Use of multiple-action agents on the heart: pathophysiological and therapeutic considerations.
The introduction of beta-adrenoreceptor antagonists into clinical practice has resulted in major progress in the treatment of hypertension, angina pectoris, and congestive heart failure. However, the first and second (beta 1 selective) generations of beta-blockers induce a series of unwanted functional and metabolic effects, suggesting the search for a third generation of beta-antagonists. The new multiple-action beta-blockers, which have important peripheral vasodilator properties, appear to be promising with regard to clinical efficacy and side effects. In hypertensive patients, the vasodilation could add a more pathophysiological mechanism and therefore could induce a better preservation of systolic function. The global cardioprotection may be further improved by the absence of long-term metabolic effects. By virtue of their peripheral and coronary vasodilating properties, multiple-action beta-blockers could exert more favorable anti-ischemic effects in patients with angina pectoris than the traditional beta-blockers. In congestive heart failure, afterload reduction, and possibly myocardial beta 2-activation induced by multiple-action beta-blockers can minimize the negative inotropic effects, leading to better toleration at the beginning of treatment. The potential benefits of multiple-action beta-blockers have been assessed by preliminary studies and should be confirmed by trials in progress.
Magnani
B
B
Institute of Cardiovascular Diseases, University of Bologna, Italy.
Rapezzi
C
C
Galié
N
N
Ortolani
P
P
D000319:Adrenergic beta-Antagonists / Q000009:adverse effects / Q000494:pharmacology / Q000627:therapeutic use*; D000787:Angina Pectoris / Q000188:drug therapy* / Q000503:physiopathology; D001794:Blood Pressure / Q000187:drug effects; D015536:Down-Regulation; D006333:Heart Failure / Q000188:drug therapy* / Q000503:physiopathology; D006801:Humans; D006973:Hypertension / Q000188:drug therapy* / Q000503:physiopathology; D009200:Myocardial Contraction / Q000187:drug effects; D016277:Ventricular Function, Left / Q000187:drug effects / Q000502:physiology
D000319:Adrenergic beta-Antagonists