Over-The-Counter Cholesterol Medication: What You Need To Know

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What are healthy cholesterol levels?

Cholesterol¹ is essential in our bodies. It is involved in:

  • Giving structure to cells

  • The synthesis and activation of many hormones and vitamins

  • The production of bile, which is important in fat breakdown

However, too much cholesterol can damage your blood vessels and increase your risk of cardiovascular disease.

To determine your cholesterol levels, a blood test called a lipoprotein panel can be given by your healthcare provider. The cholesterol test will provide a lipid profile with your cholesterol levels. These are measured in milligrams per deciliter (mg/dL).

Generally, a lipid profile¹ consists of the following:

  • Total cholesterol: A measure of the total amount of cholesterol in your blood.

  • LDL cholesterol:² This is considered your “bad” cholesterol. LDL cholesterol can build up in the walls of your blood vessels, causing a reduction in blood flow.

  • HDL cholesterol: This is your “good” cholesterol. HDL cholesterol helps to absorb and excrete LDL cholesterol from your body.

  • Triglycerides: This is a type of fat found in your blood. Too much can increase your risk of heart disease.

The standard guidelines for total cholesterol, LDL cholesterol, HDL cholesterol, and triglycerides for adults aged 20 years of age and above are:

When do cholesterol levels require treatment?

If your cholesterol is found to be high, your doctor may recommend treatment. In addition to your cholesterol levels, they may also evaluate and calculate your cardiac risk – this is your ten-year risk of having a stroke or heart attack. This evaluation will allow your doctor to determine the best treatment for you.

Your cardiac risk is determined by, but not limited to, the following risk factors:

  • Age

  • Sex

  • Ethnicity

  • Blood pressure

  • Body weight

  • Diabetes

  • Medical history – past or current health problems

  • Family health history and family history of heart disease

  • Smoking history

  • Alcohol intake and history

  • Diet

  • Current medications you are taking, such as aspirin and hypertension medications

Your risk, along with your cholesterol levels, may place you in one of three categories:³

  • Low risk: You have high cholesterol, but only zero-to-one risk factor

  • Moderate/intermediate risk: You have high cholesterol and more than two risk factors

  • High risk: You have high cholesterol and cardiovascular disease (CVD), and/or CVD equivalent conditions, such as diabetes

How is high cholesterol treated?

The cornerstone for the treatment of high cholesterol is lifestyle changes. This can include:

  • Making changes to your diet

  • Increasing physical activity

  • Decreasing or quitting smoking and alcohol

No matter your situation, your doctor will most likely recommend these changes to your lifestyle.

In some cases, depending on the severity of your situation, your doctor may suggest over-the-counter cholesterol medication or supplements, along with lifestyle changes.

If lifestyle changes alone do not lower your cholesterol levels, if you have an LDL cholesterol level of 190 mg/dL, or if you fall into the high-risk category for cardiac issues, then your doctor is likely to prescribe medications.

Let's look at some commonly prescribed cholesterol-lowering medications.

Prescription cholesterol-lowering medications

Statins

Statins are the most commonly prescribed cholesterol-lowering medications, and they are considered to be the most effective, both in lowering LDL and in the prevention of CVD.

This medication blocks the cholesterol-making enzyme in the liver, slowing down the production of cholesterol.

Based on their ability to decrease LDL cholesterol, statins can be divided into two categories:

  1. Moderate-intensity statin therapy is expected to have a 30%–50% reduction in LDL cholesterol.

  2. High-intensity statin therapy is expected to have a greater than or equal to 50% reduction in LDL cholesterol.

Side effects of statins can include:

  • Muscle aches and pains

  • Nausea and vomiting

  • Headaches

  • Diarrhea or constipation

Severe side effects include:

  • The onset of diabetes

  • Myopathy (muscle inflammation)

  • Liver damage

  • Rhabdomyolysis (damaged muscle tissue releases proteins and electrolytes into the blood)

Cholesterol absorption inhibitors

Cholesterol absorption inhibitors⁴ stop dietary cholesterol in the intestines from being absorbed. This, in turn, helps to lower LDL cholesterol in the blood.

This is a non-statin treatment used to treat high cholesterol in certain cases. For example, it may be prescribed for people with statin intolerance, or it may be taken alongside a statin if your lipid levels cannot be optimally controlled by statins alone.

The most frequently prescribed cholesterol absorption inhibitor is ezetimibe.

