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出典(authority):フリー百科事典『ウィキペディア（Wikipedia）』「2016/07/02 19:03:05」(JST)

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Hypolipidemic agents, or antihyperlipidemic agents, are a diverse group of pharmaceuticals that are used in the treatment of hyperlipidemias. They are called lipid-lowering drugs.

Classes of hypolipidemic drugs

There are several classes of hypolipidemic drugs. They may differ in both their impact on the cholesterol profile and adverse effects. For example, some may lower the "bad cholesterol" low density lipoprotein (LDL) more so than others, while others may preferentially increase high density lipoprotein (HDL), "the good cholesterol". Clinically, the choice of an agent will depend 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 from the National Cholesterol Education Program (NCEP) Adult Treatment Panel III (ATPIII).

Established

Statins 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. There is a risk of severe muscle damage (myopathy & 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.^[1]
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, there is a risk of severe muscle damage (myopathy & rhabdomyolysis).
niacin, 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.
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 (Zetia) is a selective inhibitor of dietary cholesterol absorption.
lomitapide (Juxtapid) is a microsomal triglyceride transfer protein (MTP) inhibitor.
phytosterols may be found naturally in plants. Similar to ezetimibe, phytosterols reduce the absorption of cholesterol in the gut. Hence, they are most effective when consumed with meals. However, the precise mechanism of action of phytosterols differs from ezetimibe.
orlistat (Xenical): Its primary function is to prevent the absorption of about 30% of fats from the human diet, thereby reducing caloric intake. A drug designed to treat obesity, it works by inhibiting Pancreatic lipase, an enzyme that breaks down triglycerides in the intestine.

Investigational

Investigational classes of hypolipidemic agents:

CETP inhibitors (cholesteryl ester transfer protein), 1 candidate is in trials. It is expected that these drugs will mainly increase HDL while lowering LDL;
Squalene synthase inhibitor;
ApoA-1 Milano
succinobucol(AGI-1067), a novel antioxidant, failed a phase 3 trial
Apoprotein-B inhibitor Mipomersen (approved by the FDA in 2013 homozygous familial hypercholesterolemia.^[2]^[3]).
PCSK9 Monoclonal antibody inhibitors ^[4]^[5]

References

^ 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 .
^ Pollack, Andrew (29 January 2013) F.D.A. Approves Genetic Drug to Treat Rare Disease The New York Times, Retrieved 31 January 2013
^ 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
^ Koren MJ, Scott R, Kim JB et al Lancet 2012; 380:1995-2006
^ Gugliano RP, Desai NR, Kohli P et al Lancet 2012; 380:2007-17

UpToDate Contents

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1. スタチン系およびフィブラート系以外の薬剤による脂質低下 lipid lowering with drugs other than statins and fibrates
2. 食事または栄養補助食品による脂質低下 lipid lowering with diet or dietary supplements
3. 二次予防における脂質（高コレステロール血症を含む）の治療 treatment of lipids including hypercholesterolemia in secondary prevention
4. フィブラート系薬剤による脂質低下 lipid lowering with fibric acid derivatives
5. 急性冠症候群後のコレステロール低下 cholesterol lowering after an acute coronary syndrome

English Journal

The hypolipidemic activity of chitosan nanopowder prepared by ultrafine milling.

Zhang W, Zhang J, Jiang Q, Xia W.SourceState Key Laboratory of Food Science and Technology, School of Food Science and Technology, Jiangnan University, Wuxi, Jiangsu, 214122, China.
Carbohydrate polymers.Carbohydr Polym.2013 Jun 5;95(1):487-91. doi: 10.1016/j.carbpol.2013.02.037. Epub 2013 Mar 4.
The hypolipidemic activities of high and low molecular weights of chitosan nanopowders (HMW-chitosan-NP: 315kDa; LMW-chitosan-NP: 51kDa) prepared by ultrafine milling were evaluated in rats. The results showed that the hypolipidemic activity of chitosan nanopowder was better than ordinary chitosan,
PMID 23618297

Antiobesity potential of ursolic acid stearoyl glucoside by inhibiting pancreatic lipase.

Kazmi I, Afzal M, Rahman S, Iqbal M, Imam F, Anwar F.SourcePacific University, Udaipur-313024, Rajasthan, India; Siddhartha Institute of Pharmacy, Dobachi, Near IT Park, Dehradun-248001, Uttarakhand, India.
European journal of pharmacology.Eur J Pharmacol.2013 Jun 5;709(1-3):28-36. doi: 10.1016/j.ejphar.2013.02.032. Epub 2013 Mar 13.
The present study was designed to evaluate the hypolipidemic effect of ursolic acid stearoyl glucoside (UASG) in high-fat diet-induced obesity. Two in vivo experiments such as high-fat diet-induced obesity mice model and lipid emulsion tolerance test in normal rats were performed. In vitro inhibitio
PMID 23500199

Japanese Journal

Dietary Effects of Oxidized Eicosapentaenoic Acid (EPA) and Intact EPA on Hepatic Steatosis Induced by a High-sucrose Diet and Liver-X-receptor α Agonist in Mice

Journal of Oleo Science advpub(0), 2016
NAID 130005125564

Gut Microbial Fatty Acid Metabolites Reduce Triacylglycerol Levels in Hepatocytes.

Lipids 50(11), 1093-1102, 2015-11
NAID 120005690195

牡蠣エキスの脂質低下作用 (特集牡蠣エキス)

ニューフードインダストリー 57(10), 76-84, 2015-10
NAID 40020601438

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