Anaesthetics, local Narcotics

V-Na+ CH (inactivated form) blocker (catecholamine transport inhibition) [central nervous system (CNS) stimulant, local anaesthetic, mydriatic, narcotic]... 

Local anaesthetic and CNS stimulant Cocaine. Alkaloid from leaves of Erythroxylon coca narcotic agent... 

Cocaine-derived local anaesthetics. Fig. 14.29 illustrates how simplified synthetic copies of cocaine were designed. The change from cocaine to procaine retains the local anaesthetic effects without the narcotic properties. 

A large number of new tropanyl esters and other related compounds have been prepared, with the purpose of contributing further structure-pharmacological activity relationships. Inter alia, para-substituted tropanyl benzoates (for studies of the substrate specificity of atropine esterase), benzazocines (narcotic antagonists) from 6-hydroxytropinone, 5-aryl-furan-2-carboxylic esters of pseudotropine (local anaesthetics), 2,4,5-trimethylpyrrole-3-carboxylic acid... 

Cocaine is relatively unstable and is more often administered as cocaine hydrochloride—a more stable form. Cocaine blocks nerve conduction upon local application, hence its employment as an anaesthetic (e.g. Novacaine). In large doses it is a cerebral stimulant and narcotic. Its adrenergic action is due to inhibition of reuptake of noradrenaline, creating an amphetamine-like effect, though only of very short duration. 

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