Clofibrate

Clofibride

Etofibrate

Aluminium clofibrate

In pharmacology, the 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. Clofibrate is a fibrate. ... Clofibride is a fibrate. ... Etofibrate is a fibrate. ... Aluminium clofibrate (or alfibrate) is a fibrate. ... Pharmacology (in Greek: pharmakon (φάρμακον) meaning drug, and lego (λέγω) to tell (about)) is the study of how drugs interact with living organisms to produce a change in function. ... Amphiphile (from the Greek αμφις, amphis: both and φιλíα, philia: love, friendship) is a term describing a chemical compound possessing both hydrophilic and hydrophobic properties. ... Structure of a carboxylic acid The 3D structure of the carboxyl group A space-filling model of the carboxyl group Carboxylic acids are organic acids characterized by the presence of a carboxyl group, which has the formula -C(=O)OH, usually written -COOH or -CO2H. [1] Carboxylic acids are Bronsted... Structure of the coenzyme adenosine triphosphate, a central intermediate in energy metabolism. ... Hypercholesterolemia (literally: high blood cholesterol) is the presence of high levels of cholesterol in the blood [1]. It is not a disease but a metabolic derangement that can be secondary to many diseases and can contribute to many forms of disease, most notably cardiovascular disease. ... Cholesterol is a sterol (a combination steroid and alcohol). ... Hypolipidemic agents, or antihyperlipidemic agents, are a diverse group of pharmaceuticals that are used in the treatment of hyperlipidemias. ...

Members

Fibrates prescribed commonly are:

• Bezafibrate (e.g. Bezalip®)
• Ciprofibrate (e.g. Modalim®)
• Clofibrate (largely obsolete due to side-effect profile, e.g. gallstones)
• Gemfibrozil (e.g. Lopid®)
• Fenofibrate (e.g. TriCor®)

Bezafibrate (Bezalip® and various other brand names) is a fibrate drug used for the treatment of hyperlipidaemia. ... Ciprofibrate is a fibrate. ... Clofibrate is a fibrate. ... This article does not cite any references or sources. ... Gemfibrozil is the generic name for an oral drug used to lower lipid levels. ... Fenofibrate is a drug of the fibrate class. ...

Indications

Fibrates are used as accessory therapy in many forms of hypercholesterolemia, usually in combination with statins. Trials do support its use as monotherapy. (Error? Was "do not" meant?) Hypercholesterolemia (literally: high blood cholesterol) is the presence of high levels of cholesterol in the blood [1]. It is not a disease but a metabolic derangement that can be secondary to many diseases and can contribute to many forms of disease, most notably cardiovascular disease. ... Lovastatin, the first statin to be marketed The statins (or HMG-CoA reductase inhibitors) form a class of hypolipidemic drugs used to lower cholesterol levels in people with or at risk of cardiovascular disease. ...

Although less effective in lowering LDL, fibrates improve HDL and triglyceride levels (i.e. increase HDL levels and decrease triglyceride levels), and seem to improve insulin resistance when the dyslipidemia is associated with other features of Syndrome X (hypertension and diabetes mellitus type 2). Low-density lipoprotein (LDL) refers to a class and range of lipoprotein particles, varying somewhat in their size and contents, which carry cholesterol in the blood and around the body, for use by various cells. ... High density lipoproteins (HDL) form a class of lipoproteins, varying somewhat in their size and contents, that carry cholesterol from the bodys tissues to the liver. ... {{refimprove|date=October 2007} Ausra yra maza mergaite. ... Insulin resistance is the condition in which normal amounts of insulin are inadequate to produce a normal insulin response from fat, muscle and liver cells. ... Dyslipidemia is a disruption in the amount of lipids in the blood. ... Metabolic syndrome is a combination of medical disorders that affect a large number of people in a clustered fashion. ... For other forms of hypertension, see Hypertension (disambiguation). ... For the disease characterized by excretion of large amounts of very dilute urine, see diabetes insipidus. ...

Mechanism

Fibrates are agonists of the PPARalpha receptor in muscle, liver, and other tissues. Activation of PPARalpha signaling results in:

• Increased fatty oxidation in the liver
• Decreased hepatic triglyceride secretion
• Increased lipoprotein lipase activity, and thus increased VLDL clearance
• Increased HDL
• Increased clearance of remnant particles

Side effects

Most fibrates can cause mild stomach upset and myopathy (muscle pain with CPK elevations). 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. ... Creatine Kinase Creatine kinase (CK), also known as phosphocreatine kinase or creatine phosphokinase (CPK) is an enzyme (EC 2. ...

