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Information about Hypolipidemic Agent

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 (LLD) or agents.

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 cardiovascular 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.
  • 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) with fibrates.
  • 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.
  • bile acid sequestrants (resins) are particularly effective for lowering LDL-C by sequestering the cholesterol-containing bile acids released into the gut and preventing their reabsorption from the gut. It decreases LDL by 15-30% and raises HDL by 3-5%. It has 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.
  • 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.

Investigational

Investigational classes of hypolipidemic agents:

See also

 •  • [ e]
Major Drug Groups
Gastrointestinal tract (A)Antacids • Antiemetics  • H₂-receptor antagonists • Proton pump inhibitors • Laxatives • Antidiarrhoeals
Blood and blood forming organs (B)Anticoagulants • Antiplatelets • Thrombolytics
Cardiovascular system (C)Antiarrhythmics • Antihypertensives • Diuretics • Vasodilators • Antianginals • Beta blockers • Angiotensin converting enzyme inhibitors • Antihyperlipidemics
Skin (D)Antipruritics
Reproductive system (G)Hormonal contraception • Fertility agents • Selective estrogen receptor modulators • Sex hormones
Endocrine system (H)Anti-diabetics • Corticosteroids • Sex hormones • Thyroid hormones
Infections and Infestations (J, P)Antibiotics • Antivirals • Vaccines • Antifungals • Antiprotozoals • Anthelmintics
Malignant and Immune disease (L)Anticancer agents • Immunosuppressants
Muscles, Bones, and Joints (M)Anabolic steroids • Anti-inflammatories • Antirheumatics • Corticosteroids • Muscle relaxants
Brain and Nervous system (N)Anesthetics • Analgesics • Anticonvulsants • Mood stabilizers  • Anxiolytics • Antipsychotics • Antidepressants • Nervous system stimulants
Respiratory system (R)Bronchodilators • Decongestants  • Antihistamines
 •  • [ e]
Lipid modifying agents (C10)
StatinsAtorvastatin • Cerivastatin • Fluvastatin • Lovastatin • Mevastatin • Pitavastatin • Pravastatin • Rosuvastatin • Simvastatin
FibratesClofibrate • Bezafibrate • Aluminium clofibrate • Gemfibrozil • Fenofibrate • Simfibrate • Ronifibrate • Ciprofibrate • Etofibrate • Clofibride
Bile acid sequestrantsColestyramine • Colestipol • Colextran • Colesevelam
Niacin and derivativesNiceritrol • Niacin  • Nicofuranose • Aluminium nicotinate • Nicotinyl alcohol  • Acipimox
OtherDextrothyroxine • Probucol • Tiadenol • Benfluorex • Meglutol • Omega-3-triglycerides • Magnesium pyridoxal 5-phosphate glutamate • Policosanol • Ezetimibe
Pharmacology is the study of how drugs interact with living organisms to produce a change in function.[1] If substances have medicinal properties, they are considered pharmaceuticals.
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Hyperlipidemia
Classification & external resources

ICD-10 E 78.
ICD-9 272.0 - 272.4

DiseasesDB 6255

Hyperlipidemia, hyperlipoproteinemia or dyslipidemia
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Low-density lipoprotein (LDL) belongs to the lipoprotein particle family. Its size is approx. 22 nm but since LDL particles contain a changing number of fatty acids they actually have a mass and size distribution.
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High-density lipoproteins (HDL) form a class of lipoproteins, varying somewhat in their size (8–11 nm in diameter), that carry cholesterol from the body's tissues to the liver. About thirty percent of blood cholesterol is carried by HDL.
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Cholesterol is a sterol (a combination steroid and alcohol), a lipid found in the cell membranes of all tissues, and is transported in the blood plasma of all animals. Because cholesterol is synthesized by all eukaryotes, trace amounts of cholesterol are also found in membranes of
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Liver function tests (LFTs or LFs), which include liver enzymes, are groups of clinical biochemistry laboratory blood assays designed to give information about the state of a patient's liver.
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In general, creatinine clearance is the removal of creatinine from the body. In renal physiology, creatinine clearance (CCr) is the volume of blood plasma that is cleared of creatinine per unit time.
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Evidence-based medicine (EBM) or scientific medicine is an attempt to apply more uniformly the standards of evidence gained from the scientific method to certain aspects of medical practice.
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The National Cholesterol Education Program is a program managed by the National Heart, Lung and Blood Institute, a division of the National Institutes of Health. Its goal is to reduce increased cardiovascular disease rates due to hypercholesterolemia (elevated cholesterol
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The statins (or HMG-CoA reductase inhibitors) form a class of hypolipidemic agents, used as pharmaceutical agents to lower cholesterol levels in people with or at risk of cardiovascular disease.
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MeSH D009135 In medicine, a myopathy is a neuromuscular disease in which the muscle fibers do not function for any one of many reasons, resulting in muscular weakness. "Myopathy" simply means muscle disease (myo- Greek μυσ "muscle" + -pathy Greek "suffering").
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MeSH D012206 Rhabdomyolysis is the rapid breakdown of skeletal muscle tissue due to traumatic injury, either mechanical, physical or chemical. The principal result is a large release of the CK enzymes and other cell byproducts into the blood system and acute renal failure
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fibrates are a class of amphipathic carboxylic acids. They are used for a range of metabolic disorders, mainly hypercholesterolemia (high cholesterol), and are therefore hypolipidemic agents.

