Effects of Local Anesthetics on Cellular Necrosis, Apoptosis and Inflammatory Modulation: Short Review

Abstract

Objectives: Local anesthetics (LAs) cause the loss of sensitivity to the nociceptive stimulus by the reversible blockade of the neural electrical impulse. These drugs are widely used for pain control in many clinical procedures and in other therapeutic applications. Besides the effects on voltage-gated sodium channels, LAs can modulate different cellular pathways. The review seeks to address the effects of local anesthetics on the cellular viability, apoptosis induction and inflammatory response. Methods: Data was collected from MEDLINE®, Scopus® and Web of Science, the searches were performed between November 2017 and April 2018. Results: LAs induce necrosis and apoptosis in a time and dose-dependent manner. Apoptosis occurs primarily by the intrinsic pathway through the loss of mitochondrial membrane potential. These molecules were able to reduce the release of pro-inflammatory cytokines, chemokines, COX-2, PGE2 and decrease the activation of NF-κB. Conclusion: The cytotoxic effects of LA are relate to high concentrations and prolonged exposure times. LAs activate the intrinsic pathway of apoptosis through cytochrome c release. In concentrations lower than required to perform sensory and motor block, LAs show anti-inflammatory effects.