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Clinical data
Trade namesZebeta, Concor, Selecta, others
License data
  • AU: C
Routes of
by mouth
ATC code
Legal status
Legal status
  • In general: ℞ (Prescription only)
Pharmacokinetic data
Protein binding30%[1]
Metabolism50% liver, CYP2D6, CYP3A4[3]
Elimination half-life10–12 hours[2]
  • (RS)-1-{4-[(2-Isopropoxyethoxy)methyl]phenoxy}-
CAS Number
PubChem CID
CompTox Dashboard (EPA)
ECHA InfoCard100.108.941 Edit this at Wikidata
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 Concor among others, is a beta blocker medication most commonly used for heart diseases.[4] This specifically includes high blood pressure, chest pain from not enough blood flow to the heart, and heart failure.[4][5] It is taken by mouth.[4]

Common side effects include headache, feeling tired, diarrhea, and swelling in the legs.[4] More severe side effects include worsening asthma, blocking the ability to recognize low blood sugar, and worsening heart failure.[6] There are concerns that use during pregnancy may be harmful to the baby.[7] Bisoprolol is in the beta blocker family of medications and is of the β1 selective type.[4]

Bisoprolol is on the World Health Organization's List of Essential Medicines.[8] Bisoprolol is available as a generic medication.[4] In 2017, it was the 268th most commonly prescribed medication in the United States, with more than one million prescriptions.[9][10]

Medical uses[edit]

Zebeta 5-mg oral tablet

Bisoprolol has a role in the treatment of high blood pressure (hypertension), reduced blood flow to the heart (cardiac ischemia), prevention of further cardiovascular events following a heart attack and the management of congestive heart failure.[11]

Bisoprolol may be beneficial in the treatment of high blood pressure, but it is not recommended as a first-line anti-hypertensive agent without an accompanying comorbid condition, for example, congestive heart failure.[12][13]

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.[14][15][16]

Side effects[edit]

Overdose of bisoprolol leads to fatigue, hypotension,[15] low blood sugar,[17][18] bronchospasms, and bradycardia.[15] 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.[14][15][19]


Beta-blockers should generally be avoided in people with a history of asthma or bronchospasm as they may worsen the disease.[20] A beta 1 selective beta-blocker like bisoprolol may be cautiously tried in those with controlled, mild-to-moderate asthma with cardiac comorbidities.[21] A 2014 meta-analysis found that cardioselective beta-blockers may cause detrimental changes in lung function and partially blunts b2-agonist response.[20] However, a 2017 control study found no significant association with asthma exacerbations by dose and exposure duration while a 2020 clinical trial found bisoprolol being non-inferior to placebo in bronchodilator response to salbutamol.[21][22]


Mechanism of action[edit]

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.[14] 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.[23] 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.[17][18][24]


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.[17][24] 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.[17][18][24]

Bisoprolol has a higher degree of β1-selectivity compared to other β1-selective beta blockers such as atenolol, metoprolol, and betaxolol.[24][25][26][27][28][29][30][31][32][33] However nebivolol is approximately 3.5 times more β1-selective.[34][35]

Renin-angiotensin system[edit]

Bisoprolol inhibits renin secretion by about 65% and tachycardia by about 30%.[25]


Bisoprolol has both lipid- and water-soluble properties.[17][24] It has an approximate half-life of 10–12 hours, and when ingested has high bioavailability (approx. 90%).[17][18] When being eliminated, the body evenly distributes it (50–50) between kidney excretion and liver biotransformation (then excreted).[17][18][24]


Bisoprolol was patented in 1976 and approved for medical use in 1986.[36] It was approved for medical use in the United States in 1992.[4]

Society and culture[edit]

Bisoprolol is available as a generic medication.[37]

Brand names[edit]

In India, it is sold under trade name Bisotab and is available in 2 strengths of 2.5 mg and 5 mg.[38]

In Italy, it is sold under trade name Congescor and is available in 6 strengths of 1.25 mg, 2.5 mg, 3.75 mg, 5 mg, 7.5 mg and 10 mg.


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External links[edit]

  • "Bisoprolol". Drug Information Portal. U.S. National Library of Medicine.