Eur J Clin Pharmacol. 1985;28 Suppl:73-6.

Central nervous system side-effects with hydrophilic and lipophilic beta-blockers.

Westerlund A.

Previous investigations have suggested that hydrophilic beta-blockers, which appear at low concentrations in brain tissue, are less likely to produce CNS-related side-effects than are lipophilic beta-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 beta-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 beta-blockers.

Nightmares or hallucinations were reported by all patients receiving lipophilic beta-blockers and by three patients receiving atenolol. The total number of episodes was significantly lower (p less than 0.01) for patients receiving atenolol (8) than for those receiving lipophilic beta-blockers (54). It is concluded that atenolol is significantly less likely to provoke nightmares and hallucinations than are the lipophilic beta-blockers, metoprolol and propranolol. It seems likely that this finding is due to the differences in hydrophilicity amongst these drugs.

PMID:  2865153