Pharmacology notes

Apr 15th, 2015
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LOCAL ANESTHETICS:INTRODUCTIONLocal anesthetics reversibly block impulse conduction along nerve axons and otherexcitable membranes that utilize sodium channels as the primary means of actionpotential generation.Clinically, local anesthetics are used to block pain sensation fromor sympatheticvasoconstrictor impulses tospecific areas of the body.Basic pharmacology of local anestheticsChemistry Most local anesthetic agents consist of a lipophilic group (eg, an aromatic ring)connected by an intermediate chain via an ester or amide to an ionizable group (eg, atertiary amine). In addition to the general physical properties of the molecules, specificstereochemical configurations are associated with differences in the potency ofstereoisomers (eg, bupivacaine, ropivacaine). Because ester links are more prone tohydrolysis than amide links, esters usually have a shorter duration of action.EsterPotencyProcaine = 1Duration of ActionCocaine2MediumProcaine (Novocain)1ShortTetracaine (Pontocaine)16LongBenzocaineSurface useonlyAmidesLidocaine (Xylocaine)4MediumMepivacaine(Carbocaine, Isocaine)2MediumBupivicaine (Marcaine),Ievobupivacaine (Chirocaine)16LongPrilocaine (Citanest)3MediumRopivacaine (Naropin)16LongPharmacokinetics The pharmacokinetics of the ester-based local anesthetics have not been extensivelystudied owing to their rapid breakdown in plasma (elimination half-life < 1

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