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Beta blockers vary in their lipophilicity (fat solubility) and in turn in their ability to cross the blood–brain barrier and exert effects in the central nervous system. [76] Beta blockers with greater blood–brain barrier permeability can have both neuropsychiatric therapeutic benefits and side effects, as well as adverse cognitive effects ...
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.
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]
In general, pure beta-adrenergic agonists have the opposite function of beta blockers: beta-adrenoreceptor agonist ligands mimic the actions of both epinephrine- and norepinephrine- signaling, in the heart and lungs, and in smooth muscle tissue; epinephrine expresses the higher affinity.
Additionally, beta 1 blockers can affect beta 2 receptors, particularly at high doses, and hence should not be administered to patients with peripheral vascular disease or diabetes mellitus as they may cause vasoconstriction or a delayed hypoglycaemic response, respectively. [4]
It is also a adrenergic blocker with no partial agonist action and minimal membrane stabilizing activity. [2] Being selective for beta 1 receptors, it typically has fewer systemic side effects than non-selective beta-blockers, for example, not causing bronchospasm (mediated by beta 2 receptors) as timolol may.
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 ]
Celiprolol is a medication in the class of beta blockers, used in the treatment of high blood pressure. It has a unique pharmacology: it is a selective β1 receptor antagonist, but a β2 receptor partial agonist. It is also a weak α2 receptor antagonist. It was patented in 1973 and approved for medical use in 1982. [1]