Cholesterol Absorption Inhibitors: How They Work, Benefits & Risks

Introduction: Key Points About Cholesterol Absorption Inhibitors

Cholesterol absorption inhibitors are a type of medication designed to lower cholesterol levels in the blood. They work by reducing the amount of cholesterol absorbed from the food you eat. These drugs are often prescribed when lifestyle changes or other treatments, such as statins, are not enough to manage cholesterol levels effectively. By lowering cholesterol, these medications can help reduce the risk of heart disease and stroke.

Medications in the Cholesterol Absorption Inhibitors Class

Ezetimibe (Ezetimibe)

The “generic name” refers to the active ingredient in the medication, while the brand name is the marketed name. In this list, the generic name is shown in parentheses.

How Do Cholesterol Absorption Inhibitors Work?

Cholesterol absorption inhibitors work by blocking the absorption of cholesterol in the small intestine. They specifically target a protein called NPC1L1, which is responsible for transporting cholesterol from the digestive tract into the bloodstream. By inhibiting this process, these medications reduce the amount of cholesterol entering the blood, leading to lower overall cholesterol levels. Ezetimibe is the primary drug in this class and works similarly for most patients.

Benefits of Cholesterol Absorption Inhibitors

Cholesterol absorption inhibitors are often used when other cholesterol-lowering medications, like statins, are not sufficient to bring cholesterol levels into a healthy range. They are particularly helpful for individuals who cannot tolerate high doses of statins due to side effects. This class of medication is also frequently combined with statins for a more comprehensive approach to lowering cholesterol. By reducing cholesterol absorption, these medications help lower the risk of heart disease, heart attacks, and strokes.

Potential Side Effects of Cholesterol Absorption Inhibitors

Like all medications, cholesterol absorption inhibitors can cause side effects. While many people tolerate these drugs well, it’s important to be aware of potential side effects and discuss any concerns with your healthcare provider before starting treatment. Below is a list of the most common side effects, followed by less common and rare side effects. If you experience any severe side effects, contact a healthcare provider immediately.

Common Side Effects (≥1%)

1. Diarrhea (4%): This is the most commonly reported side effect. If you experience persistent diarrhea, stay hydrated and consult your healthcare provider.
2. Upper respiratory tract infection (4%): Symptoms may include a runny nose, sore throat, or cough.
3. Joint pain (arthralgia) (3%): Some patients report mild to moderate joint discomfort.
4. Sinusitis (2%): Inflammation of the sinuses can cause headaches, facial pain, and nasal congestion.
5. Fatigue (2%): Feeling unusually tired or lacking energy is another common side effect.
6. Back pain (2%): Some patients may experience discomfort in their back muscles or spine.

Less Common Side Effects (<1%)

While less frequent, the following side effects have been reported in some patients:

1. Abdominal pain
2. Nausea
3. Muscle pain (myalgia)
4. Headache
5. Dizziness
6. Rash
7. Elevated liver enzymes

Severe Side Effects

Severe side effects are rare but can occur. These include:

1. Allergic reactions: Symptoms may include swelling of the face, lips, or throat, difficulty breathing, and severe rash. Seek emergency medical attention if you experience any of these symptoms.
2. Liver problems: Cholesterol absorption inhibitors can sometimes cause elevated liver enzymes, which may indicate liver damage. Symptoms of liver issues include yellowing of the skin or eyes (jaundice), dark urine, or severe fatigue. Your healthcare provider may monitor your liver function with blood tests during treatment.
3. Muscle problems (myopathy or rhabdomyolysis): In rare cases, cholesterol absorption inhibitors can cause severe muscle pain, weakness, or muscle breakdown (rhabdomyolysis). This condition can lead to kidney damage and requires immediate medical attention.

If you experience any of these severe side effects, stop taking the medication and contact a healthcare provider immediately. It’s important to speak with a doctor before starting cholesterol absorption inhibitors, especially if you have a history of liver disease, muscle disorders, or other chronic conditions. Our telemedicine providers are available to help you assess your risk and determine if this medication is right for you.

Drug to Drug Interactions with Cholesterol Absorption Inhibitors

Cholesterol absorption inhibitors can interact with other medications, potentially altering their effectiveness or increasing the risk of side effects. It’s essential to inform your healthcare provider about all the medications you are taking, including over-the-counter drugs and supplements. Some key drug interactions to be aware of include:

Statins

Cholesterol absorption inhibitors are often prescribed alongside statins. However, this combination can increase the risk of muscle-related issues, such as myopathy or, in rare cases, rhabdomyolysis. Your doctor may closely monitor your muscle health if you are taking both medications.

Fibrates (e.g., Fenofibrate, Gemfibrozil)

Using cholesterol absorption inhibitors with fibrates may elevate the risk of developing gallstones or liver complications. Your doctor may adjust your dosage or explore alternative cholesterol-lowering treatments if necessary.

Bile Acid Sequestrants (e.g., Cholestyramine, Colestipol)

Bile acid sequestrants can interfere with the absorption of cholesterol absorption inhibitors. To minimize this interaction, it is recommended to take cholesterol absorption inhibitors at least 2 hours before or 4 hours after taking bile acid sequestrants.

Cyclosporine

This immunosuppressant can increase the levels of cholesterol absorption inhibitors in your bloodstream, which may heighten the risk of side effects. Your healthcare provider may need to adjust your dosage or monitor your blood levels more frequently.

Warfarin

Cholesterol absorption inhibitors may enhance the effects of warfarin, a blood thinner, which could increase the risk of bleeding. If you are taking both medications, your doctor may need to monitor your blood clotting levels (INR) more closely.

Precautions and Contraindications for Cholesterol Absorption Inhibitors

Before starting cholesterol absorption inhibitors, it’s important to review your medical history with your healthcare provider to ensure this medication is appropriate for you. Key precautions and contraindications include:

Liver Disease

If you have active liver disease or elevated liver enzymes, cholesterol absorption inhibitors may not be suitable for you. Your doctor may recommend regular liver function tests to monitor for potential liver damage while you are on this medication.

Pregnancy and Breastfeeding

Cholesterol absorption inhibitors should be used with caution during pregnancy and breastfeeding. Since there is limited data on the safety of these medications in pregnant or breastfeeding women, your healthcare provider will carefully weigh the potential risks and benefits before prescribing them.

Kidney Disease

If you have kidney disease, your doctor may need to adjust your dosage or monitor your kidney function closely while you are taking cholesterol absorption inhibitors.

Allergies

If you have had an allergic reaction to cholesterol absorption inhibitors or any of their ingredients in the past, you should avoid taking this medication. Be sure to inform your healthcare provider of any known allergies.

Conclusion: Cholesterol Absorption Inhibitors as a Cholesterol Treatment Option

Cholesterol absorption inhibitors are an effective option for lowering cholesterol, particularly when used in combination with other medications like statins. However, as with any treatment, they come with potential side effects and drug interactions. It’s important to discuss your medical history, current medications, and any concerns with your healthcare provider before starting treatment. If you experience any severe side effects, contact a healthcare provider immediately.

If you have questions about whether cholesterol absorption inhibitors, such as ezetimibe, are right for you, our telemedicine providers are available to help. Schedule a virtual visit today to discuss your treatment options and receive personalized advice from the comfort of your home.

James Kingsley

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