One of the most important aspects of endodontic treatment is profound anesthesia. We as dentists are always seeking the magic bullet of patient anesthesia, a new chemical or technique that will work every time, producing deep and profound anesthesia for the patient. Over the years a constant refrain has been, “you are a great doctor, you didn’t hurt me a bit.” Therefore, I am always on the lookout for new gadgets, techniques, and anesthetics that will help me achieved the goal of total anesthesia during any dental procedure.
Articaine was synthesized in Germany in 1969 and introduced for clinical use in 1976 (1). In 2000, the FDA granted approval for the sale and distribution of articaine (brand name Septocaine) as a 4.0% solution with epinephrine 1:100,000. Because of its reported superior clinical properties—more success in achieving anesthesia, the ability to achieve more profound anesthesia, the success of buccal infiltration in the maxilla to achieve palatal anesthesia, and the success of mandibular infiltration to replace inferior alveolar block anesthesia—articaine has captured a major portion of local anesthesia usage by dentists throughout the world (2).
In a 2000 report, a majority of 94 dentists stated that articaine was more profound than “routinely used anesthetics.” In addition, the onset of effects was faster and the anesthesia achieved greater success among the difficult-to anesthetizes patients. A minority of the 94 dentists cited a reduction in the number of missed blocks and noted articaine’s effectiveness in mandibular infiltration-facilitated treatment of pediatric and apprehensive patients (3).
Other reports have indicated that articaine has low toxicity due to rapid hydrolysis (and a lack of toxicity in healthy individuals after unintentional intravascular injection), as well as a more rapid onset of surgical anesthesia, a faster elimination time than lidocaine, and better diffusion through soft tissue and bone than other anesthetics (4,5). The time to maximum drug concentrations of articaine occurs about 10 to 15 minutes after submucosal injection of articaine 4% 80mg, irrespective of 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 (5). According to Dudkiewicz et al., articaine was able to diffuse through bone onto the lingual side of each tooth in the clinical trial (6). This higher diffusion could result from articaine’s higher lipid solubility compared to lidocaine, prilocaine, and bupivacaine (2). In a study by Kanaa et al., mandibular buccal infiltration was found to be more effective with 4% articaine with epinephrine compared to 2% lidocaine with epinephrine (7). Vree and Gielen found that articaine diffuses better through soft tissue and bone than other local anesthetics. 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. Articaine is metabolized via hydrolysis into articainic acid, 75% of which in turn is excreted as such, and 25% in the glucuronidated form by the kidneys (8).
With all this literature behind articaine you would think that it would be very clinically effective. However, there is a mounting body of evidence that says that it does not outperform the old standard of lidocaine with 1:100,00 epinephrine. In a prospective, randomized, double-blind study by Mikesell et al., it was concluded that for pulpal anesthesia a 4% articaine with 1:100,000 epinephrine was similar to 2% lidocaine with 1:100,000 epinephrine in inferior alveolar nerve blocks (9). In a prospective, randomized, double blind study, Berlin et al. concluded that the efficacy of 4% articaine with 1:100,000 epinephrine was similar to the efficacy of 2% lidocaine with 1:100,000 epinephrine for intraligamentary injections (10). Claffey et al. did a prospective, randomized, double-blind study to compare the anesthetic efficacy of 4% articaine with 1:100,000 epinephrine to 2% lidocaine with 1:100,000 epinephrine for inferior alveolar nerve blocks in patients experiencing irreversible pulpitis in mandibular posterior teeth. They found that there was no significant difference (p=0.89) between the articaine and lidocaine solutions. Neither solution resulted in an acceptable rate of anesthetic success in patients with irreversible pulpitis (11).
