When to Medicate for Hyperlipidemia: Common Medications and Side Effect

Hyperlipidemia is a condition characterized by abnormally high levels of fats (lipids) in the blood, such as cholesterol and triglycerides. It can increase the risk of cardiovascular diseases, such as heart attack and stroke, by causing plaque buildup in the arteries. Hyperlipidemia can be caused by genetic factors, lifestyle factors, or underlying diseases. Depending on the type and severity of hyperlipidemia, different treatments may be needed to lower the blood lipid levels and prevent complications.

In this article, you will learn about:

  • General “Hyperlipidemia” can be divided into three types
  • In which cases does hyperlipidemia require medication?
  • Five Common Lipid-Lowering Medications
    • Statin Drugs
    • Cholesterol Absorption Inhibitors
    • Bile Acid Binding Resins
    • Fibrates
    • Niacin
  • Statin Drugs Often Interact with Certain Foods
    • Avoid Simultaneous Intake with Oats
    • Avoid Simultaneous Intake with Red Yeast Rice
    • Do Not Consume Grapefruit Juice
    • Avoid High-Intensity Eccentric Exercises
  • Frequently Asked Questions
    • What are the symptoms of hyperlipidemia?
    • What are the risk factors for hyperlipidemia?
    • What are the possible complications of hyperlipidemia?

Table of Contents

General “Hyperlipidemia” can be divided into three types:

Hyperlipidemia is a condition where the levels of lipids (fats) in the blood are abnormally high. Lipids are essential for many bodily functions, such as energy production, hormone synthesis, and cell membrane formation. However, excessive lipids can accumulate in the blood vessels and cause atherosclerosis, which increases the risk of cardiovascular diseases, such as coronary artery disease, stroke, and peripheral artery disease.

There are different types of lipids in the blood, such as cholesterol, triglycerides, phospholipids, and free fatty acids. Among them, cholesterol and triglycerides are the most commonly measured and used to diagnose hyperlipidemia. Based on the levels of these two lipids, hyperlipidemia can be divided into three types:

Type Description Causes Complications
Hypercholesterolemia Mainly elevated low-density lipoprotein cholesterol (LDL-C), also known as “bad” cholesterol. LDL-C transports cholesterol from the liver to the tissues and can deposit in the blood vessel walls. Genetic factors, diet high in saturated and trans fats, obesity, diabetes, hypothyroidism, kidney disease, etc. Atherosclerosis, coronary artery disease, angina, heart attack, stroke, etc.
Hypertriglyceridemia Mainly elevated triglycerides, which are the main form of stored fat in the body. Triglycerides are broken down into free fatty acids and glycerol to provide energy or synthesize other lipids. Diet high in carbohydrates and alcohol, obesity, diabetes, metabolic syndrome, pancreatitis, kidney disease, etc. Pancreatitis, fatty liver, insulin resistance, diabetes, etc.
Mixed hyperlipidemia Both LDL-C and triglycerides are elevated, often accompanied by low levels of high-density lipoprotein cholesterol (HDL-C), also known as “good” cholesterol. HDL-C transports excess cholesterol from the tissues to the liver for excretion. Genetic factors, diet high in calories, fats, and sugars, obesity, diabetes, metabolic syndrome, etc. Atherosclerosis, coronary artery disease, heart attack, stroke, pancreatitis, etc.

In which cases does hyperlipidemia require medication?

Hyperlipidemia is a condition where the blood contains abnormally high levels of lipids, such as cholesterol and triglycerides. These lipids can accumulate in the walls of the arteries, causing atherosclerosis and increasing the risk of cardiovascular diseases. Therefore, it is important to control the lipid levels and prevent complications.

However, not all cases of hyperlipidemia require medication. In the early stages, physicians may assess the patient’s overall health status, including the presence of other risk factors, such as hypertension, diabetes, obesity, smoking, and family history. Based on the assessment, the physician may not immediately prescribe medication, especially if there are no other comorbidities. Instead, the physician may advise the patient to adopt lifestyle modifications, such as a low-fat, high-fiber diet, regular exercise, weight management, and quitting smoking. These measures can help lower the lipid levels naturally and improve the cardiovascular health.

