Central nervous system side-effects with hydrophilic and lipophilic ?-Blockers

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Abstract
Previous investigations have suggested that hydrophilic β-Blockers, which appear at low concentrations in brain tissue, are less likely to produce CNS-related side-effects than are lipophilic β-Blockers, which occur at higher concentrations in the brain. The validity of this hypothesis was tested in a double-blind crossover study in which the hydrophilic β-blocker atenolol was compared with the lipophilic agents metoprolol and propranolol, in 14 patients with a previous history of nightmares or hallucinations when treated with lipophilic β-Blockers. Nightmares or hallucinations were reported by all patients receiving lipophilic β-Blockers but by only three patients receiving atenolol. The total number of episodes was significantly lower (p<0.01) for patients receiving atenolol (8) than for those receiving lipophilic β-Blockers (54). It is concluded that atenolol is significantly less likely to provoke nightmares and hallucinations than are the lipophilic β-Blockers, metoprolol and propranolol. It seems likely that this finding is due to the differences in hydrophilicity amongst these drugs.

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