As previously discussed, the identification and subclassification of families of neuronal sodium channels have spurred research aimed at development of more selective sodium channel blockers. The variable neuronal distribution of these isoforms and the unique role that some play in pain signaling suggest that selective blockade of these channels is feasible and may greatly improve the therapeutic index of sodium channel modulators. For example, compounds with specificity for the Nav1.7 and Nav1.8 isoforms have been identified and are currently under clinical development.
Parenteral • duration 3–6 h • Toxicity: CNS excitation • Prilocaine, mepivacaine: Like lidocaine (but also risk of methemoglobinemia with prilocaine) • Articaine: • Ropivacaine, levobupivacaine: Like bupivacaine • Procaine: • Tetracaine: • Benzocaine:
ESTERS • ChloroprocaineLike lidocaine Like lidocaine Very short procedures (not generally used topically or intravenously) Parenteral•duration30–60min•60–90minwithepinephrine•Toxicity: Like lidocaine • CocaineSame as above •alsohassympathomimetic effects Same as above Procedures requiring high surface activity and vasoconstriction Topicalorparenteral•duration1–2h•Toxicity: CNS excitation, convulsions, cardiac arrhythmias, hypertension, stroke
Bupivacaine Generic, Marcaine, Sensorcaine
Chloroprocaine Generic, Nesacaine
Dibucaine (topical) Generic, Nupercainal
Dyclonine (topical lozenge) Sepacol, Sucrets, Dyclone
Levobupivacaine Chirocaine, others
Lidocaine Generic, Xylocaine
Mepivacaine Generic, Carbocaine
Pramoxine (topical) Generic, Tronothane
Procaine Generic, Novocain
Proparacaine (ophthalmic) Generic, Alcaine, others
Ropivacaine Generic, Naropin
Tetracaine Generic, Pontocaine
Albright GA: Cardiac arrest following regional anesthesia with etidocaine or bupivacaine. Anesthesiology 1979;51:285.
American Society of Regional Anesthesia and Pain Medicine: Checklist for treatment of local anesthetic systemic toxicity. 2012. http://www.asra.com/ checklist-for-local-anesthetic-toxicity-treatment-1-18-12.pdf.
Andavan GS, Lemmens-Gruber R: Voltage-gated sodium channels: Mutations, channelopathies and targets. Curr Med Chem 2011;18:377.
Auroy Y et al: Serious complications related to regional anesthesia: Results of a prospective survey in France. Anesthesiology 1997;87:479.
Butterworth JF 4th, Strichartz GR: Molecular mechanisms of local anesthesia: A review. Anesthesiology 1990;72:711.
Catterall WA, Goldin AL, Waxman SG: International Union of Pharmacology.