Lipid-lowering agent

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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'.

Contents

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. [1]

Established

Alternative

Research

Investigational classes of hypolipidemic agents:

See also

Related Research Articles

High-density lipoprotein (HDL) is one of the five major groups of lipoproteins. Lipoproteins are complex particles composed of multiple proteins which transport all fat molecules (lipids) around the body within the water outside cells. They are typically composed of 80–100 proteins per particle. HDL particles enlarge while circulating in the blood, aggregating more fat molecules and transporting up to hundreds of fat molecules per particle.

<span class="mw-page-title-main">Low-density lipoprotein</span> One of the five major groups of lipoprotein

Low-density lipoprotein (LDL) is one of the five major groups of lipoprotein that transport all fat molecules around the body in extracellular water. These groups, from least dense to most dense, are chylomicrons, very low-density lipoprotein (VLDL), intermediate-density lipoprotein (IDL), low-density lipoprotein (LDL) and high-density lipoprotein (HDL). LDL delivers fat molecules to cells. LDL is involved in atherosclerosis, a process in which it is oxidized within the walls of arteries.

<span class="mw-page-title-main">Statin</span> Class of drugs used to lower cholesterol levels

Statins are a class of medications that reduce illness and mortality in people who are at high risk of cardiovascular disease. They are the most commonly prescribed cholesterol-lowering drugs, and are also known as HMG-CoA reductase inhibitors.

<span class="mw-page-title-main">Fibrate</span> Class of chemical compounds

In pharmacology, the fibrates are a class of amphipathic carboxylic acids and esters. They are derivatives of fibric acid. They are used for a range of metabolic disorders, mainly hypercholesterolemia, and are therefore hypolipidemic agents.

<span class="mw-page-title-main">Hypercholesterolemia</span> High levels of cholesterol in the blood

Hypercholesterolemia, also called high cholesterol, is the presence of high levels of cholesterol in the blood. It is a form of hyperlipidemia, hyperlipoproteinemia, and dyslipidemia.

Dyslipidemia is a metabolic disorder characterized by abnormally high or low amounts of any or all lipids or lipoproteins in the blood. Dyslipidemia is a risk factor for the development of atherosclerotic cardiovascular diseases (ASCVD), which include coronary artery disease, cerebrovascular disease, and peripheral artery disease. Although dyslipidemia is a risk factor for ASCVD, abnormal levels don't mean that lipid lowering agents need to be started. Other factors, such as comorbid conditions and lifestyle in addition to dyslipidemia, is considered in a cardiovascular risk assessment. In developed countries, most dyslipidemias are hyperlipidemias; that is, an elevation of lipids in the blood. This is often due to diet and lifestyle. Prolonged elevation of insulin resistance can also lead to dyslipidemia. Likewise, increased levels of O-GlcNAc transferase (OGT) may cause dyslipidemia.

<span class="mw-page-title-main">Combined hyperlipidemia</span> Medical condition

Combined hyperlipidemia is a commonly occurring form of hypercholesterolemia characterised by increased LDL and triglyceride concentrations, often accompanied by decreased HDL. On lipoprotein electrophoresis it shows as a hyperlipoproteinemia type IIB. It is the most commonly inherited lipid disorder, occurring in around one in 200 persons. In fact, almost one in five individuals who develop coronary heart disease before the age of 60 have this disorder.

The bile acid sequestrants are a group of resins used to bind certain components of bile in the gastrointestinal tract. They disrupt the enterohepatic circulation of bile acids by combining with bile constituents and preventing their reabsorption from the gut. In general, they are classified as hypolipidemic agents, although they may be used for purposes other than lowering cholesterol. They are used in the treatment of chronic diarrhea due to bile acid malabsorption.

<span class="mw-page-title-main">Gemfibrozil</span> Medication

Gemfibrozil, sold under the brand name Lopid among others, is a medication used to treat abnormal blood lipid levels. It is generally less preferred than statins. Use is recommended together with dietary changes and exercise. It is unclear if it changes the risk of heart disease. It is taken by mouth.

<span class="mw-page-title-main">Ezetimibe</span> Medication used to treat high cholesterol

Ezetimibe is a medication used to treat high blood cholesterol and certain other lipid abnormalities. Generally it is used together with dietary changes and a statin. Alone, it is less preferred than a statin. It is taken by mouth. It is also available in the fixed combinations ezetimibe/simvastatin, ezetimibe/atorvastatin, ezetimibe/rosuvastatin, and ezetimibe/bempedoic acid.