One of the most important clinical recommendations is that the dentist must be aware that articaine delivers nearly twice the concentration of active anesthetic to the patient; as a result, the dentist can use approximately one-half the amount of articaine to achieve similar anesthetic delivery. Because of articaine’s rapid onset and relatively short half-life, the dentist may want to administer more anesthetic carpules. Due to its high lipid solubility, deposition of the anesthetic in the tissues may result in adverse effects occurring more frequently if the dentist is not cautious about using additional doses. If the dentist is aware of these considerations, articaine is an effective and safe anesthetic that can be used to achieve profound anesthesia (2). Clinically, when I first started using articaine (approximately 5 years ago) I was not aware of this recommendation. A referring dentist sent me a “hot” cuspid because he could not get anesthesia. Five articaine carpules later I did get anesthesia and completed the root canal treatment. The problem occurred because the patient remained “numb” for approximately four days afterward. I had not previously been aware that such a complication could or did exist. (Currently, I still use articaine, but I limit it to one carpule of 4% 1:100,000 epinephrine.) Many articles in the literature report such occurrences. Haas and Lennon, in a 21-year retrospective study, reported that paresthesia occurred most often following the injection of articaine and prilocaine (12). The observed frequencies of paresthesia following the administration of articaine (pClinically in my practice, I have observed about a 20-25% increase in potency of anesthesia when doing endodontics. I must keep a strict eye out concerning the dosage of articaine given; however, within these limits it is a product well worth using.
References:
- Malamed SF, Gagnon S, Leblanc D. Articaine hydrochloride: A study of the safety of a new amide local anesthetic. J Am Dent Assoc 2001;132:177-185
- Wynn RL, Bergman SA, Meiller TF. Paresthesia associated with local anesthetics: A perspective on articaine AGD Impact 2003 Nov-Dec
- Anesthetics, local (articaine HCL 4% with epinephrine 1:100,000). CRA Newsletter 2002;25:1-2
- van Eeden sp, Patel MF Re: Prolonged paresthesia following inferior alveolar block using articaine. Brit J Oral Maxillofac Surg 2002;40:519-520
- Oertel R, Rahn R, Kirch W. Clinical pharmacokinetics of articaine. Clin Pharmacokinet 1997;33:417-425
- Dudkiewicz A, Schwartz S, Laliberte R. Effectiveness of mandibular infiltration in children using the local anesthetic Ultracaine (articaine hydrochloride). J Can Dent Assoc 1987;53:29-31
- Kanaa MD, Whitworth JM, Corbett IP, Meechan JG. Articaine and lidocaine mandibular buccal infiltration anesthesia: a prospective randomized double-blind cross-over study. J Endod 2006;32:296-298
- Vree TB, Gielen MJ. Clinical pharmacology and the use of articaine for local and regional anaesthesia. Best Pract Res Clin Anaesthesiol 2005;19:293-308
- Mikesell P, Nusstein J, Reader A, Beck M, Weaver J. A comparison of articaine and lidocaine for inferior alveolar nerve blocks. J Endod 2005;31:265-70
- Berlin J, Nusstein J, Reader A, Beck M, Weaver J. Efficacy of articaine and lidocaine in a primary intraligamentary injection administered with a computer-controlled local anesthetic delivery system. Oral Surg Oral Med Oral Pathol Oral Radiol Endod. 2005;99:361-366
- Claffey E, Reader A, Nusstein J, Beck M Weaver. Anesthetic efficacy of articaine for inferior alveolar nerve blocks in patients with irreversible pulpitis. J Endod 2004;30:568-71
- Hass DA, Lennon D. A 21 year retrospective study of reports of paresthesia following local anesthetic administration. J Can Dent Assoc. 1995 ;61:319-30
- Hellerup S, Jensen R. Nerve injury caused by mandibular block analgesia. Int J Oral Maxillofac Surg. 2005 9
Review Synopsis
Product
Septocaine Articaine Anesthesia
The Good
None noted.
The Bad
None noted.
The Bottom Line
I must keep a strict eye out concerning the dosage of articaine given; however, within these limits it is a product well worth using.