How Does Lisinopril Work? All About Its Mechanism of Action

Lisinopril (Zestril, Qbrelis) belongs to a group of medications called angiotensin-converting enzyme (ACE) inhibitors. All ACE inhibitors are approved to treat high blood pressure. Lisinopril is also FDA-approved to treat heart failure and to prevent death after a heart attack. It also has many off-label uses, such as treating kidney disease from diabetes.

But how does lisinopril work? Here, we’ll dive into lisinopril’s mechanism of action and how it benefits the heart.

What’s lisinopril’s mechanism of action?

Lisinopril works in a few ways:

• It blocks an enzyme (protein) called ACE. This enzyme is responsible for converting the hormone angiotensin I into angiotensin II. This is a hormone that narrows your blood vessels and increases blood pressure. So, blocking the production of angiotensin II lowers blood pressure.

• It decreases levels of a hormone called aldosterone. Aldosterone is responsible for regulating salt and water levels in your body. Usually, it increases the amount of salt in the blood and the amount of potassium that leaves the body through your urine. Lowering aldosterone levels causes more salt and water to leave your body through the urine. This lowers your blood pressure.

• Lisinopril decreases how hard the heart has to work by widening (dilating) your blood vessels and allowing blood to flow more easily. This is helpful in heart failure, where the heart can’t pump enough blood to meet the needs of the rest of the body.

• After a heart attack, lisinopril’s ability to dilate blood vessels reduces stress on the heart.

• In kidney disease, lisinopril dilates the blood vessels in the kidneys and helps them relax. This can prevent long-term kidney damage.

• Lisinopril can reduce the amount of protein in the urine, a sign of kidney damage.

Promotion disclosure

Lisinopril

Avg retail price

$13.61(Save 42.76%)

GoodRx discount

$7.79

See all discounts

How it works

Use GoodRx to find medications, pharmacies, and discounts.

GoodRx discounts can help you pay less for your prescription.

Bring your free coupon or savings card to the pharmacy.

Who should take lisinopril?

Lisinopril is FDA-approved for a few health conditions and scenarios. These include:

• High blood pressure (hypertension). ACE inhibitors are a first-choice medication to treat high blood pressure in many people.

• Heart failure. ACE inhibitors are also a first-choice medication for heart failure in most people.

• After a heart attack. Many people will need to start taking an ACE inhibitor if they’ve had a heart attack.

But lisinopril is also used to treat many other health conditions. These are “off-label” uses. Examples include chronic kidney disease (CKD) and kidney disease caused by diabetes. If you have CKD and high protein in your urine, your healthcare provider may recommend an ACE inhibitor such as lisinopril. And ACE inhibitors are first-choice medications to treat kidney problems caused by diabetes.

What are the benefits of lisinopril?

Lisinopril has many benefits. By lowering your blood pressure, lisinopril lowers your risk of heart disease, heart attack, and more. But it has many other, perhaps lesser-known, benefits as well. These include:

• Increasing your chance of survival after a heart attack

• Reducing your risk of developing diabetes if you have high blood pressure

• Slowing down the progression of kidney disease, especially in people who have a lot of protein in the urine

• Reducing the risk of eye problems caused by diabetes (diabetic retinopathy)

Other less-studied, possible benefits include preventing migraines and improving sperm count and quality.

Good to know: As mentioned, lisinopril can have positive effects on the kidneys. But in some cases, lisinopril can worsen existing kidney problems (or cause kidney problems, in rare cases). If you have kidney disease, you may need a lower dose of lisinopril.

How is lisinopril different from other ACE inhibitors?

ACE inhibitors are generally considered equally effective in treating high blood pressure. But there are differences to consider if you’re comparing lisinopril and other ACE inhibitors. Some differences include:

• How many doses you need per day. Lisinopril can be taken once daily. But some ACE inhibitors are dosed multiple times per day, such as captopril. Benazepril (Lotensin) and enalapril (Vasotec) are also sometimes taken twice daily.

• Whether you need to take your medication with food. Most ACE inhibitors, including lisinopril, can be taken with or without food. But captopril has more specific dosage instructions. It should be taken 1 to 2 hours before a meal.

• Some ACE inhibitors come in multiple forms. Lisinopril (and enalapril) come in liquid form and pill form. But if you have trouble swallowing pills, these ACE inhibitors may be a good option for you.

• How they’re activated. Many ACE inhibitors are made active by the liver. But lisinopril isn’t. So it may be a good option for you if you have liver problems.

Why trust our experts?

Written by:

Alexa Mader, PharmD

Alexa Mader has been a practicing pharmacist since 2018. She earned her Doctor of Pharmacy degree from the University of Georgia College of Pharmacy.

Edited by:

Amy B. Gragnolati, PharmD, BCPS

Amy Gragnolati, PharmD, BCPS, is a pharmacy editor for GoodRx. Amy currently holds her pharmacist license in Georgia and California.

Reviewed by:

Austin Ulrich, PharmD, BCACP

Austin Ulrich, PharmD, BCACP, is a board-certified ambulatory care clinical pharmacist. In his early career, he provided direct patient care in a variety of settings, including hospital and community pharmacies, and in a primary care clinic as a clinical pharmacist.

Our editorial standards

Meet our experts