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Bezafibrate
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| Systematic (IUPAC) name | |
| 2-[4-[2-[(4-chlorobenzoyl)amino] ethyl]phenoxy]-2-methyl-propanoic acid |
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| Identifiers | |
| CAS number | |
| ATC code | C10 |
| PubChem | |
| Chemical data | |
| Formula | C19H20ClNO4 |
| Mol. mass | 361. IUPAC Nomenclature is a system of naming Chemical compounds and of describing the science of Chemistry in general CAS registry numbers are unique numerical identifiers for Chemical compounds Polymers biological sequences mixtures and Alloys They are also referred to The Anatomical Therapeutic Chemical Classification System is used for the classification of drugs It is controlled by the WHO Collaborating Centre for Drug A section of the Anatomical Therapeutic Chemical Classification System. PubChem is a Database of chemical Molecules The system is maintained by the National Center for Biotechnology Information (NCBI a component A chemical formula is a way of expressing information about the Atoms that constitute a particular Chemical compound, and how the relationship between those atoms changes Carbon (kɑɹbən is a Chemical element with the symbol C and its Atomic number is 6 Hydrogen (ˈhaɪdrədʒən is the Chemical element with Atomic number 1 Chlorine (ˈklɔriːn from the Greek word 'χλωρóς' ( khlôros, meaning 'pale green' is the Chemical element with Atomic number 17 and Nitrogen (ˈnaɪtɹəʤɪn is a Chemical element that has the symbol N and Atomic number 7 and Atomic weight 14 Oxygen (from the Greek roots ὀξύς (oxys (acid literally "sharp" from the taste of acids and -γενής (-genēs (producer literally begetteris the The molecular mass (abbreviated m of a substance, more commonly referred to as molecular weight and abbreviated as MW, is the Mass of one 819 |
| Pharmacokinetic data | |
| Bioavailability | ? |
| Metabolism | ? |
| Half life | ? |
| Excretion | ? |
| Therapeutic considerations | |
| Pregnancy cat. |
? |
| Legal status |
RX/POM |
| Dependence Liability | N/A |
| Routes | oral |
Bezafibrate (Bezalip and various other brand names) is a fibrate drug used for the treatment of hyperlipidaemia. In Pharmacology, bioavailability is used to describe the fraction of an administered Dose of unchanged drug that reaches the Systemic circulation, one of Drug metabolism is the Metabolism of drugs, their Biochemical modification or degradation usually through specialized enzymatic systems The biological half-life of a substance is the time it takes for a substance (drug radioactive nuclide or other to lose half of its pharmacologic physiologic or radiologic activity Excretion is the process of eliminating waste products of Metabolism and other non-useful materials The pregnancy category of a pharmaceutical agent is an assessment of the risk of fetal injury due to the pharmaceutical if it is used as directed by the mother during The regulation of therapeutic goods, that is drugs and therapeutic devices, varies by jurisdiction In Pharmacology and Toxicology, a route In Pharmacology, the fibrates are a class of amphipathic Carboxylic acids They are used for a range of metabolic disorders mainly Hypercholesterolemia A drug, broadly speaking is any chemical substance that when absorbed into the body Hyperlipidemia, hyperlipoproteinemia or dyslipidemia is the presence of raised or abnormal levels of Lipids and/or Lipoproteins in the It helps to lower LDL cholesterol and triglyceride in the blood, and increase HDL. Low-density lipoprotein ( LDL) is a type of Lipoprotein that transports Cholesterol and Triglycerides from the Liver to peripheral (more properly known as, TAG or triacylglyceride) is Glyceride in which the Glycerol is Esterified with three Fatty acids It is the Blood is a specialized Bodily fluid that delivers necessary substances to the body's cells such as nutrients and oxygen—and transports Waste products High-density lipoproteins ( HDL) is one of the 5 major groups of Lipoproteins ( Chylomicrons, VLDL, IDL, LDL, HDL
Contents |
History
Bezafibrate was first introduced by Boehringer Mannheim in 1977.
Mode of action
Like the other fibrates, bezafibrate is an agonist of PPARα; some studies suggest it may have some activity on PPARγ and PPARδ as well. In the field of Molecular biology, the peroxisome proliferator-activated receptors ( PPARs) are a group of Nuclear receptor Proteins that function
Uses
Bezafibrate improves markers of combined hyperlipidemia, effectively reducing LDL and triglycerides and improving HDL levels. In Medicine, combined hyperlipidemia (or - aemia) is a commonly occurring form of Hypercholesterolemia (elevated Cholesterol levels characterised [1] The main effect on cardiovascular morbidity is in patients with the metabolic syndrome, the features of which are attenuated by bezafibrate. Metabolic syndrome is a combination of medical disorders that increase the risk of developing Cardiovascular disease and diabetes. [2] Studies show that in patients with impaired glucose tolerance, bezafibrate may delay progress to diabetes[3], and in those with insulin resistance it slowed progress in the HOMA severity marker. Insulin resistance is the condition in which normal amounts of Insulin are inadequate to produce a normal Insulin response from Fat, Muscle The homeostatic model assessment (HOMA is a method used to quantify Insulin resistance and Beta-cell function [4]
Side-effects
The main toxicity is hepatic (abnormal liver enzymes), and myopathy and rarely rhabdomyolysis have been reported. The liver is a vital organ in the human body and is present in Vertebrates and some other animals 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 Rhabdomyolysis is the rapid breakdown ( Lysis) of Skeletal muscle tissue ( rhabdomyo) due to injury to muscle tissue
Other uses
The Australian biotech company Giaconda combines bezafibrate with chenodeoxycholic acid in an anti-hepatitis C drug combination called Hepaconda. Giaconda is an Australian Biotechnology company headquartered in Sydney. Chenodeoxycholic acid (also known as chenodesoxycholic acid) is a Bile acid. Hepatitis C is a blood-borne infectious disease that is caused by the Hepatitis C virus ( HCV) affecting the Liver.
References
- ^ Secondary prevention by raising HDL cholesterol and reducing triglycerides in patients with coronary artery disease: the Bezafibrate Infarction Prevention (BIP) study. Circulation 2000;102:21-7. PMID 10880410.
- ^ Tenenbaum A, Motro M, Fisman EZ, Tanne D, Boyko V, Behar S. Bezafibrate for the secondary prevention of myocardial infarction in patients with metabolic syndrome. Arch Intern Med 2005;165:1154-60. PMID 15911729.
- ^ Tenenbaum A, Motro M, Fisman EZ, Schwammenthal E, Adler Y, Goldenberg I, Leor J, Boyko V, Mandelzweig L, Behar S. Peroxisome proliferator-activated receptor ligand bezafibrate for prevention of type 2 diabetes mellitus in patients with coronary artery disease. Circulation 2004;109:2197-202. PMID 15123532
- ^ Tenenbaum A, Fisman EZ, Boyko V, Benderly M, Tanne D, Haim M, Matas Z, Motro M, Behar S. Attenuation of progression of insulin resistance in patients with coronary artery disease by bezafibrate. Arch Intern Med 2006;166:737-41. PMID 16606809.
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