Beta blocker

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Beta blocker

Beta blockers (sometimes written as ß-blocker) are a class of drugs

Medication

A pharmaceutical drug, also referred to as medicine or medicament, can be loosely defined as any substance intended for use in the diagnosis, cure, mitigation, treatment, or prevention of disease....
used for various indications, but particularly for the management of cardiac arrhythmia

Cardiac arrhythmia

Cardiac arrhythmia is a term for any of a large and heterogeneous group of conditions in which there is abnormal Electrical conduction system of the heart in the heart....
s, cardioprotection after myocardial infarction

Myocardial infarction

Myocardial infarction , commonly known as a heart attack, occurs when the Blood flow to part of the heart is interrupted. This is most commonly due to occlusion of a coronary artery following the rupture of a Vulnerable plaque, which is an unstable collection of lipids and white blood cells in the wall of an artery....
(heart attack), and hypertension

Hypertension

Hypertension, also referred to as high blood pressure, HTN or HPN, is a medical condition in which the blood pressure is chronically elevated....
. Propranolol

Propranolol

Propranolol is a non-selective beta blocker mainly used in the treatment of hypertension. It was the first successful beta blocker developed. It is the only drug proven effective for the prophylaxis of migraines in children....
was the first clinically useful beta adrenergic receptor antagonist

Receptor antagonist

A receptor antagonist is a type of receptor ligand or drug that does not provoke a biological response itself upon binding to a Receptor , but blocks or dampens agonist-mediated responses....
. Invented by Sir James W. Black

James W. Black

Sir James Whyte Black, Order of Merit, Royal Society, Royal Society of Edinburgh, Royal College of Physicians is a Scotland Physician and Pharmacology who invented Propranolol, synthesized Cimetidine and was awarded the Nobel Prize in Physiology or Medicine in 1988 for these discoveries....
, it revolutionized the medical management of angina pectoris and is considered to be one of the most important contributions to clinical medicine and pharmacology

Pharmacology

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Encyclopedia

Beta blockers (sometimes written as ß-blocker) are a class of drugs

Medication

Cardiac arrhythmia

Myocardial infarction

Hypertension

Hypertension, also referred to as high blood pressure, HTN or HPN, is a medical condition in which the blood pressure is chronically elevated....
. Propranolol

Propranolol

Receptor antagonist

James W. Black

Pharmacology

Pharmacology is the study of drug action. More specifically it is the study of the interactions that occur between a living organism and exogenous chemicals that alter normal biochemical function....
of the 20th century. Beta blockers may also be referred to as beta-adrenergic blocking agents, beta-adrenergic antagonists, or beta antagonists.

Pharmacology

There are three known types of beta receptor, designated ß₁, ß₂ and ß₃. ß₁-Adrenergic receptors are located mainly in the heart and in the kidneys. ß₂-Adrenergic receptors are located mainly in the lungs, gastrointestinal tract, liver, uterus, vascular smooth muscle, and skeletal muscle. ß₃-receptors are located in fat cells.

Examples of beta-blockers include: Sectral (acebutolol), Zebeta (bisoprolol), Brevibloc (esmolol), Inderal (propranolol), Tenormin (atenolol

Atenolol

Atenolol is a beta-1 receptor selective antagonist, a drug belonging to the group of beta blocker, a class of drugs used primarily in cardiovascular diseases....
), Normodyne (labetalol), Coreg (carvedilol), Lopressor (metoprolol), and Bystolic (nebivolol).

ß-Receptor antagonism

Stimulation of ß₁ receptors by epinephrine induces a positive chronotropic

Chronotropic

Chronotropic effects are those that change the heart rate.Chronotropic drugs may change the heart rate by affecting the nerves controlling the heart, or by changing the rhythm produced by the sinoatrial node....
and inotropic effect on the heart and increases cardiac conduction velocity and automaticity. Stimulation of ß₁ receptors on the kidney causes renin release. Stimulation of ß₂ receptors induces smooth muscle

Smooth muscle

Smooth muscle is a type of non-striated muscle, found within the tunica media layer of large and small arteries and veins, the urinary bladder, uterus, male and female reproductive tracts, gastrointestinal tract, respiratory tract, the ciliary muscle, and iris of the eye....
relaxation, induces tremor in skeletal muscle

Skeletal muscle

They generally contract voluntarily , although they can contract involuntarily through Reflex action. The whole muscle is wrapped in a special type of connective tissue, epimysium....
, and increases glycogenolysis

Glycogenolysis

Glycogenolysis is the catabolism of glycogen by removal of a glucose monomer through cleavage with inorganic phosphate to produce glucose-1-phosphate....
in the liver

Liver

The liver is a vital organ present in vertebrates and some other animals; it has a wide range of functions, a few of which are detoxification, protein synthesis, and production of biochemicals necessary for digestion....
and skeletal muscle

Skeletal muscle

Lipolysis

Lipolysis is the breakdown of fat stored in fat cells. During this process, free fatty acids are released into the bloodstream and circulate throughout the body....
.

