Bisoprolol

Last updated
Bisoprolol
Bisoprolol.svg
Bisoprolol ball-and-stick.png
Clinical data
Trade names Zebeta, Monocor, others
AHFS/Drugs.com Monograph
MedlinePlus a693024
Pregnancy
category
  • AU:C
Routes of
administration 		By mouth
ATC code
Legal status
Legal status
Pharmacokinetic data
Bioavailability >90%
Protein binding 30% [4]
Metabolism 50% liver, CYP2D6, CYP3A4 [5]
Elimination half-life 10–12 hours [6]
Excretion Kidney, fecal (<2%)
Identifiers
  • (RS)-1-{4-[(2-Isopropoxyethoxy)methyl]phenoxy}-
    3-(isopropylamino)propan-2-ol
CAS Number
PubChem CID
IUPHAR/BPS
DrugBank
ChemSpider
UNII
KEGG
ChEBI
ChEMBL
CompTox Dashboard (EPA)
ECHA InfoCard 100.108.941 OOjs UI icon edit-ltr-progressive.svg
Chemical and physical data
Formula C18H31NO4
Molar mass 325.449 g·mol−1
3D model (JSmol)
Chirality Racemic mixture
  • O(c1ccc(cc1)COCCOC(C)C)CC(O)CNC(C)C
  • InChI=1S/C18H31NO4/c1-14(2)19-11-17(20)13-23-18-7-5-16(6-8-18)12-21-9-10-22-15(3)4/h5-8,14-15,17,19-20H,9-13H2,1-4H3 Yes check.svgY
  • Key:VHYCDWMUTMEGQY-UHFFFAOYSA-N Yes check.svgY
   (verify)

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]

Contents

Common side effects include headache, feeling tired, diarrhea, and swelling in the legs. [7] More severe side effects include worsening asthma, blocking the ability to recognize low blood sugar, and worsening heart failure. [9] There are concerns that use during pregnancy may be harmful to the baby. [10]

Bisoprolol was patented in 1976 and approved for medical use in 1986. [11] It was approved for medical use in the United States in 1992. [7]

Bisoprolol is on the World Health Organization's List of Essential Medicines [12] and is available as a generic medication. [7] [13] In 2020, it was the 267th most commonly prescribed medication in the United States, with more than 1 million prescriptions. [14] [15]

Medical uses

Zebeta 5-mg oral tablet 000859lg Zebeta 5 MG Oral Tablet.jpg
Zebeta 5-mg oral tablet

Bisoprolol is used for prevention of cardiovascular events following a heart attack in patients with risk factors for disease progression, [16] in the management of congestive heart failure with reduced ejection fraction, [17] and as a second-line agent for hypertension. [18]

Bisoprolol may be beneficial in the treatment of high blood pressure, but it is not recommended as a first-line antihypertensive agent. It can be an adjunct to first-line antihypertensive agents in patients with accompanying comorbidities, for example, congestive heart failure, where selected beta blockers can be added in patients who remain mildly to moderately symptomatic despite appropriate doses of an angiotensin-converting-enzyme inhibitor. [19]

In cardiac ischemia, the drug is used to reduce the activity of the heart muscle, thereby reducing its oxygen and nutrient demands and allowing its reduced blood supply to still transport sufficient amounts of oxygen and nutrients to meet its needs. [20] [21] [22]

Side effects

An overdose of bisoprolol can lead to fatigue, hypotension, [21] hypoglycemia, [23] [24] bronchospasms, and bradycardia. [21] Bronchospasms and hypoglycemia occur because at high doses, the drug can be an antagonist for β2 adrenergic receptors located in the lungs and liver. Bronchospasm occurs due to the blockage of β2 receptors in the lungs. Hypoglycemia occurs due to decreased stimulation of glycogenolysis and gluconeogenesis in the liver via β2 receptors. [20] [21] [25]

There have been no reported cases of clinically evident drug-induced liver injury associated with bisoprolol. [26]

Cautions

Non-selective beta-blockers should be avoided in people with asthma or bronchospasm as they may cause exacerbations and worsening of symptoms. [27] [28] [29] β1 selective beta-blockers like bisoprolol have not been shown to cause an increase in asthma exacerbations, [28] and may be cautiously tried in those with controlled, mild-to-moderate asthma with cardiac comorbidities.

