RT Book, Section A1 Hadzic, Admir SR Print(0) ID 1183901558 T1 Local Anesthetics: Clinical Pharmacology and Selection T2 Hadzic's Peripheral Nerve Blocks and Anatomy for Ultrasound-Guided Regional Anesthesia, 3e YR 2021 FD 2021 PB McGraw-Hill PP New York, NY SN 9780071838931 LK accessanesthesiology.mhmedical.com/content.aspx?aid=1183901558 RD 2024/03/29 AB Local anesthetics (LAs) have been used for more than a century to block nociceptive signals. They bind to the specific receptor sites on the sodium (Na+) channels in nerve cells to interrupt nerve conduction by blocking the entrance of ions across the cell membrane. LAs also activate a number of downstream pathways in neurons by G protein-coupled receptors and interact with calcium, potassium, and hyperpolarization-gated ion channels, ligand-gated channels. The clinical properties of the LAs are determined by their chemical and pharmacologic properties with a significant variation in individual patients’ responses. The current developments in LAs focus on formulations of local anesthetic that prolong the duration of the action. Formulations of encapsulated slow-release LAs, on-demand release, and those with a selective nociceptive block are being developed. This chapter discusses the mechanism of action of LAs and their clinical use. The prevention and treatment of toxicity and allergy by LAs are explained in Chapter 9.