Members

Fibrates prescribed commonly are:
  • Bezafibrate (e.g.

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Hypertriglyceridemia
Classification & external resources

ICD-10 E78.1, E78.2, E78.3
ICD-9 272.1

In medicine, hypertriglyceridemia (or "Hypertriglyceridaemia") denotes high (hyper-) blood levels (-emia
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MeSH D009135 In medicine, a myopathy is a neuromuscular disease in which the muscle fibers do not function for any one of many reasons, resulting in muscular weakness. "Myopathy" simply means muscle disease (myo- Greek μυσ "muscle" + -pathy Greek "suffering").
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MeSH D012206 Rhabdomyolysis is the rapid breakdown of skeletal muscle tissue due to traumatic injury, either mechanical, physical or chemical. The principal result is a large release of the CK enzymes and other cell byproducts into the blood system and acute renal failure
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For the band, see Niacin (band).


Niacin, also known as nicotinic acid or vitamin B3, is a water-soluble vitamin whose derivatives such as NADH, NAD, NAD+
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Hyperglycemia
Classification & external resources

ICD-10 R73.9
ICD-9 790.6

Hyperglycemia, hyperglycaemia, or high blood sugar is a condition in which an excessive amount of glucose circulates in the blood plasma.
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<noinclude> </noinclude> Hepatotoxicity (from hepatic toxicity) implies chemical-driven liver damage. Liver plays central role in transformation and clearance of most chemicals and is susceptible to the toxicity from these agents.
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The bile acid sequestrants are a group of medications used for binding certain components of bile in the gastrointestinal tract. They disrupt the enterohepatic circulation of bile acids by sequestering them and preventing their reabsorption from the gut.
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Ezetimibe (IPA: [ɛˈzɛtəmɪb]) is an anti-hyperlipidemic medication which is used to lower cholesterol levels. It acts by decreasing cholesterol absorption in the intestine.
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Phytosterols (also called plant sterols) are a group of steroid alcohol, phytochemicals naturally occurring in plants. They are white powders with mild, characteristic odor, insoluble in water and soluble in alcohols.
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Torcetrapib (CP-529414, Pfizer) was a drug being developed to treat hypercholesterolemia (elevated cholesterol levels) and prevent cardiovascular disease.

Mechanism


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Farnesyl-diphosphate farnesyltransferase (or squalene synthase) is an enzyme which converts farnesyl pyrophosphate into squalene.

Squalene synthase is considered to be an enzyme of eukaryotes or advanced organisms, although at least one prokaryote has been shown to
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A naturally-occurring mutated strain of the apoA-1 protein found in human HDL. First identified by Cesare Sirtori in Milan, it has been shown to significantly reduce arterial plaque.

Discovered by accident, the mutation was found to be present in about 3.
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A section of the Anatomical Therapeutic Chemical Classification System.

C Cardiovascular system

Lipid modifying agents, plain

C10AA HMG CoA reductase inhibitors

C10AA01 Simvastatin
C10AA02 Lovastatin

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gastrointestinal tract (GI tract), also called the digestive tract, or the alimentary canal, is the system of organs within multicellular animals that takes in food, digests it to extract energy and nutrients, and expels the remaining waste.
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A section of the Anatomical Therapeutic Chemical Classification System.

A Alimentary tract and metabolism

A01 Stomatological preparations
A02 Drugs for acid related disorders
A03 Drugs for functional gastrointestinal disorders

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An antacid is any substance, generally a base, which counteracts stomach acidity. In other words, antacids are stomach acid neutralizers.

Action mechanism

Antacids perform a neutralization reaction, i.e.
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An anti-emetic is a drug that is effective against vomiting and nausea. Anti-emetics are typically used to treat motion sickness and the side effects of opioid analgesics, general anaesthetics and chemotherapy directed against cancer.
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