A 2014 meta-analysis found that unlike non-selective beta-blockers, β1 selective beta-blockers (bisoprolol) showed only a small impact on lung function, with patients remaining responsive to salbutamol (β2 -agonist) rescue therapy and endorses the use of bisoprolol in select patients with controlled asthma. [27] [30] This was supported by a 2020 clinical trial where bisoprolol had no significant impact on bronchodilation post salbutamol administration. [31]

Pharmacology

Mechanism of action

Bisoprolol is cardioprotective because it selectively and competitively blocks catecholamine (adrenaline) stimulation of β1 adrenergic receptors (adrenoreceptors), which are mainly found in the heart muscle cells and heart conduction tissue (cardiospecific), but also found in juxtaglomerular cells in the kidney. [20] Normally, adrenaline and noradrenaline stimulation of the β1 adrenoreceptor activates a signalling cascade (Gs protein and cAMP) which ultimately leads to increased myocardial contractility and increased heart rate of the heart muscle and heart pacemaker, respectively. [32] Bisoprolol competitively blocks the activation of this cascade, so decreases the adrenergic tone/stimulation of the heart muscle and pacemaker cells. Decreased adrenergic tone shows less contractility of heart muscle and lowered heart rate of pacemakers. [23] [24] [33]

β1-selectivity

Bisoprolol β1-selectivity is especially important in comparison to other nonselective beta blockers. The effects of the drug are limited to areas containing β1 adrenoreceptors, which is mainly the heart and part of the kidney. [23] [33] Bisoprolol, whilst β1 adrenoceptor selective can help patients to avoid certain side-effects associated with non-selective beta-blocker activity [6] at additional adrenoceptors (α1 and β2), it does not signify its superiority in treating beta-blocker indicated cardiac conditions such as heart failure but could prove beneficial to patients with specific comorbidities. [34] [35]

Bisoprolol has a higher degree of β1-selectivity compared to atenolol, metoprolol and betaxolol. [36] With a selectivity ranging from being 11 to 15 times more selective for β1 over β2. [33] [37] [38] [39] [40] [41] [42] [43] [44] [45] However, nebivolol is approximately 3.5 times more β1-selective. [46] [47]

Renin-angiotensin system

Bisoprolol inhibits renin secretion by about 65% and tachycardia by about 30%. [37]

Pharmacokinetics

After ingestion, bisoprolol is absorbed and has a high bioavailability of approximately 90% with plasma half-life of 10-12 hours. [23] [24] Typically, half the circulating bisoprolol is metabolized by the liver, the rest passing unchanged through the kidneys before elimination; less than 2% may be excreted in the feces. [23] [24] [33]

Bisoprolol soluble in both lipids and water. [23] [33] It is classified as a beta blocker with moderate lipophilicity and hence intermediate potential for crossing the blood–brain barrier. [48] This in turn may result in fewer effects in the central nervous system as well as a lower risk of neuropsychiatric side effects than highly lipophilic beta blockers like propranolol but greater such effects than beta blockers with low lipophilicity like atenolol. [48]

The plasma protein binding of bisoprolol is approximately 35%, the volume of distribution is 3.5 L/kg and the total clearance is approximately 15 L/h. Bisoprolol is eliminated from the body in two ways - 50% of the substance is converted in the liver to inactive metabolites, which are then excreted in the kidneys. The remaining 50% is eliminated unchanged via the kidneys. [49] Since elimination is equal in liver and kidney, no dose adjustment is required in patients with hepatic or renal impairment.

The pharmacokinetics of bisoprolol are linear and independent of age. [6]

In patients with chronic heart failure, the plasma level of bisoprolol is higher and the half-life is longer than in healthy subjects when compared across studies. There is a lack of evidence directly comparing bisoprolol pharmacokinetics between healthy subjects and chronic heart failure subjects. [50] [51] through

Society and culture

Brand names

In India, it is sold under the brand name Bisotab. [52] In Italy, it is sold under the brand name Congescor.[ citation needed ] In Germany and parts of Europe, bisoprolol is sold under the brand name Bisoprolol-ratiopharm by Ratiopharm (Teva) and Concor COR.[ citation needed ]

Related Research Articles

<span class="mw-page-title-main">Beta blocker</span> Class of medications used to manage abnormal heart rhythms

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. They are also widely used to treat high blood pressure, although they are no longer the first choice for initial treatment of most patients.

