β-blocker
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β-blocker
Beta blockers, also spelled β-blockers, are a class of medications that are predominantly used to manage abnormal heart rhythms (arrhythmia), and to protect the heart from a second heart attack after a first heart attack (secondary prevention). They are also widely used to treat high blood pressure, although they are no longer the first choice for initial treatment of most people. Beta blockers are competitive antagonists that block the receptor sites for the endogenous catecholamines epinephrine (adrenaline) and norepinephrine (noradrenaline) on adrenergic beta receptors, of the sympathetic nervous system, which mediates the fight-or-flight response. Beta-adrenergic receptors are found on cells of the heart muscles, Smooth muscle tissue, smooth muscles, airways, Artery, arteries, kidneys, and other tissues that are part of the sympathetic nervous system and lead to stress responses, especially when they are stimulated by epinephrine (adrenaline). Beta blockers interfere with t ...
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Atenolol
Atenolol is a beta blocker medication primarily used to treat high blood pressure and angina, heart-associated chest pain. Although used to treat high blood pressure, it does not seem to improve mortality rate, mortality in those with the condition. Other uses include the prevention of migraines and treatment of certain arrhythmia, irregular heart beats. It is taken oral administration, orally (by mouth) or by intravenous injection (injection into a vein). It can also be used with other blood pressure medications. Common side effects include fatigue (medical), feeling tired, heart failure, dizziness, depression (mood), depression, and shortness of breath. Other serious side effects include bronchospasm, bronchial spasm. Use is not recommended during pregnancy and alternative drugs are preferred when breastfeeding. It works by blocking Beta-1 adrenergic receptor, β1-adrenergic receptors in the heart, thus decreasing heart rate, cardiac contractility, force of heart beats, and b ...
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Heart Attack
A myocardial infarction (MI), commonly known as a heart attack, occurs when Ischemia, blood flow decreases or stops in one of the coronary arteries of the heart, causing infarction (tissue death) to the heart muscle. The most common symptom is retrosternal Angina, chest pain or discomfort that classically radiates to the left shoulder, arm, or jaw. The pain may occasionally feel like heartburn. This is the dangerous type of acute coronary syndrome. Other symptoms may include shortness of breath, nausea, presyncope, feeling faint, a diaphoresis, cold sweat, Fatigue, feeling tired, and decreased level of consciousness. About 30% of people have atypical symptoms. Women more often present without chest pain and instead have neck pain, arm pain or feel tired. Among those over 75 years old, about 5% have had an MI with little or no history of symptoms. An MI may cause heart failure, an Cardiac arrhythmia, irregular heartbeat, cardiogenic shock or cardiac arrest. Most MIs occur d ...
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Beta-2 Adrenergic Receptor
The beta-2 adrenergic receptor (β2 adrenoreceptor), also known as ADRB2, is a cell membrane-spanning beta-adrenergic receptor that binds epinephrine (adrenaline), a hormone and neurotransmitter whose signaling, via adenylate cyclase stimulation through trimeric Gs proteins, increases cAMP, and, via downstream L-type calcium channel interaction, mediates physiologic responses such as smooth muscle relaxation and bronchodilation. Robert Lefkowitz and Brian Kobilka's study of the beta-2 adrenergic receptor as a model system earned them the 2012 Nobel Prize in Chemistry "for studies of G-protein-coupled receptors". The official symbol for the human gene encoding the β2 adrenoreceptor is ''ADRB2''. Gene The gene is intronless. Different polymorphic forms, point mutations, and/or downregulation of this gene are associated with nocturnal asthma, obesity and type 2 diabetes. Structure The 3D crystallographic structure (see figure and links to the right) of the β2-adrener ...
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Norepinephrine
Norepinephrine (NE), also called noradrenaline (NA) or noradrenalin, is an organic compound, organic chemical in the catecholamine family that functions in the brain and human body, body as a hormone, neurotransmitter and neuromodulator. The name "noradrenaline" (from Latin '':wikt:ad-, ad'', "near", and '':wikt:ren, ren'', "kidney") is more commonly used in the United Kingdom and the rest of the world, whereas "norepinephrine" (from Ancient Greek :wikt:ἐπί, ἐπῐ́ (''epí''), "upon", and :wikt:νεφρός, νεφρός (''nephrós''), "kidney") is usually preferred in the United States. "Norepinephrine" is also the international nonproprietary name given to norepinephrine (drug), the drug. Regardless of which name is used for the substance itself, parts of the body that produce or are affected by it are referred to as noradrenergic. The general function of norepinephrine is to mobilize the brain and body for action. Norepinephrine release is lowest during sleep, rise ...
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Heart
The heart is a muscular Organ (biology), organ found in humans and other animals. This organ pumps blood through the blood vessels. The heart and blood vessels together make the circulatory system. The pumped blood carries oxygen and nutrients to the tissue, while carrying metabolic waste such as carbon dioxide to the lungs. In humans, the heart is approximately the size of a closed fist and is located between the lungs, in the middle compartment of the thorax, chest, called the mediastinum. In humans, the heart is divided into four chambers: upper left and right Atrium (heart), atria and lower left and right Ventricle (heart), ventricles. Commonly, the right atrium and ventricle are referred together as the right heart and their left counterparts as the left heart. In a healthy heart, blood flows one way through the heart due to heart valves, which prevent cardiac regurgitation, backflow. The heart is enclosed in a protective sac, the pericardium, which also contains a sma ...
