What is a Local anaesthetic?

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Local anaesthetic agents can be described as drugs which are used clinically to produce reversible loss of sensation in a circumscribed area of the body. At high concentrations, many drugs, which are used for other purposes possess local anaesthetic or membrane stabilising properties. These include Beta-adrenoceptor antagonists, opioid analgesics, anticonvulsants and antihistamines. Most of the clinically useful local anaesthetic agents consist of an aromatic ring linked by a carbonyl containing moiety through a carbon chain to a substituted amino group.

There are classes of local anaesthetic drugs defined by the nature of the carbonyl-containing linkage group. The ester agents include cocaine, procaine, amethocaine and chloroprocaine, whilst the amides include lignocaine, prilocaine, mepivacaine and bupivacaine. There are important practical differences between these two groups of local anaesthetic agents. Esters are relatively unstable in solution and are rapidly hydrolysed in the body by plasma cholinesterase (and other esterases). One of the main breakdown products is para-amino benzoate (PABA) which is associated with allergic phenomena and hypersensitivity reactions. In contrast, amides are relatively stable in solution, are slowly metabolised by hepatic amidases and hypersensitivity reactions to amide local anaesthetics are extremely rare. In current clinical practice esters have largely been superseded by the amides.

Their Mode of Action

Combination of weak base and strong acid. Hydrolysis in tissues at weak alkalinepH results in liberation of active free base which is then taken up by lipid around nerve. Basic action is to stabilise nerve membrane. Reduces Na+ permeability and thus prevents rise in intracellular Na+ needed to propagate action potential.pH 7.4B.HCL + NaHCo ¨ B. + NaCl + HCo

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