BBB: crosses freely
- Readily enters the CNS
- Brain exposure approaches unbound plasma exposure
- Lipophilicity/low efflux often favor entry
- CNS efficacy and CNS toxicity are both more likely
- BBB crossing can change with active transport
Interaction at a glance
Mechanism
- Readily enters the CNS
- Lipophilicity/low efflux often favor entry
- BBB crossing can change with active transport
Magnitude / time course
- Brain exposure approaches unbound plasma exposure
Clinical consequence
- CNS efficacy and CNS toxicity are both more likely
Self-check
- Key risk with BBB: crosses freely?
CNS efficacy and CNS toxicity are both more likely.
- What can change BBB crossing even for freely crossing drugs?
Active transport.
Drugs in this interaction (27)
All interaction examples · Open BBB: crosses freely in the interactive console ↗