Beta blockers inhibit these normal epinephrine-mediated sympathetic

Sympathetic nervous system

The Sympathetic Nervous System is a branch of the autonomic nervous system along with the enteric nervous system and parasympathetic nervous system....
actions, but have minimal effect on resting subjects. That is, they reduce the effect of excitement/physical exertion on heart rate and force of contraction, dilation of blood vessels and opening of bronchi, and also reduce tremor and breakdown of glycogen

Glycogen

Glycogen is a polysaccharide of glucose which functions as the secondary short term energy storage in animal cells. It is made primarily by the liver and the muscles, but can also be made by the brain and stomach....
.

It is therefore expected that non-selective beta blockers have an antihypertensive

Antihypertensive

Antihypertensives are a class of medication that are used in medicine and pharmacology to treat hypertension . There are many classes of antihypertensives, which?by varying means?act by lowering blood pressure....
effect. The antihypertensive mechanism appears to involve reduction in cardiac output (due to negative chronotropic and inotropic effects), reduction in renin

Renin

Renin , also known as Angiotensinogenase, is a circulating enzyme that participates in the body's renin-angiotensin system that mediates extracellular volume , and arterial vasoconstriction....
release from the kidneys, and a central nervous system

Central nervous system

The central nervous system is the part of the nervous system that functions to coordinate the activity of all parts of the bodies of multicellular organisms....
effect to reduce sympathetic

Sympathetic nervous system

The Sympathetic Nervous System is a branch of the autonomic nervous system along with the enteric nervous system and parasympathetic nervous system....
activity (for those ß-blockers that do cross the blood-brain barrier, e.g. Propranolol).

Antianginal effects result from negative chronotropic

Chronotropic

Chronotropic effects are those that change the heart rate.Chronotropic drugs may change the heart rate by affecting the nerves controlling the heart, or by changing the rhythm produced by the sinoatrial node....
properties of beta blockers allow the lifesaving property of Heart rate control. Beta blockers are readily titrated to optimal rate control in many pathologic states.

The antiarrhythmic effects of beta blockers arise from sympathetic nervous system blockade – resulting in depression of sinus node function and atrioventricular node

Atrioventricular node

The atrioventricular node is a part of electrical control system of the heart that co-ordinates heart rate. It electrically connects atrial and ventricular chambers....
conduction, and prolonged atrial

Atrium (anatomy)

In anatomy, the atrium , sometimes called auricle, refers to a chamber or space. It may be the atrium of the lateral ventricle in the brain or the blood collection chamber of a heart....
refractory periods. Sotalol

Sotalol

Sotalol is a medication used in individuals with rhythm disturbances of the heart, and to treat hypertension in some individuals....
, in particular, has additional antiarrhythmic properties and prolongs action potential

Action potential

An action potential is a self-regenerating wave of electrochemical activity that allows nerve cells to carry a signal over a distance. It is the primary electrical signal generated by nerve cells, and arises from changes in the permeability of the nerve cell's axonal Cell membranes to specific ions....
duration through potassium channel

Potassium channel

In the field of cell biology, potassium channels are the most widely distributed type of ion channel and are found in virtually all living organisms....
blockade.

Blockade of the sympathetic nervous system on renin release leads to reduced aldosterone via the renin angiotensin aldosterone system

Renin-angiotensin system

The renin-angiotensin system or the renin-angiotensin-aldosterone system is a hormone system that regulates blood pressure and water balance....
with a resultant decrease in blood pressure due to decreased sodium and water retention.

Intrinsic sympathomimetic activity

Also referred to as intrinsic sympathomimetic activity, this term is used particularly with beta blockers that can show both agonism and antagonism at a given beta receptor, depending on the concentration of the agent (beta blocker) and the concentration of the antagonized agent (usually an endogenous compound such as norepinephrine

Norepinephrine

Norepinephrine or noradrenaline is a catecholamine with dual roles as a hormone and a neurotransmitter.As a stress hormone, norepinephrine affects parts of the brain where attention and responding actions are controlled....
). See partial agonist

Partial agonist

Partial agonists bind and activate a given receptor, but have only partial efficacy#Pharmacology at the receptor relative to a full agonist. They may also be considered ligands which display both agonistic and antagonistic effects - when both a full agonist and partial agonist are present, the partial agonist actually acts as a competitive...
for a more general description.

Some beta blockers (e.g. oxprenolol

Oxprenolol

Oxprenolol is a non-selective beta blocker with some intrinsic sympathomimetic amine activity. It is used for the treatment of angina pectoris and abnormal heart rhythms....
, pindolol

Pindolol

Pindolol is a beta blocker drug....
, penbutolol

Penbutolol

Penbutolol is a medication in the class of beta blockers, used in the treatment of hypertension.External links...
and acebutolol

Acebutolol

Acebutolol is a beta blocker for the treatment of hypertension and arrhythmias....
) exhibit intrinsic sympathomimetic activity (ISA). These agents are capable of exerting low level agonist activity at the ß-adrenergic receptor while simultaneously acting as a receptor site antagonist

Receptor antagonist

Bradycardia

Bradycardia , as applied to adult medicine, is defined as a resting heart rate of under 60 beats per minute, though it is seldom symptomatic until the rate drops below 50 beat/min....
with sustained beta blocker therapy.

