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| Clinical data | |
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| Trade names | Lopid, others |
| AHFS/Drugs.com | Monograph |
| MedlinePlus | a686002 |
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| Routes of administration | By mouth |
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| Pharmacokinetic data | |
| Bioavailability | Close to 100% |
| Protein binding | 95% |
| Metabolism | Liver (CYP3A4) |
| Eliminationhalf-life | 1.5 hours |
| Excretion | Kidney 94% Feces 6% |
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| CompTox Dashboard(EPA) | |
| ECHA InfoCard | 100.042.968 |
| Chemical and physical data | |
| Formula | C15H22O3 |
| Molar mass | 250.338 g·mol−1 |
| 3D model (JSmol) | |
| Melting point | 61 to 63 °C (142 to 145 °F) |
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Gemfibrozil, sold under the brand nameLopid among others, is a medication used to treatabnormal blood lipid levels.[2] It is generally less preferred thanstatins.[2][3] Use is recommended together with dietary changes and exercise.[2] It is unclear if it changes the risk ofheart disease.[2] It is taken by mouth.[2]
Common side effects include headache, dizziness, feeling tired, and intestinal upset.[2] Serious side effects may includeangioedema,gallstones,liver problems, andmuscle breakdown.[2] Use inpregnancy andbreastfeeding is of unclear safety.[4] It belongs to thefibrates group of medications and works by decreasing the breakdown of lipids infat cells.[2]
Gemfibrozil was patented in 1968, and came into medical use in 1982.[5] It is available as ageneric medication.[3] In 2022, it was the 231st most commonly prescribed medication in the United States, with more than 1 million prescriptions.[6][7]
The exact mechanism of action of gemfibrozil is unknown; however, several theories exist regarding the very low density lipoprotein (VLDL) effect; it can inhibit lipolysis and decrease subsequent hepatic fatty acid uptake as well as inhibit hepatic secretion of VLDL; together these actions decrease serum VLDL levels and increase HDL-cholesterol; the mechanism behind HDL elevation is currently unknown.
Gemfibrozil increases the activity of extrahepaticlipoprotein lipase (LL), thereby increasing lipoprotein triglyceride lipolysis. It does so by activatingperoxisome proliferator-activated receptor alpha (PPARα) 'transcription factor ligand', a receptor that is involved in metabolism of carbohydrates and fats, as well as adipose tissue differentiation. This increase in the synthesis of lipoprotein lipase thereby increases the clearance of triglycerides. Chylomicrons are degraded, VLDLs are converted to LDLs, and LDLs are converted to HDL. This is accompanied by a slight increase in secretion of lipids into the bile and ultimately the intestine. Gemfibrozil also inhibits the synthesis and increases the clearance ofapolipoprotein B, a carrier molecule for VLDL.[10]
Gemfibrozil was selected from a series of related compounds synthesized in the laboratories of the American companyParke-Davis in the late 1970s. It came from research for compounds that lower plasma lipid levels in humans and in animals.[11]
Gemfibrozil has been detected inbiosolids (the solids remaining aftersewage treatment) at concentrations up to 2650 ng/g wet weight.[12] This indicates that it survives thewastewater treatment process. It is also detected asenvironmental persistent micropollutant inaquifers and ingroundwaters inkarstic areas.[13]
