Calcium antagonists can be classified using in vitro toxicity and potency indices

Ravi Shrivastava, Gareth John, Roy Massingham

Research output: Contribution to journalArticlepeer-review

2 Scopus citations

Abstract

The toxicity of eleven calcium antagonists from different chemical families was determined in rat hepatocyte primary cultures. The calcium antagonist potency of the same compounds was also determined in isolated rabbit aortic rings contracted with high K+. The hepatocytotoxicity of the calcium antagonists was not directly linked to blockade of voltage‐operated calcium channels, since there was no correlation between the rank order of hepatotoxicity and that for calcium antagonist potency. The toxicity and calcium antagonist potency of each calcium antagonist examined were used to calculate an in vitro therapeutic index value for each compound. It was observed that therapeutic indices fell into three distinct groups and we therefore propose that the in vitro therapeutic index can be used to subclassify the calcium antagonist group of drugs. The proposed classification corresponds very closely with one already suggested by Spedding on pharmacological grounds. In conclusion, the in vitro therapeutic index may provide a useful tool in the characterization and subclassification of novel calcium antagonist compounds.

Original languageEnglish
Pages (from-to)329-332
Number of pages4
JournalJournal of Applied Toxicology
Volume12
Issue number5
DOIs
StatePublished - Oct 1992
Externally publishedYes

Keywords

  • calcium antagonists
  • classification
  • hepatotoxicity
  • in vitro
  • potency

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