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Trade namesZebeta, Concor, Selecta, others
  • (RS)-1-{4-[(2-Isopropoxyethoxy)methyl]phenoxy}-
Clinical data
Drug classBeta blocker[1]
Main usesHigh blood pressure, angina, heart failure[1][2]
Side effectsHeadache, feeling tired, diarrhea, swelling in the legs[1]
  • AU: C
  • US: C (Risk not ruled out)
Routes of
By mouth
Defined daily dose10 mg[3]
External links
License data
Legal status
  • In general: ℞ (Prescription only)
Protein binding30%[4]
Metabolism50% liver, CYP2D6, CYP3A4[5]
Elimination half-life10–12 hours[6]
Chemical and physical data
Molar mass325.449 g·mol−1
3D model (JSmol)
ChiralityRacemic 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 checkY

Bisoprolol, marketed under the tradename Zebeta among others, is a medication of the beta blocker type most commonly used for heart diseases.[1] This specifically includes high blood pressure, chest pain from not enough blood flow to the heart, and heart failure.[1][2] It is taken by mouth.[1]

Common side effects include headache, feeling tired, diarrhea, and swelling in the legs.[1] More severe side effects include worsening asthma, blocking the ability to recognize low blood sugar, and worsening heart failure.[7] There are concerns that use during pregnancy may be harmful to the baby.[8] Bisoprolol is in the beta blocker family of medications, specifically the β1 selective type.[1]

Bisoprolol was patented in 1976 and approved for medical use in 1986.[9] It is on the World Health Organization's List of Essential Medicines.[10] Bisoprolol is available as a generic medication.[1] The wholesale cost in the developing world is about US$3–5 per month.[11] In the UK it costs the NHS just less than £1 per month as of 2020.[12] In the United States, as of 2015, it costs about $25–50 a month.[13] In 2017, it was the 268th most commonly prescribed medication in the United States, with more than one million prescriptions.[14][15]

Medical uses

Zebeta 5-mg oral tablet

Bisoprolol is beneficial in treatment for high blood pressure (hypertension), reduced blood flow to the heart (cardiac ischemia); congestive heart failure, and preventive treatment before and primary treatment after heart attacks, decreasing the chances of recurrence.[16] Bisoprolol targets hypertension (elevated blood pressure).[17][18] In cardiac ischemia, the drug is used to reduce the activity of the heart muscle, so reduces oxygen and nutrient demand, and reduced blood supply can still transport sufficient amounts of oxygen and nutrients.[19][20][21]


The dose in adults generally ranges from 1.25 mg per day to 10 mg per day.[1] Doses should be started low in heart failure while in high blood pressure and angina they may be started at 5 to 10 mg per day.[22] The maximum recommended dose is 20 mg per day.[22]

The defined daily dose of bisoprolol is 10 mg.[23]

Side effects

Poor tolerance by elderly individuals with heart failure Top: Chest radiograph showed cardiomegaly and electrocardiogram revealed atrial fibrillation Bottom: after discontinuation, the CTR reduced to 57%, and sinus rhythm

Overdose of bisoprolol leads to fatigue, hypotension,[20] low blood sugar,[24][25] bronchospasms, and bradycardia.[20] Bronchospasms and low blood sugar because at high doses drug can be an antagonist for β2 adrenergic receptors located in lung and in liver. Bronchospasm is due to blockage in lungs of β2 receptor and low blood sugar because of decreased stimulation of glycogenolysis and gluconeogenesis in the liver via β2 receptor.[19][20][26]


Beta-blockers should generally be avoided in people with a history of asthma or bronchospasm as they may make the disease worse.[7] A beta 1 selective beta blocker like bisoprolol may be tried in those in whom other options are not available.[7]


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.[19] Normally, adrenaline and noradrenaline stimulation of the β1 adrenoreceptor activates a signalling cascade (Gs protein and cAMP) which ultimately leads to increased contractility and increased heart rate of the heart muscle and heart pacemaker, respectively.[27] 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.[24][25][28]


Selectivity of various β-blockers

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.[24][28] Bisoprolol minimizes the side effects that might occur from administration of a nonspecific beta blocker where blockage of the other adrenoreceptors (β2, β3, α1, α2) occurs. The other receptors elicit a variety of responses in the body, and their blockage could cause a wide range of reactions, but β1 adrenoreceptors are cardiospecific for the most part, making bisoprolol ideal for treatment of cardiac events.[24][25][28]

Bisoprolol has a higher degree of β1-selectivity compared to other β1-selective beta blockers such as atenolol, metoprolol, and betaxolol.[28][29][30][31][32][33][34][35][36][37] However nebivolol is approximately 3.5 times more β1-selective.[38][39]

Renin-angiotensin system

Bisoprolol inhibits renin secretion by about 65% and tachycardia by about 30%.[29]


Bisoprolol has both lipid- and water-soluble properties.[24][28] It has an approximate half-life of 10–12 hours, and when ingested has high bioavailability (approx. 90%).[24][25] When being eliminated, the body evenly distributes it (50–50) between kidney excretion and liver biotransformation (then excreted).[24][25][28]

Society and culture

Bisoprolol is available as a generic medication.[40]


The wholesale cost in the developing world is about US$2.98–4.94 per month.[11] In the United States, as of 2015, it costs about $25–50 a month.[13] In 2017, it was the 268th most commonly prescribed medication in the United States, with more than one million prescriptions.[14][15]


Bisoprolol was patented in 1976 and approved for medical use in 1986.[9] It was approved for medical use in the United States in 1992.[1]


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External links

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