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Beta blockers are known primarily for their reductive effect on heart rate, although this is not the only mechanism of action of importance in congestive heart failure. [17] Beta blockers, in addition to their sympatholytic β 1 activity in the heart, influence the renin–angiotensin system at the kidneys.
Acebutolol is a cardioselective beta-1 blocker which also considered a partial agonist due to its intrinsic sympathomimetic activity (ISA). This means it provides low-grade beta stimulation at rest but acting as typical beta-blockers when sympathetic activity is high. [3]
Figure 1: The chemical structure of dichloroisoprenaline or dichloroisoproterenol (), abbreviated DCI — the first β-blocker to be developed. β adrenergic receptor antagonists (also called beta-blockers or β-blockers) were initially developed in the 1960s, for the treatment of angina pectoris but are now also used for hypertension, congestive heart failure and certain arrhythmias. [1]
Beta-blockers with intrinsic sympathomimetic activity: acebutolol, pindolol; Some common side effects include increased airway resistance for non-selective beta-blockers, exacerbation of peripheral vascular diseases, and hypotension [15] Beta-blockers are contraindicated in patients with second- or third-degree atrioventricular block.
Oxprenolol (brand names Trasacor, Trasicor, Coretal, Laracor, Slow-Pren, Captol, Corbeton, Slow-Trasicor, Tevacor, Trasitensin, Trasidex) is a non-selective beta blocker with some intrinsic sympathomimetic activity. It is used for the treatment of angina pectoris, abnormal heart rhythms and high blood pressure.
The presence of hydroxy group in the benzene ring at 3rd and 4th position shows maximum alpha- and beta-adrenergic activity. [medical citation needed] For maximum sympathomimetic activity, a drug must have: Amine group two carbons away from an aromatic group; A hydroxyl group at the chiral beta position in the R-configuration
Labetalol is a beta blocker, or an antagonist of the β-adrenergic receptors. It is specifically a non-selective antagonist of the β 1-and β 2-adrenergic receptors. [17] Labetalol has intrinsic sympathomimetic activity. [17] It is also an antagonist of the α 1-adrenergic receptor, and hence is additionally an alpha blocker.
Landiolol, sold under the brand name Onoact among others, is a medication used for the treatment of tachycardia, atrial fibrillation, and atrial flutter. [1] [4] It is a beta-adrenergic blocker; [4] an ultra short-acting, β1-superselective intravenous adrenergic antagonist, which decreases the heart rate effectively with less negative effect on blood pressure or myocardial contractility.