Hyperlipidemia is abnormally high levels of any or all lipids or lipoproteins in the blood. The term hyperlipidemia refers to the laboratory finding itself and is also used as an umbrella term covering any of various acquired or genetic disorders that result in that finding. Hyperlipidemia represents a subset of dyslipidemia and a superset of hypercholesterolemia. Hyperlipidemia is usually chronic and requires ongoing medication to control blood lipid levels.

<span class="mw-page-title-main">Torcetrapib</span> Chemical compound

Torcetrapib was a drug being developed to treat hypercholesterolemia and prevent cardiovascular disease. Its development was halted in 2006 when phase III studies showed excessive all-cause mortality in the treatment group receiving a combination of atorvastatin (Lipitor) and torcetrapib.

<span class="mw-page-title-main">Fenofibrate</span> Drug of the fibrate class, mainly used to reduce cholesterol levels

Fenofibrate, is an oral medication of the fibrate class used to treat abnormal blood lipid levels. It is less commonly used compared than statins because it treats a different type of cholesterol abnormality to statins. While statins have strong evidence for reducing heart disease and death, there is evidence to suggest that fenofibrate also reduces the risk of heart disease and death. However, this seems only to apply to specific populations of people with elevated triglyceride levels and reduced high-density lipoprotein (HDL) cholesterol. Its use is recommended together with dietary changes.

Cholesterol absorption inhibitors are a class of compounds that prevent the uptake of cholesterol from the small intestine into the circulatory system. Most of these molecules are monobactams but show no antibiotic activity. An example is ezetimibe Another example is Sch-48461. The "Sch" is for Schering-Plough, where these compounds were developed. Phytosterols are also cholesterol absorption inhibitors.

<span class="mw-page-title-main">Familial hypercholesterolemia</span> Genetic disorder characterized by high cholesterol levels

Familial hypercholesterolemia (FH) is a genetic disorder characterized by high cholesterol levels, specifically very high levels of low-density lipoprotein cholesterol, in the blood and early cardiovascular diseases. The most common mutations diminish the number of functional LDL receptors in the liver or produce abnormal LDL receptors that never go to the cell surface to function properly. Since the underlying body biochemistry is slightly different in individuals with FH, their high cholesterol levels are less responsive to the kinds of cholesterol control methods which are usually more effective in people without FH. Nevertheless, treatment is usually effective.

<span class="mw-page-title-main">Colesevelam</span> Pharmaceutical drug

Colesevelam is a bile acid sequestrant administered orally. It was developed by GelTex Pharmaceuticals and later acquired by Genzyme. It is marketed in the U.S. by Daiichi Sankyo under the brand name Welchol and elsewhere by Genzyme as Cholestagel. In Canada, it is marketed by Valeant as Lodalis.

<span class="mw-page-title-main">PCSK9</span> Mammalian protein found in humans

Proprotein convertase subtilisin/kexin type 9 (PCSK9) is an enzyme encoded by the PCSK9 gene in humans on chromosome 1. It is the 9th member of the proprotein convertase family of proteins that activate other proteins. Similar genes (orthologs) are found across many species. As with many proteins, PCSK9 is inactive when first synthesized, because a section of peptide chains blocks their activity; proprotein convertases remove that section to activate the enzyme. The PCSK9 gene also contains one of 27 loci associated with increased risk of coronary artery disease.

<span class="mw-page-title-main">Lomitapide</span> Chemical compound

Lomitapide, sold under the brand name Juxtapid in the US and Lojuxta in the EU, is a medication used as a lipid-lowering agent for the treatment of familial hypercholesterolemia, developed by Aegerion Pharmaceuticals. It has been tested in clinical trials as single treatment and in combinations with atorvastatin, ezetimibe and fenofibrate.

Inclisiran, sold under the brand name Leqvio, is a medication used for the treatment of high low-density lipoprotein (LDL) cholesterol and for the treatment of people with atherosclerotic cardiovascular disease (ASCVD), ASCVD risk-equivalents, and heterozygous familial hypercholesterolemia (HeFH). It is a small interfering RNA (siRNA) that acts as an inhibitor of a proprotein convertase, specifically, inhibiting translation of the protein PCSK9.

Bempedoic acid, sold under the brand name Nexletol among others, is a medication for the treatment of hypercholesterolemia.

