2009
DOI: 10.1517/17425250903146903
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Prediction of antiepileptic drug efficacy: the use of intracerebral microdialysis to monitor biophase concentrations

Abstract: Biophase concentrations of antiepileptic drugs can differ significantly from pharmacokinetics in plasma. A crucial determinant in the disposition of antiepileptic drugs to the brain is represented by the blood-brain barrier. There is growing evidence that this barrier can alter the availability of antiepileptic drugs at the target site. The permeability of the blood-brain barrier becomes particularly relevant in epileptic conditions and in drug refractory situations. In vivo, intracerebral microdialysis is a v… Show more

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Cited by 13 publications
(2 citation statements)
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“…In this case, a straightforward method to reliably estimate unbound drug concentrations in the brain is essential. Intracerebral microdialysis allows direct measurements of C u,b in preclinical species. , However, it should be acknowledged that this methodology is often characterized by high experimental complexity, low throughput, a propensity to generate artifacts, low recovery, and highly scattered data, especially for lipophilic compounds, thus limiting their application to support compound optimization in early drug discovery. These experimental limitations are important for compounds that are substrates of efflux transporters expressed at the BBB for which the free drug concentration hypothesis does not apply; therefore, C u,p cannot be used as a surrogate of C u,b .…”
Section: Introductionmentioning
confidence: 99%
“…In this case, a straightforward method to reliably estimate unbound drug concentrations in the brain is essential. Intracerebral microdialysis allows direct measurements of C u,b in preclinical species. , However, it should be acknowledged that this methodology is often characterized by high experimental complexity, low throughput, a propensity to generate artifacts, low recovery, and highly scattered data, especially for lipophilic compounds, thus limiting their application to support compound optimization in early drug discovery. These experimental limitations are important for compounds that are substrates of efflux transporters expressed at the BBB for which the free drug concentration hypothesis does not apply; therefore, C u,p cannot be used as a surrogate of C u,b .…”
Section: Introductionmentioning
confidence: 99%
“…Intracerebral microdialysis can provide important data to determine the blood–brain barrier transport characteristics and extracellular/biophase concentrations of a compound (Clinckers et al ., 2009). A prerequisite is that the intracerebral implantation of a microdialysis probe does not significantly alter the barrier's physiological and restrictive properties.…”
Section: Discussionmentioning
confidence: 99%