Agents with ISA are not used in post-myocardial infarction

Myocardial infarction

a₁-Receptor antagonism

Some beta blockers (e.g. labetalol

Labetalol

Labetalol is a mixed alpha/beta antagonistic drug used to treat hypertension....
and carvedilol

Carvedilol

Carvedilol is a beta blocker indicated in the treatment of mild to moderate congestive heart failure . It is marketed under various trade names including Coreg , Dilatrend , Eucardic , and Carloc as a generic drug ., and as a controlled-release formulation, marketed in the US as Coreg CR ....
) exhibit mixed antagonism of both ß- and a₁-adrenergic receptor

Adrenergic receptor

The adrenergic receptors are a class of G protein-coupled receptors that are targets of the catecholamines. Adrenergic Receptor s specifically bind and are activated by their endogenous ligands, the catecholamines adrenaline and noradrenaline ....
s, which provides additional arteriolar

Arteriole

An arteriole is a small diameter blood vessel that extends and branches out from an artery and leads to capillary. Arterioles have thin muscle walls and are the primary site of vascular resistance....
vasodilating action.

Other effects

Beta blockers decrease nocturnal melatonin

Melatonin

Melatonin , also known chemically as N-acetyl-5-methoxytryptamine, is a naturally occurring hormone found in most animals, including humans, and some other living organisms, including algae....
release, perhaps partly accounting for sleep disturbance caused by some agents.

Beta blockers protect against social anxiety: "Improvement of physical symptoms has been demonstrated with beta-blockers such as propranolol; however, these effects are limited to the social anxiety experienced in performance situations." (example- an inexperienced symphony soloist)

Beta blockers can impair the relaxation of bronchial muscle (mediated by beta-2) and so should be avoided by asthmatics.

They can also be used to treat glaucoma because they decrease intraocular pressure

Intraocular pressure

Intraocular pressure is the fluid pressure inside the eye....
by lowering aqueous humor secretion.

Clinical use

Large differences exist in the pharmacology of agents within the class, thus not all beta blockers are used for all indications listed below.

Indications for beta blockers include:

Hypertension
Hypertension

Hypertension, also referred to as high blood pressure, HTN or HPN, is a medical condition in which the blood pressure is chronically elevated....
Angina
Mitral valve prolapse
Mitral valve prolapse

Mitral valve prolapse is a valvular heart disease characterized by the displacement of an abnormally thickened mitral valve leaflet into the atria of the heart during systole....
Cardiac arrhythmia
Cardiac arrhythmia

Cardiac arrhythmia is a term for any of a large and heterogeneous group of conditions in which there is abnormal Electrical conduction system of the heart in the heart....
Atrial fibrillation
Atrial fibrillation

Atrial fibrillation is a cardiac arrhythmia that involves the two upper chambers of the heart. It can often be identified by taking a pulse and observing that the heartbeats don't occur at regular intervals, but a conclusive indication of AF is the absence of P waves on an electrocardiogram ....
Congestive heart failure
Congestive heart failure

Heart failure is a condition in which a problem with the structure or function of the heart impairs its ability to supply sufficient blood flow to meet the body's needs....
Myocardial infarction
Myocardial infarction

Myocardial infarction , commonly known as a heart attack, occurs when the Blood flow to part of the heart is interrupted. This is most commonly due to occlusion of a coronary artery following the rupture of a Vulnerable plaque, which is an unstable collection of lipids and white blood cells in the wall of an artery....
Glaucoma
Glaucoma

Glaucoma is a group of diseases of the optic nerve involving loss of ganglion cell in a characteristic pattern of optic atrophy. Raised intraocular pressure is a significant risk factor for developing glaucoma ....
Migraine
Migraine

Migraine is a neurology syndrome characterized by altered bodily perceptions, headaches, and nausea. Physiologically, the migraine headache is a neurological condition more common to women than to men....
prophylaxis
Prophylaxis

Prophylaxis is any medical or public health procedure whose purpose is to prevent, rather than treat or cure a disease. Roughly, prophylactic measures are divided between primary prophylaxis and secondary prophylaxis ....
Symptomatic control (tachycardia
Tachycardia

The word tachycardia comes from the Greek words tachys and kardia .Tachycardia typically refers to a heartrate that exceeds the range of the normal resting heartrate, based upon age:...
, tremor
Tremor

Tremor is an unintentional, somewhat rhythmic, muscle movement involving to-and-fro movements of one or more body parts. It is the most common of all involuntary movements and can affect the hands, arms, head, face, vocal cords, trunk, and legs....
) in anxiety
Anxiety

Anxiety is a psychological and physiological state characterized by cognitive, somatic, emotional, and behavioral components. These components combine to create an unpleasant feeling that is typically associated with uneasiness, fear, or worry....
and hyperthyroidism
Hyperthyroidism

Hyperthyroidism is the term for overactive tissue within the thyroid gland,resulting in overproduction and thus an excess of circulating free thyroid hormones: thyroxine , triiodothyronine , or both....
Essential tremor
Essential tremor

Essential tremor is a progressive neurological disorder whose most recognizable feature is a tremor of the arms that is apparent during voluntary movements such as eating and writing....
Phaeochromocytoma, in conjunction with a-blocker
Alpha blocker

Alpha-1 blockers constitute a variety of drugs which block Adrenergic receptor#Alpha .CE.B1 receptors in arteries and smooth muscles....