References

  1. ↑ Alenghat, Francis J.; Davis, Andrew M. (2019). "Management of Blood Cholesterol". JAMA. 321 (8): 800–801. doi:10.1001/jama.2019.0015. ISSN   0098-7484. PMC   6679800 . PMID   30715135.
  2. ↑ AMDA – The Society for Post-Acute and Long-Term Care Medicine (February 2014), "Ten Things Physicians and Patients Should Question", Choosing Wisely: an initiative of the ABIM Foundation , AMDA – The Society for Post-Acute and Long-Term Care Medicine, retrieved 20 April 2015.
  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. ↑ Wójcicki, J.; Pawlik, A.; Samochowiec, L.; Kaldo??Ska, M.; Myśliwiec, Z. (1995). "Clinical evaluation of lecithin as a lipid-lowering agent". Phytotherapy Research. 9 (8): 597–599. doi:10.1002/ptr.2650090814. S2CID   71032494.
  6. ↑ "Omega-3 Supplements: In Depth". NCCIH. 2018-05-01. Retrieved 2021-02-02.
  7. ↑ Stough, Con K; Pase, Matthew P; Cropley, Vanessa; Myers, Stephen; Nolidin, Karen; King, Rebecca; Camfield, David; Wesnes, Keith; Pipingas, Andrew; Croft, Kevin; Chang, Dennis; Scholey, Andrew B (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. 11 (1): 11. doi: 10.1186/1475-2891-11-11 . PMC   3310777 . PMID   22390677.
  8. ↑ Doggrell, SA (May 2005). "Berberine--a novel approach to cholesterol lowering". Expert Opinion on Investigational Drugs. 14 (5): 683–5. doi:10.1517/13543784.14.5.683. PMID   15926873. S2CID   1708378.
  9. ↑ Koppen, Laura M.; Whitaker, Andrea; Rosene, Audrey; Beckett, Robert D. (October 2017). "Efficacy of Berberine Alone and in Combination for the Treatment of Hyperlipidemia: A Systematic Review". Journal of Evidence-Based Complementary & Alternative Medicine. 22 (4): 956–968. doi:10.1177/2156587216687695. PMC   5871262 . PMID   29228784.
  10. ↑ Cicero, Arrigo F. G.; Fogacci, Federica; Zambon, Alberto (9 February 2021). "Red Yeast Rice for Hypercholesterolemia: JACC Focus Seminar". Journal of the American College of Cardiology. 77 (5): 620–628. doi:10.1016/j.jacc.2020.11.056. hdl: 11585/827471 . ISSN   0735-1097. PMID   33538260. S2CID   231803755.
  11. ↑ "Pharmanex Inc. v. Shalala, United States District Court, D. Utah, Central Division Mar 1, 2001 Case No. 2:97CV262K". Casetext. Retrieved 21 June 2019.
  12. ↑ Ahangarpour, Akram; Heidari, Hamid; Fatemeh, Ramezani Ali Akbari; Pakmehr, Mostafa; Shahbazian, Hajeye; Ahmadi, Iraj; Mombeini, Zahra; Mehrangiz, Babadi Hajani (2014). "Effect of Boswellia serrata supplementation on blood lipid, hepatic enzymes and fructosamine levels in type2 diabetic patients". Journal of Diabetes and Metabolic Disorders. 13 (1): 29. doi: 10.1186/2251-6581-13-29 . PMC   3929136 . PMID   24495344.
  13. ↑ Schulze, Friedrich; Glos, Sabrina; Petruschka, Dörte; Altenburg, Christiane; Maas, Renke; Benndorf, Ralf; Schwedhelm, Edzard; Beil, Ulrich; Böger, Rainer H. (May 2009). "L-Arginine enhances the triglyceride-lowering effect of simvastatin in patients with elevated plasma triglycerides". Nutrition Research (New York, N.Y.). 29 (5): 291–297. doi:10.1016/j.nutres.2009.04.004. PMID   19555809.
  14. ↑ Kristensen, M; Jensen, MG; Aarestrup, J; Petersen, KE; Søndergaard, L; Mikkelsen, MS; Astrup, A (3 February 2012). "Flaxseed dietary fibers lower cholesterol and increase fecal fat excretion, but magnitude of effect depend on food type". Nutrition & Metabolism. 9: 8. doi: 10.1186/1743-7075-9-8 . PMC   3307491 . PMID   22305169.
  15. ↑ Pollack, Andrew (29 January 2013) F.D.A. Approves Genetic Drug to Treat Rare Disease The New York Times, Retrieved 31 January 2013
  16. ↑ Staff (29 January 2013) 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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