Articaine

General information

Articaine is an aminoamide that also contains an ester group, which is rapidly hydrolysed by plasma esterases. It is 4-methyl-3([2-(propylamino)propionamido)]-2-thiophenecarboxylic acid, methyl ester hydrochloride. The thiophene group increases its lipid solubility while the ester group enables it to undergo plasma esterase hydrolysis as well as hepatic enzyme metabolism. Articaine is formulated as a 4% solution with adrenaline. It is the most widely used local anesthetic agent in dentistry in some parts of Europe.

The rapid breakdown of articaine to an inactive metabolite means that it has low systemic toxicity. However, the risk of intravascular injection is high in dentistry, and articaine can cause central nervous system and cardiovascular toxicity. However, articaine is slightly more potent than lidocaine and causes less nervous system toxicity [ ].

The safety of articaine has been studied in a series of three randomized trials [ ]. The adverse effects deemed to be related to articaine were headache, paresthesia/hyperesthesia after injection, infection, and rash. There was one case of mouth ulceration. The overall incidence of adverse effects was comparable to that of lidocaine.

Organs and systems