BBB: transporter-sensitive CNS exposure
- CNS exposure depends on active transport
- Efflux or uptake can dominate BBB penetration
- Transporter inhibition may change brain levels
- Plasma AUC may not predict CNS AUC well
- Important for centrally active drugs
Interaction at a glance
- CNS exposure depends on active transport
Mechanism
- Efflux or uptake can dominate BBB penetration
Mechanism / modifiers
- Transporter inhibition may change brain levels
- Important for centrally active drugs
Magnitude / time course
- CNS exposure depends on active transport
- Plasma AUC may not predict CNS AUC well
Self-check
- Which transport processes can dominate BBB penetration?
Efflux or uptake. - Does plasma AUC reliably predict CNS AUC for transporter-sensitive exposure?
It may not.
Drugs in this interaction (13)
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