Lipid-lowering agent

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Fat reducing drug

title: "Lipid-lowering agent" type: doc version: 1 created: 2026-02-28 author: "Wikipedia contributors" status: active scope: public tags: ["lipid-lowering-agents"] description: "Fat reducing drug" topic_path: "general/lipid-lowering-agents" source: "https://en.wikipedia.org/wiki/Lipid-lowering_agent" license: "CC BY-SA 4.0" wikipedia_page_id: 0 wikipedia_revision_id: 0

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Lipid-lowering agents, also sometimes referred to as hypolipidemic agents, cholesterol-lowering drugs, or antihyperlipidemic agents are a diverse group of pharmaceuticals that are used to lower the level of lipids and lipoproteins, such as cholesterol, in the blood (hyperlipidemia). The American Heart Association recommends the descriptor 'lipid lowering agent' be used for this class of drugs rather than the term 'hypolipidemic'.

Classes

The several classes of lipid lowering drugs may differ in both their impact on the cholesterol profile and adverse effects. For example, some may lower low density lipoprotein (LDL) levels more so than others, while others may preferentially increase high density lipoprotein (HDL). Clinically, the choice of an agent depends on the patient's cholesterol profile, cardiovascular risk, and the liver and kidney functions of the patient, evaluated against the balancing of risks and benefits of the medications. In the United States, this is guided by the evidence-based guideline most recently updated in 2018 by the American College of Cardiology & American Heart Association.

Established

  • Statins (HMG-CoA reductase inhibitors) are particularly well suited for lowering LDL, the cholesterol with the strongest links to vascular diseases. In studies using standard doses, statins have been found to lower LDL-C by 18% to 55%, depending on the specific statin being used. A risk exists of muscle damage (myopathy and rhabdomyolysis) with statins. Hypercholesterolemia is not a risk factor for mortality in persons older than 70 years and risks from statin drugs are more increased after age 85.
  • Fibrates are indicated for hypertriglyceridemia. Fibrates typically lower triglycerides by 20% to 50%. Level of the good cholesterol HDL is also increased. Fibrates may decrease LDL, though generally to a lesser degree than statins. Similar to statins, the risk of muscle damage exists.
  • Nicotinic acid, like fibrates, is also well suited for lowering triglycerides by 20–50%. It may also lower LDL by 5–25% and increase HDL by 15–35%. Niacin may cause hyperglycemia and may also cause liver damage. The niacin derivative acipimox is also associated with a modest decrease in LDL. Introduced in 1955.
  • Bile acid sequestrants (resins, e.g. cholestyramine) are particularly effective for lowering LDL-C by sequestering the cholesterol-containing bile acids released into the intestine and preventing their reabsorption from the intestine. It decreases LDL by 15–30% and raises HDL by 3–5%, with little effect on triglycerides, but can cause a slight increase. Bile acid sequestrants may cause gastrointestinal problems and may also reduce the absorption of other drugs and vitamins from the gut.
  • Ezetimibe is a selective inhibitor of dietary cholesterol absorption.
  • Lomitapide is a microsomal triglyceride transfer protein inhibitor.
  • PCSK9 inhibitors are monoclonal antibodies for refractory cases. (e.g. Evolocumab, Inclisiran) They are used in combination with statins.
  • Probucol decreases LDL independently of the LDL receptor, and decreases HDL-C by enhancing its liver receptor and reducing ABCA1-dependent transport. The reduction of HDL-C, combined with early uncertainties around its mechanism of action, has historically lead to its discontinuation and replacement by statins in Western countries. However, instead of lowering reverse cholesterol transport by HDL particles, probucol seems to increase it. Introduced in the 1970s. It predated the statins by about a decade.

Alternative

  • Lecithin has been shown to effectively decrease cholesterol concentration by 33%, lower LDL by 38% and increase HDL by 46%.
  • Phytosterols may be found naturally in plants. Similar to ezetimibe, phytosterols reduce the absorption of cholesterol in the gut, so they are most effective when consumed with meals. However, their precise mechanism of action differs from ezetimibe.
  • Omega-3 supplements taken at high doses can reduce levels of triglycerides. They are associated with a very modest increase in LDL (~5%).
  • Choline
  • Pycnogenol
  • Berberine
  • Red yeast rice is the natural source from which statins were discovered, but the FDA currently disallows any RYR with significant amounts of statin to be sold as a dietary supplement
  • Boswellia serrata
  • L-arginine may enhance the effects of a Statin, but will not lead to a reduction in cholesterol alone.
  • Flaxseed oil

Research

Investigational classes of hypolipidemic agents:

References

References

  1. (2019). "Management of Blood Cholesterol". JAMA.
  2. (February 2014). "Ten Things Physicians and Patients Should Question". AMDA – The Society for Post-Acute and Long-Term Care Medicine.
  3. Koren MJ, Scott R, Kim JB et al Lancet 2012; 380:1995-2006
  4. Gugliano RP, Desai NR, Kohli P et al Lancet 2012; 380:2007-17
  5. (August 2015). "Did we abandon probucol too soon?". Current Opinion in Lipidology.
  6. (February 2021). "New Horizons for Probucol, an Old, Mysterious Drug". Journal of Atherosclerosis and Thrombosis.
  7. (1995). "Clinical evaluation of lecithin as a lipid-lowering agent". Phytotherapy Research.
  8. (2018-05-01). "Omega-3 Supplements: In Depth".
  9. (December 2012). "A randomized controlled trial investigating the effect of Pycnogenol and BacopaCDRI08 herbal medicines on cognitive, cardiovascular, and biochemical functioning in cognitively healthy elderly people: the Australian Research Council Longevity Intervention (ARCLI) study protocol (ANZCTR12611000487910)". Nutrition Journal.
  10. (May 2005). "Berberine--a novel approach to cholesterol lowering.". Expert Opinion on Investigational Drugs.
  11. (October 2017). "Efficacy of Berberine Alone and in Combination for the Treatment of Hyperlipidemia: A Systematic Review". Journal of Evidence-Based Complementary & Alternative Medicine.
  12. (9 February 2021). "Red Yeast Rice for Hypercholesterolemia: JACC Focus Seminar". Journal of the American College of Cardiology.
  13. "Pharmanex Inc. v. Shalala, United States District Court, D. Utah, Central Division Mar 1, 2001 Case No. 2:97CV262K".
  14. (2014). "Effect of Boswellia serrata supplementation on blood lipid, hepatic enzymes and fructosamine levels in type2 diabetic patients". Journal of Diabetes and Metabolic Disorders.
  15. (May 2009). "L-Arginine enhances the triglyceride-lowering effect of simvastatin in patients with elevated plasma triglycerides". Nutrition Research (New York, N.Y.).
  16. (3 February 2012). "Flaxseed dietary fibers lower cholesterol and increase fecal fat excretion, but magnitude of effect depend on food type.". Nutrition & Metabolism.
  17. Pollack, Andrew (29 January 2013) [https://www.nytimes.com/2013/01/30/business/fda-approves-genetic-drug-to-treat-rare-disease.html F.D.A. Approves Genetic Drug to Treat Rare Disease] The New York Times, Retrieved 31 January 2013
  18. Staff (29 January 2013) [https://web.archive.org/web/20130202205414/http://www.fda.gov/NewsEvents/Newsroom/PressAnnouncements/ucm337195.htm FDA approves new orphan drug Kynamro to treat inherited cholesterol disorder] U.S. Food and Drug Administration, Retrieved 31 January 2013

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