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
- What is the main clinical risk of BBB: crosses freely?
CNS efficacy and CNS toxicity are both more likely.
- What does “BBB: crosses freely” indicate?
BBB crossing can change with active transport.
Drugs in this interaction (27)
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