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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 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 ...
The cardio-selective beta-1 blockers could cause adverse effects including bradycardia, reduced exercise ability, hypotension, atrioventricular nodal blockage and heart failure. [5] Other possible adverse effects include nausea and vomiting , abdominal discomfort , dizziness , weakness , headache , fatigue , and dryness in mouth and eye . [ 5 ]
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. Betaxolol also shows greater affinity for beta 1 receptors than metoprolol.
Beta blockers exert their pharmacological effect, decreased heart rate, by binding to and competitively antagonising a type of receptor called beta adrenoceptors. [1]In pharmacology, the term mechanism of action (MOA) refers to the specific biochemical interaction through which a drug substance produces its pharmacological effect. [2]
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.
A Beta-2 adrenergic antagonist (β 2-adrenoceptor antagonist) is an adrenergic antagonist which blocks the beta-2 adrenergic receptors of cells, with either high specificity (an antagonist which is selective for β 2 adrenoceptors) like Butaxamine and ICI-118,551, or non-specifically (an antagonist for β 2 and for β 1 or β 3 adrenoceptors) like the non-selective betablocker Propranolol.
ADRB-1 antagonists are a class of drugs also referred to as Beta Blockers β1-selective antagonists are used to manage abnormal heart rhythms and block the action of substances like adrenaline on neurons, allowing blood to flow more easily which lowers blood pressure and cardiac output. They may also shrink vascular tumors.