Angiotensin II Receptor Blockers: Uses, most common brand names, and safety information
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The actions of the angiotensin-converting enzyme (ACE) within the renin-angiotensin-aldosterone system (RAAS) were discovered in the late 1950s. Converting angiotensin I to angiotensin II by this enzyme causes vasoconstriction, sympathetic nervous stimulation, and increased aldosterone production.
In 1975, Capoten (captopril) became the first drug approved by the U.S Food and Drug Administration (FDA) in a new class called angiotensin-converting enzyme inhibitors (ACE inhibitors). After early clinical trials showed Capoten to be an effective treatment of hypertension, researchers worked to determine if affecting other receptors or enzymes in this pathway may be beneficial.
Saralasin was the first angiotensin II receptor antagonist developed in the 1970s. It was limited in its use due to poor oral bioavailability. Research over the next decade led to Cozaar (losartan), the first successful ARB that was approved by the FDA in 1995.
The list below includes the best ARBs approved by the U.S. Food and Drug Administration (FDA) and their pricing:
List of angiotensin II receptor blockers
|Diovan is indicated to treat hypertension, heart failure, and to reduce the risk of cardiovascular death following a heart attack.
|Edarbi is indicated to treat hypertension.
|Atacand is indicated to treat hypertension and CHF.
|Teveten is indicated to treat hypertension.
|Avapro is indicated to treat hypertension and nephropathy in type 2 diabetes.
|Cozaar is indicated to treat hypertension and nephropathy in type 2 diabetes.
|Benicar is indicated to treat hypertension
|Micardis is indicated to treat hypertension and for cardiovascular risk reduction in patients unable to take ACE inhibitors.
Sometimes ARBs are combined with other blood pressure lowering medications in products such as:
What are angiotensin II receptor blockers?
Angiotensin II receptor blockers are antihypertensive drugs that relax your blood vessels to lower blood pressure and increase blood flow from the heart. ARBs are typically used to treat hypertension (high blood pressure), heart failure, and other cardiovascular diseases. They are also used to maintain or improve kidney function in patients with chronic kidney disease (CKD) and are often prescribed following a myocardial infarction (heart attack).
ARBs are commonly prescribed to patients who cannot tolerate ACE inhibitor therapy, which is typically due to their persistent, dry cough. They are oral medications taken by mouth usually once a day. ARBs can be combined with other blood pressure medications such as diuretics, beta-blockers, or calcium channel blockers in hypertensive patients with severe heart disease.
How do angiotensin II receptor blockers work?
Blood pressure and fluid and electrolyte balance is controlled by the renin-angiotensin-aldosterone system. The kidneys release an enzyme (renin) that metabolizes angiotensinogen into angiotensin I. Angiotensin I is then converted into angiotensin II by the angiotensin-converting enzyme (ACE). Angiotensin II primarily acts on 2 receptors, AT1 and AT2. Stimulating the AT1 receptor causes reabsorption of sodium from the kidneys, retention of water, vasoconstriction, aldosterone secretion, and sympathetic nervous system activation. AT2 stimulation has the opposite effect. It results in vasodilation and the production of nitric oxide and bradykinin.
ARBs selectively block or antagonize angiotensin II at the AT1 receptors in the tissues of your smooth muscle and adrenal gland. This inhibition blocks vasoconstriction and aldosterone secretion with minimal effect on your heart rate.
What conditions are angiotensin II receptor blockers used to treat?
Angiotensin II receptor blockers are a class of medications used to treat or prevent:
- Hypertension (high blood pressure)
- Heart failure
- Heart attacks
- Congestive heart failure (CHF)
- Left ventricular dysfunction
- Coronary artery disease (CAD)
- Chronic kidney disease (CKD)
- Diabetic nephropathy
Are angiotensin II receptor blockers safe?
When taken as prescribed, ARBs are relatively safe and effective. Your healthcare provider should be aware of your medical conditions, including:
- Kidney disease
- Allergy to ARBs
- History of angioedema
- Hyperkalemia (high potassium levels)
- Hyponatremia (low sodium levels)
- Volume depletion
- Renal artery stenosis
- Are pregnant or plan on becoming pregnant as they may cause fetal harm and/or death
You should also make sure they are aware of all the medications you take, including prescription drugs, over-the-counter medications, and supplements, including:
- Salt substitutes that contain potassium
- Potassium supplements
- Tekturna (aliskiren)
- Medications that are metabolized in the liver by the CYP450 such as Dilantin (phenytoin), Tegretol (carbamazepine), and Nizoral (ketoconazole)
Can you take angiotensin II receptor blockers while you are pregnant or breastfeeding?
The use of drugs that affect the renin-angiotensin system such as ARBs are known to cause birth defects, fetal renal damage, or death. The use of ARBs should be stopped immediately when pregnancy is confirmed.
There is limited published evidence on the safe use of ARBs during lactation. Because of the possible risk of adverse events for the infant, the use of ARBs is generally not recommended.
You should always discuss the risks and benefits of any medication you need with your doctor if you are pregnant, plan on becoming pregnant, or are breastfeeding.
What are the common side effects of angiotensin II receptor blockers?
Some common adverse effects of ARBs include:
- Hyperkalemia (high blood potassium)
- Hypotension (low blood pressure)
- Stomach pain
- Upper respiratory tract infections
- Elevated liver enzymes
ARBs can sometimes cause severe adverse events, including:
- Serious hypersensitivity reactions, including angioedema
- Kidney failure
- Liver failure
- Low white blood cells counts (neutropenia)
This is not a complete list of side effects and we encourage you to consult with your healthcare professional for medical advice about any possible side effects.
How much do angiotensin II receptor blockers cost?
Angiotensin II receptor blockers are very expensive with an average cost of around $1,000-5,000 per year.
You can purchase angiotensin for $49 per month from NiceRx if eligible for assistance. Prices at the pharmacy vary by location, strength, and quantity, as well as your insurance status.
Related resources for angiotensin II receptor blockers
The content on this website is intended for information purposes only. It does not constitute medical advice. The information on this website should not be relied upon and is not a substitute for professional medical advice. You should always speak to your doctor regarding the risks and benefits of any treatment.