Enhancement of local anaesthesia action by organic acid salts. (I): Possible change of excitability in nerve fibre membrane.

Measurements of action potentials recorded from giant nerve fibres of the crayfish abdomen showed that by addition of an organic acid salt to a local anaesthetic solution, the onset of anaesthetic action became more rapid and the duration of action was prolonged. Similar results were also obtained in rat vagal nerves. The chemical structure of compounds having these enhancing effects was found to have, in common, a carboxyl group connected with either a benzene ring or an aliphatic hydrocarbon. Topical application of anaesthetic solutions to the skin of flexor side of the forearm in humans revealed that the duration of anaesthesia evaluated by the apparent decrease of the number of pain points was significantly prolonged by the addition of salicylate. The use of local anaesthetics combined with organic acid salts would be promising in clinical practice to enhance their action greatly.

[1]  R. Poster Pharmacology, 3rd edn: by R. G. Penn, Ballière Tindall, London, 1980. £4.75 (x + 320 pages) ISBN 0 7020 0822 2 , 1982 .

[2]  H. Horie,et al.  Inhibitory Effects of Myrmicacin on the Sodium Channel in the Squid Giant Axon , 1981 .

[3]  T. Iwadare,et al.  Myrmic Acids: A Group of New Inhibitors Analogous to Myrmicacin (β-Hydroxydecanoic Acid) , 1979, Botanical Gazette.

[4]  T. Iwadare,et al.  Inhibiting Effects of Myrmicacin and Homologous Compounds on Cleavage of Hemicentrotus pulcherrimus Eggs , 1979 .

[5]  T. Iwadare,et al.  Inhibiting Effects of Myrmicacin on Pollen Growth and Pollen Tube Mitosis , 1978, Botanical Gazette.

[6]  M. Singer Interaction of local anesthetics and salicylate with phospholipid membranes. , 1973, Canadian journal of physiology and pharmacology.

[7]  H. Schildknecht,et al.  Myrmicacin, the first insect herbicide. , 1971, Angewandte Chemie.

[8]  R. Montoya Combined effects of some local anesthetics with sodium benzoate. , 1970, Pharmacology.

[9]  A. Rodallec,et al.  [Raise by diethylaminoethanol and sodium para-aminobenzoates and benzoates of the desensitization of the cornea in rabbits produced by procaine (novocaine) and some other local anesthetics]. , 1966, Therapie.

[10]  Junji Hasegawa,et al.  Advances in Biology of Skin , 1961 .

[11]  H. Wolff,et al.  CHAPTER VIII – STRUCTURES AND PROCESSES INVOLVED IN THE SENSATION OF ITCH* , 1960 .

[12]  L. Goodman,et al.  THE PHARMACOLOGICAL BASIS OF THERAPEUTICS , 1966 .