Beta blockers

class of medications that are particularly used to manage cardiac arrhythmias, and to protect the heart from a second heart attack after a first heart attack

Propranolol is a medication of the beta blocker class. It is used to treat high blood pressure, some types of irregular heart rate, thyrotoxicosis, capillary hemangiomas, akathisia, performance anxiety, and essential tremors, as well as to prevent migraine headaches, and to prevent further heart problems in those with angina or previous heart attacks. It can be taken orally, rectally, or by intravenous injection. The formulation that is taken orally comes in short-acting and long-acting versions. Propranolol appears in the blood after 30 minutes and has a maximum effect between 60 and 90 minut

Metoprolol, sold under the brand names Lopressor and Toprol-XL among others, is a medication used to treat angina, high blood pressure and a number of conditions involving an abnormally fast heart rate. It is also used to prevent further heart problems after myocardial infarction and to prevent headaches in those with migraines. It is a beta blocker, specifically a selective β1 receptor blocker, and is taken by mouth or is given intravenously.

Bisoprolol, sold under the brand names Bisotab, Concor, Corbis and Zebeta among others, is a beta blocker which is selective for the beta-1 receptor and used for cardiovascular diseases, including tachyarrhythmias, high blood pressure, angina, and heart failure. It is taken by mouth.

Atenolol is a beta blocker medication primarily used to treat high blood pressure and heart-associated chest pain. Although used to treat high blood pressure, it does not seem to improve mortality in those with the condition. Other uses include the prevention of migraines and treatment of certain irregular heart beats. It is taken orally (by mouth) or by intravenous injection (injection into a vein). It can also be used with other blood pressure medications.

Carvedilol, sold under the brand name Coreg among others, is a beta blocker medication, that may be prescribed for the treatment of high blood pressure (hypertension) and chronic heart failure with reduced ejection fraction (also known as HFrEF or systolic heart failure). Beta-blockers as a collective medication class are not recommended as routine first-line treatment of high blood pressure for all patients, due to evidence demonstrating less effective cardiovascular protection and a less favourable safety profile when compared to other classes of blood pressure-lowering medications.

Timolol is a beta blocker medication used either by mouth or as eye drops. As eye drops it is used to treat increased pressure inside the eye such as in ocular hypertension and glaucoma. By mouth it is used for high blood pressure, chest pain due to insufficient blood flow to the heart, to prevent further complications after a heart attack, and to prevent migraines.

Sotalol, sold under the brand name Betapace among others, is a medication used to treat and prevent abnormal heart rhythms. Evidence does not support a decreased risk of death with long term use. It is taken by mouth or given by injection into a vein.

Nebivolol is a beta blocker used to treat high blood pressure and heart failure. As with other β-blockers, it is generally a less preferred treatment for high blood pressure. It may be used by itself or with other blood pressure medication. It is taken by mouth.

Labetalol is a medication used to treat high blood pressure and in long term management of angina. This includes essential hypertension, hypertensive emergencies, and hypertension of pregnancy. In essential hypertension it is generally less preferred than a number of other blood pressure medications. It can be given by mouth or by injection into a vein.

Pindolol, sold under the brand name Visken among others, is a non-selective beta blocker which is used in the treatment of hypertension. It is also an antagonist of the serotonin 5-HT1A receptor, preferentially blocking inhibitory 5-HT1A autoreceptors, and has been researched as an add-on therapy to various antidepressants, such as clomipramine and the selective serotonin reuptake inhibitors (SSRIs), in the treatment of depression and obsessive–compulsive disorder (OCD).

Betaxolol is a beta blocker used in the treatment of hypertension and angina.

Nadolol, sold under the brand name Corgard among others, is a medication used to treat high blood pressure, heart pain, atrial fibrillation, and some inherited arrhythmic syndromes. It has also been used to prevent migraine headaches and complications of cirrhosis. It is taken orally.

Esmolol, sold under the brand name Brevibloc, is a cardio selective beta1 receptor blocker with rapid onset, a very short duration of action, and no significant intrinsic sympathomimetic or membrane stabilising activity at therapeutic dosages.

Carteolol is a non-selective beta blocker used to treat glaucoma. It is administered in the form of eye drops.

Oxprenolol, sold under the brand name Trasicor among others, is a non-selective beta blocker with some intrinsic sympathomimetic activity. It is used for the treatment of angina pectoris, abnormal heart rhythms, and high blood pressure.

Alprenolol, or alfeprol, alpheprol, and alprenololum (Gubernal, Regletin, Yobir, Apllobal, Aptine, Aptol Duriles), is a non-selective beta blocker as well as a 5-HT1A and 5-HT1B receptor antagonist, used in the treatment of angina pectoris. It is no longer marketed by AstraZeneca, but may still be available from other pharmaceutical companies or generically.

