Details

Autor(en) / Beteiligte

• Sun, Jing-jing
• Xie, Lin
• Liu, Xiao-dong

Titel

Transport of carbamazepine and drug interactions at blood-brain barrier

Ist Teil von

• Acta pharmacologica Sinica, 2006-02, Vol.27 (2), p.249-253

Ort / Verlag

United States: Nature Publishing Group

Erscheinungsjahr

2006

Quelle

MEDLINE

Beschreibungen/Notizen

• Aim： To investigate the characteristics of carbamazepine （CBZ） transport and drug interactions at the blood-brain barrier. Methods： Cultured rat brain microvascular endothelial cells （rBMEC） were used as an in vitro model of the blood-brain barrier （BBB）. When cells became confluent, CBZ uptake over time was recorded by incubation of the cells in a medium containing 10 mg/L CBZ at 37℃. The steady-state uptake of CBZ by rBMEC was tested for different CBZ concentrations at 37℃. The effects of various agents on the steady-state uptake of CBZ and efflux of CBZ from rBMEC were also studied. Results： The uptake of CBZ by rBMEC was time- and concentration-dependent. The steady-state uptake occurred at 30 min for incubation. The steady-state uptake was significantly increased （P〈0.01） by treatment with dinitrophenol. The co-administration of cyclosporine A significantly increased the steady-state uptake of CBZ by the rBMEC, whereas co-administration of olanzapine significantly decreased the uptake in a concentration- and temperature-dependent manner. The efflux of CBZ from rBMEC was inhibited by CsA. Conclusion： The transport of CBZ at the BBB is mediated by many transporters. Some specific ABC （ATP-binding cassette, ABC ） efflux transporters may be involved in the transport of CBZ. Drugs influence the transport of CBZ at the BBB in different ways.