Articaine (Septocaine®)

Articaine is the newest addition to the local anesthetic arsenal and was approved by the Food and
Drug Administration in April 2000. It has been in use in Europe since 1976 and in Canada since
1983. Its approval in the US has been delayed by the FDA due to the presence of a preservative
which the agency said was unnecessary in single use carpules and was a potential allergen. It was
approved when the French company Septodent finally removed the preservative from American
shipments.
Articaine has the same PKa and toxicity as Lidocaine,
however it is metabolized differently. It has a half life
in the body less than 1/4 as long as that of lidocaine
and only 1/5 as long as mepivicaine.
This means that more of the drug can be injected later
in the dental procedure with less likelihood of blood
concentrations building to toxic levels. Articaine is formulated in a 4.0% solution with
vasoconstrictor. The presence of the vasoconstrictor retards the systemic absorption of the
anesthetic allowing higher concentrations of the drug to remain in the area of injection and
slowing the absorption into the bloodstream. The higher local concentration of the drug
produces a high level of the uncharged radical (RN) to be present at the membrane which brings
about very rapid absorption of the drug. (The concept of membrane permeability is discussed on
page 4 in this course.) In addition, the benzene ring on the left end of the molecule has been
replaced with a thiophene ring. This modification allows for faster and more complete absorption
through the nerve cell membrane. The ability of this drug to penetrate barriers is so great that it
has been used to penetrate thick bone to produce anesthesia in a way that other anesthetics
cannot. Articaine has become the local anesthetic of choice in most countries into which it has
been introduced. I have found that it produces profound anesthesia (in most patients) when used
as an infiltration (field block) for mandibular premolars and anterior teeth instead of the
traditional mandibular nerve block..
With clinical reports of profound anesthesia, fast onset, and success in difficult-to-anesthetize
patients, Septocaine has become the most used dental anesthetic brand name in the US, although
lidocaine still remains the most used type of anesthetic. Recently, the same articaine
formulation became available from a second company under the name Cook-Waite Zorcaine.
Because of its bone penetrating ability, articaine has become popular for producing
profound anesthesia in lower premolars and lower anterior teeth using localized field
blocks (infiltrations) without resorting to mandibular blocks.
Articaine and prolonged numbness and paresthesia
Unfortunately, one complication concerning the use of articaine has arisen. There have been
persistent reports of unexplained paresthesia (burning, tingling, and sometimes sharp shooting
pains in tissues previously anesthetized with this anesthetic) in a low percentage of patients.
This effect has been noted only when articaine is used in major nerve blocks such as the
mandibular block. It has not been noted in field blocks. So far, no common factor has been
found to explain the link between articaine and persistent paresthesia, however the higher
concentration of anesthetic molecules in the anesthetic solution (4% for articaine instead of 2%
for lidocaine or 3% for mepivicaine without vasoconstrictor) probably is a factor. The statistics
produced for this phenomenon so far have been quite inconsistent. The incidence for persistent
paresthesia have ranged between 1 in 5,286 for 2002 to 1 in 45,900 in 2004. The incidence for
persistent paresthesia for other types of dental local anesthetic solutions ranged between 1 in
25,850 to 1 in 68,675 during the same timeframe (all statistics approximate; CRA June 2005; vol
29, issue 6).
• 10% of cases of paresthesia lasted for 24 hours or less.
• 52% of cases of paresthesia lasted 1 to 4 weeks.
• 29% of cases of paresthesia lasted 1 month to 1 year.
• 10% of cases of paresthesia lasted for over a year.
• The most common link with articaine and paresthesia was administration of mandibular
nerve block injections. For this reason a number of dentists have abandoned the use of
articaine for mandibular nerve blocks, but still use it for infilatration anesthesia (field
blocks) of mandibular anterior teeth and bicuspids.
In defense of articaine, it should be noted that prolonged paresthesia and numbness are very
uncommon occurrances, and the chances of getting this type of injury are quite slim.
Furthermore, 75% of these cases are associated with the lingual nerve (the one that makes the
tongue numb when you get a lower tooth filled). This leads one to question why this should be
the case when the vast bulk of the anesthetic solution is actually delivered at the site of the
inferior alveolar nerve while only a few drops are delivered to the lingual nerve while
withdrawing the needle. If the anesthetic itself is the culprit in the paresthesia, it would make
sense if the symptoms should occur more frequently in the distribution of the inferior alveolar
nerve (the chin, lip and teeth) rather than in the tongue.
Finally, many dentists are beginning to use articaine for mandibular blocks since this anesthetic
produces vastly fewer anesthetic failures than lidocaine or mepivicaine.