Beta blockers have also been used in the following conditions:

Hypertrophic obstructive cardiomyopathy
Cardiomyopathy

Cardiomyopathy, which literally means "heart muscle disease," is the deterioration of the function of the myocardium for any reason. People with cardiomyopathy are often at risk of arrhythmia or sudden cardiac death or both....
Acute dissecting aortic aneurysm
Aortic aneurysm

An aortic aneurysm is a general term for any swelling of the aorta, usually representing an underlying weakness in the wall of the aorta at that location....
Marfan syndrome
Marfan syndrome

Marfan syndrome is a genetic disorder of the connective tissue.It is sometimes inherited as a Autosomal dominant trait. It is carried by a gene called FBN1, which encodes a connective protein called fibrillin-1....
(chronic treatment with propranolol slows progression of aortic dilation and its complications)
Prevention of variceal bleeding in portal hypertension
Portal hypertension

In medicine, portal hypertension is hypertension in the portal vein and its tributaries.It is often defined as a portal pressure gradient of 5 mm Hg or greater....
Possible mitigation of hyperhidrosis
Hyperhidrosis

Hyperhidrosis is the condition characterized by abnormally increased perspiration, in excess of that required for regulation of body temperature....
Social anxiety disorder and other anxiety disorders

Congestive heart failure

Although beta blockers were once contraindicated in congestive heart failure

Congestive heart failure

Heart failure is a condition in which a problem with the structure or function of the heart impairs its ability to supply sufficient blood flow to meet the body's needs....
, as they have the potential to worsen the condition, studies in the late 1990s showed their positive effects on morbidity and mortality in congestive heart failure. Bisoprolol

Bisoprolol

Bisoprolol is a drug belonging to the group of beta blockers, a class of drugs used primarily in cardiovascular diseases. More specifically, it is a selective type ?1 adrenergic receptor blocker....
, carvedilol

Carvedilol

Metoprolol

Metoprolol is a selective beta blocker used in treatment of several diseases of thecardiovascular system, especially hypertension. It is marketed under the brand name Lopressor or Lopresor, respectively, by Novartis, and Toprol-XL ; Selokeen ; as Minax by Alphapharm , Metrol by Arrow Pharmaceuticals , as '...
are specifically indicated as adjuncts to standard ACE inhibitor

ACE inhibitor

ACE inhibitors, or inhibitors of angiotensin-converting enzyme, are a group of pharmaceuticals that are used primarily in treatment of hypertension and congestive heart failure, in some cases as the drugs of first choice....
and diuretic

Diuretic

A diuretic is any drug that elevates the rate of urination and thus provides a means of forced diuresis. There are several categories of diuretics....
therapy in congestive heart failure.

Beta blockers are primarily known for their reductive effect on heart rate, although this is not the only mechanism of action of importance in congestive heart failure

Congestive heart failure

Heart failure is a condition in which a problem with the structure or function of the heart impairs its ability to supply sufficient blood flow to meet the body's needs....
. Beta blockers, in addition to their sympatholytic B1 activity in the heart, influence the renin/angiotensin system at the kidneys. Beta blockers cause a decrease in renin secretion, which in turn reduce the heart oxygen demand by lowering extracellular volume and increasing the oxygen carrying capacity of blood. Beta blockers sympatholytic activity reduce heart rate, thereby increasing the ejection fraction of the heart despite an initial reduction in ejection fraction.

Trials have shown that beta blockers reduce the absolute risk of death by 4.5% over a 13 month period. As well as reducing the risk of mortality, the number of hospital visits and hospitalizations were also reduced in the trials.

Anxiety and performance enhancement

Some people, particularly musicians, use beta blockers to avoid stage fright

Stage fright

Stage fright or performance anxiety is the anxiety, fear, or persistent phobia which may be aroused in an individual by the requirement to performance in front of an audience, whether actually or potentially ....
and tremor during public performance and auditions. The physiological symptoms of the fight/flight response associated with performance anxiety

Stage fright

Panic

Panic is a sudden fear which dominates or replaces thinking and often affects groups of people or animals. Panics typically occur in disaster situations, or violent situations which may endanger the overall health of the affected group....
(pounding heart, cold/clammy hands, increased respiration, sweating, etc.) are significantly reduced, thus enabling anxious individuals to concentrate on the task at hand. Officially, beta blockers are not approved for anxiolytic

Anxiolytic

An anxiolytic is a Medication prescribed for the treatment of symptoms of anxiety. Some anxiolytics have been shown to be useful in the treatment of anxiety disorders as have antidepressants such as the class of selective serotonin reuptake inhibitors ....
use by the U.S. Food and Drug Administration

Food and Drug Administration

The U.S. Food and Drug Administration is an Government agency of the United States Department of Health and Human Services and is responsible for regulating and supervising the safety of foods, dietary supplements, Medications, vaccines, Biopharmaceutical, blood transfusion, medical devices, Electromagnetic radiation-emitting devices, veteri...
.

