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Cardioselective beta-blockers: Uses, common brands, and safety information

Cardioselective beta-blockers are prescription medications that help decrease blood pressure, and lower stress on the heart

Beta-blockers are commonly prescribed medications to treat high blood pressure (hypertension) and heart problems, including irregular heart rhythm and heart failure. These drugs work by blocking beta receptors found on the heart and blood vessels, although they can also affect beta receptors found in the kidneys, lungs, and other parts of the body. 

Cardioselective beta-blockers work by binding to beta-1 receptors, which are abundant in the heart muscle. Compared to nonselective beta-blockers, cardioselective beta-blockers carry a lower risk of certain side effects, such as worsening lung function in those with COPD or other lung diseases. 

Continue reading to learn more about cardioselective beta-blockers, how they work, their side effects, and more. 

List of cardioselective beta-blockers
Drug name SingleCare savings Learn more
Tenormin (atenolol) Get Tenormin coupons Tenormin details
Zebeta (bisoprolol) Get bisoprolol coupons Bisoprolol details
Lopressor (metoprolol tartrate) Get Lopressor coupons Lopressor details
Toprol XL (metoprolol succinate) Get Toprol XL coupons Toprol XL details
Bystolic (nebivolol) Get Bystolic coupons Bystolic details
Brevibloc (esmolol) Get esmolol coupons Esmolol details
Kerlone (betaxolol) Get betaxolol coupons Betaxolol details
Sectral (acebutolol) Get acebutolol coupons Acebutolol details

Other cardioselective beta-blockers

  • Celiprolol
  • Practolol
  • Xamoterol

What are cardioselective beta-blockers?

Beta-blockers, or beta-adrenergic blocking agents, are medications that help decrease blood pressure and lower stress on the heart. There are two types of beta-blockers: nonselective and cardioselective. 

Nonselective beta-blockers, also known as first-generation beta-blockers, can bind to beta-1 and beta-2 receptors found in the heart, lungs, and blood vessels. Examples of nonselective beta-blockers include carvedilol, nadolol, timolol, sotalol, labetalol, and pindolol. Propranolol is a nonselective beta-blocker that was the first beta-blocker to be widely used in medicine for angina, or chest pain. 

Cardioselective beta-blockers inhibit the binding of beta-1 receptors, mostly found in the heart. These medications help treat hypertension, arrhythmias, acute myocardial infarctions (heart attacks), and congestive heart failure. Examples of cardioselective beta-blockers include atenolol, acebutolol, bisoprolol, esmolol, and metoprolol. These medications are sometimes combined with other blood pressure lowering medications, including vasodilators, ACE inhibitors, diuretics, alpha blockers, and calcium channel blockers.

How do cardioselective beta-blockers work?

Cardioselective beta-blockers work by blocking beta-1 receptors, which prevents epinephrine from binding to these receptors. As a result, these medications block the effects of epinephrine, also known as adrenaline, in order to decrease heart rate and the contractility of the heart. 

Epinephrine is a neurotransmitter and hormone that is naturally released from the adrenal glands to regulate blood pressure and heart functions. It is also involved with the fight-or-flight response, or an acute response that arises during stressful situations. During the fight-or-flight response, the body’s sympathetic nervous system produces a flood of adrenaline to prepare the body for an impending threat.  

Normally, epinephrine binds to beta-1 adrenergic receptors in the heart, kidneys, lungs, and smooth muscles of the arterial blood vessels. Too much stimulation of beta-1 receptors on the heart muscles can lead to an increased heart rate and an irregular heart rhythm, as well as increased pressure on the heart. Stimulation of beta-1 receptors in the kidney also leads to the release of renin, an enzyme that can act to increase blood pressure. Beta-blockers are antagonists that block the effects of epinephrine to slow heart rate and relieve pressure on the blood vessels. 

What are cardioselective beta-blockers used for?

Cardioselective beta-blockers are often prescribed for a number of conditions affecting the heart and blood vessels. They have FDA-approved and off-label uses. 

  • High blood pressure
  • Chronic chest pain
  • Heart failure
  • Heart attacks
  • Left ventricular dysfunction after a heart attack
  • Irregular heart rhythm

Types of cardioselective beta-blockers

Cardioselective beta-blockers with ISA

Certain cardioselective beta-blockers have intrinsic sympathomimetic activity (ISA). These beta-blockers have actions that can increase vascular resistance, which leads to increased blood pressure. Beta-blockers with ISA can also increase heart rate and have less of an effect on the reduction of cardiac output. Cardioselective beta-blockers with ISA include celiprolol and acebutolol. 

Cardioselective beta-blockers without ISA

In some cases, cardioselective beta-blockers without ISA may be preferred over cardioselective beta-blockers with ISA. Beta-blockers without ISA may have more beneficial effects on blood pressure and heart rate than other beta-blockers. They may also have more of an effect on reducing cardiac output to decrease stress on the heart. Cardioselective beta-blockers without ISA include bisoprolol, metoprolol, and atenolol. 

