Piperidine local anesthetics action on biological membranes

Anesthetics constitute a chemically diverse group of drugs. There are inhalational agents (noble gases, nitrous oxide), ethers, hydrocarbons benzodiazepines(valium, versed), opoids and others. Most of local anesthetics (LA) have a characteristic molecular pattern with a tertiary amine at one end and an aromatic ring at the other, separated by a linking ester or amide group. Piperidine local anesthetics, such as mepivacaine, ropivacaine, and bupivacaine are widely used in clinical practice (differing only in the length of the alkyl chain attached to the tertiary amine in molecule).

The physiological basis for the local anesthetic action is known (they prevent transmission of nerve impulses by blocking inward migration of Na), but the precise molecular nature of the process is not completely clear. Some studies suggest that they directly act on sodium channels but some other suggest that they interact with lipid bilayers and in this way could modify channel activity.

ModMol: Projects/Anesthetics (last edited 2011-02-15 20:59:06 by localhost)