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Penbutolol (brand names Levatol, Levatolol, Lobeta, Paginol, Hostabloc, Betapressin) is a medication in the class of beta blockers, used in the treatment of high blood pressure. Penbutolol is able to bind to both beta-1 adrenergic receptors and beta-2 adrenergic receptors (the two subtypes), thus making it a non-selective β blocker. Penbutolol is a sympathomimetic drug with properties allowing it to act as a partial agonist at β adrenergic receptors.

Talinolol is a beta blocker.

Bopindolol (), sold under the brand name Sandonorm among others, is a beta blocker used to treat hypertension. It has been marketed in a number of countries throughout the world, for instance in Europe.

Levobunolol (trade names AKBeta, Betagan, Vistagan, among others) is a non-selective beta blocker. It is used topically in the form of eye drops to manage ocular hypertension (high pressure in the eye) and open-angle glaucoma.

Bevantolol (INN) was a drug candidate for angina and hypertension that acted as both a beta blocker and a calcium channel blocker. It was discovered and developed by Warner-Lambert but in January 1989 the company announced that it had withdrawn the New Drug Application; the company's chairman said: "Who needs the 30th beta blocker?" it wasn't marketed in the US, UK, or Europe and the authors of a Cochrane review could find no product monograph for it.

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.

Urapidil is a sympatholytic antihypertensive drug. It acts as an α1-adrenoceptor antagonist and as an 5-HT1A receptor agonist. Although an initial report suggested that urapidil was also an α2-adrenoceptor agonist, this was not substantiated in later studies that demonstrated it was devoid of agonist actions in the dog saphenous vein and the guinea-pig ileum. Unlike some other α1-adrenoceptor antagonists, urapidil does not elicit reflex tachycardia, and this may be related to its weak β1-adrenoceptor antagonist activity, as well as its effect on cardiac vagal drive. Urapidil is currently not a

Practolol (Eraldin, Dalzic, Praktol, Cardiol, Pralon, Cordialina, Eraldina, Teranol) is a beta blocker selective for the β1-adrenergic receptor that has been used in the emergency treatment of cardiac arrhythmias. Practolol is no longer used as it is highly toxic despite the similarity of its chemical formula to propranolol.

Mepindolol (Betagon) is a non-selective beta blocker. It is used to treat glaucoma. ==Synthesis== upright=2 The first reported synthesis of mepindolol in 1971 used 4-hydroxy-2-methylindole {9) with epichlorohydrin and then isopropylamine to add the sidechain which was known to produce beta blockers, by analogy with drugs discovered by Imperial Chemical Industries, such as propanolol. The requisite intermediate was synthesized in a multi-step procedure from 4-benzyloxyindole-2-carboxylic acid (1) which was converted into (9) by conventional chemistry.

Epanolol is a beta blocker. developed by Imperial Chemical Industries. ==Synthesis== upright=2 The ester methyl 4-benzyloxyphenylacetate (1) is treated with ethylenediamine to give the amide (3). Separately, 2-cyanophenol (4) is reacted with epichlorohydrin and sodium hydroxide to produce the benzonitrile derivative (5). Combination of (3) and (5) by heating in propanol gives (6). Lastly, catalytic hydrogenation removes the benzyl protecting group and yields epanolol.

Bupranolol is a non-selective beta blocker without intrinsic sympathomimetic activity (ISA), but with strong membrane stabilizing activity. Its potency is similar to propranolol.

Tertatolol (Artex, Artexal, Prenalex) is a medication in the class of beta blockers, used in the treatment of high blood pressure. It was discovered by the French pharmaceutical company Servier and is marketed in Europe.

Butaxamine (INN; also known as butoxamine) is a β2-selective beta blocker. Its primary use is in experimental situations in which blockade of β2 receptors is necessary to determine the activity of the drug (i.e. if the β2 receptor is completely blocked, but the given effect is still present, the given effect is not a characteristic of the β2 receptor). It has no clinical use. An alternative name is α-(1-[tert-butylamino]ethyl)-2,5-dimethoxybenzyl alcohol.

Dichloroisoprenaline (DCI), also known as dichloroisoproterenol, was the first beta blocker ever to be developed. It is non-selective for the β1-adrenergic and β2-adrenergic receptors. DCI has low potency and acts as a partial agonist/antagonist at these receptors.

