Gemfibrozil
Systematic (IUPAC) name
5-(2,5-dimethylphenoxy)-2,2-dimethyl-pentanoic acid
Identifiers
CAS number	25812-30-0
ATC code	C10AB04
PubChem	3463
DrugBank	APRD00293
Chemical data
Formula	C15H22O3
Mol. mass	250.333 g/mol
Pharmacokinetic data
Bioavailability	Close to 100%
Protein binding	95%
Metabolism	Hepatic (CYP3A4)
Half life	1.5 hours
Excretion	Renal 94% Feces 6%
Therapeutic considerations
Pregnancy cat.	Category C Image File history File links No higher resolution available. ... 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. ... The Anatomical Therapeutic Chemical Classification System is used for the classification of drugs. ... A section of the Anatomical Therapeutic Chemical Classification System. ... PubChem is a database of chemical molecules. ... The DrugBank database available at the University of Alberta is a unique bioinformatics and cheminformatics resource that combines detailed drug (i. ... A chemical formula (also called molecular formula) is a concise way of expressing information about the atoms that constitute a particular chemical compound. ... General Name, Symbol, Number carbon, C, 6 Chemical series nonmetals Group, Period, Block 14, 2, p Appearance black (graphite) colorless (diamond) Atomic mass 12. ... This article is about the chemistry of hydrogen. ... General Name, Symbol, Number oxygen, O, 8 Chemical series Nonmetals, chalcogens Group, Period, Block 16, 2, p Appearance colorless (gas) very pale blue (liquid) Atomic mass 15. ... The molecular mass (abbreviated MM) of a substance, formerly also called molecular weight and abbreviated as MW, is the mass of one molecule of that substance, relative to the unified atomic mass unit u (equal to 1/12 the mass of one atom of carbon-12). ... In pharmacology, bioavailability is used to describe the fraction of an administered dose of medication that reaches the systemic circulation, one of the principal pharmacokinetic properties of drugs. ... Many drugs are bound to Blood plasma proteins. ... Drug metabolism is the metabolism of drugs, their biochemical modification or degradation, usually through specialized enzymatic systems. ... It has been suggested that Effective half-life be merged into this article or section. ... Excretion is the process of eliminating waste products of metabolism and other materials that are of no use. ... 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 pregnancy. ...
Legal status	By Prescription The regulation of therapeutic goods, that is drugs and therapeutic devices, varies by jurisdiction. ...
Routes	Oral

Gemfibrozil is the generic name for an oral drug used to lower lipid levels. It belongs to a group of drugs known as fibrates. It is most commonly sold as the brand name, Lopid. Other brand names include Jezil and Gen-Fibro. In pharmacology and toxicology, a route of administration is the path by which a drug, fluid, poison or other substance is brought into contact with the body 1. ... In biological nomenclature, a generic name or the name of a genus (sometimes genus name) is the name of a genus. ... Lipids are a class of hydrocarbon-containing organic compounds. ... In pharmacology, the fibrates are a class of amphipathic carboxylic acids. ...

Actions

• Increases activity of Peroxisome proliferator-activated receptor-alpha (PPARα), a receptor which is involved in metabolism of carbohydrates and fats, as well as adipose tissue differentiation. This increases synthesis of lipoprotein lipase therefore increasing clearance of triglycerides.

PPAR gamma In cell biology, peroxisome proliferator-activated receptors (PPARs) are a group of nuclear receptor isoforms that exist across biology. ... Lactose is a disaccharide found in milk. ... For other uses, see Fat (disambiguation). ... It has been suggested that Subcutaneous fat be merged into this article or section. ...

Therapeutic effects

• Reduce triglyceride levels
• Reduce Very low density lipoprotein (VLDL) levels
• Modest reduction of Low density lipoprotein (LDL) levels
• Moderate increase in High density lipoprotein (HDL) levels

It has been suggested that Medium Chain Triglycerides be merged into this article or section. ... Very Low Density Lipoprotein (VLDL) is a lipoprotein subclass. ... Low-density lipoprotein (LDL) is a class of lipoprotein particles that varies in size (18-25 nm in diameter) and contents (while carrying fatty acid molecules in blood and around the body). ... High-density lipoproteins (HDL) form a class of lipoproteins, varying somewhat in their size (8–11 nm in diameter), that carry cholesterol from the bodys tissues to the liver. ...

Nontherapeutic effects and toxicities

• GI distress
• Musculoskeletal pain
• Increased incidence of gallstones
• Hypokalemia

Hypokalemia is a potentially fatal condition in which the body fails to retain sufficient potassium to maintain health. ...

Indications

• Hyperlipidemia (Type III): Gemfibrozil is the drug of choice for therapy.
• Hypertriglyceridemia (Type IV): Gemfibrozil, though not as effective as nicotinic acid, is better tolerated.

Hypercholesterolemia (literally: high blood cholesterol) is the presence of high levels of cholesterol in the blood. ... In medicine, hypertriglyceridemia (or Hypertriglyceridaemia) denotes high (hyper-) blood levels (-emia) of triglycerides, the most abundant fatty molecule in most organisms. ... Niacin, also known as nicotinic acid or vitamin B3, is a water-soluble vitamin whose derivatives such as NADH play essential roles in energy metabolism in the living cell. ...

Contraindications and Precautions

• Gemfibrozil should not be given to these patients:
  • Hepatic dysfunction
  • Renal dysfunction

• Gemfibrozil should be used with caution in these higher risk categories:
  • Biliary tract disease
  • pregnant women
  • obese patients
  • Native Americans

Drug Interactions

• Anticoagulants. Gemfibrozil potentiates the action of coumadin and indanedione anticoagulants.
• Lovastatin. Risk of myopathy when gemfibrozil is given to patients receiving lovastatin.

Warfarin (also known under the brand name Coumadin®) is an anticoagulant medication that can be administered orally. ... In medicine, a myopathy is a neuromuscular disease in which the muscle fibers dysfunction for any one of many reasons, resulting in muscular weakness. ... Categories: Stub | Hypolipidemic agents ...

External links

• DrugBank Gemfibrozil
• NIH Gemfibrozil Drug Info}
• Lopid International Study
• Safety of Statins - Circulation. 2004;109:III-50 – III-57