<span class="mw-page-title-main">Propranolol</span> Beta blocker drug

Propranolol, sold under the brand name Inderal among others, is a medication of the beta blocker class. It is used to treat high blood pressure, a number of types of irregular heart rate, thyrotoxicosis, capillary hemangiomas, performance anxiety, and essential tremors, as well to prevent migraine headaches, and to prevent further heart problems in those with angina or previous heart attacks. It can be taken orally 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 minutes when taken orally.

<span class="mw-page-title-main">Adrenergic receptor</span> Class of G protein-coupled receptors

The adrenergic receptors or adrenoceptors are a class of G protein-coupled receptors that are targets of many catecholamines like norepinephrine (noradrenaline) and epinephrine (adrenaline) produced by the body, but also many medications like beta blockers, beta-2 (β2) agonists and alpha-2 (α2) agonists, which are used to treat high blood pressure and asthma, for example.

<span class="mw-page-title-main">Isoprenaline</span> Medication for slow heart rate

Isoprenaline, or isoproterenol, is a medication used for the treatment of bradycardia, heart block, and rarely for asthma. It is a non-selective β adrenoceptor agonist that is the isopropylamine analog of epinephrine (adrenaline).

<span class="mw-page-title-main">Moxonidine</span> Antihypertensive medication

Moxonidine (INN) is a new-generation alpha-2/imidazoline receptor agonist antihypertensive drug licensed for the treatment of mild to moderate essential hypertension. It may have a role when thiazides, beta-blockers, ACE inhibitors, and calcium channel blockers are not appropriate or have failed to control blood pressure. In addition, it demonstrates favourable effects on parameters of the insulin resistance syndrome, apparently independent of blood pressure reduction. It is also a growth hormone releaser. It is manufactured by Solvay Pharmaceuticals under the brand name Physiotens and Moxon.

<span class="mw-page-title-main">Labetalol</span> Medication used to treat high blood pressure

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.

<span class="mw-page-title-main">Carvedilol</span> Blood pressure medication

Carvedilol, sold under the brand name Coreg among others, is a medication used to treat high blood pressure, congestive heart failure (CHF), and left ventricular dysfunction in people who are otherwise stable. For high blood pressure, it is generally a second-line treatment. It is taken by mouth.

<span class="mw-page-title-main">Penbutolol</span> Chemical compound

Penbutolol 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, 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.

<span class="mw-page-title-main">Beta-1 adrenergic receptor</span> Protein-coding gene in the species Homo sapiens

The beta-1 adrenergic receptor, also known as ADRB1, can refer to either the protein-encoding gene 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.

<span class="mw-page-title-main">Nebivolol</span> Chemical compound

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.

<span class="mw-page-title-main">Adrenergic antagonist</span>

An adrenergic antagonist is a drug that inhibits the function of adrenergic receptors. There are five adrenergic receptors, which are divided into two groups. The first group of receptors are the beta (β) adrenergic receptors. There are β1, β2, and β3 receptors. The second group contains the alpha (α) adrenoreceptors. There are only α1 and α2 receptors. Adrenergic receptors are located near the heart, kidneys, lungs, and gastrointestinal tract. There are also α-adreno receptors that are located on vascular smooth muscle.

<span class="mw-page-title-main">Beta-adrenergic agonist</span> Medications that relax muscles of the airways

Beta adrenergic agonists or beta agonists are medications that relax muscles of the airways, causing widening of the airways and resulting in easier breathing. They are a class of sympathomimetic agents, each acting upon the beta adrenoceptors. In general, pure beta-adrenergic agonists have the opposite function of beta blockers: beta-adrenoreceptor agonist ligands mimic the actions of both epinephrine- and norepinephrine- signaling, in the heart and lungs, and in smooth muscle tissue; epinephrine expresses the higher affinity. The activation of β1, β2 and β3 activates the enzyme, adenylate cyclase. This, in turn, leads to the activation of the secondary messenger cyclic adenosine monophosphate (cAMP); cAMP then activates protein kinase A (PKA) which phosphorylates target proteins, ultimately inducing smooth muscle relaxation and contraction of the cardiac tissue.

