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Review
. 2020 May 2;12(5):417.
doi: 10.3390/pharmaceutics12050417.

Interpretation of Drug Interaction Using Systemic and Local Tissue Exposure Changes

Young Hee Choi  1
Affiliations
Review

Interpretation of Drug Interaction Using Systemic and Local Tissue Exposure Changes

Young Hee Choi. Pharmaceutics. .

Abstract

Systemic exposure of a drug is generally associated with its pharmacodynamic (PD) effect (e.g., efficacy and toxicity). In this regard, the change in area under the plasma concentration-time curve (AUC) of a drug, representing its systemic exposure, has been mainly considered in evaluation of drug-drug interactions (DDIs). Besides the systemic exposure, the drug concentration in the tissues has emerged as a factor to alter the PD effects. In this review, the status of systemic exposure, and/or tissue exposure changes in DDIs, were discussed based on the recent reports dealing with transporters and/or metabolic enzymes mediating DDIs. Particularly, the tissue concentration in the intestine, liver and kidney were referred to as important factors of PK-based DDIs.

Keywords: drug interaction; pharmacokinetics; systemic exposure; tissue-specific.

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Conflict of interest statement

The authors declare no conflict of interest.

Figures

Figure 1
Figure 1
Representative transporters and metabolic enzymes in enterocytes (A), hepatocytes (B) and renal proximal renal tubules (C), which are possibly involved in DDIs.
See this image and copyright information in PMC

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