How Does Carvedilol Work? All About Its Mechanism of Action
Key takeaways:
Carvedilol (Coreg) is a beta blocker. It lowers blood pressure and heart rate.
Carvedilol’s mechanism of action is to block various receptors (binding sites) in the body, including beta-1, beta-2, and alpha-1 receptors. By blocking alpha-1 receptors, carvedilol lowers blood pressure more than most beta blockers. It’s considered a first-choice medication for heart failure.
Carvedilol can worsen symptoms in people with lung conditions like asthma. If you have asthma, a selective beta blocker like metoprolol succinate (Toprol XL) may be a better option.
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Table of contents
Carvedilol (Coreg) belongs to a group of medications called beta blockers. Beta blockers help lower the stress on your heart. This is useful for people with certain heart problems. In fact, carvedilol is a first-choice option for people with heart failure. Here, we’ll talk about carvedilol’s mechanism of action and how it can help the heart.
What is carvedilol’s mechanism of action?
Carvedilol works by lowering the amount of stress on the heart. It can help treat many heart-related health conditions, including heart failure.
Beta blockers such as carvedilol produce heart benefits by attaching to certain areas in the body called receptors. The receptors that beta blockers may bind to include:
Beta-1
Beta-2
Alpha-1
There are two main types of beta blockers: selective and non-selective. Selective beta blockers only bind to beta-1 receptors. Examples include metoprolol tartrate (Lopressor), metoprolol succinate (Toprol XL), and atenolol (Tenormin). Non-selective beta blockers block both beta-1 and beta-2 receptors. Examples include carvedilol, labetalol, and propranolol (Inderal LA, Innopran XL). Additionally, carvedilol and labetalol also block alpha-1 receptors.
Carvedilol affects the heart by:
Blocking beta-1 receptors: Beta-1 receptors are found in the heart. Turning on these receptors causes your heart to beat faster and harder. This leads to an increased heart rate and higher blood pressure. By blocking these receptors, carvedilol slows down your heart rate and reduces blood pressure.
Blocking beta-2 receptors: Beta-2 receptors also control heart rate and how hard your heart beats. They also control how wide or narrow your blood vessels and airways are. By blocking these receptors, carvedilol slows your heart rate. But it can also cause your airways to contract (tighten). So carvedilol may worsen the symptoms of certain lung problems like asthma.
Blocking alpha-1 receptors: Alpha-1 receptors tighten blood vessels and increase heart rate. By blocking them, carvedilol slows your heart rate and relaxes your blood vessels, which lowers blood pressure.
Having antioxidant and anti-inflammatory effects: Oxidative stress and inflammation play a role in heart-related problems. Carvedilol lowers inflammation and increases antioxidants, which may be another way it’s beneficial for heart conditions.
When is carvedilol prescribed?
Carvedilol is FDA approved to treat three heart-related conditions:
Heart failure: In studies, carvedilol lowered the risk of hospitalization and death in people with a type of heart failure called heart failure with reduced ejection fraction (HFrEF). In HFrEF, the heart pumps out significantly less blood than what’s expected.
High blood pressure: Beta blockers aren’t usually a first-choice option for lowering blood pressure. But they may be added to other blood pressure medications in some cases.
Lower the risk of death after a heart attack: Beta blockers are a go-to medication for people who’ve had a heart attack because they lower stress on the heart. This may help decrease your risk of serious complications, including death.
Besides its FDA-approved uses, carvedilol may also be prescribed for off-label uses. Examples include atrial fibrillation and angina (chest pain).
How is carvedilol different from other beta blockers?
What separates carvedilol from most other beta blockers is its alpha-1 blocking effects. Labetalol is the only other beta blocker that blocks alpha-1 receptors.
In certain situations, carvedilol’s effect on multiple receptors is beneficial. For example, in heart failure, carvedilol’s effects on beta and alpha receptors helps improve heart function in various ways. So it’s a better option than most other beta blockers for heart failure (except for metoprolol succinate, which is also a first-choice option). And carvedilol’s alpha-blocking effect helps it lower blood pressure more than other beta blockers.
But in other cases, carvedilol’s effects on various receptors can be more harmful. For example, in people with asthma and other lung problems, carvedilol can tighten the airways and lead to breathing problems. This is due to its effect on beta-2 receptors.
The bottom line
Carvedilol is a beta blocker that treats various heart conditions, including heart failure. Carvedilol’s mechanism of action is to block beta-1, beta-2, and alpha-1 receptors. This helps slow down your heart rate and lower blood pressure. Carvedilol may also have anti-inflammatory effects that help benefit the heart.
Carvedilol’s alpha-1 blocking effect makes it different from other beta blockers. For example, it’s often a first-choice option for heart failure. And it’s less likely to affect blood sugar or triglyceride levels. But it can also worsen symptoms in people with asthma or other lung conditions. If you need a beta blocker, your healthcare provider can help you decide which is the best option for you.
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References
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Ayashi, S., et al. (2016). Role of antioxidant property of carvedilol in mild to moderate hypertensive patients: A prospective open-label study. Indian Journal of Pharmacology.
Dandona, P., et al. (2007). Antioxidant activity of carvedilol in cardiovascular disease. Journal of Hypertension.
Farzam, K., et al. (2023). Beta blockers. StatPearls.
McTavish, D., et al. (1993). Carvedilol. A review of its pharmacodynamic and pharmacokinetic properties, and therapeutic efficacy. Drugs.
Molenaar, P., et al. (2006). Carvedilol blocks β2- more than β1-adrenoceptors in human heart. Cardiovascular Research.
Romano, V., et al. (2021). The effects of beta (2)-adrenergic receptors activation on the cardiovascular system and on the skeletal muscle: A narrative review. Journal of Human Sport and Exercise.
Singh, S., et al. (2023). Carvedilol. StatPearls.
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