Drug Protein Binding | Plasma Protein Binding | Tissue Protein Binding | pharmacokinetics

Basic concepts and features of plasma protein binding, Plasma Protein bounded and
Free Drug. Types of Plasma Protein. Different Binding Site of Albumin with examples. Drug -tissue proteins Binding
Plasma Proteins: Albumin, Globulin, Glycoproteins, Lipoproteins.

principles of protein binding
• only free drug can distribute into tissues and exert its action, and is subject to metabolism and elimination
• affinity of a protein binding site for a drug determines bound/unbound concentrations, and reversibility of interaction
• saturation of binding sites may result in a large increase in unbound drug concentration, which could cause toxicity
• if albumin concentration is decreased (liver failure or nephrotic syndrome), dose of highly bound drug must be lowered to avoid toxicity
• competition for binding sites between drugs and endogenous substrates can result in interactions and toxicity
• significant drug interactions can occur due to competitive protein binding
 e.g. ASA displaces several drugs which are highly bound to plasma proteins such as phenytoin, increasing risk of toxicity
• in general, only drugs that are highly protein bound, e.g. more than 90%, are involved in drug interactions due to competitive binding

00:00 Introduction

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