Since they lower heart rate and reduce tremor, beta blockers have been used by some Olympic

Olympic Games

The Olympic Games are an international multi-sport event established for both summer and winter sports. There have been two generations of the Olympic Games; the first were the Ancient Olympic Games held at Olympia, Greece, Greece....
marksmen

Marksman

A marksman is a person that is skilled in precision shooting, using projectile weapons, such as with a rifle but most commonly with a sniper rifle, to shoot at small long-range targets at a considerable distance away from the target....
to enhance performance, though beta blockers are banned by the International Olympic Committee

International Olympic Committee

The International Olympic Committee is an organization based in Lausanne, Switzerland, created by Pierre de Coubertin and Demetrios Vikelas on June 23, 1894....
(IOC). Although they have no recognisable benefit to most sports, it is acknowledged that they are beneficial to sports such as archery and shooting. A recent, high-profile transgression took place in the 2008 Beijing Olympic Games, where 50m Pistol silver medallist, and 10m Air-pistol bronze medallist Kim Jong-su tested positive for the Beta-blocker, propranolol

Propranolol

Adverse effects

Adverse drug reaction

An adverse drug reaction or adverse drug event is an expression that describes the unwanted, negative consequences associated with the use of given medications....
s (ADRs) associated with the use of beta blockers include: nausea

Nausea

Nausea is the sensation of unease and discomfort in the stomach with an urge to vomit....
, diarrhea

Diarrhea

In medicine, diarrhea, also spelled diarrhoea , is characterized by frequent loose or liquid bowel movements. The spelling of "diarrhea" is an appropriation of the Greek "diarrhoia" meaning "a flowing through." ....
, bronchospasm

Bronchospasm

Bronchospasm or "Bronchial Spasm" is a sudden constriction of the muscles in the walls of the bronchioles. It is caused by the release of substances from mast cells or basophils under the influence of anaphylatoxins....
, dyspnea

Dyspnea

Dyspnea or dyspnoea , from Latin language dyspnoea, from Greek language dyspnoia from dyspnoos, shortness of breath) or shortness of breath is perceived to be difficulty of breathing or painful breathing that a patient is aware of....
, cold extremities, exacerbation of Raynaud's syndrome, bradycardia

Bradycardia

Hypotension

In physiology and medicine, hypotension refers to an abnormally low blood pressure. This is best understood as a physiologic state, rather than a disease....
, heart failure, heart block

Heart block

A heart block is a disease in the electrical conduction system of the heart of the heart. This is opposed to coronary artery disease, which is disease of the blood vessels of the heart....
, fatigue, dizziness

Dizziness

Dizziness describes a number of subjective symptoms, which the patient may describe as feelings of lightheadedness, floating, wooziness, giddiness, confusion, disorientation or loss of balance....
, abnormal vision, decreased concentration, hallucinations, insomnia

Insomnia

Insomnia is a symptom of a sleep disorder characterized by persistent difficulty falling sleep or staying asleep despite the opportunity. Insomnia is a symptom, not a stand-alone diagnosis or a disease....
, nightmares, clinical depression

Clinical depression

Major depressive disorder is a mental disorder characterized by a pervasive depression , low self-esteem, and anhedonia in normally enjoyable activities....
, sexual dysfunction

Sexual dysfunction

Sexual dysfunction or sexual malfunction is difficulty during any stage of the sexual act that prevents the individual or couple from enjoying sexual activity....
, erectile dysfunction

Erectile dysfunction

Erectile dysfunction is a sexual dysfunction characterized by the inability to develop or maintain an erection of the penis sufficient for satisfactory sexual performance....
and/or alteration of glucose

Glucose

Glucose , a monosaccharide also known as grape sugar, blood sugar, or corn sugar, is a very important carbohydrate in biology....
and lipid

Lipid

Lipids are broadly defined as any fat-soluble , naturally-occurring molecule, such as fats, oils, waxes, cholesterol, sterols, fat-soluble vitamins , monoglycerides, diglycerides, phospholipids, and others....
metabolism

Metabolism

Metabolism is the set of chemical reactions that occur in living organisms in order to maintain life. These processes allow organisms to grow and reproduce, maintain their structures, and respond to their environments....
. Mixed a₁/ß-antagonist therapy is also commonly associated with orthostatic hypotension

Orthostatic hypotension

Orthostatic hypotension is a form of hypotension in which there is a sudden fall in blood pressure, typically greater than 20/10 mm Hg, that occurs when a person assumes a standing , usually after a prolonged period of rest....
. Carvedilol

Carvedilol

Edema

File:Oedema.jpgEdema or Oedema , formerly known as dropsy or hydropsy, is an abnormal accumulation of fluid beneath the skin, or in one or more cavities of the body....
.

Central nervous system

Central nervous system

The central nervous system is the part of the nervous system that functions to coordinate the activity of all parts of the bodies of multicellular organisms....
(CNS) adverse effects (hallucinations, insomnia, nightmares, depression) are more common in agents with greater lipid solubility, which are able to cross the blood-brain barrier

Blood-brain barrier

The blood-brain barrier is a metabolic or cellular structure in the central nervous system that restricts the passage of various chemical substances and microscopic objects between the bloodstream and the neural tissue itself, while still allowing the passage of substances essential to metabolism function ....
into the CNS. Similarly, CNS adverse effects are less common in agents with greater aqueous solubility (listed below).

