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Pharmacol Ther. 2010 Aug;127(2):165-74. doi: 10.1016/j.pharmthera.2010.04.011. Epub 2010 May 28.

The application of drug dose equivalence in the quantitative analysis of receptor occupation and drug combinations.

Author information

1
Department of Pharmacology, School of Medicine, Center for Substance Abuse Research (RJT), Temple University, Philadelphia, PA 19140, USA.

Abstract

In this review we show that the concept of dose equivalence for two drugs, the theoretical basis of the isobologram, has a wider use in the analysis of pharmacological data derived from single and combination drug use. In both its application to drug combination analysis with isoboles and certain other actions, listed below, the determination of doses, or receptor occupancies, that yield equal effects provide useful metrics that can be used to obtain quantitative information on drug actions without postulating any intimate mechanism of action. These other drug actions discussed here include (1) combinations of agonists that produce opposite effects, (2) analysis of inverted U-shaped dose-effect curves of single agents, (3) analysis on the effect scale as an alternative to isoboles and (4) the use of occupation isoboles to examine competitive antagonism in the dual receptor case. New formulas derived to assess the statistical variance for additive combinations are included, and the more detailed mathematical topics are included in the Appendix.

PMID:
20546783
PMCID:
PMC4036078
DOI:
10.1016/j.pharmthera.2010.04.011
[Indexed for MEDLINE]
Free PMC Article

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