Articaine: Designed for Effective Dental Anesthesia

In the quest for safe and successful dental care, there are endless choices to make—whether it's choosing a new bonding agent or handpiece, deciding on the best treatment plan, or figuring out which days and hours to keep the office open for appointments. There's also a choice between different types of local anesthetic agents, such as articaine and and lidocaine. “Lidocaine is a great drug, but when articaine was developed for the unique challenges of dentistry, it just upped the game,” noted Kathy Bassett, BSDH, RDH, MEd. “Articaine is superior in a number of important ways, so there’s no reason for dentistry not to routinely use it at this point.”

Although articaine has been around for quite a while, it is still considered the “new kid on the block” in the United States. While many dental professionals still solely rely on lidocaine because it’s the anesthetic they know and trust, noted Bassett, articaine offers some significant benefits over lidocaine that many might find surprising.

The History

Lidocaine, first introduced in the 1940s, was developed to meet a critical need for pain management in medicine. It was later co-opted for use in dentistry and became the gold standard for dental pain management globally.

Articaine, first available in Germany and Switzerland in 1976, was developed specifically for dentistry, responding to the unique challenges of dental local anesthesia. Available in Europe for more than 40 years, it has been in use in the United States for almost 25 years. As articaine’s popularity has increased, it more recently has been adopted for use in medicine as well.

As more clinicians use articaine, its record as a safe and profoundly effective local anesthetic expands. In fact, Bassett proposes that articaine be the first choice for dental local anesthesia.

Pharmacological Advantage

While both lidocaine and articaine are safe and effective options with well established histories of success, articaine is the first hybrid local anesthetic with both ester and amide properties. This pharmacological advantage addresses dentistry’s requirements for safe, profound, and durable local anesthesia.

More specifically, due to its protein binding affinity, articaine readily diffuses through tissue and nerve membranes. "In most cases, you can administer half the volume of articaine to achieve the same anesthesia outcome," said Bassett. "Milligram per milligram, articaine is inherently less toxic than lidocaine, making it even safer. This is especially beneficial for patients with compromised organ functions."

Safety & Efficiency

Another property that is especially important for patients with compromising medical conditions is articaine’s unique metabolic pathway that avoids liver metabolism, as 90% to 95% of articaine is detoxified prior to reaching the liver. “One of the main benefits is articaine’s fast half-life,” Bassett said. This allows it to be cleared from the circulatory system in 15 to 45 minutes vs lidocaine’s almost 2 hours, which reduces the amount of time the drug is being metabolized in the body. This is an important treatment consideration for those seeking to reduce the impact of any drug in circulation, such as patients who are pregnant or lactating.

“It’s really a conversation of pharmacology and the nature of the tissues,” Bassett said. “Articaine has a strong affinity for lipids in nerve membranes and surrounding tissues, thus improving drug diffusion and the subsequent onset of anesthesia of ~1 to 9 minutes. This has been demonstrated by the current clinical practice of using a combination of buccal and lingual infiltrations with articaine to achieve profound anesthesia in the mandible. Research1 has further noted that with buccal infiltrations in the maxilla, higher concentrations of articaine diffuse through soft tissues and bone into the palatal tissues when compared to lidocaine. This demonstrates the superior diffusibilty of articaine, which is also noted for specific applications2 such as pulpitis, where articaine efficacy significantly exceeds all other local anesthetics."

A Little Goes a Long Way

Articaine is available in 2 formulations: first marketed as 4% articaine with 1:100,000 epinephrine, and later, with 1:200,000 epinephrine. The product information recommends 4% articaine with 1:200,000 epinephrine as the first choice for procedures needing more rigorous hemostasis, and then to use the 1:100,000 epinephrine formulation.

Ultimately, articaine achieves more profound anesthesia with smaller volumes, and it has a shorter half-life, Bassett advised. “It allows dental clinicians to get their patients numb quickly and trust that they will stay numb throughout the procedure,” she concluded.

References

_{1. Al-Mahalawy H, Abuohashish H, Chathoth S, Al-Masoud N, Al-Jandan B. Articaine versus lidocaine concentration in palatal tissues after supraperiosteal buccal infiltration anesthesia.}

_{J Oral Maxillofac Surg. 2018;76:315.e1–315.e7.}

_{2. Martin E, Nimmo A, Lee A, Jennings E. Articaine in dentistry: an overview of the evidence and meta-analysis of the latest randomised controlled trials on articaine safety and efficacy compared to lidocaine for routine dental treatment [published correction appears in BDJ Open. 2021 Aug 11;7(1):29]. BDJ Open. 2021;7(1):27. Published 2021 Jul 17. doi:10.1038/s41405-021-00082-5.}