In combination with statin drugs, fibrates cause an increased risk of rhabdomyolysis (idiosyncratic destruction of muscle tissue, leading to renal failure). A powerful statin drug, cerivastatin (Lipobay®), was withdrawn because of this complication. The less lipophilic statins are less prone to cause this reaction, and are probably safer when combined with fibrates. Lovastatin, the first statin to be marketed The statins (or HMG-CoA reductase inhibitors) form a class of hypolipidemic drugs used to lower cholesterol levels in people with or at risk of cardiovascular disease. ... Rhabdomyolysis is the rapid breakdown of skeletal muscle tissue due to traumatic injury, either mechanical, physical or chemical. ... For other uses of Muscles, see Muscles (disambiguation). ... Renal failure or kidney failure is a situation in which the kidneys fail to function adequately. ... Lovastatin, the first statin to be marketed The statins (or HMG-CoA reductase inhibitors) form a class of hypolipidemic drugs used to lower cholesterol levels in people with or at risk of cardiovascular disease. ... In pharmacology, cerivastatin (Baycol®, Lipobay®) is a synthetic member of the class of statins, used to lower cholesterol and prevent cardiovascular disease. ... This article or section does not cite its references or sources. ... Lovastatin, the first statin to be marketed The statins (or HMG-CoA reductase inhibitors) form a class of hypolipidemic drugs used to lower cholesterol levels in people with or at risk of cardiovascular disease. ...

Pharmacology

PPAR

Although used clinically since at least the 1930s[1], the mechanism of action of fibrates remained unelucidated until, in the 1990s, it was discovered that fibrates activate PPAR (peroxisome proliferator-activated receptors), especially PPARα. The PPARs are a class of intracellular receptors that modulate carbohydrate, fat metabolism and adipose tissue differentiation. Image File history File links Size of this preview: 800 × 471 pixelsFull resolution (3448 × 2032 pixel, file size: 2. ... Image File history File links Size of this preview: 800 × 471 pixelsFull resolution (3448 × 2032 pixel, file size: 2. ... In cell biology, peroxisome proliferator-activated receptors (PPARs) are a group of nuclear receptor isoforms that exist across biology. ... The 1930s (years from 1930–1939) were described as an abrupt shift to more radical and conservative lifestyles, as countries were struggling to find a solution to the Great Depression, also known as the World Depression. ... For the band, see 1990s (band). ... In cell biology, peroxisome proliferator-activated receptors (PPARs) are a group of nuclear receptor isoforms that exist across biology. ... In biochemistry, a receptor is a protein on the cell membrane or within the cytoplasm that binds to a specific factor (a ligand), such as a neurotransmitter, hormone, or other substance, and initiates the cellular response to the ligand. ... The smooth endoplasmic reticulum is responsible for some carbohydrate metabolism. ... Fatty acids are an important source of energy for many organisms. ... Adipose tissue is one of the main types of connective tissue. ...

Activation of PPARs causes transcription of a number of genes on the DNA that facilitate lipid metabolism. For other uses, see Gene (disambiguation). ... The structure of part of a DNA double helix Deoxyribonucleic acid, or DNA, is a nucleic acid molecule that contains the genetic instructions used in the development and functioning of all known living organisms. ... Fatty acids are an important source of energy for many organisms. ...

Fibrates are structurally and pharmacologically related to the thiazolidinediones, a novel class of anti-diabetic drugs that also act on PPARs (more specifically PPARγ) The medication class of thiazolidinedione was introduced in the late 1990s as an adjunctive therapy for diabetes mellitus (type II) and related diseases. ... An anti-diabetic drug or oral hypoglycemic agent is used to treat diabetes mellitus. ... In cell biology, peroxisome proliferator-activated receptors (PPARs) are a group of nuclear receptor isoforms that exist across biology. ...

Fibrates are a substrate of (metabolized by) CYP3A4.^[1] Cytochrome P450 3A4 (abbreviated CYP3A4) (EC 1. ...