An observation period of 3-6 months is often set for patients with mild to moderate hyperlipidemia who are undergoing lifestyle modifications. If the patient can control lipid levels through diet, regular exercise, and eliminating unhealthy habits during this period, there may be no need for medication. However, if lipid levels do not improve or worsen after the observation period, the physician may recommend medication as an adjunct therapy. The choice of medication depends on the type and severity of hyperlipidemia, the patient’s response, and the potential side effects.

Five Common Lipid-Lowering Medications:

Lipid-lowering medications are drugs that can reduce the levels of cholesterol and/or triglycerides in the blood. They work by different mechanisms, such as inhibiting the synthesis, absorption, or reabsorption of lipids, or increasing their breakdown or excretion. They are effective in lowering the risk of cardiovascular events, such as heart attack and stroke, in patients with hyperlipidemia. However, they also have some side effects that need to be monitored. The following are five common types of lipid-lowering medications:

Statin Drugs:

Statin drugs are the most widely used and effective lipid-lowering medications. They include Atorvastatin, Fluvastatin, Pravastatin, Rosuvastatin, and Simvastatin. Statins inhibit the key enzyme HMG-CoA reductase, which is involved in the synthesis of cholesterol in the liver. By reducing cholesterol synthesis, statins lower the levels of low-density lipoprotein (LDL) cholesterol, also known as the “bad” cholesterol, in the blood. They also increase the levels of high-density lipoprotein (HDL) cholesterol, also known as the “good” cholesterol, which can help remove excess cholesterol from the arteries. Statins have been shown to reduce the risk of cardiovascular diseases and strokes by 20-40% in patients with hyperlipidemia.

Common side effects of statins include nausea, fatigue, headache, and occasional muscle soreness. These are usually mild and transient, and can be alleviated by adjusting the dose or switching to another statin. However, in rare cases, statins can cause serious side effects, such as elevation of liver enzymes, which can indicate liver damage, or rhabdomyolysis, which is a breakdown of muscle tissue that can lead to kidney failure. Rhabdomyolysis is characterized by dark brown urine, muscle weakness, and pain. Patients who take statins should have regular blood tests to monitor their liver function and muscle enzymes, and report any symptoms of rhabdomyolysis to their physician immediately.

Cholesterol Absorption Inhibitors:

Cholesterol absorption inhibitors are another type of lipid-lowering medications that can be used alone or in combination with statins. Ezetimibe is the only drug in this category that is currently available. It works by blocking the absorption of dietary cholesterol in the small intestine, thereby reducing the amount of cholesterol that enters the bloodstream. It can lower the LDL cholesterol levels by 15-20%. It can also slightly increase the HDL cholesterol levels and lower the triglyceride levels. Cholesterol absorption inhibitors can enhance the effect of statins, especially in patients who have high cholesterol absorption or low cholesterol synthesis.

Common side effects of cholesterol absorption inhibitors include headache, muscle pain, and diarrhea. These are usually mild and resolve with time. However, in rare cases, cholesterol absorption inhibitors can also cause elevation of liver enzymes or rhabdomyolysis, especially when used with statins. Therefore, patients who take cholesterol absorption inhibitors should also have regular blood tests and report any symptoms of liver or muscle damage.

Bile Acid Binding Resins:

Bile acid binding resins are another type of lipid-lowering medications that can be used alone or in combination with statins. Cholestyramine Resin is a common drug in this category. It works by binding to bile acids in the gastrointestinal tract, preventing their reabsorption into the bloodstream. Bile acids are substances that are produced by the liver from cholesterol and help digest fats. By increasing the excretion of bile acids, bile acid binding resins reduce the amount of cholesterol that is available for the liver to make more bile acids. This stimulates the liver to use more cholesterol from the blood, lowering the LDL cholesterol levels by 15-30%. Bile acid binding resins can also lower the triglyceride levels, but they may increase the HDL cholesterol levels only slightly or not at all.

