The concept of fraction of drug transported (ft ) with special emphasis on BBB efflux of CNS and antiretroviral drugs

B Prasad; J D Unadkat

doi:10.1002/cpt.72

The concept of fraction of drug transported (ft ) with special emphasis on BBB efflux of CNS and antiretroviral drugs

Clin Pharmacol Ther. 2015 Apr;97(4):320-3. doi: 10.1002/cpt.72. Epub 2015 Feb 13.

Authors

B Prasad¹, J D Unadkat

Affiliation

¹ Department of Pharmaceutics, University of Washington, Seattle, Washington, USA.

PMID: 25669655
DOI: 10.1002/cpt.72

Abstract

The fraction of drug transported (ft) into or out of a tissue is a concept useful to understand the impact of transporters on absorption, distribution, metabolism, and excretion (ADME) and tissue distribution of a drug. Here, ft is utilized to explain the impact of transporters on central nervous system (CNS) distribution of drugs, drug interactions (DDI), and to predict the unbound brain concentration (Cu,b) of the drug. The latter is important to ascertain if Cu,b is sufficient for efficacy.

MeSH terms

Animals
Antiretroviral Therapy, Highly Active*
Antiviral Agents / pharmacokinetics*
Biological Transport
Blood-Brain Barrier / metabolism*
Carrier Proteins / metabolism
Central Nervous System / metabolism*
Drug Interactions
Humans
Membrane Transport Proteins / metabolism
Pharmaceutical Preparations / metabolism*

Substances

Antiviral Agents
Carrier Proteins
Membrane Transport Proteins
Pharmaceutical Preparations