Ezetimibe has been shown to be relatively safe and produces few side effects. However, some side effects that you may experience include:

  • Abdominal pain

  • Nausea and vomiting

  • Constipation

  • Nausea

  • Dizziness

PCSK9 inhibitors

This is a relatively new class of drug that lowers LDL cholesterol and triglycerides and increases HDL cholesterol. PCSK9 inhibitors can be used alongside statin therapy or for people with statin intolerance. It is believed to be a highly safe drug, with very few side effects and adverse reactions.

PCSK9 inhibitors⁵ block PCSK9 activity and increase the capacity to clear LDL cholesterol from the blood. They are administered via an injection.

Common PCSK9 inhibitors include:

  • Alirocumab

  • Evolocumab

  • Inclisiran

Side effects of PCSK9 include:

  • Injection site reactions, such as pain and/or swelling

  • Nasopharyngitis (swelling of nasal passages and back of the throat)

Over-the-counter cholesterol medications and supplements

Over-the-counter cholesterol medications and supplements tend to be suitable for people with high cholesterol but mild cardiac risk. In some circumstances, they may be used in place of prescription medications for patients who are unable to tolerate statins or other prescription cholesterol-lowering medications.

Below are some of the most well-researched and best-understood products:

Niacin

Niacin, also known as nicotinic acid and vitamin B3, is available both over-the-counter and by prescription.

Prescription niacin has been shown to lower LDL cholesterol and triglycerides and increase HDL cholesterol. Over-the-counter niacin may be able to lower cholesterol, but likely at a much lower rate. You should not take over-the-counter niacin unless advised by your physician. Niacin can cause liver problems if not closely monitored.

Niacin is used as a second line of therapy, in conjunction with other lipid-lowering agents, the most common being ezetimibe.

Major side effects from niacin therapy have been observed, so it is important you seek medical advice before taking this supplement. Side effects include:

  • Widening of blood vessels, causing flushing and itchy skin

  • Gastric ulceration

  • Palpitations

  • Abdominal pain, leading to nausea and vomiting

  • Gout

Omega-3 fatty acids

There are three main omega-3s:⁶

  • EPA

  • DHA

  • ALA

Omega-3 fatty acids are well documented for their triglyceride-lowering benefits.

Omega-3 is available as prescription formulations and dietary over-the-counter supplements, the most common being fish oil. You can also get omega-3 through food, such as fish, seafood, nuts and seeds, and plant oils (flaxseed, walnut, canola, and soybean).

Prescription formulations include:

  • Lovaza

  • Vascepa

Common side effects of omega-3 include:

  • Gas and flatulence

  • Bloating

  • Diarrhea

  • Elevated LDL cholesterol levels

Soluble fibers

Soluble fiber can be found in food such as whole grains, fruit, and vegetables or through supplements, the most popular ones containing psyllium husk.

Soluble fiber works by absorbing cholesterol-containing bile acids, leading to the clearance of LDL cholesterol from the blood, which lowers LDL cholesterol in your body.

Generally, consuming soluble fiber through food is not likely to cause any serious side effects or adverse reactions. However, consuming a soluble fiber supplement, such as those that contain psyllium husk, may have some side effects, including:

  • Bloating

  • Flatulence

  • Nausea

  • Stomach pain

  • Diarrhea

  • Constipation

Soluble fiber supplements may interfere with the effectiveness of some cholesterol-lowering medications. It is important to speak with your doctor before taking any.

Risks of over-the-counter cholesterol medication and supplements

In most cases, taking over-the-counter medications and supplements is generally safe and effective when you follow the directions on the label and as directed by your healthcare provider.

However, there is always a risk involved in using OTC medications and supplements, including:

  • Improper self-diagnosis or taking a medication that is not right for you

  • Incorrect and/or inappropriate dosage

  • Adverse drug reactions and interactions

  • Allergic reactions

  • Incorrect duration of use

It is important to consult with your pharmacist or doctor before taking any over-the-counter cholesterol medications or supplements and to follow the instructions on the drug label.

Do not stop taking your prescribed cholesterol-lowering medication, unless advised to do so by your healthcare provider. If illness occurs when taking over-the-counter medications, seek medical advice.

The lowdown

Treatment for high cholesterol will be on a case-by-case basis, depending on your cardiac risk and cholesterol goals.

However, lifestyle changes will always be the first place to start lowering your cholesterol levels. Medications, whether prescription or over-the-counter, will be the next line of defense if lifestyle changes are not enough. Every medication, whether prescribed or over-the-counter, comes with benefits, but they also come with side effects and risks, so a medication that works for someone else may not necessarily work for you.

It is important to speak with a health professional first when it comes to treating your high cholesterol.

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