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Mini Reviews in Medicinal Chemistry 2016It has been over half a century since propranolol, the first beta-blocker, was developed for medical treatment. Since that time a large number of compounds from this... (Review)
Review
It has been over half a century since propranolol, the first beta-blocker, was developed for medical treatment. Since that time a large number of compounds from this group have been synthesised and many are now in clinical use. The structure, function, pharmacokinetics, and mechanism of beta-blockers have been established. The possibilities for their use in treating different conditions continue to evolve. Since the discovery of later generation beta-blockers, such as carvedilol and nebivolol, the search for new compounds continues, and may include known substances with beta-blocking properties which could extend their therapeutic potential.
Topics: Adrenergic beta-Antagonists; Chemistry, Pharmaceutical; Glaucoma; Humans; Hypertension; Hyperthyroidism; Migraine Disorders; Molecular Structure
PubMed: 26471965
DOI: 10.2174/1389557515666151016125948 -
The American Journal of Medicine Jul 2019Beta-blockers are commonly used medications, and they have been traditionally considered "cardioprotective." Their clinical use appears to be more widespread than the... (Review)
Review
Beta-blockers are commonly used medications, and they have been traditionally considered "cardioprotective." Their clinical use appears to be more widespread than the available evidence base supporting their role in cardioprotection. Beta-blockers counteract neurohumoral activation in heart failure with reduced ejection fraction and offer both symptomatic improvement and reduction in adverse events. On the other hand, the use of beta-blockers in uncomplicated hypertension results in suboptimal outcomes compared to the established first-line antihypertensive agents. Providers at all levels should be familiar with common misconceptions regarding beta-blocker use in routine clinical practice.
Topics: Adrenergic beta-Antagonists; Cardiotonic Agents; Coronary Artery Disease; Heart Failure; Humans; Hypertension
PubMed: 30817899
DOI: 10.1016/j.amjmed.2019.01.039 -
Autonomic Neuroscience : Basic &... Jun 2009It is necessary to note at very beginning, that up to now a comparative approach to the discussion of the structure and function of synthetic and endogenous... (Review)
Review
It is necessary to note at very beginning, that up to now a comparative approach to the discussion of the structure and function of synthetic and endogenous beta-adrenergic agonists for biomedical and clinical sciences does not appear to be available in the literature. Maybe, one of the reasons for this lies in the differential relations and constant attention of investigators either to the synthetic beta-adrenergic blockers on one hand or to endogenous beta-adrenergic receptor antagonists (EBARA) on the other. Therefore, the main goal of this article is to attempt to overcome this. It is clear now that there are several common properties and relevant features among synthetic beta-adrenergic receptor blockers, endogenous nonspecific beta-adrenergic antagonists (ENBARA) and relative endogenous specific beta-adrenergic antagonists (RESBARA). They are predominantly related to the reduction of adrenergic influence, namely, beta-adrenergic receptor neurotransmission, and, at an intracellular molecular level, to inhibition of adenylate cyclase and a decrease in cyclic AMP content. Other relevant and individual differences are also available and are also discussed.
Topics: Adrenergic beta-2 Receptor Antagonists; Adrenergic beta-Antagonists; Animals; Humans; Receptors, Adrenergic, beta-2
PubMed: 19328045
DOI: 10.1016/j.autneu.2009.02.005 -
Journal of Cardiovascular Pharmacology... Jul 2013The development and subsequent clinical application of the β-adrenergic receptor blocking drugs represent one of the major advances in human pharmacotherapeutics. No... (Review)
Review
The development and subsequent clinical application of the β-adrenergic receptor blocking drugs represent one of the major advances in human pharmacotherapeutics. No other class of synthetic drugs has demonstrated such widespread therapeutic utility for the treatment and prevention of so many cardiovascular diseases. In addition, these drugs have proven to be molecular probes that have contributed to our understanding of the disease, and on the molecular level, both the structure and function of the 7 transmembrane G protein receptors that mediate the actions of many different hormones, neurotransmitters, and drugs. The evolution of β-blocker drug development has led to refinements in their pharmacodynamic actions that include agents with relative β1-selectivity, partial agonist activity, concomitant α-adrenergic blockers activity, and direct vasodilator activity. In addition, long-acting and ultra-short-acting formulations of β-blockers have also demonstrated a remarkable record of clinical safety in patients of all ages.
Topics: Adrenergic beta-Antagonists; Cardiovascular Diseases; Humans
PubMed: 23637119
DOI: 10.1177/1074248413484986 -
AACN Clinical Issues in Critical Care... May 1992Use of beta (beta)-adrenergic blocking agents began in the 1960s and has risen dramatically since then. Newer agents offer more actions and fewer side effects. Uses for... (Review)
Review
Use of beta (beta)-adrenergic blocking agents began in the 1960s and has risen dramatically since then. Newer agents offer more actions and fewer side effects. Uses for the drugs continue to increase as their safety and efficacy become increasingly apparent. beta block, today, has widespread application in cardiovascular disease. In addition, these agents are used in the management of endocrine disorders, neurologic situations, psychiatric disorders, gastrointestinal problems, and sensory disorders. Many new beta blockers are still investigational, and some show even greater promise for therapeutic applications in the future.
