The importance of lipid solubility and receptor selectivity of β-adrenoceptor blocking drugs for the occurrence of symptoms and side-effects in out-patients

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Abstract
Theodorsen L, Brørs O (Department of Pharmacotherapeutics. University of Oslo, Oslo, Norway). The importance of lipid solubility and receptor selectivity of β-adrenoceptor blocking drugs for the occurrence of symptoms and side-effects in out-patients. Short-term studies indicate that the side-effects of adrenergic β-receptor blockade may be influenced by lipid solubility and receptor selectivity of the blockers. The aim of the present study was to investigate the extent to which lipid solubility and receptor selectivity are related to the occurrence of symptoms during ordinary β-blocker treatment in out-patients. Two hundred and five patients (mean age 60 years) on β-blockade were interviewed about their symptoms. Eighty-five per cent of the patients had been on β-blocker treatment for more than 1 year. The blockers most commonly used were atenolol (51.0%). timolol (20.0%). propranolol (18.5%) and metoprolol (7.8%). β-Blocker treatment was associated with a significantly increased frequency of central nervous system and peripheral symptoms. The increase in central nervous system symptoms was significantly smaller in those on β-blockers with low rather than with intermediate (P = 0.015) or high lipid solubility (P = 0.007). The increase in peripheral symptoms was not significantly different with β1-selective and non-selective blockers. The results indicate that the liability of β-blockers to cause side-effects on the central nervous system is determined partly by their lipid solubility, and that receptor selectivity has only a small impact on their tendency to cause peripheral side-effects.

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