Similar pharmacological actions of chlordimeform and local anesthetics

Add time:09/04/2019    Source:sciencedirect.com

The toxic symptoms of the pesticide, chlordimeform, resemble those observed following systemic local anesthetic overdose. In view of similarities in the chemical structures of chlordimeform and the local anesthetic agent phenacaine, additional comparisons between the actions of chlordimeform and local anesthetics were made. Chlordimeform had effects on the frog sciatic nerve preparation similar to those of local anesthetics (i.e., blocked conduction, increased threshold, prolonged refractory period). Chlordimeform was 0.6 times as active as procaine, less active in the ionized form, and more active on the desheathed preparation. Chlordimeform lethality was reduced by pretreatment with diazepam or pentobarbital, but not by diphenylhydantoin, trimethadione, or mephenesin pretreatment. These pretreatments have a comparable effect on local anesthetic toxicity. Chlordimeform lethality was slighly increased by agents possessing “local anesthetic activity” such as imipramine, pyribenzamine, and phenoxybenzamine. These and other results indicate that a number of the pharmacological and toxic actions of chlordimeform in mammals may be due to actions that are similar to those of local anesthetic agents.

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