Articaine Hydrochloride

Interaction between a local anesthetic drug, articaine (ART) and human serum albumin (HSA) was investigated in the absence and presence of paracetamol (PAR) and caffeine (CAF) using spectroscopic, voltammetric, and computational techniques for the first time. The results demonstrated that increasing concentrations of ART in HSA solution led to a decrease in HSA fluorescence signal, indicating the ART-HSA complex formation via the static quenching mechanism. The binding strength of the complex was moderate (binding constant, K_a = 5.87 × 10³ M^-1 in fluorescence and 6.31 × 10³ M^-1 in voltammetric at 298 K). Thermodynamic analysis (ΔS = +28.32 J mol^-1 K^-1; ΔH = -30.17 kJ/mol) of the binding reaction suggested involvement of hydrophobic interactions, van der Waal's forces and hydrogen bonding in stabilizing the ART-HSA complex. Significant microenvironmental alterations near the Trp and Tyr residues of HSA consequent to the ART-HSA complex formation. ART predominantly binds to Sudlow's site I of HSA with more negative binding energy and stronger hydrophobic interactions compared to Site II. The stability of the ART-HSA complex at Site I over a 100 ns timeframe, supported by stable hydrogen bonding and compact HSA structure throughout the molecular dynamics simulations. The effect of PAR and CAF on the binding strength between ART and HSA was also examined, and presence of PAR and CAF in the reaction mixture produced significant reduction in the binding affinity of ART to HSA. These findings underscore the competitive binding between ART, PAR, and CAF, which impacts their pharmacokinetics and efficacy. This study provides valuable insights into the complex interactions between anesthetic drugs and common pharmaceuticals, potentially guiding clinical practices and drug development.

Articaine is a dental anesthetic that has been developed and widely used in recent years. This study aimed to compare the anesthetic efficacy and safety of infiltration anesthesia with 4 % Articaine (with 1:100,000 epinephrine) and block anesthesia with 2 % Lidocaine (with 1:100,000 epinephrine) in the mandibular third molar extraction.

This prospective, randomized, split-mouth clinical trial was planned to involve 30 adults with the bilateral mandibular third molars. Participants were randomly assigned to receive 4 % Articaine (Articaine group) by infiltration anesthesia on one side and 2 % Lidocaine (Lidocaine group) by block anesthesia on the opposite side. Parameters such as the heart rate, blood pressure, oxygen saturation, anesthetic usage, operation duration, pain score, satisfaction, and adverse events were recorded and analyzed.

Finally, 26 participants receiving the bilateral mandibular third molar extraction were included. There were no significant differences in the heart rate, blood pressure, oxygen saturation, and maximum fluctuations during the extraction procedure between the two groups, except the maximum heart rate fluctuation showing statistical significance. Additionally, the amount of anesthetic used was significantly lower in the Articaine group (1.5 ± 0.4 cartridges) than in the Lidocaine group (2.2 ± 0.5 cartridges) (P < 0.001). There were no significant differences in the operation duration, pain score, and satisfaction between the two groups, and no adverse events were reported in either group.

Using 4 % Articaine for infiltration anesthesia offers comparable pain control to 2 % Lidocaine for block anesthesia in the mandibular third molar extraction surgery. Using 4 % Articaine can safely achieve similar pain control with lower doses and less invasive anesthesia techniques.