<span class="mw-page-title-main">Landiolol</span> Chemical compound

Landiolol (INN) is an ultra short-acting, β1-superselective intravenous adrenergic antagonist, which decreases the heart rate effectively with less negative effect on blood pressure or myocardial contractility. In comparison to other beta blockers, landiolol has the shortest elimination half-life, ultra-rapid onset of effect, and predictable effectiveness with inactive metabolites. The pure S-enantiomer structure of landiolol is believed to develop less hypotensive side effects in comparison to other β-blockers. This has a positive impact on the treatment of patients when reduction of heart rate without decrease in arterial blood pressure is desired. Landiolol was developed by modifying the chemical structure of esmolol to produce a compound with a higher rate of cardioselectivity and a greater potency without increasing its duration of action. It is sold as landiolol hydrochloride. Based on its positive benefit risk profile, landiolol has been granted the marketing authorization and introduced to the European markets under the brand names Rapibloc, Raploc, Runrapiq, Landibloc mid 2016. Landiolol is available in Japan under the brand names Onoact (50 mg) and Corbeta.

<span class="mw-page-title-main">ICI-118,551</span> Chemical compound

ICI-118,551 is a selective β2 adrenergic receptor (adrenoreceptor) antagonist or beta blocker. ICI binds to the β2 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.

<span class="mw-page-title-main">Olodaterol</span> Chemical compound

Olodaterol is an ultra-long-acting β adrenoreceptor agonist (ultra-LABA) used as an inhalation for treating people with chronic obstructive pulmonary disease (COPD). It is manufactured by Boehringer Ingelheim.

<span class="mw-page-title-main">Discovery and development of beta-blockers</span>

β adrenergic receptor antagonists 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. In the 1950s, dichloroisoproterenol (DCI) was discovered to be a β-antagonist that blocked the effects of sympathomimetic amines on bronchodilation, uterine relaxation and heart stimulation. Although DCI had no clinical utility, a change in the compound did provide a clinical candidate, pronethalol, which was introduced in 1962.

β2-adrenoceptor agonists are a group of drugs that act selectively on β2-receptors in the lungs causing bronchodilation. β2-agonists are used to treat asthma and COPD, diseases that cause obstruction in the airways. 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. The structure of the binding site and the nature of the binding is also well known, as is the structure activity relationship.

A Beta-2 adrenergic antagonist is an adrenergic antagonist which blocks the beta-2 adrenergic receptors of cells, with either high specificity like Butaxamine and ICI-118,551, or non-specifically like the non-selective betablocker Propranolol.

The β3 adrenergic receptor agonist or β3-adrenoceptor agonist, also known as β3-AR agonist, are a class of medicine that bind selectively to β3-adrenergic receptors.

Autonomic drugs can either inhibit or enhance the functions of the parasympathetic and sympathetic nervous systems. This type of drug can be used to treat a wide range of diseases, such as glaucoma, asthma, urinary, gastrointestinal and cardiopulmonary disorders.

References

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  36. ↑ Muresan L, Cismaru G, Muresan C, Rosu R, Gusetu G, Puiu M, et al. (September 2022). "Beta-blockers for the treatment of arrhythmias: Bisoprolol - a systematic review" (PDF). Annales Pharmaceutiques Françaises. 80 (5): 617–634. doi:10.1016/j.pharma.2022.01.007. PMID   35093388. S2CID   246428722. Archived (PDF) from the original on 2024-04-19. Retrieved 2023-10-26.
  37. 1 2 Harting J, Becker KH, Bergmann R, Bourgois R, Enenkel HJ, Fuchs A, et al. (February 1986). "Pharmacodynamic profile of the selective beta 1-adrenoceptor antagonist bisoprolol". Arzneimittel-Forschung. 36 (2): 200–208. PMID   2870720.
  38. ↑ Kaumann AJ, Lemoine H (October 1985). "Direct labelling of myocardial beta 1-adrenoceptors. Comparison of binding affinity of 3H-(-)-bisoprolol with its blocking potency". Naunyn-Schmiedeberg's Archives of Pharmacology. 331 (1): 27–39. doi:10.1007/bf00498849. PMID   2866449. S2CID   22328991.
  39. ↑ Klockow M, Greiner HE, Haase A, Schmitges CJ, Seyfried C (February 1986). "Studies on the receptor profile of bisoprolol". Arzneimittel-Forschung. 36 (2): 197–200. PMID   2870719.
  40. ↑ Manalan AS, Besch HR, Watanabe AM (August 1981). "Characterization of [3H](+/-)carazolol binding to beta-adrenergic receptors. Application to study of beta-adrenergic receptor subtypes in canine ventricular myocardium and lung". Circulation Research. 49 (2): 326–336. doi: 10.1161/01.res.49.2.326 . PMID   6113900.
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