title: The importance of lipid solubility and receptor selectivity of beta-adrenoceptor blocking drugs for the occurrence of symptoms and side-effects in out-patients.
abstract: Short-term studies indicate that the side-effects of adrenergic beta-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 beta-blocker treatment in out-patients. Two hundred and five patients (mean age 60 years) on beta-blockade were interviewed about their symptoms. Eighty-five per cent of the patients had been on beta-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%). beta-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 beta-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 beta 1-selective and non-selective blockers. The results indicate that the liability of beta-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.
authors.affiliation: Department of Pharmacotherapeutics, University of Oslo, Norway.
authors.forename: L
authors.initials: L
authors.lastname: Theodoresen
authors.forename: O
authors.initials: O
authors.lastname: Brørs
mesh_terms: D000319:Adrenergic beta-Antagonists / Q000009:adverse effects* / Q000378:metabolism; D000328:Adult; D000368:Aged; D000369:Aged, 80 and over; D000553:Ambulatory Care; D005260:Female; D006801:Humans; D008055:Lipids; D008297:Male; D008875:Middle Aged; D011943:Receptors, Adrenergic, beta / Q000378:metabolism; D012995:Solubility
chemical_list: D000319:Adrenergic beta-Antagonists; D008055:Lipids; D011943:Receptors, Adrenergic, beta