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Bisoprolol, sold under the brand name Zebeta among others, is a beta blocker which is selective for the beta-1 receptor [7] and used for cardiovascular diseases, [7] including tachyarrhythmias, high blood pressure, angina, and heart failure. [7] [8] It is taken by mouth. [7]
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.
ATC code C07 Beta blocking agents is a therapeutic subgroup of the Anatomical Therapeutic Chemical Classification System, a system of alphanumeric codes developed by the World Health Organization (WHO) for the classification of drugs and other medical products. [1] [2] [3] Subgroup C07 is part of the anatomical group C Cardiovascular system. [4]
Beta 2 blockers cease action of beta-2 receptor by blocking the receptor and preventing it from being activated. [6] Similar to beta-1 receptor , the activated beta-2 receptor will lead to the detach of alpha subunit of Gs protein and attachment of adenylate cyclase . [ 6 ]
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 ...
Esmolol, sold under the brand name Brevibloc, is a cardio selective beta 1 receptor blocker with rapid onset, [3] a very short duration of action, and no significant intrinsic sympathomimetic or membrane stabilising activity at therapeutic dosages. It is a class II antiarrhythmic. [4]
[12] [13] Other beta blockers are also used. [12] [13] However, the controversial yet possible phenomenon of "unopposed α-stimulation" with administration of selective beta blockers to block non-selective sympathomimetics potentially makes dual alpha-1 and beta blockers like labetalol and carvedilol more favorable for such purposes.
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 ]