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Meta-analyses
Meta-analysis is a method of synthesis of quantitative data from multiple independent studies addressing a common research question. An important part of this method involves computing a combined effect size across all of the studies. As such, this statistical approach involves extracting effect sizes and variance measures from various studies. By combining these effect sizes the statistical power is improved and can resolve uncertainties or discrepancies found in individual studies. Meta-analyses are integral in supporting research grant proposals, shaping treatment guidelines, and influencing health policies. They are also pivotal in summarizing existing research to guide future studies, thereby cementing their role as a fundamental methodology in metascience. Meta-analyses are often, but not always, important components of a systematic review. History The term "meta-analysis" was coined in 1976 by the statistician Gene Glass, who stated ''"Meta-analysis refers to the analysi ...
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Pharmacology
Pharmacology is the science of drugs and medications, including a substance's origin, composition, pharmacokinetics, pharmacodynamics, therapeutic use, and toxicology. More specifically, it is the study of the interactions that occur between a living organism and chemicals that affect normal or abnormal biochemical function. If substances have medicinal properties, they are considered pharmaceuticals. The field encompasses drug composition and properties, functions, sources, synthesis and drug design, molecular and cellular mechanisms, organ/systems mechanisms, signal transduction/cellular communication, molecular diagnostics, interactions, chemical biology, therapy, and medical applications and antipathogenic capabilities. The two main areas of pharmacology are pharmacodynamics and pharmacokinetics. Pharmacodynamics studies the effects of a drug on biological systems, and pharmacokinetics studies the effects of biological systems on a drug. In broad terms, pharmacod ...
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Angina Pectoris
Angina, also known as angina pectoris, is chest pain or pressure, usually caused by insufficient blood flow to the heart muscle (myocardium). It is most commonly a symptom of coronary artery disease. Angina is typically the result of partial obstruction or spasm of the arteries that supply blood to the heart muscle. The main mechanism of coronary artery obstruction is atherosclerosis as part of coronary artery disease. Other causes of angina include abnormal heart rhythms, heart failure and, less commonly, anemia. The term derives , and can therefore be translated as "a strangling feeling in the chest". An urgent medical assessment is suggested to rule out serious medical conditions. There is a relationship between severity of angina and degree of oxygen deprivation in the heart muscle. However, the severity of angina does not always match the degree of oxygen deprivation to the heart or the risk of a heart attack (myocardial infarction). Some people may experience s ...
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Pronethalol
Pronethalol (also known as nethalide or compound 38,174; trade name Alderlin) was an early non-selective beta blocker clinical candidate. It was the first beta blocker to be developed by James Black and associates at Imperial Chemical Industries, and the first to enter clinical use, in November 1963. However, it was never used widely due to carcinogenicity in mice, which was thought to result from formation of a carcinogenic naphthalene epoxide metabolite, and was superseded by propranolol from 1965 onward. See also * Beta blocker Beta blockers, also spelled β-blockers, are a class of medications that are predominantly used to manage abnormal heart rhythms ( arrhythmia), and to protect the heart from a second heart attack after a first heart attack ( secondary prevention ... * Discovery and development of beta-blockers * Naphthylaminopropane References Beta blockers 2-Naphthyl compounds Naphthylethylamines Phenylethanolamines {{antihypertensive-stub ...
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James Black (pharmacologist)
Sir James Whyte Black (14 June 1924 – 22 March 2010) 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. Black established a Veterinary Physiology department at the University of Glasgow, where he became interested in the effects of adrenaline on the human heart. He went to work for ICI Pharmaceuticals in 1958 and, while there, developed propranolol, a beta blocker used for the treatment of heart disease. Black was also responsible for the development of cimetidine, an H2 receptor antagonist, a drug used to treat stomach ulcers. Early life and education Black was born on 14 June 1924 in Uddingston, Lanarkshire, the fourth of five sons of a Baptist family which traced its origins to Balquhidder, Perthshire. His father was a mining engineer. ...
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Beta-3 Adrenergic Receptor
The beta-3 adrenergic receptor (β3-adrenoceptor), also known as ADRB3, is a beta-adrenergic receptor, and also denotes the human gene encoding it. Function Actions of the β3 receptor include *Enhancement of lipolysis in adipose tissue. *Thermogenesis in skeletal muscle Page 163 It is located mainly in adipose tissue and is involved in the regulation of lipolysis and thermogenesis. Some β3 agonists have demonstrated antistress effects in animal studies, suggesting it also has a role in the central nervous system (CNS). β3 receptors are found in the gallbladder, urinary bladder, and in brown adipose tissue. Their role in gallbladder physiology is unknown, but they are thought to play a role in lipolysis and thermogenesis in brown fat. In the urinary bladder it is thought to cause relaxation of the bladder and prevention of urination. Mechanism of action Beta adrenergic receptors are involved in the epinephrine- and norepinephrine-induced activation of adenylate cyclase t ...
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Beta-1 Adrenergic Receptor
The beta-1 adrenergic receptor (β1 adrenoceptor), also known as ADRB1, can refer to either the protein-encoding gene (gene ADRB1) or one of the four adrenergic receptors. It is a G-protein coupled receptor associated with the Gs heterotrimeric G-protein that is expressed predominantly in cardiac tissue. In addition to cardiac tissue, beta-1 adrenergic receptors are also expressed in the cerebral cortex. Historical Context W. B. Cannon postulated that there were two chemical transmitters or sympathins while studying the sympathetic nervous system in 1933. These E and I sympathins were involved with excitatory and inhibitory responses. In 1948, Raymond Ahlquist published a manuscript in the ''American Journal of Physiology'' establishing the idea of adrenaline having distinct actions on both alpha and beta receptors. Shortly afterward, Eli Lilly Laboratories synthesized the first beta-blocker, dichloroisoproterenol. General Information Structure ADRB-1 is a transmembra ...
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