ACEIs/ARBs

• Introduction

About angiotensin-converting enzyme (ACE) inhibitors & angiotensin receptor blockers (ARBs)

ACE inhibitors and ARBs are two types of oral (taken by mouth) prescription medicines commonly recommended for people with kidney disease. They represent two different medicine categories but work in similar ways

They are considered “kidney protection” medicines – they can help keep your glomeruli (small filters in your kidneys) healthy and lower your urine albumin-creatinine ratio (uACR) level. They can also lower your risk of cardiovascular disease (CVD, including heart failure, heart attack, or stroke).

• Mechanism of action

ACE inhibitors and ARBs both work by lowering the effects of angiotensin-2 (pronounced: an-jee-oh-TEN-sin 2) in the body. Angiotensin-2 is also known as AT2. AT2 is a hormone made by your body that helps balance your blood pressure. When your blood pressure starts to go too low, the body makes AT2 to help bring it up.

The main way AT2 works is by narrowing your blood vessels, especially in the kidneys. When there is too much AT2, the blood vessels in your kidneys are not able to relax. This can cause high blood pressure and/or kidney damage. It can also make heart failure and other types of CVD worse.

Both medicine categories lower the effects of AT2, but in different ways:

ACE inhibitors slow down how much AT2 your body makes.

ARBs block the receptors (buttons) that AT2 uses to narrow your blood vessels.

Although ACE inhibitors and ARBs work in separate ways, the result is the same – keep your blood vessels relaxed and lower the pressure in your kidneys (and throughout your body)

youtu.be/HMPq4Kic8ac?si=zzrTvzpoBotSQwGF 

https://youtu.be/xIlaQuRaZmk?si=m9k0ZN1YErOIIi_z

• pharmacokinetics properties

The pharmacokinetic and pharmacodynamic properties of nonpeptide angiotensin antagonists in humans are reviewed in this paper. Representatives of this new therapeutic class share common features: lipophilia, intermediate bioavailability, high affinity for plasma proteins and liver metabolism; some have active metabolites. Angiotensin II antagonists block the blood pressure response to exogenous angiotensin II in healthy volunteers, decrease baseline blood pressure in both normal and hypertensive patients, produce a marked rise in plasma renin activity and endogenous angiotensin II and increase renal blood flow without altering glomerular filtration rate. These effects are dose-dependent, but their time course varies between the drugs owing to pharmacokinetic and pharmacodynamic differences. Additionally, the extent of blood pressure reduction is dependent on physiological factors such as sodium and water balance. The characterisation of their pharmacokinetic-pharmacodynamic relationships deserves further refinement for designing optimal therapeutic regimens and proposing dosage adaptations in specific conditions

• Types

There are many different options to choose from. All of them are taken by mouth and most are available as low-cost generic options. Most are taken once a day, although some may need to be taken more often (2-3 times per day).

• ACE inhibitors have generic names that end in “-pril”. Common examples include:

1. benazepril (Lotensin)

2. lisinopril (Zestril, Prinivil)

3. quinapril (Accupril)

4. ramipril (Altace)

5. ARBs have generic names that end in “-sartan”. Common examples include:

6. irbesartan (Avapro)

7. losartan (Cozaar)

8. olmesartan (Benicar)

9. valsartan (Diovan)

People should not mix medicines from these classes. In other words, use an ACE inhibitor OR an ARB, not both together

ACE inhibitors have generic names that end in “-pril”. ARBs have generic names that end in “-sartan”.

• Additional considerations

Acute kidney injury (AKI)

ACE inhibitors and ARBs are not likely to cause acute kidney injury (AKI). However, when combined with other factors, your risk of developing AKI goes up. The most common factors that can lead to AKI (when mixed with an ACE inhibitor or ARB) include:

Taking a non-steroidal anti-inflammatory drug (NSAID), such as:

ibuprofen (Motrin, Advil)

naproxen (Aleve)

diclofenac tablets or capsules (Cataflam, Zipsor)

celecoxib (Celebrex)

meloxicam (Mobic)

aspirin (only if more than 325 mg per day)

Taking a loop diuretic (water pill) such as:

furosemide (Lasix)

torsemide (Demadex)

bumetanide (Bumex)

Dehydration (not drinking enough water to meet your body’s needs)

Sometimes combining ACE inhibitors/ARBs with NSAIDs and/or diuretics cannot be avoided. Many people may need these medicines to manage their other health conditions. It is important to talk with your doctor about your risk factors for AKI and how you can lower your risk.

• Pregnancy

ACE inhibitors and ARBs should not be used during pregnancy, especially during the second and third trimesters. They can increase the risk of harm to the baby, including fetal death.

•  Interactions

1. Drug Drug interaction

2. Drug Food interaction

• Are there any foods or drinks to avoid?

Salt substitutes such as ‘LoSalt’ contain potassium chloride, which can cause high blood potassium levels. Speak to your doctor if you’re using this. A regular high alcohol intake can worsen high blood pressure, which could counteract the effect of your medication. However, binge drinking can lower blood pressure temporarily. If you’re taking blood pressure medication, this could cause light-headedness and even fainting. Keep your alcohol intake to a minimum

• Effectiveness

All ACE inhibitors and ARBs provide “kidney protection” and other benefits, including:

lower blood pressure

lower uACR levels for people with albuminuria

slow the damage to the glomeruli (small filters in the kidneys) that happens in kidney disease

slow the damage to the heart muscles that happens in heart failure

lower risk of heart attack or stroke (especially in people who have already had one before)

One myth about these medicines is they only benefit people who have high blood pressure. This is not true. People with kidney disease or heart failure can still benefit from an ACE inhibitor or ARB even if they do not have high blood pressure. If you do not have high blood pressure, a lower dose may be recommended for you to prevent low blood pressure symptoms.

All ACE inhibitors and ARBs are considered equally effective. This means they all work about the same as each other.