This type of drug may cause gastrointestinal side effects, such as constipation, bloating, indigestion, and nausea. These can be reduced by increasing the fluid and fiber intake, taking the drug with meals, and starting with a low dose and gradually increasing it. Bile acid binding resins may also interfere with the absorption of other drugs, such as warfarin, thyroid hormones, and some vitamins. Therefore, patients who take bile acid binding resins should take their other medications at least one hour before or four hours after taking the resin.

Fibrates:

Fibrates are another type of lipid-lowering medications that are mainly used to treat high triglyceride levels. Fenofibrate and Gemfibrozil are common drugs in this category. They work by activating a protein called peroxisome proliferator-activated receptor alpha (PPAR-alpha), which regulates the metabolism of lipids in the liver and muscles. By activating PPAR-alpha, fibrates increase the breakdown of triglycerides and the production of HDL cholesterol. They can lower the triglyceride levels by 20-50% and increase the HDL cholesterol levels by 10-20%. They can also lower the LDL cholesterol levels by 5-20%, but this effect is variable and depends on the initial triglyceride levels. Fibrates have been shown to reduce the risk of cardiovascular events, especially in patients with high triglyceride and low HDL cholesterol levels.

Common side effects of fibrates include stomach upset, headache, and rash. These are usually mild and subside with time. However, in rare cases, fibrates can also cause elevation of liver enzymes, gallstones, or rhabdomyolysis, especially when used with statins. Therefore, patients who take fibrates should also have regular blood tests and report any symptoms of liver, gallbladder, or muscle damage.

Niacin:

Niacin, also known as vitamin B3, is another type of lipid-lowering medication that can be used alone or in combination with statins. It works by inhibiting the production and release of very-low-density lipoprotein (VLDL) cholesterol, which is a precursor of LDL cholesterol, in the liver. It can lower the LDL cholesterol levels by 5-25%, the triglyceride levels by 20-50%, and increase the HDL cholesterol levels by 15-35%. Niacin has been shown to reduce the risk of cardiovascular events, especially in patients with low HDL cholesterol levels.

Common side effects of niacin include flushing, itching, burning, and tingling sensations in the skin, especially in the face and neck. These are caused by the dilation of blood vessels and can be reduced by taking aspirin or ibuprofen before taking niacin, taking niacin with food, and starting with a low dose and gradually increasing it. Other side effects of niacin include stomach upset, headache, dizziness, and blurred vision. These are usually mild and resolve with time. However, in rare cases, niacin can also cause elevation of blood glucose, uric acid, or liver enzymes, or rhabdomyolysis, especially when used with statins. Therefore, patients who take niacin should also have regular blood tests and report any symptoms of diabetes, gout, liver, or muscle damage.

Statin Drugs Often Interact with Certain Foods:

Avoid Simultaneous Intake with Oats:

Oats, rich in dietary fiber, can reduce the absorption of statin drugs. It’s advised to consume oats 2-4 hours apart from statin drugs to avoid interference. Dietary fiber can bind to statins in the gastrointestinal tract and prevent them from entering the bloodstream. A study found that oat consumption reduced the bioavailability of simvastatin by 12.5%.

Avoid Simultaneous Intake with Red Yeast Rice:

Red yeast rice supplements may increase the concentration of statins in the blood, leading to a higher risk of side effects. This is because red yeast rice contains monacolin K, a natural compound that is identical to lovastatin, a type of statin. Taking red yeast rice with statins can result in excessive lowering of cholesterol levels and increased risk of liver damage, muscle pain, or kidney failure. Therefore, it is recommended to avoid red yeast rice supplements when taking statins.

Do Not Consume Grapefruit Juice:

Grapefruit juice interacts with statins, affecting their metabolism and increasing the risk of side effects. It is recommended to avoid grapefruit juice entirely when taking statins. Grapefruit juice contains compounds called furanocoumarins, which inhibit an enzyme called CYP3A4 in the liver and intestines. This enzyme is responsible for breaking down statins and other drugs. When CYP3A4 is inhibited, more statins enter the bloodstream and stay longer, increasing the potential for adverse reactions. 

