In vitro P-glycoprotein efflux inhibition by atypical antipsychotics is in vivo nicely reflected by pharmacodynamic but less by pharmacokinetic changes.

@article{Schmitt2012InVP,
  title={In vitro P-glycoprotein efflux inhibition by atypical antipsychotics is in vivo nicely reflected by pharmacodynamic but less by pharmacokinetic changes.},
  author={Ulrich Schmitt and Katrin M Kirschbaum and Birk Poller and Manisha Kusch-Poddar and Juergen Drewe and Christoph Hiemke and H. Cem Gutmann},
  journal={Pharmacology, biochemistry, and behavior},
  year={2012},
  volume={102 2},
  pages={312-20}
}
BACKGROUND P-glycoprotein (P-gp), an efflux transporter of the blood-brain barrier, limits the access of multiple xenobiotics to the central nervous system (CNS). Thus drug-dependent inhibition, induction or genetic variation of P-gp impacts drug therapy. METHODS We investigated atypical antipsychotics and their interaction with P-gp. Amisulpride, clozapine, N-desmethylclozapine, olanzapine, and quetiapine were assessed in vitro on their inhibitory potential and in vivo on their disposition… CONTINUE READING

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