IADR Abstract Archives
PK/PD Study of 2% Lidocaine With or Without 1:100,000 Epinephrine
Objectives: Lidocaine is the most widely used and safest amide-type local anesthetic in dentistry. Nonetheless, it can cause some side effects on cardiovascular and central nervous systems. The aim of this study was to evaluate the pharmacodynamic (PK) and pharmacokinetic (PD) parameters of 2% lidocaine alone or associated with 1:100,000 epinephrine after infiltrative injection in the maxillary molar region in healthy participants for crown-root scaling.
Methods: Twenty volunteers underwent crown-root scaling in the upper molars region with infiltration of 2% lidocaine associated (n=10) or not (n=10) with 1:100,000 epinephrine. For PK parameters, lidocaine and its the main metabolite (MEGX) concentrations were measured in sequential saliva samples (at 0.25, 0.5, 0.75, 1, 1.5, 2, 3, 4, 5, 6 8, 11, 24, 48, 72 and 96 h) through LC MS/MS. PK analyses were carried out using WinNolin software (version 8.1). For PD parameters, the variation of following data were obtained using a vital signs monitoring device: systolic, diastolic, and mean blood pressure, oximetry and heart rate.
Results: Maximum concentration of lidocaine (Cmax – ng/mL) was significantly higher (p=.001) in saliva of patients undergoing crown-root scaling with 2% lidocaine associated with 1:100,000 epinephrine (6974.13±7119.47) compared to those without this vasoconstrictor (1195.7±2522.08). For MEGX metabolite, the Area Under the Curve (AUC h″ng/μL) valures were significantly higher (p=.029) when 1:100,000 epinephrine was used (87990.52±46465.57) in comparison to procedures performed without this vasoconstrictor (44070.66±35627.83). Increased values, despite not statistically significant, were observed for AUC in volunteers anesthetized with 2% lidocaine with 1:100,000 epinephrine (p=.074). Finally, significant differences were not found for PD parameters.
Conclusions: It is possible to use saliva samples to determine PK parameters of 2% lidocaine alone or associated with 1:100,000 epinephrine after infiltrative injection in the maxillary molar region in healthy participants for crown-root scaling. The use of epinephrine as a vasoconstrictor promoted a higher Cmax for lidocaine and higher AUC for MEGX, the main metabolite of lidocaine.
Methods: Twenty volunteers underwent crown-root scaling in the upper molars region with infiltration of 2% lidocaine associated (n=10) or not (n=10) with 1:100,000 epinephrine. For PK parameters, lidocaine and its the main metabolite (MEGX) concentrations were measured in sequential saliva samples (at 0.25, 0.5, 0.75, 1, 1.5, 2, 3, 4, 5, 6 8, 11, 24, 48, 72 and 96 h) through LC MS/MS. PK analyses were carried out using WinNolin software (version 8.1). For PD parameters, the variation of following data were obtained using a vital signs monitoring device: systolic, diastolic, and mean blood pressure, oximetry and heart rate.
Results: Maximum concentration of lidocaine (Cmax – ng/mL) was significantly higher (p=.001) in saliva of patients undergoing crown-root scaling with 2% lidocaine associated with 1:100,000 epinephrine (6974.13±7119.47) compared to those without this vasoconstrictor (1195.7±2522.08). For MEGX metabolite, the Area Under the Curve (AUC h″ng/μL) valures were significantly higher (p=.029) when 1:100,000 epinephrine was used (87990.52±46465.57) in comparison to procedures performed without this vasoconstrictor (44070.66±35627.83). Increased values, despite not statistically significant, were observed for AUC in volunteers anesthetized with 2% lidocaine with 1:100,000 epinephrine (p=.074). Finally, significant differences were not found for PD parameters.
Conclusions: It is possible to use saliva samples to determine PK parameters of 2% lidocaine alone or associated with 1:100,000 epinephrine after infiltrative injection in the maxillary molar region in healthy participants for crown-root scaling. The use of epinephrine as a vasoconstrictor promoted a higher Cmax for lidocaine and higher AUC for MEGX, the main metabolite of lidocaine.