Adverse effects associated with ß₂-adrenergic receptor antagonist activity (bronchospasm, peripheral vasoconstriction, alteration of glucose and lipid metabolism) are less common with ß₁-selective (often termed "cardioselective") agents, however receptor selectivity diminishes at higher doses. Beta blockade, especially of the beta-1 receptor at the macula densa inhibits renin release, thus decreasing the release of aldosterone

Aldosterone

Aldosterone is a hormone that increases the reabsorption of sodium and water and the release of potassium in the kidneys. This increases the volume of fluid in the body, and drives blood pressure up....
. This causes hyponatremia

Hyponatremia

Hyponatremia is an electrolyte disturbance in which the sodium concentration in the blood plasma is too low .Severe or rapidly progressing hyponatremia can result in swelling of the brain , and the symptoms of hyponatremia are mainly neurology....
and hyperkalemia

Hyperkalemia

Hyperkalemia Hyperkalaemia is an elevated blood level of the electrolyte potassium. The prefix hyper- means high . The middle kal refers to kalium, which is neo-Latin for potassium....
.

A 2007 study revealed that diuretics and beta-blockers used for hypertension increase a patient's risk of developing diabetes while ACE inhibitors and Angiotensin II receptor antagonist

Angiotensin II receptor antagonist

Angiotensin II receptor antagonists, also known as angiotensin receptor blockers , AT1-receptor antagonists or sartans, are a group of pharmaceuticals which modulate the renin-angiotensin-aldosterone system....
s (Angiotensin Receptor Blockers) actually decrease the risk of diabetes. Clinical guidelines in Great Britain, but not in the United States, call for avoiding diuretics and beta-blockers as first-line treatment of hypertension due to the risk of diabetes.

Beta blockers must not be used in the treatment of cocaine

Cocaine

Cocaine is a crystalline tropane alkaloid that is obtained from the leaves of the coca plant. The name comes from "coca" in addition to the alkaloid suffix -ine, forming cocaine....
, amphetamine

Amphetamine

Amphetamine and related drugs such as methamphetamine are a group of drugs that act by increasing levels of norepinephrine, serotonin, and dopamine in the brain....
, or other alpha adrenergic stimulant

Stimulant

Stimulant drugs are drugs that temporarily increase alertness and awareness. They usually have increased side-effects with increased effectiveness, and the more powerful variants are therefore often prescription medicines or illegal drugs....
overdose. The blockade of only beta receptors increases hypertension

Hypertension

Hypertension, also referred to as high blood pressure, HTN or HPN, is a medical condition in which the blood pressure is chronically elevated....
, reduces coronary blood flow, left ventricular function, and cardiac output

Cardiac output

Cardiac output is the volume of blood being pumped by the heart, in particular by a ventricle in a minute. This is measured in dm3 min-1 ....
and tissue perfusion by means of leaving the alpha adrenergic system stimulation unopposed. The appropriate antihypertensive

Antihypertensive

Antihypertensives are a class of medication that are used in medicine and pharmacology to treat hypertension . There are many classes of antihypertensives, which?by varying means?act by lowering blood pressure....
drugs to administer during hypertensive crisis resulting from stimulant abuse are vasodilators like nitroglycerin

Nitroglycerin

Nitroglycerin , also known as nitroglycerine, , trinitroglycerin, trinitroglycerine, 1,2,3-trinitroxypropane and glyceryl trinitrate, is a heavy, colorless, oily, explosive liquid obtained by nitration glycerol....
, diuretics like furosemide

Furosemide

Furosemide or frusemide is a loop diuretic used in the treatment of congestive heart failure and edema. It is most commonly marketed by Sanofi-Aventis under the brand name Lasix....
and alpha blockers like phentolamine

Phentolamine

Phentolamine is a reversible nonselective alpha-adrenergic Receptor antagonist. ...
.

Glucagon

Glucagon

Glucagon is an important hormone involved in carbohydrate metabolism. Produced by the pancreas, it is released when the glucose level in the blood is low , causing the liver to convert stored glycogen into glucose and release it into the bloodstream....
has been used in the treatment of overdose.

Examples of beta blockers

Non-selective agents

Alprenolol
Alprenolol

Alprenolol is a medication in the class of beta blockers, used in the treatment of angina pectoris.It is no longer marketed by AstraZeneca....
Carteolol
Carteolol

Carteolol is a beta blocker used to treat glaucoma.External links...
Levobunolol
Levobunolol

Levobunolol is a beta blocker. It is used topically to manage glaucoma.External links...
Mepindolol
Metipranolol
Metipranolol

Metipranolol hydrochloride is a non-selective beta blocker used in eye drops to treat glaucoma....
Nadolol
Nadolol

Nadolol is a non-selective beta-blocker used in the treatment of hypertension, Migraine, and angina pectoris....
Oxprenolol
Oxprenolol

Oxprenolol is a non-selective beta blocker with some intrinsic sympathomimetic amine activity. It is used for the treatment of angina pectoris and abnormal heart rhythms....
Penbutolol
Penbutolol

Penbutolol is a medication in the class of beta blockers, used in the treatment of hypertension.External links...
Pindolol
Pindolol

Pindolol is a beta blocker drug....
Propranolol
Propranolol

Propranolol is a non-selective beta blocker mainly used in the treatment of hypertension. It was the first successful beta blocker developed. It is the only drug proven effective for the prophylaxis of migraines in children....
Sotalol
Sotalol

Sotalol is a medication used in individuals with rhythm disturbances of the heart, and to treat hypertension in some individuals....
Timolol
Timolol

Timolol maleate is a non-selective beta blocker. In its oral form , it is used to treat hypertension and prevent myocardial infarctions, and occasionally to prevent migraine headaches....

