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Importance of Protein Binding for the Interpretation of Serum or Plasma Drug Concentrations
Author(s) -
GREENBLATT DAVID J.,
SELLERS EDWARD M.,
KOCHWESER JAN
Publication year - 1982
Publication title -
the journal of clinical pharmacology
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.92
H-Index - 116
eISSN - 1552-4604
pISSN - 0091-2700
DOI - 10.1002/j.1552-4604.1982.tb02671.x
Subject(s) - drug , interpretation (philosophy) , plasma protein binding , pharmacology , plasma concentration , blood proteins , chemistry , medicine , computer science , programming language
The extent of drug binding to plasma protein does not influence the concentration of unbound drug in plasma at steady state but does influence the interpretation of total drug concentrations. An increase in free fraction (reduction in the extent of binding) decreases the therapeutic and toxic ranges for total drug concentrations. Conversely, a reduction in free fraction (increase in the extent of binding) increases these ranges. Laboratories generally measure total rather than unbound drug concentrations, and clinicians must use caution in interpreting these total drug concentrations in clinical situations where the extent of binding of extensively bound drugs may be altered. Free drug serum or plasma concentrations are inherently more reliable indices of the intensity of drug action than are total concentrations. Methodology for routine measurement of free concentration is becoming available and should ultimately be utilized for therapeutic monitoring of drugs that are highly bound to protein.