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Related Concept Videos

Protein-Drug Binding: Mechanism and Kinetics01:16

Protein-Drug Binding: Mechanism and Kinetics

Protein-drug binding refers to the interaction between drugs and proteins within the body. This binding process can occur intracellularly, involving drug interactions with enzymes or receptors within cells, or extracellularly, involving plasma proteins in the blood.
Various forces drive these interactions, including hydrogen bonds, hydrophobic interactions, ionic bonds, electrostatic interactions, and van der Waals forces. These bonds enable drugs to bind to specific sites on proteins,...
Factors Affecting Protein-Drug Binding: Protein-Related Factors01:20

Factors Affecting Protein-Drug Binding: Protein-Related Factors

Drug binding to proteins is a key aspect of pharmacokinetics and can influence a drug's distribution, absorption, and elimination in the body. Several factors, including the drug's physiochemical properties, protein concentration, disease states, and the number of binding sites on the protein, influence this process.
The physicochemical properties of a drug play a significant role in its ability to bind to proteins. Lipophilic drugs, which dissolve in fats, oils, and lipids, can be bound by...
Factors Affecting Protein-Drug Binding: Drug-Related Factors01:18

Factors Affecting Protein-Drug Binding: Drug-Related Factors

Drug binding to proteins is a complex phenomenon influenced by various drug-related factors, each playing a significant role in the interaction between drugs and proteins within the body.
One crucial factor in drug-protein binding is the drug's lipophilicity or its affinity for fat. More lipophilic drugs tend to have higher binding extents. For example, highly lipophilic drugs like cloxacillin exhibit substantial protein binding, with as much as 95% of the drug binding to proteins. In contrast,...
Factors Affecting Protein-Drug Binding: Patient-Related Factors01:29

Factors Affecting Protein-Drug Binding: Patient-Related Factors

Protein-drug binding, a pivotal aspect of pharmacokinetics, is subject to considerable variability influenced by an array of patient-related factors. The intricate interplay of age, individual differences, and pathological conditions significantly impact the binding dynamics and subsequent pharmacological effects.
Age stands as a key determinant in protein-drug binding. Neonates, characterized by low albumin content, experience heightened concentrations of unbound drugs such as phenytoin and...
Drug Distribution: Plasma Protein Binding01:29

Drug Distribution: Plasma Protein Binding

Drugs predominantly attach to plasma proteins, with only a small percentage remaining unbound. The unbound portion can be calculated as one minus the bound fraction. Acidic drugs form large, inactive complexes by reversibly binding to plasma albumin, which prevents them from diffusing across biological barriers. These drug-protein complexes act as reservoirs for the drugs. As the concentration of unbound drugs decreases, these complexes quickly dissociate to release the free drug, maintaining...
Protein-Drug Binding: Determination Methods01:22

Protein-Drug Binding: Determination Methods

Determining protein-drug binding can be achieved through indirect and direct methods, each providing valuable insights into the interaction between proteins and drugs.
Indirect methods involve isolating the bound drug from its free form in biological samples such as blood, serum, or plasma. These techniques aim to measure the percentage of drugs bound to proteins. Equilibrium dialysis is a commonly used method where the free drug concentration at equilibrium is measured by separating the bound...

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The Importance of Correct Protein Concentration for Kinetics and Affinity Determination in Structure-function Analysis
19:16

The Importance of Correct Protein Concentration for Kinetics and Affinity Determination in Structure-function Analysis

Published on: March 17, 2010

When is protein binding important?

Jules Heuberger1, Stephan Schmidt, Hartmut Derendorf

  • 1Department of Pharmaceutics, University of Florida, Gainesville, Florida, USA.

Journal of Pharmaceutical Sciences
|May 8, 2013
PubMed
Summary
This summary is machine-generated.

Misinterpreting classic research on protein binding can lead to drug development pitfalls. This paper clarifies when protein binding is clinically relevant to avoid such errors.

Keywords:
drug interactionin vitro modelsin vitro/in vivo correlations (IVIVC)microdialysispharmacokineticsprotein binding

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Area of Science:

  • Pharmacology
  • Drug Development
  • Biochemistry

Background:

  • A seminal 2002 paper by Benet and Hoener significantly influenced the perception of protein binding in drug development.
  • The authors' original message and limitations are frequently misinterpreted, leading to incorrect conclusions about the importance of protein binding.

Purpose of the Study:

  • To revisit and clarify the implications of protein binding in drug development.
  • To address the misinterpretation of the 2002 paper and highlight when protein binding is clinically significant.

Main Methods:

  • Re-evaluation of the assumptions and limitations outlined in the classic Benet and Hoener paper.
  • Analysis of clinical scenarios where protein binding plays a crucial role.

Main Results:

  • The classic paper's findings are often overgeneralized, leading to the erroneous belief that protein binding is unimportant.
  • Clinically relevant changes in protein binding necessitate careful consideration during drug development.

Conclusions:

  • Understanding the nuances of protein binding is critical to avoid major pitfalls in drug development.
  • This work aims to guide researchers in determining the clinical relevance of protein binding for specific drug candidates.