Document Detail

The role of unbound drug in pharmacokinetics/pharmacodynamics and in therapy.
MedLine Citation:
PMID:  16533165     Owner:  NLM     Status:  MEDLINE    
The evolution of research on drug protein binding is discussed with the unbound concentration (Cu) and the unbound fraction (fu) as protagonists. Particular attention is paid to the mechanisms via which alterations in binding affect the pharmacokinetics (PK) and the effect, or independently the pharmacodynamics (PD). Apart from albumin, the important alpha-acid glycoprotein (AGP), as well as specific drug classes and applications in the clinic and development (routine monitoring, cancer and HIV therapy, allometry) are addressed. The flaws with the classical method of indirectly calculating the Cu or the unbound PK/PD parameters, based on the fu in vitro, are related to the intrinsic complexity and variability in the outcomes. Increased focus is urged on directly estimating the unbound PK/PD and also on using population statistical methods.
Rosario Calvo; John C Lukas; Monica Rodriguez; Nerea Leal; Elena Suarez
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Publication Detail:
Type:  Journal Article    
Journal Detail:
Title:  Current pharmaceutical design     Volume:  12     ISSN:  1381-6128     ISO Abbreviation:  Curr. Pharm. Des.     Publication Date:  2006  
Date Detail:
Created Date:  2006-03-14     Completed Date:  2007-03-29     Revised Date:  -    
Medline Journal Info:
Nlm Unique ID:  9602487     Medline TA:  Curr Pharm Des     Country:  Netherlands    
Other Details:
Languages:  eng     Pagination:  977-87     Citation Subset:  IM    
Department of Pharmacology, Faculty of Medicine, University of the Basque Country, Leioa, Vizcaya, Spain.
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MeSH Terms
Anti-Retroviral Agents / pharmacokinetics,  pharmacology*,  therapeutic use
Antineoplastic Agents / pharmacokinetics,  pharmacology*,  therapeutic use
Blood Proteins / metabolism*
Drug Monitoring / methods
HIV Infections / drug therapy,  metabolism*
Models, Animal
Models, Biological
Neoplasms / drug therapy,  metabolism*
Orosomucoid / metabolism
Protein Binding
Serum Albumin / metabolism
Species Specificity
Reg. No./Substance:
0/Anti-Retroviral Agents; 0/Antineoplastic Agents; 0/Blood Proteins; 0/Orosomucoid; 0/Serum Albumin

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