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Human alpha-1-glycoprotein and its interactions with drugs
1Department of Medicine, Emory University School of Medicine, Atlanta, GA 30322, USA. zisrail@emory.edu
Drug Metabolism Reviews
|August 10, 2001
Summary
Alpha 1-acid glycoprotein (AAG) is increasingly recognized as a key determinant in drug action, influencing distribution and disposition. Understanding AAG drug binding is crucial for predicting and guiding patient therapy.
Area of Science:
- Pharmacology
- Biochemistry
- Clinical Pharmacy
Background:
- Drug binding to plasma proteins significantly impacts pharmacokinetics and pharmacodynamics.
- Plasma albumin has long been recognized as a major drug-binding protein.
- Alpha 1-acid glycoprotein (AAG) has emerged as another critical plasma protein for drug binding, particularly for basic drugs.
Purpose of the Study:
- To review the importance of drug binding to alpha 1-acid glycoprotein (AAG).
- To highlight the clinical implications of AAG as a drug-binding macromolecule.
- To discuss factors influencing AAG binding and its role in drug interactions.
Main Methods:
- Literature review of studies on drug binding to AAG.
- Analysis of physiological, pathological, and genetic factors affecting AAG binding.
- Examination of AAG's role in drug-drug interactions and displacement phenomena.
Main Results:
- Hundreds of structurally diverse drugs bind to AAG.
- Despite lower concentrations than albumin, AAG can be the primary drug-binding protein with significant clinical impact.
- AAG binding influences drug disposition, drug-drug interactions, and therapeutic outcomes.
Conclusions:
- AAG is a crucial determinant of drug action, distribution, and disposition.
- Understanding AAG-drug interactions is vital for optimizing pharmacotherapy.
- Future development of rapid assays for AAG binding will enhance drug development and clinical practice.
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