How is articaine primarily metabolized?

Articaine is primarily metabolized through a combination of plasma esterases and cytochrome P450 (CYP) enzymes, with a significant portion being broken down by plasma esterases. About 95% of articaine is hydrolyzed by these plasma esterases, which are found in the blood. This rapid hydrolysis results in the formation of a pharmacologically active metabolite known as articainic acid. The remaining 5-10% is metabolized by CYP enzymes in the liver.

This metabolism profile is particularly significant because it highlights articaine's relatively fast onset and shorter duration of action compared to some other local anesthetics, which rely more heavily on hepatic metabolism. The primary role of plasma esterases in the rapid breakdown of articaine could explain its broad use in dental procedures. The rapid metabolism also results in a lower potential for toxicity and a favorable safety profile.

Understanding this metabolism pathway is crucial, as it informs clinicians about potential drug interactions and the implications for patients with liver dysfunction, where hepatic metabolism might be compromised.