Part 1 comments on the types of local anaesthetics (LAs); it provides a better understanding of the mechanisms of action of LAs, and their pharmacokinetics and toxicity. It reviews the newer LAs such as levobupivacaine, ropivacaine, and articaine, and examines the newer structurally different LAs. The addition of adjuvants such as adrenaline, bicarbonate, clonidine, and corticosteroids is explored. Comment is made on the delivery of topical LAs via bioadhesive plasters and gels and controlled-release local anaesthetic matrices. Encapulation matrices such as liposomes, microemulsions, microspheres and nanospheres, hydrogels and liquid polymers are discussed as well. New innovations pertaining to LA formulations have indeed led to prolonged action and to novel delivery approaches.