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 2022, it was the 249th 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 are 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 a 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 is 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]

Society and culture

Brand names

In India, it is sold under the brand name Bisotab. [52]

Related Research Articles

<span class="mw-page-title-main">Beta blocker</span> Medications for 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 people.

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

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 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) antagonists and alpha-2 (α2) agonists, which are used to treat high blood pressure and asthma, for example.

<span class="mw-page-title-main">Atenolol</span> Beta blocker medication

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 or by intravenous injection. It can also be used with other blood pressure medications.

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

Isoprenaline, also known as isoproterenol and sold under the brand name Isuprel among others, is a sympathomimetic medication which is used in the treatment of acute bradycardia, heart block, and rarely for asthma, among other indications. It is used by injection into a vein, muscle, fat, or the heart, by inhalation, and in the past under the tongue or into the rectum.

<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 beta blocker medication, that may be prescribed for the treatment of high blood pressure (hypertension) and chronic heart failure with reduced ejection fraction. 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.

<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

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

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.

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

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

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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.

Autonomic drugs are substances that 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 an disorders, including glaucoma, asthma, and disorders of the urinary, gastrointestinal and circulatory systems.

References

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  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.
  41. ↑ Schliep HJ, Schulze E, Harting J, Haeusler G (April 1986). "Antagonistic effects of bisoprolol on several beta-adrenoceptor-mediated actions in anaesthetized cats". European Journal of Pharmacology. 123 (2): 253–261. doi:10.1016/0014-2999(86)90666-7. PMID   3011461.
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