Updated: Apr 20, 2021
Articaine really has some mystery surrounding it, but honestly there isn’t anything to be afraid of when it comes to this anesthetic solution.
A little articaine history for you…I promise it won’t be mind numbing.
Articaine was formulated for dentistry. Can I get a woot woot! In comparison it is still considered the new kid on the nerve block. In 1969, the year is was first created we called this anesthetic carticaine. However, in 1976 it transitioned into what we now know as articaine. You might call it by its trade name of Septocaine (others are Zorcaine and Orabloc). It’s popularity over the years has risen. In Europe and Canada this solution is a regular go to and is becoming so for the USA.
In my opinion, this amide-based anesthetic has been given a bad rep over the years causing clinicians to steer clear of using it, or only using it for maxillary injections and reserved for only certain patients. When in reality, it should become our go-to anesthetic.
Why you ask?
Well, articaine is 90% metabolized by cholinesterase in the blood stream, leaving the last 10% to be processed by the liver then kidneys. This makes it ideal for liver and kidney compromised patients, because so much less of the anesthetic contacts these organs compared to other amide anesthetics. For example, lidocaine practically makes the liver do all the hard work.
Also, the half-life of the solution, on average, is about 45 minutes (depending on the literature 27-60 min). Which reduces the opportunity for toxic effects, which is a major plus for our anesthetic drugs.
Even better, nursing moms can clear it from their system quickly. While there is not strong evidence that the anesthetic is found in breast milk, this could help alleviate concerns regarding breast feeding after anesthetic delivery (it has a nursing classification as S+, which is good). And by the way, the pump and dump method is considered an outdated procedure, (read here for more). Articaine is even gaining popularity for our pregnant patients. Even though it is a FDA pregnancy category C, newer research has shown no adverse side effects when articaine was given to pregnant patients. It was a small sample size, around 200 pregnant women, and all the pregnancies and deliveries resulted in healthy babies. The gaining popularity is due to its quick half-life which shortens the exposure time and its reduced strain on the liver, by being metabolized by the cholinesterase in the blood. (please note the FDA has assigned lidocaine and prilocaine a category B, which is still considered to be the safest selection)
Another bonus of articaine is its ability to diffuse through bone better than most anesthetic solutions. This is due to the chemical formulation. While articaine is considered an amide anesthetic it has a small little tweak to its molecular make-up by having a thiophen ring instead of a benzene ring. (UGH chemistry right?). Basically, this small switch makes the solution more lipid soluble so it can diffuse through tissue easier. Using it for palatal injections and mandibular infiltration works well. Especially if you are working with children for example. Instead of giving an inferior alveolar (IA) injection you could infiltrate around the molars and achieve profound anesthesia to the pulpal and sometimes even lingual tissue. If you happen to work in a state in which dental hygienists can only do mandibular infiltration, load your syringe with this solution to increase your success.
Also, the anesthetic has an ester-linkage which is why it can metabolize in the blood stream.
DON'T BE SCARED....
Now let me address the biggest concern people have about the use of articaine, and that is for nerve blocks and the potential cause for paresthesia. The research coming out which debunks this entire theory is on the rise. However, some textbooks and therefore many schools continue to teach this as an adverse reaction and do not allow its use for IA injections. Even Stanley Malamed, who I consider the Guru of oral anesthesia, has worked to change this concern. Here’s the thing, there is no statistical evidence that this anesthetic causes more paresthesia than any other. It has been deemed rare for this to happen with only 14 cases of parasthesia happening out of 11 million injections. Wait…pause and read that again. Only 14 cases in 11,000,000, that is a .0013% of happening. In fact, in a different study, there were more parasthesia cases with lidocaine than with articaine.
To refute this concern even more is understanding why it became such a hot topic. One write up I read indicated that the frenzy of concern came from a letter from an insurance company which went to thousands of dentists stating they had seen a rise in reversible and non-reversible paresthesia, and informing them they should increase their malpractice insurance coverage. Later, the letter was retracted stating they had not completed any scientific study, nor was there an increase in malpractice claims. However, the seed of doubt was planted and easily bloomed throughout our industry.
As with any local anesthetic considerations must be made. Articaine does have formulations with vasoconstrictors. The common formulation is 4% articaine with 1:100,000 epi and 4% articaine with 1:200,000 epi. When vasoconstrictors are added care must be made for patients who can have adverse reactions to these. Such as our patients with uncontrolled diabetes and hyperthyroidism. Also, patients with severe cardiac issues should have modifications made. Using the solution with the 1:200,000 epi should be selected for cardiac compromised patients. Since it’s part of the amide family, an allergic reaction is rare. Usually, it will be due to the preservative included to keep the vasoconstrictor with a stable shelf-life. If you have a patient who has a true allergy to sulfites, use of any anesthetic with vasoconstrictor is strictly prohibited.
Let’s not forget about proper dosage as well. Articaine is all weight dependent. You can administer 3.2 mg/lb., or, for you kilogram loving folks 7.0 mg/kg.
Now, I challenge you to boldly load your syringe with this awesome little solution and confidently give your best shot!
Bassett, DiMarco, Naughton: Local Anesthesia for the Dental Professionals 2nd ed
Malamed: Handbook of Local Anesthesia 6th ed
de Ridder, Politis: Unclarities About Articaine: Contraindications. Stoameduj.com
"Alternate Anesthetic Solutions For The Inferior Alveolar Nerve Block" ENDODONTICS: Colleagues of Excellence, Winter 2009.