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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 ...
Sir James Whyte Black (14 June 1924 – 22 March 2010 [2]) was a Scottish physician and pharmacologist.Together with Gertrude B. Elion and George H. Hitchings, he shared the Nobel Prize for Medicine in 1988 for pioneering strategies for rational drug-design, which, in his case, led to the development of propranolol and cimetidine.
While once a first-line treatment for hypertension, the role of beta blockers was downgraded in June 2006 in the United Kingdom to fourth-line, as they do not perform as well as other drugs, particularly in the elderly, and evidence is increasing that the most frequently used beta blockers at usual doses carry an unacceptable risk of provoking ...
Metoprolol is classified as a moderately lipophilic beta blocker. [37] More lipophilic beta blockers tend to cross the blood–brain barrier more readily, with greater potential for effects in the central nervous system as well as associated neuropsychiatric side effects. [37] Metoprolol binds mainly to human serum albumin with an unbound ...
Prior to their discovery, the non-selective beta-agonist isoprenaline was used. The aim of the drug development through the years has been to minimise side effects, achieve selectivity and longer duration of action. The mechanism of action is well understood and has facilitated the development.
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]
Nebivolol is a beta blocker used to treat high blood pressure and heart failure. [5] As with other β-blockers, it is generally a less preferred treatment for high blood pressure. [6] It may be used by itself or with other blood pressure medication. [6] It is taken by mouth. [6] Common side effects include dizziness, feeling tired, nausea, and ...