Antihyperlipidemic Drugs: Understanding Options to Lower High Cholesterol and Triglyceride Levels

Antihyperlipidemic Drugs
Antihyperlipidemic Drugs


What are Antihyperlipidemic Drugs?

Antihyperlipidemic drugs, also known as lipid-lowering drugs or hypolipidemic drugs, are medications that help to lower abnormally high levels of lipids (fats) in the blood. The primary lipids targeted are low-density lipoprotein (LDL) cholesterol, very low-density lipoprotein (VLDL) triglycerides, and total cholesterol. Abnormal elevation of these lipids is known as hyperlipidemia. These drugs help to reduce the risk of cardiovascular disease by lowering cholesterol and triglyceride levels.

Statins

Statins are the most commonly prescribed class of antihyperlipidemic drugs. They work by blocking an enzyme called HMG-CoA reductase, which the liver needs to produce cholesterol. Popular statin drugs include atorvastatin (Lipitor), rosuvastatin (Crestor), simvastatin (Zocor), pravastatin (Pravachol), lovastatin (Mevacor), and fluvastatin (Lescol). Statins effectively lower total cholesterol and LDL cholesterol levels by 20-60%. They also moderately reduce triglyceride levels. Side effects of statins are usually mild but may include muscle pain or weakness. Rarely, severe muscle damage called rhabdomyolysis can occur. Statins also increase the risk of diabetes mellitus slightly.

Fibrates

Fibrates like fenofibrate (Tricor) and gemfibrozil (Lopid) work by activating Antihyperlipidemic Drugs -activated receptor alpha (PPARĪ±). This lowers triglyceride levels by 20-50% and raises high-density lipoprotein (HDL) cholesterol levels slightly. Although fibrates do lower LDL cholesterol somewhat, they are not as effective as statins. Side effects may include digestive issues like nausea, gas, and diarrhea. Fibrates can also interact with some other medications. They are generally used when triglyceride levels are very high (>500 mg/dL) or in combination with statins.

Niacin

Niacin supplements contain vitamin B3, which is a type of nicotinic acid. It works through various mechanisms like inhibiting hormone-sensitive lipase in adipose tissue and liver. This helps lower LDL cholesterol levels by 10-25%, triglyceride levels by 20-50%, and raises HDL cholesterol levels by 15-35%. However, niacin commonly causes unpleasant side effects like flushing, itching, and gastric upset when taken in high doses. Liver injury can also occur rarely. Niacin should not be used without medical supervision due to its side effect profile and potential drug interactions. Combination niacin/statin pills are available for better safety and tolerability.

Cholesterol Absorption Inhibitors

Ezetimibe (Zetia) works by inhibiting cholesterol absorption from the small intestine. It lowers LDL cholesterol levels modestly by 15-20% when taken alone and up to 55% in combination with statins. Ezetimibe also lowers triglyceride levels to some extent. It is generally well-tolerated with few significant side effects. Combination pills of ezetimibe and a statin such as ezetimibe/simvastatin (Vytorin) offer greater LDL lowering effects. Cholesterol absorption inhibitors are used as additional therapy if LDL goals are not met with a statin alone.

PCSK9 Inhibitors

Proprotein convertase subtilisin/kexin type 9 (PCSK9) inhibitors offer a powerful new option for patients with very high cholesterol levels. PCSK9 promotes LDL receptor breakdown in the liver, thereby reducing clearance of LDL from the blood. PCSK9 inhibitors like evolocumab (Repatha) and alirocumab (Praluent) bind to and inhibit PCSK9 activity. This allows more LDL receptors to recycle, significantly increasing the removal of LDL cholesterol from the blood. PCSK9 inhibitors lower LDL by up to 60% as monotherapy and up to 75-80% when used along with statins. Common side effects include influenza-like illness and reactions at the injection site. More research is still needed on long term safety and cardiovascular outcomes. PCSK9 inhibitors are generally reserved for very high risk patients or those unable to reach cholesterol goals using other treatments.

Bile Acid Sequestrants

Bile acid sequestrants work by binding to bile acids in the intestine. This prevents their reabsorption and forces the liver to use cholesterol to produce more bile acids. Popular bile acid sequestrants include colesevelam (Welchol), colestipol (Colestid), and colestipol (Colestipol). They lower LDL cholesterol by 15-30% but have significant side effects like bloating, gas, and constipation due to interruption of bile acid recycling. Bile acid sequestrants must be taken with a full glass of water and many find the side effects intolerable. They are generally reserved for use with statins, fibrates or niacin when more LDL lowering is needed.

Injectable Medications

For patients who cannot tolerate oral medications, are unable to adhere to daily pills, or require additional therapy, injectable options are available. Alirocumab (Praluent) and evolocumab (Repatha), which are PCSK9 inhibitors, are given as self-administered subcutaneous injections every two weeks or monthly. Inclisiran, an interfering RNA therapy targeting PCSK9 mRNA, is administered as two initial subcutaneous doses followed by injections every six months for maintenance. These long-acting injectable therapies offer significant LDL lowering with minimal side effects. However, they generally result in higher treatment costs than oral pills.

Making Lifestyle Changes for Heart Health

While medications play an important role in managing high cholesterol and triglyceride levels, non-drug factors can also significantly impact lipid levels. Even modest weight loss through diet and exercise can reduce cardiovascular disease risk factors. Limiting consumption of saturated and trans fats, added sugars, and excess alcohol is recommended. Following a Mediterranean-style diet rich in whole grains, fruits, vegetables, legumes, and healthy fats like olive oil may help lower LDL cholesterol levels. Quitting smoking and limiting stress are additional heart-healthy lifestyle steps worth adopting. Making positive changes like these, in addition to an antihyperlipidemic treatment plan prescribed by a doctor, provides the best chance at reaching lipid goals.

Various classes of antihyperlipidemic drugs targeting different pathways are available to help lower cholesterol and triglyceride levels when lifestyle modifications alone are not effective. Close medical monitoring is needed due to potential side effects and drug interactions.

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Priya Pandey is a dynamic and passionate editor with over three years of expertise in content editing and proofreading. Holding a bachelor's degree in biotechnology, Priya has a knack for making the content engaging. Her diverse portfolio includes editing documents across different industries, including food and beverages, information and technology, healthcare, chemical and materials, etc. Priya's meticulous attention to detail and commitment to excellence make her an invaluable asset in the world of content creation and refinement.(LinkedIn- https://www.linkedin.com/in/priya-pandey-8417a8173/)

 

 

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