Topics: Adrenergic beta-Antagonists; Adult; Aged; Aging; Cardiovascular Diseases; Child; Endocrine System Diseases; Humans; Mental Disorders; Migraine Disorders; Nervous System Diseases; Racial Groups
PubMed: 1349490
DOI: 10.4037/15597768-1992-2016 -
The American Journal of Medicine Jul 1992To review the clinical and biochemical effects of beta-adrenergic blocking drugs on hyperthyroidism. (Review)
Review
PURPOSE
To review the clinical and biochemical effects of beta-adrenergic blocking drugs on hyperthyroidism.
MATERIALS AND METHODS
Studies published since 1972 were identified through a computerized search of MEDLINE and extensive searching of the bibliographies of the articles identified. Based on an understanding of the differences in beta-blocker metabolism in euthyroid and hyperthyroid patients, we reviewed the differences in pharmacokinetics and metabolic and clinical outcomes during their use in hyperthyroidism, as reported in the articles reviewed.
RESULTS
beta Blockers have been used to modify the severity of the hyperadrenergic symptoms of hyperthyroidism for the past 20 years. The clinical efficacy of these agents is affected by hyperthyroid-induced alterations in their gastrointestinal absorption, hepatic metabolism, and renal excretion. The mechanisms whereby these clinical changes are effected is unknown. The agents differ in their beta 1 cardioselectivity, membrane-stabilizing activity, intrinsic sympathomimetic activity, and lipid solubility. They do not appear to alter synthesis or secretion of thyroid hormone by the thyroid gland. Their effects on thyroxine metabolism are contradictory. Decreased thyroxine to triiodothyronine conversion is caused by some, but not all, beta blockers, and this appears to correlate with membrane-stabilizing activity. There does not appear to be any alteration in catecholamine sensitivity during beta-adrenergic blockade.
CONCLUSIONS
The principal mechanism of action of beta blockers in hyperthyroidism is to antagonize beta-receptor-mediated effects of catecholamines. beta Blockers are effective in treating hypermetabolic symptoms in a variety of hyperthyroid states. Used alone, they offer significant symptomatic relief. They are also useful adjuvants to antithyroid medications, surgery, and radioactive iodide treatment in patients with Graves' disease and toxic nodular goiters.
Topics: Adrenergic beta-Antagonists; Humans; Hyperthyroidism
PubMed: 1352658
DOI: 10.1016/0002-9343(92)90681-z -
Reviews on Recent Clinical Trials 2014Patients with chronic heart failure have prolonged sympathetic stimulation and subsequent worsening of the failing heart function. Beta-blockers (non-selective,...
Patients with chronic heart failure have prolonged sympathetic stimulation and subsequent worsening of the failing heart function. Beta-blockers (non-selective, cardio-selective, and non-selective with ancillary properties) counteract the effects of prolonged sympathetic stimulation. Beta-blocker therapy results in the improvement of the left ventricular systolic and diastolic function, reversal remodeling, heart rate control, effective prevention of the malignant arrhythmias, and lowering of the both cardiac afterload and preload in patients with chronic heart failure.
Topics: Adrenergic beta-Antagonists; Child; Chronic Disease; Heart Failure; Humans
PubMed: 25198736
DOI: 10.2174/1574887109666140908125402 -
Journal of the American College of... Jun 2023
Topics: Humans; Adrenergic beta-Antagonists
PubMed: 37316111
DOI: 10.1016/j.jacc.2023.04.028 -
Revue Medicale Suisse May 2024
Topics: Humans; Adrenergic beta-Antagonists
PubMed: 38783677
DOI: 10.53738/REVMED.2024.20.875.1051 -
Chirality May 2020The modern β-adrenergic agonists (β-blockers) possess one or more than one chiral center in their structure. Two enantiomers exhibit distinct pharmacodynamic and... (Review)
Review
The modern β-adrenergic agonists (β-blockers) possess one or more than one chiral center in their structure. Two enantiomers exhibit distinct pharmacodynamic and pharmacokinetic behaviors. Current progress in drug designing has resulted in the ability to understand the role of chirality in modern therapeutics. Furthermore, with a greater understanding of the molecular structure of precise drug targets, development of new drugs is directed towards the pure enantiomers instead of its racemates. The present review deals with a discussion on the stereochemical facets of chiral clinical β-blockers. This review provides details of stereo-selectivity in the pharmacological behavior of some of β-blockers and their metabolites. An effort has been made on highlighting the distinction between the therapeutic behavior of the racemic mixtures and pure enantiomers.
Topics: Adrenergic beta-Antagonists; Humans; Stereoisomerism
PubMed: 32105373
DOI: 10.1002/chir.23200