ß₁-Selective agents

Acebutolol
Acebutolol

Acebutolol is a beta blocker for the treatment of hypertension and arrhythmias....
Atenolol
Atenolol

Atenolol is a beta-1 receptor selective antagonist, a drug belonging to the group of beta blocker, a class of drugs used primarily in cardiovascular diseases....
Betaxolol
Betaxolol

Betaxolol is a selective beta blocker used in the treatment of hypertension and glaucoma. Being selective for beta1 receptors, it typically has fewer systemic adverse drug reactions than non-selective beta-blockers, for example, not causing bronchospasm as timolol may....
Bisoprolol
Bisoprolol

Bisoprolol is a drug belonging to the group of beta blockers, a class of drugs used primarily in cardiovascular diseases. More specifically, it is a selective type ?1 adrenergic receptor blocker....
Esmolol
Esmolol

Esmolol is a cardioselective beta-blocker with rapid onset, a very short duration of action, and no significant intrinsic sympathomimetic or membrane stabilising activity at therapeutic dosages....
Metoprolol
Metoprolol

Metoprolol is a selective beta blocker used in treatment of several diseases of thecardiovascular system, especially hypertension. It is marketed under the brand name Lopressor or Lopresor, respectively, by Novartis, and Toprol-XL ; Selokeen ; as Minax by Alphapharm , Metrol by Arrow Pharmaceuticals , as '...
Nebivolol
Nebivolol

Nebivolol is a highly cardioselective beta blocker with nitric oxide-potentiating vasodilatory effect used in treatment of hypertension and, in Europe, also for left ventricular failure....
Amosulalol
Amosulalol

Amosulalol is a beta blocker....
Landiolol
Landiolol

Landiolol is a drug which acts as a highly cardioselective, ultra short-acting beta blocker. It is used as an anti-arrhythmic agent....
Tilisolol
Tilisolol

Tilisolol is a beta blocker....

Mixed a₁/ß-adrenergic antagonists

Arotinolol
Arotinolol

Arotinolol is a medication in the class of mixed alpha/beta blockers. ...
Carvedilol
Carvedilol

Carvedilol is a beta blocker indicated in the treatment of mild to moderate congestive heart failure . It is marketed under various trade names including Coreg , Dilatrend , Eucardic , and Carloc as a generic drug ., and as a controlled-release formulation, marketed in the US as Coreg CR ....
Celiprolol
Celiprolol

Celiprolol is a medication in the class of beta blockers, used in the treatment of hypertension.External links*...
Labetalol
Labetalol

Labetalol is a mixed alpha/beta antagonistic drug used to treat hypertension....

ß₂-Selective agents

Butaxamine
Butaxamine

Butaxamine is a Beta-2 adrenergic receptor beta blocker. It's primary use is in experimental situations which blockade of Beta-2 adrenergic receptor is necessary to determine the activity of the drug ....
(weak a-adrenergic agonist activity) - No common clinical utility, used in experimental situations.

Side Effects / Health Consequences

Low Blood Pressure
Slow Heart Rate
Impaired Circulation
Loss of Sleep
Heart Failure
Asthma
Nausea
Headaches
Dizziness
Muscle Cramps
Peyronie's disease
Peyronie's disease

Peyronie's disease is a connective tissue disorder involving the growth of fibrous plaques in the soft tissue of the penis affecting as many as 1-4% of men....

Comparative information

Pharmacological differences

Agents with intrinsic sympathomimetic action (ISA)

Acebutolol, carteolol, celiprolol, mepindolol, oxprenolol, pindolol

Agents with greater aqueous solubility

, celiprolol, nadolol, sotalol

Agents with membrane stabilising activity

Acebutolol, betaxolol, pindolol, propranolol

Agents with antioxidant
Antioxidant

An antioxidant is a molecule capable of slowing or preventing the Redox of other molecules. Oxidation is a chemical reaction that transfers electrons from a substance to an oxidizing agent....
effect

Carvedilol
Nebivolol

Indication differences

Agents specifically indicated for cardiac arrhythmia
Cardiac arrhythmia

Cardiac arrhythmia is a term for any of a large and heterogeneous group of conditions in which there is abnormal Electrical conduction system of the heart in the heart....

Esmolol
Esmolol

Esmolol is a cardioselective beta-blocker with rapid onset, a very short duration of action, and no significant intrinsic sympathomimetic or membrane stabilising activity at therapeutic dosages....
, sotalol
Sotalol

Sotalol is a medication used in individuals with rhythm disturbances of the heart, and to treat hypertension in some individuals....
, landiolol
Landiolol

Landiolol is a drug which acts as a highly cardioselective, ultra short-acting beta blocker. It is used as an anti-arrhythmic agent....

Agents specifically indicated for congestive heart failure
Congestive heart failure

Heart failure is a condition in which a problem with the structure or function of the heart impairs its ability to supply sufficient blood flow to meet the body's needs....