Who can take cardioselective beta-blockers?


Cardioselective beta-blockers are commonly prescribed to adults with high blood pressure or heart disease. They are also used to manage chronic chest pain in people with coronary artery disease. The American College of Cardiology recommends a cardioselective beta-blocker to help reduce the risk of death in those with heart failure or reduced left ventricular function. These medications are usually taken as daily tablets in both men and women, and they should only be used as prescribed by a healthcare provider. 


The use of beta-blockers in the elderly is usually safe and recommended for certain cardiovascular conditions. However, older patients may be more likely to have problems with kidney, liver, and heart function. Some evidence and guidelines suggest avoiding the use of a beta-blocker to treat high blood pressure in older patients over the age of 60 unless they also have another condition like heart failure. If treatment is recommended, older adults are usually started on a lower dose of a beta-blocker. 


Certain beta-blockers may be recommended for children, especially children with chronic heart failure. The exact dose and type of drug prescribed will depend on the child’s condition, age, and other factors. 

Are cardioselective beta-blockers safe?

Cardioselective beta-blockers are generally safe medications to take. Compared to nonselective beta-blockers, cardioselective beta-blockers may have a lower risk of causing bronchospasms. Therefore, these drugs may be safer for people with lung diseases, such as chronic obstructive pulmonary disease or asthma. 


No current recalls available. 


Cardioselective beta-blockers have specific contraindications. The use of cardioselective beta-blockers should be avoided in people with a history of edema, or fluid retention, who are not already being treated with a diuretic. Cardioselective beta-blockers should not be used in people with complete or second-degree heart block, which is a type of heart rhythm disorder. Beta-blockers should also not be used in those with severe bradycardia (slow heart rate), cardiogenic shock, decompensated heart failure, or sick sinus syndrome. Beta-blockers can slow the heart rate and worsen the effects of these problems. 

Cardioselective beta-blockers are not generally recommended for people with severe asthma or COPD. Although the risk is lower with cardioselective beta-blockers than nonselective beta-blockers, there is still a risk of an exacerbation, or acute worsening of respiratory symptoms. A healthcare provider should be consulted to determine whether a cardioselective beta-blocker would be appropriate in someone with mild to moderate lung disease. 

The dose of certain cardioselective beta-blockers may need to be adjusted in those with liver or kidney disease.

Those who are allergic to any of the ingredients in beta-blockers should avoid taking these medications. 

Cardioselective beta-blockers may interact with other medications including high blood pressure medications, heart rhythm medications, certain antidepressants, nitrates, antidiabetic drugs, NSAIDs, and drugs used for allergy and cold symptoms. Discuss with a doctor other medications you may be using, such as prescription medications, over-the-counter medicines, and herbal supplements before using a cardioselective beta-blocker. 

Are cardioselective beta-blockers controlled substances?

No, cardioselective beta-blockers are not controlled substances.

Common cardioselective beta-blockers side effects

The most common side effects of cardioselective beta-blockers include:

  • Dizziness
  • Headache
  • Fatigue
  • Weakness
  • Dry mouth or eyes
  • Nausea
  • Vomiting
  • Stomach discomfort

Beta-blockers may also cause other adverse effects such as slow heartbeat (bradycardia) and low blood pressure (hypotension). Less common side effects of cardioselective beta-blockers include memory problems, confusion, and sexual dysfunction, including erectile dysfunction

When blood sugar levels fall, a person with diabetes normally experiences a rapid heart rate (tachycardia), tremors, and irritability. Cardioselective beta-blockers can mask certain signs of hypoglycemia in patients with diabetes, including tachycardia. Blood sugar levels may need to be monitored more closely in patients with diabetes. A person with diabetes should also take extra precautions, such as having sugar tablets or juice on hand, to treat hypoglycemia. 

Allergic reactions are possible with cardioselective beta-blockers. Seek immediate medical attention if you experience hives, rash, trouble breathing, or swelling of the face or throat while taking a cardioselective beta-blocker. 

Overdose with beta-blockers is also possible. Signs of an overdose may include severe low blood pressure, cardiac arrest, heart failure, bronchospasm, nausea, vomiting, mental impairment, and coma.

This is not a complete list of side effects, and others may occur. Consult a healthcare provider for other possible side effects, drug interactions, warnings, and precautions before taking a cardioselective beta-blocker. 

How much do cardioselective beta-blockers cost?

Beta-blockers are available in both brand and generic forms. They can be administered as an oral tablet or intravenous solution, although a healthcare provider will help determine the most appropriate formulation depending on the condition being treated. 

Medicare and insurance plans usually cover beta-blockers. However, the costs with or without insurance can vary depending on the drug, strength, and quantity prescribed. Savings options, such as the SingleCare discount card, are available for all types of patients at participating pharmacies. Savings cards may help lower the cost of a medication to a price that is more affordable than the copay with insurance.