See also

• statin

Lovastatin, the first statin to be marketed The statins (or HMG-CoA reductase inhibitors) form a class of hypolipidemic drugs used to lower cholesterol levels in people with or at risk of cardiovascular disease. ... Hypolipidemic agents, or antihyperlipidemic agents, are a diverse group of pharmaceuticals that are used in the treatment of hyperlipidemias. ... A section of the Anatomical Therapeutic Chemical Classification System. ... Lovastatin, the first statin to be marketed The statins (or HMG-CoA reductase inhibitors) form a class of hypolipidemic drugs used to lower cholesterol levels in people with or at risk of cardiovascular disease. ... Atorvastatin (INN) (IPA: ) is a member of the drug class known as statins, used for lowering cholesterol and thereby reducing cardiovascular disease. ... In pharmacology, cerivastatin (Baycol®, Lipobay®) is a synthetic member of the class of statins, used to lower cholesterol and prevent cardiovascular disease. ... Fluvastatin (Lescol®, Canef®) is a member of the drug class of statins, used to treat hypercholesterolemia and to prevent cardiovascular disease. ... Lovastatin is a member of the drug class of statins, used for lowering cholesterol (hypolipidemic agent) in those with hypercholesterolemia and so preventing cardiovascular disease. ... Mevastatin molecular structure Mevastatin, compactin, ML-236B is a hypolipidemic agent that belongs to the statins class. ... Pitavastatin (usually as a calcium salt) is a novel member of the medication class of statins[1]. Like the other statins, it is an inhibitor of HMG-CoA reductase, the enzyme that catalyses the first step of cholesterol synthesis. ... Categories: Stub | Hypolipidemic agents ... Rosuvastatin is a member of the drug class of statins, used to treat hypercholesterolemia and related conditions, and to prevent cardiovascular disease. ... Simvastatin (INN) (IPA: ) is a hypolipidemic drug belonging to the class of pharmaceuticals called statins. It is used to control hypercholesterolemia (elevated cholesterol levels) and to prevent cardiovascular disease. ... Clofibrate is a fibrate. ... Bezafibrate (Bezalip® and various other brand names) is a fibrate drug used for the treatment of hyperlipidaemia. ... Aluminium clofibrate (or alfibrate) is a fibrate. ... Gemfibrozil is the generic name for an oral drug used to lower lipid levels. ... Fenofibrate is a drug of the fibrate class. ... Simfibrate is a fibrate. ... Ronifibrate is a fibrate. ... Ciprofibrate is a fibrate. ... Etofibrate is a fibrate. ... Clofibride is a fibrate. ... In pharmacology, bile acid sequestrants a group of medication used for binding bile in the gastrointestinal tract. ... Cholestyramine (Questran®, Questran Light®, Cholybar®) is a bile acid sequestrant, which binds bile in the gastrointestinal tract to prevent its reabsorption. ... Colestipol is a bile acid sequestrant. ... Colextran is a bile acid sequestrant. ... Colesevelam is a bile acid sequestrant. ... Niceritrol is a niacin derivative used as a hypolipidemic agent. ... Niacin, also known as nicotinic acid or vitamin B3, is a water-soluble vitamin whose derivatives such as NADH, NAD, NAD+, and NADP play essential roles in energy metabolism in the living cell and DNA repair. ... Nicofuranose is a niacin derivative used as a hypolipidemic agent. ... Aluminium nicotinate is a niacin derivative used as a hypolipidemic agent. ... Nicotinyl alcohol is a niacin derivative used as a hypolipidemic agent. ... Acipimox is a niacin derivative used as a hypolipidemic agent. ... Ezetimibe/simvastatin (IPA: ) is a drug combination used for the treatment of dyslipidemia. ... Thyroxine, or 3:5,3:5 tetra­iodothyronine (often abbreviated as T4) is the major hormone secreted by the follicular cells of the thyroid gland. ... Probucol is a powerful antioxidant drug normally used to prevent vascular disease caused by the free radicals in the body. ... Tiadenol is a hypolipidemic agent. ... Benfluorex is an anorectic and hypolipidemic agent. ... Meglutol (INN, also known as 3-hydroxy-3-methylglutaric acid, β-hydroxy-β-methylglutaric acid, and dicrotalic acid) is a hypolipidemic agent. ... Omega-3 fatty acids are a family of polyunsaturated fatty acids which have in common a carbon-carbon double bond in the ω-3 position. ... Magnesium pyridoxal 5-phosphate glutamate (trade name Sedalipid) is a hypolipidemic agent. ... Policosanol (or polycosanol) is the generic term for a natural extract of plant waxes. ... Ezetimibe (IPA: ) is an anti-hyperlipidemic medication which is used to lower cholesterol levels. ...

References

1. ^ http://www.stacommunications.com/journals/cardiology/2004/June/Pdf/034.pdf