI: 10.1111/bcpt.12357 DOI: https://doi.org/10.1111/bcpt.12357

46. Aps, J.; Badr, N. Narrative Review: The Evidence for Neurotoxicity of Dental Local Anesthetics. J. Dent. Anesth. Pain Med. 2020, 20(2), 63-72. DOI: 10.17245/jdapm.2020.20.2.63 DOI: https://doi.org/10.17245/jdapm.2020.20.2.63

47. Malanin, K; Kalimo, K. Hypersensitivity to the local anesthetic articaine hydrochloride. Anesth. Prog. 1995, 42(3-4), 144-145.

48. Ho, J.-P. T. F.; van Riet, T. C. T.; Afrian, Y.; Sem, K. T. H. C. J.; Spijker, R.; de Lange, J.; Lindeboom, J. A. Adverse Effects Following Dental Local Anesthesia: A Literature Review. J. Dent. Anesth. Pain Med. 2021, 21(6), 507-525. DOI: 10.17245/jdapm.2021.21.6.507 DOI: https://doi.org/10.17245/jdapm.2021.21.6.507

49. Hascoët, E., Mahé, J., Meillard, H., Théophile, H., Cloitre, A., & Lesclous Anaphylactic Reactions to Local Anesthetics in Dental Practice: A Nationwide French Retrospective Study. Clin. Oral Investig. 2021, 26(2), 1667–1676. DOI: 10.1007/s00784-021-04139-5 DOI: https://doi.org/10.1007/s00784-021-04139-5

50. Jevon, P.; Shamsi, S. Management of Anaphylaxis in the Dental Practice: An Update. Br. Dent. J. 2020, 229(11), 721–728. DOI: 10.1038/s41415-020-2454-1 DOI: https://doi.org/10.1038/s41415-020-2454-1

51. Tomoyasu, Y.; Mukae, K.; Suda, M.; Hayashi, T.; Ishii, M.; Sakaguchi, M.; Watanabe, Y.; Jinzenji, A.; Arai, Y.; Higuchi, H.; Maeda, S.; Miyawaki, T. Allergic Reactions to Local Anesthetics in Dental Patients: Analysis of Intracutaneous and Challenge Tests. Open Dent. J. 2011, 5(1), 146–149. DOI: 10.2174/1874210601105010146 DOI: https://doi.org/10.2174/1874210601105010146

52. Bina, B.; Hersh, E. V.; Hilario, M.; Alvarez, K.; McLaughlin, B. True Allergy to Amide Local Anesthetics: A Review and Case Presentation. Anesth. Prog. 2018, 65(2), 119–123. DOI: 10.2344/anpr-65-03-06 DOI: https://doi.org/10.2344/anpr-65-03-06

53. Lin, Y.; Li, X.; Sun, Y.; Liu, X.; Lu, Z. Local tissue necrosis of hard palate mucosa caused by articaine hydrochloride and epinephrine tartrate injection: one case report. J. Oral Sci. Res. 2021, 37(5), 479-480.

54. Roth, J. V.; Shields, A. A Dilemma: How Does One Treat Anaphylaxis in the Sulfite Allergic Patient since Epinephrine Contains Sodium Metabisulfite? Anesth. Analg. 2004, 98(5), Art. No: 1499. DOI: 10.1213/01.ane.0000120092.39021.f2 DOI: https://doi.org/10.1213/01.ANE.0000120092.39021.F2

Downloads

Published

2025-08-13

Issue

Section

Articles

How to Cite

Articaine – the queen of infiltrative anaesthesia? A peculiar amino-amide local anaesthetic and its use in the dental practice from a pharmacological perspective. (2025). Prospects in Pharmaceutical Sciences, 24(1), 31-38. https://doi.org/10.56782/pps.569

Similar Articles

You may also start an advanced similarity search for this article.