Chapter35LocalAnesthetics.pptVIP

Local Anesthetics Definition When used locally, it can block nerve impulse transduction from local to brain. Structural Classification esters，amides，aminoesters，aminoketones，aminoformate，amidines ect.. Esters Local Anesthetics Esters local anesthetics have common basic structure, that is, the aromatic acid and amino alcohol. Procaine Hydrochloride is the representative drug. Procaine was obtained through the structural modification of natural alkaloid Cocaine. Benzoate moiety is very important Methoxycarbonyl is not needed for maintaining activity Tropane bicycles moiety is not necessary Methyl amino benzoate have local anesthetic effect The aminoalkyl side chain is very important Preparation of 　Procaine Hydrochloride Amides local anesthetics Discovery of Lidocaine is based on the investigation of the chemical structure of Gramine, an alkaloid. Lidocaine Hydrochloride 2- Diethylamino -N- 2,6-dimethylphenyl acetamide hydrochloride monohydrate N- 2, 6-二甲苯基 -2- 二乙氨基 乙酰胺盐酸盐一水合物 Metabolism of Lidocaine Preparation of Lidocaine Aminoketone Local Anesthetics Aminoether Local Anesthetics Aminoformate Local Anesthetics Amidine Local Anesthetics Structure and Action of Local Anesthetics Usually including three basic moiety：①lipophilic aromatic ring；②middle functional linker；③hydrophilic amino group. The lipophilic moiety guaranty the suitable lipo-solubility. Hydrophilic amino moiety usually is tertiary amino, this in one hand guaranties the suitable hrdro-solubility for transportation; while in another hand offer the structural basis for combination with Na+ ion channel. Act on sodium ion channel of nerve cell membrane, low down the excitation of nerve cell, therefore block the transmission of nerve impulse. Butyrocaine and Amides are able to form zwitterion * Chapter 3.5 Local Anesthetics Before the use of local anesthetics, to alleviate a patient’s pain, surgeons must perform the operation very fast, for example: Removing a patient’s breast----half