Avoid High-Intensity Eccentric Exercises:

High-intensity eccentric exercises,, can increase the risk of statin-induced myopathy. This is a condition where statins cause muscle damage, pain, weakness, or inflammation. Low-intensity exercises like jogging, brisk walking, or swimming are recommended for individuals taking statins. Eccentric exercises involve lengthening of the muscle fibers under tension, which can cause more microtrauma and inflammation than concentric exercises, where the muscle fibers shorten. Statins may impair the repair and regeneration of muscle tissue after eccentric exercise, leading to more severe and prolonged muscle damage. A study found that statin users who performed eccentric exercise had higher levels of creatine kinase, a marker of muscle injury, than non-users.

Frequently Asked Questions

What are the symptoms of hyperlipidemia?

Hyperlipidemia is a condition where the levels of lipids (fats) in the blood are too high. This can increase the risk of cardiovascular diseases and other health problems. However, hyperlipidemia often does not cause any noticeable symptoms until it is severe or has caused damage to the organs. Some of the possible signs and symptoms of hyperlipidemia are:

  • Chest pain (angina): This is a feeling of pressure, tightness, or discomfort in the chest, usually triggered by physical or emotional stress. It occurs when the blood flow to the heart is reduced due to narrowed or blocked arteries.
  • Heart palpitations: This is a sensation of the heart beating too fast, too slow, or irregularly. It can be caused by various factors, such as stress, caffeine, medication, or heart rhythm disorders. Hyperlipidemia can also contribute to heart palpitations by affecting the electrical signals in the heart.
  • Xanthomas: These are yellowish, raised, fatty deposits that form on the skin, especially around the eyes, elbows, knees, or buttocks. They are caused by high levels of cholesterol or triglycerides in the blood, which accumulate in the skin cells.
  • Pancreatitis: This is an inflammation of the pancreas, a gland that produces digestive enzymes and hormones. It can cause severe abdominal pain, nausea, vomiting, fever, and diarrhea. One of the possible causes of pancreatitis is high levels of triglycerides in the blood, which can damage the pancreas.

What are the risk factors for hyperlipidemia?

Hyperlipidemia can be influenced by both modifiable and non-modifiable risk factors. Modifiable risk factors are those that can be changed or controlled by lifestyle choices or medical treatment. Non-modifiable risk factors are those that cannot be changed, such as age, gender, or genetics. Some of the common risk factors for hyperlipidemia are:

Modifiable Risk Factors Non-Modifiable Risk Factors
  • Poor diet: Eating foods that are high in saturated fat, trans fat, cholesterol, or sugar can raise the levels of lipids in the blood. Examples of such foods are red meat, butter, cheese, pastries, candies, and soft drinks.
  • Lack of exercise: Physical activity can help lower the levels of lipids in the blood by increasing the metabolism, burning calories, and improving the function of the blood vessels. The American Heart Association recommends at least 150 minutes of moderate-intensity aerobic exercise or 75 minutes of vigorous-intensity aerobic exercise per week for adults.
  • Obesity: Having excess body weight, especially around the waist, can increase the levels of lipids in the blood by altering the production and regulation of hormones and enzymes that affect lipid metabolism. A healthy body mass index (BMI) for adults is between 18.5 and 24.9 kg/m2.
  • Smoking: Smoking can increase the levels of lipids in the blood by damaging the lining of the blood vessels, reducing the amount of oxygen in the blood, and increasing the production of free radicals that cause oxidative stress. Quitting smoking can improve the lipid profile and reduce the risk of cardiovascular diseases.
  • Diabetes: Diabetes is a condition where the blood sugar levels are too high due to insufficient or ineffective insulin, a hormone that regulates glucose metabolism. High blood sugar levels can increase the levels of lipids in the blood by impairing the function of the liver and the pancreas, which are involved in lipid metabolism. Managing diabetes with medication, diet, and exercise can help lower the levels of lipids in the blood.
  • Medication: Some medications can affect the levels of lipids in the blood by interfering with the synthesis, absorption, or excretion of lipids. Examples of such medications are steroids, oral contraceptives, beta-blockers, diuretics, and antiretroviral drugs. Consulting with a doctor before taking any medication can help prevent or minimize the adverse effects on the lipid profile.
  • Age: As people get older, their levels of lipids in the blood tend to increase due to changes in the hormone levels, body composition, and organ function. The risk of hyperlipidemia increases after the age of 45 for men and after the age of 55 for women.
  • Gender: Men tend to have higher levels of lipids in the blood than women before menopause, due to the protective effect of estrogen, a female hormone that lowers the levels of lipids in the blood. However, after menopause, women tend to have higher levels of lipids in the blood than men, due to the decline of estrogen and the increase of androgen, a male hormone that raises the levels of lipids in the blood.
  • Genetics: Some people inherit genes that predispose them to have high levels of lipids in the blood, regardless of their lifestyle or environmental factors. This is called familial hyperlipidemia, which can be classified into different types based on the type and level of lipids that are elevated in the blood. Familial hyperlipidemia can increase the risk of early-onset cardiovascular diseases and requires medical treatment.

What are the possible complications of hyperlipidemia?

Hyperlipidemia can lead to serious complications if left untreated, as the excess lipids in the blood can accumulate in the walls of the arteries and form plaques, which are hard, thick, and narrow deposits that obstruct the blood flow. This condition is called atherosclerosis, which can affect any artery in the body and cause various diseases depending on the location and severity of the blockage. Some of the possible complications of hyperlipidemia are:

  • Heart disease: This is a general term for any disorder that affects the heart or the blood vessels that supply blood to the heart. Atherosclerosis can reduce the blood flow to the heart and cause angina, myocardial infarction (heart attack), or heart failure. Heart disease is the leading cause of death worldwide.
  • Stroke: This is a sudden interruption of the blood flow to the brain, which can damage the brain cells and impair the brain function. Atherosclerosis can cause stroke by either blocking the arteries that supply blood to the brain (ischemic stroke) or rupturing the arteries and causing bleeding in the brain (hemorrhagic stroke). Stroke is the second leading cause of death and disability worldwide.
  • Peripheral artery disease: This is a narrowing or blockage of the arteries that supply blood to the limbs, especially the legs. Atherosclerosis can cause peripheral artery disease by reducing the blood flow to the muscles and tissues of the legs, which can cause pain, numbness, weakness, or ulceration. Peripheral artery disease can increase the risk of infection, gangrene, and amputation.

Reference

  1. Cholesterol Treatment Trialists’ (CTT) Collaboration. (2010). Efficacy and safety of more intensive lowering of LDL cholesterol: a meta-analysis of data from 170,000 participants in 26 randomised trials. The Lancet, 376(9753), 1670-1681. 
  2. Deichmann, R., Lavie, C., & Andrews, S. (2010). Coenzyme Q10 and statin-induced mitochondrial dysfunction. Ochsner Journal, 10(1), 16-21. 
  3. Garg, A., & Grundy, S. M. (1990). Management of dyslipidemia in NIDDM. Diabetes Care, 13(2), 153-169. 
  4. Liu, J., Zhang, J., Shi, Y., Grimsgaard, S., Alraek, T., & Fønnebø, V. (2006). Chinese red yeast rice (Monascus purpureus) for primary hyperlipidemia: a meta-analysis of randomized controlled trials. Chinese Medicine, 1(1), 4. 
  5. Muldoon, M. F., Barger, S. D., Ryan, C. M., Flory, J. D., Lehoczky, J. P., Matthews, K. A., & Manuck, S. B. (2000). Effects of lovastatin on cognitive function and psychological well-being. The American Journal of Medicine, 108(7), 538-546.

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