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 diazepam. In contrast, infants with increased drug binding and substantial renal clearance often need higher doses of drugs like digoxin for therapeutic efficacy.

Older people, marked by reduced albumin content and elevated levels of α1-acid glycoprotein, undergo alterations in free drug concentration. These age-related changes impact drug binding and contribute to nuanced shifts in pharmacokinetics and pharmacodynamics.

Interindividual variations in drug binding are frequently attributed to genetic and environmental factors. Genetic predispositions play a pivotal role in dictating the individual's response to drug therapy, shaping the intricate landscape of protein-drug interactions.

Pathological conditions majorly affect protein content, thereby affecting protein-drug binding. Hypoalbuminemia (an abnormally low blood albumin level), stemming from aging, trauma, or burns, poses a substantial threat to binding efficacy. Similarly, hyperlipoproteinemia (an abnormally high blood lipid level) affects the binding of lipophilic drugs.

The factors governing protein-drug binding carry profound consequences for both pharmacokinetics and pharmacodynamics. Diminished plasma protein-drug binding culminates in increased concentrations of unbound drugs. This, in turn, amplifies drug clearance, triggers redistribution, and can accentuate therapeutic or toxic actions. The delicate balance in protein-drug binding becomes a critical determinant in the efficacy and safety of drug therapies.

From Chapter 4:

article

Now Playing

4.14 : Factors Affecting Protein-Drug Binding: Patient-Related Factors

Pharmacokinetics: Drug Distribution and Protein Binding

29 Views

article

4.1 : Drug Distribution: Overview

Pharmacokinetics: Drug Distribution and Protein Binding

96 Views

article

4.2 : Factors Affecting Drug Distribution: Tissue Permeability

Pharmacokinetics: Drug Distribution and Protein Binding

85 Views

article

4.3 : Factors Affecting Drug Distribution: Physiological Barriers

Pharmacokinetics: Drug Distribution and Protein Binding

116 Views

article

4.4 : Factors Affecting Drug Distribution: Organ Perfusion Rate

Pharmacokinetics: Drug Distribution and Protein Binding

54 Views

article

4.5 : Factors Affecting Drug Distribution: Miscellaneous Factors

Pharmacokinetics: Drug Distribution and Protein Binding

147 Views

article

4.6 : Volume of Distribution

Pharmacokinetics: Drug Distribution and Protein Binding

59 Views

article

4.7 : Protein-Drug Binding: Mechanism and Kinetics

Pharmacokinetics: Drug Distribution and Protein Binding

124 Views

article

4.8 : Drug Binding to Blood Components

Pharmacokinetics: Drug Distribution and Protein Binding

51 Views

article

4.9 : Tissue-Drug Binding: Localization of Drugs and its Significance

Pharmacokinetics: Drug Distribution and Protein Binding

44 Views

article

4.10 : Protein-Drug Binding: Determination Methods

Pharmacokinetics: Drug Distribution and Protein Binding

76 Views

article

4.11 : Factors Affecting Protein-Drug Binding: Drug-Related Factors

Pharmacokinetics: Drug Distribution and Protein Binding

46 Views

article

4.12 : Factors Affecting Protein-Drug Binding: Protein-Related Factors

Pharmacokinetics: Drug Distribution and Protein Binding

79 Views

article

4.13 : Factors Affecting Protein-Drug Binding: Drug Interactions

Pharmacokinetics: Drug Distribution and Protein Binding

53 Views

We use cookies to enhance your experience on our website.

By continuing to use our website or clicking “Continue”, you are agreeing to accept our cookies.

Learn More