Medications for high cholesterol
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Common Medications for High Cholesterol: Statins, Bile-Acid Sequestrants, and More
Statins are the most widely used and effective medications for lowering high cholesterol, especially low-density lipoprotein (LDL) cholesterol. Statins work by inhibiting an enzyme involved in cholesterol production in the liver. Simvastatin and atorvastatin are among the most commonly prescribed statins, with the majority of adults using cholesterol-lowering medication reporting statin use alone 56. Statins can reduce total and LDL cholesterol by 15-35% 1.
Other medications include bile-acid sequestrants (such as cholestyramine and colestipol), which bind bile acids in the intestine and help remove cholesterol from the body. Nicotinic acid (niacin) is another option, particularly for patients with both high LDL cholesterol and high triglycerides 1. For severe cases, combinations of statins, nicotinic acid, and bile-acid sequestrants may be used for greater effect 1.
New and Emerging Cholesterol-Lowering Drugs: PCSK9 Inhibitors, CETP Inhibitors, and ASGR1 Targeting
Recent advances have led to the development of new drug classes. PCSK9 inhibitors, which can be administered orally or by injection, target a protein that affects LDL receptor levels, helping to further lower LDL cholesterol when statins are not enough 2. There is growing interest in developing more oral PCSK9 inhibitors for easier administration and fewer side effects 2.
CETP inhibitors, such as obicetrapib, are another new class. When combined with high-intensity statins, obicetrapib can significantly lower LDL cholesterol (by up to 51%) and increase HDL cholesterol, offering another option for patients at high cardiovascular risk who do not reach their cholesterol goals with statins alone 7.
Targeting ASGR1, a liver receptor, is a novel approach that promotes cholesterol excretion from the body. Anti-ASGR1 antibodies have shown promise in lowering cholesterol and may work well in combination with existing drugs like statins and ezetimibe 9.
Effectiveness and Use of Cholesterol-Lowering Medications
The use of prescription cholesterol-lowering medications has increased over time, especially among adults aged 60 and older 35. In the United States, about one in four adults aged 40 and over reported using these medications by 2012, with statins being the most common 5. The effectiveness of these medications in reducing cardiovascular disease risk is well established, especially when combined with lifestyle changes 56.
However, many people with high cholesterol remain undiagnosed or untreated, and the percentage of those who achieve effective cholesterol control is still relatively low in many countries 10. This highlights the need for better screening and treatment strategies worldwide 10.
Special Considerations: Age, Race/Ethnicity, and Individualized Treatment
Older adults often have higher cholesterol levels and are at greater risk for cardiovascular disease, but the benefits and risks of cholesterol-lowering medications must be carefully weighed, especially in the very old or those with frailty or disability. Treatment decisions should be individualized based on the patient's overall health and functional status 8.
There are also differences in how cholesterol-lowering treatments are recommended and prescribed across racial and ethnic groups. Non-Hispanic Black and Hispanic patients are more likely to receive lifestyle change recommendations rather than medication, especially at younger ages, which may reflect disparities in care 4.
Conclusion
Statins remain the mainstay of cholesterol-lowering therapy, with other options like bile-acid sequestrants, niacin, PCSK9 inhibitors, CETP inhibitors, and new targets like ASGR1 expanding the range of available treatments. While medication use is increasing, many people with high cholesterol are still not effectively treated. Individualized care, attention to disparities, and ongoing development of new therapies are key to improving cholesterol management and reducing cardiovascular risk.
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