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Antihypertensive agents comprise multiple classes of compounds that are intended to manage hypertension (high blood pressure). Antihypertensive therapy aims to maintain a blood pressure goal of <140/90 mmHg in all patients, as well as to prevent the progression or recurrence of cardiovascular diseases (CVD) in hypertensive patients with established CVD. [2]
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 ...
[11] [28] Compared to placebo, beta-blockers have a greater benefit in stroke reduction, but no difference on coronary heart disease or all-cause mortality. [32] However, three-quarters of active beta-blocker treatments in the randomised controlled trials included in the review used atenolol, and none used the newer vasodilating beta-blockers. [33]
The role for β-blockers in general in hypertension was downgraded in June 2006 in the United Kingdom, and later in the United States, as they are less appropriate than other agents such as ACE inhibitors, calcium channel blockers, thiazide diuretics and angiotensin receptor blockers, particularly in the elderly. [18] [19] [20]
In particular, beta-blockers are no longer recommended as first-line treatment due to relative adverse risk of stroke and new-onset of type 2 diabetes when compared to other medications, [3] while certain specific beta-blockers such as atenolol appear to be less useful in overall treatment of hypertension than several other agents. [36]
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]
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]
Carvedilol is a nonselective beta blocker and alpha-1 blocker. [5] How it improves outcomes is not entirely clear but may involve dilation of blood vessels. [5] Carvedilol was patented in 1978 and approved for medical use in the United States in 1995. [5] [8] It is on the World Health Organization's List of Essential Medicines. [9]
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