[Drug binding to blood proteins: characteristics, roles and pathophysiological changes].

Bull Acad Natl Med

Unité Fonctionnelle de Pharmacologie et Toxicologie, CHIC, 40 Avenue de Verdun, F-94010 Creteil.

Published: March 2007

AI Article Synopsis

  • HSA (Human Serum Albumin) and AGP (Alpha-1 Acid Glycoprotein) are the main plasma proteins that bind drugs tightly, influencing their distribution and elimination.
  • Restrictive binding by these proteins can affect how long a drug stays active in the body, while low binding (permissive) allows drugs to move freely without significant retention.
  • Changes in how these proteins bind drugs can impact other pharmacokinetic factors and have important effects on treatment outcomes.

Article Abstract

HSA and AGP are the only plasma proteins capable of binding drugs through specific sites with high affinity. As such, they can limit drug distribution and, sometimes, drug elimination. Such binding is called restrictive. Low binding capacities are said to be permissive, as they do not lead to drug retention. Modifications of restrictive binding can influence other pharmacokinetic parameters and also have clinical implications.

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