Bisoprolol
Bisoprolol

Bisoprolol is a drug belonging to the group of beta blockers, a class of drugs used primarily in cardiovascular diseases. More specifically, it is a selective type ?1 adrenergic receptor blocker....
, carvedilol
Carvedilol

Carvedilol is a beta blocker indicated in the treatment of mild to moderate congestive heart failure . It is marketed under various trade names including Coreg , Dilatrend , Eucardic , and Carloc as a generic drug ., and as a controlled-release formulation, marketed in the US as Coreg CR ....
, sustained-release metoprolol
Metoprolol

Metoprolol is a selective beta blocker used in treatment of several diseases of thecardiovascular system, especially hypertension. It is marketed under the brand name Lopressor or Lopresor, respectively, by Novartis, and Toprol-XL ; Selokeen ; as Minax by Alphapharm , Metrol by Arrow Pharmaceuticals , as '...
, nebivolol
Nebivolol

Nebivolol is a highly cardioselective beta blocker with nitric oxide-potentiating vasodilatory effect used in treatment of hypertension and, in Europe, also for left ventricular failure....

Agents specifically indicated for glaucoma
Glaucoma

Glaucoma is a group of diseases of the optic nerve involving loss of ganglion cell in a characteristic pattern of optic atrophy. Raised intraocular pressure is a significant risk factor for developing glaucoma ....

Betaxolol
Betaxolol

Betaxolol is a selective beta blocker used in the treatment of hypertension and glaucoma. Being selective for beta1 receptors, it typically has fewer systemic adverse drug reactions than non-selective beta-blockers, for example, not causing bronchospasm as timolol may....
, carteolol
Carteolol

Carteolol is a beta blocker used to treat glaucoma.External links...
, levobunolol
Levobunolol

Levobunolol is a beta blocker. It is used topically to manage glaucoma.External links...
, metipranolol
Metipranolol

Metipranolol hydrochloride is a non-selective beta blocker used in eye drops to treat glaucoma....
, timolol
Timolol

Timolol maleate is a non-selective beta blocker. In its oral form , it is used to treat hypertension and prevent myocardial infarctions, and occasionally to prevent migraine headaches....

Agents specifically indicated for myocardial infarction
Myocardial infarction

Myocardial infarction , commonly known as a heart attack, occurs when the Blood flow to part of the heart is interrupted. This is most commonly due to occlusion of a coronary artery following the rupture of a Vulnerable plaque, which is an unstable collection of lipids and white blood cells in the wall of an artery....

Atenolol
Atenolol

Atenolol is a beta-1 receptor selective antagonist, a drug belonging to the group of beta blocker, a class of drugs used primarily in cardiovascular diseases....
, metoprolol
Metoprolol

Metoprolol is a selective beta blocker used in treatment of several diseases of thecardiovascular system, especially hypertension. It is marketed under the brand name Lopressor or Lopresor, respectively, by Novartis, and Toprol-XL ; Selokeen ; as Minax by Alphapharm , Metrol by Arrow Pharmaceuticals , as '...
, propranolol
Propranolol

Propranolol is a non-selective beta blocker mainly used in the treatment of hypertension. It was the first successful beta blocker developed. It is the only drug proven effective for the prophylaxis of migraines in children....

Agents specifically indicated for migraine
Migraine

Migraine is a neurology syndrome characterized by altered bodily perceptions, headaches, and nausea. Physiologically, the migraine headache is a neurological condition more common to women than to men....
prophylaxis

Timolol
Timolol

Timolol maleate is a non-selective beta blocker. In its oral form , it is used to treat hypertension and prevent myocardial infarctions, and occasionally to prevent migraine headaches....
, propranolol
Propranolol

Propranolol is a non-selective beta blocker mainly used in the treatment of hypertension. It was the first successful beta blocker developed. It is the only drug proven effective for the prophylaxis of migraines in children....

Propranolol

Propranolol is a non-selective beta blocker mainly used in the treatment of hypertension. It was the first successful beta blocker developed. It is the only drug proven effective for the prophylaxis of migraines in children....
is the only agent indicated for control of tremor, portal hypertension

Portal hypertension

In medicine, portal hypertension is hypertension in the portal vein and its tributaries.It is often defined as a portal pressure gradient of 5 mm Hg or greater....
and esophageal variceal bleeding, and used in conjunction with a-blocker therapy in phaeochromocytoma.

Footnotes

External links

by Blair Tindall, New York Times, October 17, 2004. (Discusses the use of beta blockers among professional musicians)
by Blair Tindall. Condensed version of above article.
by Carl Elliott, The Atlantic, August 20, 2008. (Discusses the use of propranolol by a North Korean pistol shooter in the 2008 Olympics)

Beta blocker

Pharmacology

ß-Receptor antagonism

Intrinsic sympathomimetic activity

a1-Receptor antagonism

Other effects

Clinical use

Congestive heart failure

Anxiety and performance enhancement

Adverse effects

Examples of beta blockers

Non-selective agents

ß1-Selective agents

Mixed a1/ß-adrenergic antagonists

ß2-Selective agents

Side Effects / Health Consequences

Comparative information

Pharmacological differences

Indication differences

Footnotes

External links

a₁-Receptor antagonism

ß₁-Selective agents

Mixed a₁/ß-adrenergic antagonists

ß₂-Selective agents