Landiolol, sold under the brand names Onoact, Rapibloc®, Sibboran® and Rapiblyk® among others, is a medication used for the treatment of supraventricular tachycardia, atrial fibrillation, and atrial flutter in perioperative, postoperative or other circumstances where short-term control of the ventricular rate with a short-acting agent is desirable. With the exception of the USA, landiolol is also indicated for non-compensatory sinus tachycardia where, in the physician's judgment, the rapid heart rate requires specific intervention. It is a β-adrenergic blocker; an ultra short-acting, β1-super-

Cloranolol (Tobanum) is a beta blocker. ==Synthesis== β-Adrenergic blocker. Prepn: == References ==

Metipranolol (OptiPranolol, Betanol, Disorat, Trimepranol) is a non-selective beta blocker used in eye drops to treat glaucoma. It is rapidly metabolized into desacetylmetipranolol.

Amosulalol (INN) is an antihypertensive drug. It has much higher affinity for α1-adrenergic receptors than for β-adrenergic receptors. It is not approved for use in the United States. ==Synthesis== upright=2|class=skin-invert-image

Iodocyanopindolol (), also known as ICYP, is a synthetic compound derived from pindolol, primarily used as a radioligand in pharmacological research. It functions as a non-selective β-adrenoceptor antagonist and a serotonin 5-HT1A and 5-HT1B receptor antagonist. Its 125I-radiolabelled derivative, [125I]-iodocyanopindolol ([125I]-ICYP), is widely employed to map the distribution and density of β-adrenoceptors and serotonin receptors in tissues, particularly in the brain, heart, and other organs. Iodocyanopindolol is not used clinically but remains a critical tool in studying receptor pharmacolo

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.

Cyanopindolol is a drug related to pindolol which acts as both a β1 adrenoceptor antagonist and a 5-HT1A receptor antagonist. Its radiolabelled derivative iodocyanopindolol has been widely used in mapping the distribution of beta adrenoreceptors in the body.

Arotinolol (INN, marketed under the tradename Almarl) is a medication in the class of mixed alpha/beta blockers. It also acts as a β3 receptor agonist. A 1979 publication suggests arotinolol as having first been described in the scientific literature by Sumitomo Chemical as "β-adrenergic blocking, antiarrhythmic compound S-596".

Bucindolol is a non-selective beta blocker with additional weak alpha-blocking properties and intrinsic sympathomimetic activity in some model systems but not in human hearts. It was under review by the FDA in the United States for the treatment of heart failure in 2009, but was rejected due to issues pertaining to integrity of data submitted.

Isamoltane (developmental code name CGP-361A) is a beta blocker (β-adrenergic receptor antagonist) with additional serotonin 5-HT1A and 5-HT1B receptor antagonist activity. It has about 5-fold higher affinity for the serotonin 5-HT1B receptor (Ki = 21nM) over the serotonin 5-HT1A receptor (Ki = 112nM). It has anxiolytic effects in rodents. The drug was under development by Novartis and AstraZeneca for the treatment of anxiety disorders in the 1990s but was never marketed.

Carazolol is a high affinity inverse agonist (also referred to as a beta blocker) of the β-adrenergic receptor.

Befunolol (INN) is a beta blocker with intrinsic sympathomimetic activity used in the management of open-angle glaucoma. It also acts as a β adrenoreceptor partial agonist. Befunolol was introduced in Japan in 1983 by Kakenyaku Kako Co. under the trade name Bentos.

Xipranolol is a beta blocker.

Tazolol is a beta blocker with some utility in the treatment of heart disease.

Adaprolol is a beta blocker.

Tilisolol (INN, trade name Selecal) is a beta blocker.

ICI-118,551 is a selective β2 adrenergic receptor (adrenoreceptor) antagonist or beta blocker. ICI binds to the ��2 subtype with at least 100 times greater affinity than β1 or β3, the two other known subtypes of the beta adrenoceptor. The compound was developed by Imperial Chemical Industries, which was acquired by AkzoNobel in 2008.

Alfurolol is a beta blocker.

Ancarolol is a beta blocker.

Flusoxolol is a selective beta-1 receptor blocker.

Hydroxytertatolol is a beta blocker. It is a derivative of tertatolol.

chemical compound

Xibenolol is a beta blocker.

Butofilolol (trade name Cafide) is a beta-blocker drug for the treatment of essential hypertension (high blood pressure). It is not known to be marketed anywhere.

Arnolol is a beta blocker.

Bufuralol is a potent beta-adrenoceptor antagonist with partial agonist activity. It is metabolized by CYP2D6.

Indenolol is a beta-adrenergic blocker for the treatment of hypertension (high blood pressure). It was investigated in the 1980s, but is not known to be marketed . It is a derivative of a phenolic 4-indenol. ==References==