Introduction
Illustrated mechanism of action
Examples of Medication Brand Names (with Images)
Indication
Side Effects
Precautions & Contraindications
Monographs
Reference
Angiotensin Receptor Blockers (ARBs) are medications primarily used to treat hypertension, heart failure, and chronic kidney disease. They work by blocking the angiotensin II type 1 receptor (AT1R), thereby preventing the vasoconstrictive and aldosterone-releasing effects of angiotensin II within the renin-angiotensin-aldosterone system (RAAS). The development of ARBs was built upon the discovery of RAAS in the early 20th century, followed by the introduction of ACE inhibitors in the 1970s and 1980s. However, due to side effects associated with ACE inhibitors, such as cough and angioedema, ARBs emerged in the 1990s as a more targeted alternative, with losartan becoming the first FDA-approved ARB in 1995.
In the renin-angiotensin-aldosterone system (RAAS), renin (secreted by the kidneys) converts angiotensinogen (from the liver) into angiotensin I. Angiotensin I is then converted to angiotensin II by angiotensin-converting enzyme (ACE), primarily in the lungs.
Angiotensin II is a powerful vasoconstrictor that acts by binding to angiotensin II type 1 receptors (AT₁R). This binding causes:
• Vasoconstriction, which increases blood pressure.
• Aldosterone secretion, leading to sodium and water retention, thereby increasing blood volume and pressure.
• Cardiac and vascular remodeling, which contributes to the progression of hypertension and heart failure.
Angiotensin Receptor Blockers (ARBs)—such as losartan, valsartan, and candesartan—selectively block AT₁ receptors, preventing angiotensin II from exerting its harmful effects. As a result, ARBs cause:
• Vasodilation (reduced vascular resistance)
• Decreased aldosterone release (less sodium and water retention)
• Lower blood pressure
• Protection against cardiac and vascular remodeling
Importantly, ARBs do not block AT₂ receptors, which may exert beneficial effects, including:
• Vasodilation
• Anti-inflammatory actions
• Anti-proliferative effects
This selectivity allows ARBs to effectively reduce blood pressure while potentially preserving or enhancing protective pathways.
The first ARB developed. It’s commonly used to protect the kidneys in diabetics and to reduce stroke risk.
One of the newer ARBs, known for its strong blood pressure-lowering effect. Often used when other medications aren't effective enough
Strong at lowering blood pressure, but in some cases, it can cause gastrointestinal side effects like sprue-like enteropathy.
What do angiotensin II receptor blockers (ARBs) treat? Healthcare providers prescribe ARBs for:
• High blood pressure (hypertension), to lower the amount of force on the blood vessels as blood flows through the body.
• Heart attack, to prevent a heart attack or limit heart damage after an event.
• Heart failure, to help the heart pump more blood to the body.
• Stroke, to open blood vessels, allowing blood clots to move through without causing a stroke.
• Fatty liver disease, to prevent inflammation in the liver.
• Kidney disease, to slow kidney damage, especially related to diabetes.
Common Side Effects:
• Dizziness (especially when standing up quickly)
• Headache
• Fatigue
• Elevated potassium levels in the blood (hyperkalemia)
• Low blood pressure (especially during the initial period of use)
• Kidney problems (especially in patients with pre-existing kidney conditions)
Less Common Side Effects:
• Abdominal pain or nausea
• Skin rash or itching
• Joint or muscle pain
• Mild cough (less frequent than with ACE inhibitors)
Rare or Serious Side Effects:
• Severe allergic reactions (very rare)
• Swelling of the face, tongue, or throat (angioedema) – rare but serious
• Acute kidney failure in some cases
• Hypersensitivity reactions: History of allergy to ACE inhibitors or components, angioedema (from previous ACE inhibitor use, idiopathic, or hereditary), or current use of aliskiren in diabetic patients.
• Pregnancy: ACE inhibitors can cause serious fetal harm, including oligohydramnios, renal failure, skull defects, and even fetal death due to disrupted fetal kidney function and decreased angiotensin II levels.
• Renal impairment: May worsen kidney function and cause hyperkalemia; close monitoring is essential.
• Aortic stenosis: May cause severe hypotension due to reduced afterload.
• Hypovolemia or dehydration: Risk of worsening volume depletion.
Wilkins B, Hullikunte S, Simmonds M, Sasse A, Larsen P, Harding SA. Improving the Prescribing Gap For Guideline Recommended Medications Post Myocardial Infarction. Heart Lung Circ. 2019 Feb;28(2):257-262. [PubMed]26.Shaikh A. A Practical Approach to Hypertension Management in Diabetes. Diabetes Ther. 2017 Oct;8(5):981-989. [PMC free article] [PubMed]27.Gubler MC, Antignac C. Renin-angiotensin system in kidney development: renal tubular dysgenesis. Kidney Int. 2010 Mar;77(5):400-6. [PubMed]17:54
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