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beta-Adrenoreceptor-blocking agents and the blood-brain barrier
Clinical Science (London, England : 1979)
|December 1, 1980
Summary
Beta-receptor blockers distribute differently in the brain. Lipophilic agents like propranolol reach high brain concentrations, potentially causing central nervous system side effects, unlike hydrophilic atenolol.
Area of Science:
- Neurosurgery
- Pharmacology
- Clinical Neuroscience
Background:
- Beta-adrenoreceptor-blocking agents (beta-receptor blockers) are used in neurosurgical patients.
- Understanding drug distribution in the central nervous system is crucial for managing side effects.
Purpose of the Study:
- To investigate the penetration and concentration of oral beta-receptor blockers in cerebrospinal fluid and brain tissue.
- To correlate drug concentrations with potential central nervous system side effects.
Main Methods:
- Oral beta-receptor blockers were administered to 16 neurosurgical patients for 3-22 days.
- Cerebrospinal fluid and brain tissue concentrations were measured and compared to plasma concentrations.
- Lipophilic (propranolol, metoprolol) and hydrophilic (atenolol) agents were assessed.
Main Results:
- Lipophilic beta-receptor blockers achieved cerebrospinal fluid concentrations similar to free plasma concentrations.
- Brain tissue concentrations of lipophilic agents were high (brain/plasma ratio ~15:1), while hydrophilic atenolol concentrations were low (brain/plasma ratio ~0.1:1).
- Cerebrospinal fluid concentrations poorly predicted brain concentrations.
Conclusions:
- High brain tissue concentrations of lipophilic beta-receptor blockers may explain associated central nervous system side effects.
- Drug lipophilicity significantly influences penetration into brain tissue.
- Atenolol exhibits limited brain penetration compared to lipophilic beta-receptor blockers.