The applied pharmacology of beta-adrenoceptor antagonists (beta blockers) in relation to clinical outcomes

Abstract

Despite the fact that beta blockers were introduced into clinical practice 25 years ago, new beta blockers with differing kinetic and dynamic profiles continue to be developed and marketed. This overview assesses some of the more extensively studied agents from the point of view of proof of utility and the validity of claims for therapeutic advances. The clinical data suggests that despite the expectations of improvements based on kinetic and dynamic consideration, none of the newer agents have been shown unequivocally, either in terms of efficiency or tolerability, to be an advance over the reference agents, the beta 1 antagonists atenolol and metoprolol. This may be either because such improvements will not occur or because of shortcomings in the design and duration of comparative studies. There are trends to suggest that celiprolol has lesser effects on bronchial function and that it has a lesser impact on lipoprotein profiles. Approaches are suggested that might enable clinicians to appraise for themselves the validity of claims for the improved efficiency of new beta blockers.

Effect of chemically bonded stationary phases and mobile phase composition on β‐blockers retention in RP‐HPLC

“…The β-blockers can be used in the treatment of hypertension, angina pectoris, arrhythmia and congestive heart failure (Hardman and Limbird, 1996;Frishman, 1984;Fitzgerald, 1991;Brooks and Gillies, 1992). High-performance liquid chromatography (HPLC) method is most frequently used for analyses of these drugs (Saarinen et al, 1995;Maguregui et al, 1995;Gonzalez et al, 1995).…”

The design, synthesis and pharmacological characterization of novel β2-adrenoceptor antagonists

“…Therefore, experimental or clinical effects of ICI‐118,551 may be obscured by events independent of simple blockade of β 2 ‐adrenoceptor. Other problems with ICI‐118,551 that make it ill‐suited to in vivo or clinical studies are that it is extensively metabolized by the liver into less selective derivatives and is potentially carcinogenic (Fitzgerald, 1991).…”

Detection of beta-blockers in human urine by GC-MS-MS-EI: perspectives for the antidoping control

“…Beta-adrenergic receptors antagonists (beta blockers, BB) (see Fig. 1 for molecular structures) are a class of drugs widely used in clinical pharmacology, for the treatment of cardiovascular diseases (hypertension, ischemic heart disease, certain arrhytmias), and of glaucoma, for the prophylaxis of migraine, and for controlling acute panic symptoms in anxiety-provoking situations [1,[4][5][6][7][8]. As for other receptor-active agents, pharmacological properties of BB depend on both receptors localization in the various tissues and the activity of the corresponding sympathetic nerves; this explains why BB does not affect heart function at rest but are very effective during exercise and/or stress, i.e.…”