engleski

The role of sodium and potassium channels in cardiotoxicity induced by local anaesthetics

Widely used local anesthetics such as bupivacaine, levobupivacaine, ropivacaine and lidocaine, are voltage-gated sodium channels blockers very effective in inhibition of the conduction of action potentials in excitable tissues, specifically neural tissues, thus preventing the conduction of sense of pain. One important feature of local anesthetics is their ability to not only inhibit sodium channels but also, in toxicologically relevant concentrations, block voltage gated cardiac K channels, and potassium repolarizing current. Although very effective drugs, local anesthetics have cardiovascular toxicity which is the consequence of their direct effect on myocardium, i.e. decrease in contractility and inhibition of the conductive musculature. Genetic mutations in cardiac Na channels (as well as K channels) can disrupt equilibrium of ionic currents underlying normal cardiac conduction and contractility, and result in arrythmogenic phenotypes. Thus, it is very important to consider pharmacogenomic approach to LAs usage ; determination of the potential genetic heterogeneity to directly influence drug targets and interfere with drug mechanisms of action could be helpful in decision on which drugs should be use in therapy for certain individual.

local anaesthetics; ion channels; cardiotoxcity

nije evidentirano