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Antiepileptic drugs modulate P-glycoproteins in the brain: A mice study with 11C-desmethylloperamide by Lieselotte Moerman; Leonie wyffels; Dominique Slaets; Robrecht Raedt; Paul Boon; Filip De Vos is a Medicine article available to read on EtoBox.

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P-glycoprotein transporters (P-gp) located at the blood-brain barrier (BBB) are likely to play a role in refractory epilepsy. In vitro studies already pointed out that several antiepileptic drugs (AEDs) are substrate of P-gp. This study proposes a new in vivo approach to investigate the interaction between some AEDs and P-gp located at the BBB. 11 C-desmethylloperamide ( 11 C-dLop), a radiolabelled substrate of P-gp, was intravenously administrated after pretreatment with saline or AEDs (sodium valproate, levetiracetam, topiramate and phenytoin) at their human therapeutic and four times their therapeutic dose. The effect of the different pretreatment on the intracerebral concentration of 11 C-dLop was determined to indirectly investigate possible in vivo interactions between AEDs and P-gp. Pretreatment with levetiracetam, topiramate and phenytoin at therapeutic doses significantly decreased intracerebral concentration of 11 C-dLop. Pretreatment with a therapeutic dose of sodium valproate did not influence brain uptake of 11 C-dLop. In case of pretreatment with supratherapeutic doses of AED, 11 C-dLop brain uptake was not different compared to pretreatment with saline. The metabolis

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Author

Lieselotte Moerman; Leonie wyffels; Dominique Slaets; Robrecht Raedt; Paul Boon; Filip De Vos

Publisher

Elsevier Science; Elsevier ; Elsevier BV (ISSN 0920-1211)

Published

2011

Language

EN

Field

Medicine (Health Sciences)