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Drug Binding to Plasma Proteins
(Springer Nature Switzerland AG, 2021)
After absorption, most drugs will distribute heterogeneouslyacross tissues and organs, with the total drug concentration in plasmagenerally not being representative of the total concentration in other tissues.The main ...
Free drug theory
(Springer, 2021)
The free drug theory (sometimes also termed free drug hypothesis) provides a conceptual framework increasingly used to understand pharmacokinetics/pharmacodynamics (PK/PD) relationships [1]. It underlines the central role ...
Enantioselective analysis of unbound tramadol, O-desmethyltramadol and N-desmethyltramadol in plasma by ultrafiltration and LC-MS/MS: Application to clinical pharmacokinetics
(ELSEVIER SCIENCE BVAMSTERDAM, 2013-08-02)
This study describes the enantioselective analysis of unbound and total concentrations of tramadol and its main metabolites O-desmethyltramadol (M1) and N-desmethyltramadol (M2) in human plasma. Sample preparation was ...
Impact of fraction unbound, CYP3A, and CYP2D6 in vivo activities, and other potential covariates to the clearance of tramadol enantiomers in patients with neuropathic pain
(Wiley-Blackwell, 2016-04-01)
The pharmacokinetics of tramadol is characterized by a large interindividual variability, which is partially attributed to polymorphic CYP2D6 metabolism. The contribution of CYP3A, CYP2B6, fraction unbound, and other ...
Brain-to-Plasma Concentration Ratio and Unbound Partition Coefficient
(Springer Nature Switzerland AG, 2021)
The brain-to-plasma concentration ratio (or totalbrain-to-plasma ratio, or simply, brain-to-plasma ratio, Kp, also referred toas B/P ratio or BB) is, as suggested by the name, the ratio between the total(bound and unbound) ...
Current state and future perspectives in QSAR models to predict blood-brain barrier penetration in central nervous system drug R&D
(Bentham Science Publishers, 2017-02)
The Blood-Brain Barrier (BBB) is a physical and biochemical barrier that restricts the entry of certain drugs to the Central Nervous System (CNS), while allowing the passage of others. The ability to predict the permeability ...
Enantioselective inhibition of human CYP2C19 by the chiral pesticide ethofumesate: Prediction of pesticide-drug interactions in humans
(2021-08-25)
Ethofumesate is a chiral herbicide that may display enantioselective behavior in humans. For this reason, the enantioselective potential of ethofumesate and its main metabolite ethofumesate-2-hydroxy to cause pesticide-drug ...
Combined Microdialysis-Tumor Homogenate Method for the Study of the Steady State Compartmental Distribution of a Hydrophobic Anticancer Drug in Patient-Derived Xenografts
(Springer, 2014-03)
PURPOSE: To develop a reproducible microdialysis-tumor homogenate method for the study of the intratumor distribution of a highly hydrophobic anticancer drug (SN-38; 7-ethyl-10-hydroxycamptothecin) in neuroblastoma ...