Is there a place for local anesthetics structurally different from classical amid or ester local anesthetics?
OBJECTIVE
The aim of this review is to describe the pharmacology, toxicology and chemistry of the new group of local anesthetics of phenylcarbamic acid type.


RESULTS
Basic esters of alkoxy-substituted phenylcarbamic acid have shown high local anesthetic potency, while maintaining a relatively safe toxicity profile. Their potency uniquely increases with the decreasing pH of the external medium. This is of importance when using local anesthesics in inflamed tissues, where the action of common local anesthetics is often problematic.


CONCLUSIONS
The most potent phenylcarbamic anesthetics exceed the potency of the most common clinically used local anesthetics 100-300 times. Due to the unique pH dependency of these local anesthetics, further study of their action is required.
Vegh
Vladimir
V
Department of Pharmaceutical Chemistry, Faculty of Pharmacy, Comenius University, Bratislava, Slovakia. vegh@fpharm.uniba.sk
Cizmarik
Jozef
J
Hahnenkamp
Klaus
K
D000577:Amides / Q000737:chemistry / Q000494:pharmacology; D000779:Anesthetics, Local / Q000009:adverse effects / Q000737:chemistry* / Q000494:pharmacology*; D000818:Animals; D002219:Carbamates / Q000737:chemistry / Q000494:pharmacology; D004305:Dose-Response Relationship, Drug; D004952:Esters / Q000737:chemistry / Q000494:pharmacology; D006801:Humans; D006863:Hydrogen-Ion Concentration; D007928:Lethal Dose 50; D015394:Molecular Structure; D048448:Phenylcarbamates / Q000009:adverse effects / Q000737:chemistry* / Q000494:pharmacology*; D010880:Piperidines / Q000737:chemistry / Q000494:pharmacology; D012584:Sciatic Nerve / Q000187:drug effects; D013329:Structure-Activity Relationship
D000577:Amides; D000779:Anesthetics, Local; D002219:Carbamates; D004952:Esters; D048448:Phenylcarbamates; D010880:Piperidines; C013549:heptacaine; C010618:pentacaine; C046030:carbizocaine