beta-Adrenoreceptor-blocking agents and the blood-brain barrier.
1. Sixteen neurosurgical patients received (oral) beta-adrenoreceptor-blocking agents (beta-receptor blockers) for 3-22 days. 2. Lipophilic beta-receptor blockers (propranolol) and metoprolol appeared in cerebrospinal fluid at concentrations similar to the free drug plasma concentration. 3. Cerebrospinal fluid concentrations of beta-receptor blockers were poor predictors of brain concentrations. 4. Both lipophilic beta-receptor blockers appeared in high concentrations in the brain: the brain/plasma ratio was approximately 15:1. 5. Hydrophilic atenolol appeared at low concentrations in brain tissue (about 20 times lower than the lipophilic beta-receptor blockers): the brain/plasma ratio was approximately 0.1:1. 6. Central nervous system-related side effects associated mainly with lipophilic beta-receptor blockers possibly result from high brain tissue concentrations.
D001262:Atenolol / Q000097:blood / Q000134:cerebrospinal fluid*; D001812:Blood-Brain Barrier; D001921:Brain / Q000378:metabolism; D006801:Humans; D007700:Kinetics; D008790:Metoprolol / Q000097:blood / Q000134:cerebrospinal fluid*; D011412:Propanolamines / Q000134:cerebrospinal fluid*; D011433:Propranolol / Q000097:blood / Q000134:cerebrospinal fluid*
D011412:Propanolamines; D001262:Atenolol; D011433:Propranolol; D008790:Metoprolol