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Protein Binding

Definition

The reversible binding of drugs to plasma proteins (primarily albumin). Only the unbound (free) fraction of a drug is pharmacologically active. Highly protein-bound drugs can be displaced by other drugs, increasing free drug levels and potentially causing toxicity.

Example

Warfarin is 99% protein-bound; even a small displacement by another drug can double the free warfarin level, significantly increasing bleeding risk.

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