Overview
| Trade Names: | Apo-Gemfibrozil; Bolutol; Cholespid; Decrelip; Fibratol; Fibrocit; Gemfibril; Gemfibromax; Gemlipid; Gen-Fibro; Genlip; Gevilon; Hipolixan; Jezil; Lipozid; Lipur; Lopid; Novo-Gemfibrozil; Nu-Gemfibrozil |
|---|---|
| PharmGKB Accession Id: | PA449750 |
Description
A lipid-regulating agent that lowers elevated serum lipids primarily by decreasing serum triglycerides with a variable reduction in total cholesterol. These decreases occur primarily in the VLDL fraction and less frequently in the LDL fraction. Gemfibrozil increases HDL subfractions HDL2 and HDL3 as well as apolipoproteins A-I and A-II. Its mechanism of action has not been definitely established. PubChem (source: Drug Bank)
Indication
For treatment of adult patients with very high elevations of serum triglyceride levels (types IV and V hyperlipidemia) who are at risk of developing pancreatitis (inflammation of the pancreas) and who do not respond adequately to a strict diet. (source: Drug Bank)
ATC Therapeutic Category
- C10AB:Fibrates
Pharmacology, Interactions, and Contraindications
Mechanism Of Action
Gemfibrozil increases the activity of extrahepatic lipoprotein lipase (LL), thereby increasing lipoprotein triglyceride lipolysis. 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 of apolipoprotein B, a carrier molecule for VLDL. (source: Drug Bank)
Pharmacology
Gemfibrozil, a fibric acid antilipemic agent similar to clofibrate, is used to treat hyperlipoproteinemia and as a second-line therapy for type IIb hypercholesterolemia. It acts to reduce triglyceride levels, reduce VLDL levels, reduce LDL levels (moderately), and increase HDL levels (moderately). (source: Drug Bank)
Food Interactions
Take 30 minutes before meals. (source: Drug Bank)
Absorption, Distribution, Metabolism, Elimination & Toxicity
Biotransformation
Hepatic. Gemfibrozil mainly undergoes oxidation of a ring methyl group to successively form a hydroxymethyl and a carboxyl metabolite. (source: Drug Bank)
Protein Binding
95% (source: Drug Bank)
Absorption
Well absorbed from gastrointestinal tract (within 1-2 hours). (source: Drug Bank)
Toxicity
Oral, mouse: LD<sub>50</sub> = 3162 mg/kg. Symptoms of overdose include abdominal cramps, diarrhea, joint and muscle pain, nausea, and vomiting. (source: Drug Bank)
Isomeric SMILES Code:
CC1=CC(=C(C=C1)C)OCCCC(C)(C)C(=O)O (source: Drug Bank)
The following genes are in curated knowledge about this drug.
| Gene | Relationship | Evidence | |
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ABCB1 |
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ACE |
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APOE |
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C3 |
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CYP2C8 |
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CYP2C9 |
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CYP3A4 |
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ESRRA |
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SLCO1B1 |
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SLCO2B1 |
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A list of non-curated publications that mention this drug along with other genes is available.
Drug Targets
| Gene | Description | |
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| LPL |
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(source: Drug Bank) |
| PPARA |
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(source: Drug Bank) |
| SLCO1B1 |
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(source: Drug Bank) |
The following drugs are in curated knowledge about this drug.
| Drug | Relationship | Evidence | |
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ezetimibe |
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montelukast |
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repaglinide |
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warfarin |
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A list of non-curated publications that mention this drug along with other drugs is available.
Drug Interactions
| Drug | Description | |
|---|---|---|
| acenocoumarol |
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Gemfibrozil increases the anticoagulant effect (source: Drug Bank) |
| atorvastatin |
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Increased risk of myopathy/rhabdomyolysis (source: Drug Bank) |
| cerivastatin |
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Increased risk of myopathy/rhabdomyolysis (source: Drug Bank) |
| dicumarol |
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Gemfibrozil increases the anticoagulant effect (source: Drug Bank) |
| fluvastatin |
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Increased risk of myopathy/rhabdomyolysis (source: Drug Bank) |
| lovastatin |
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Increased risk of myopathy/rhabdomyolysis (source: Drug Bank) |
| pioglitazone |
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Increases the effect and toxicity of rosiglitazone/pioglitazone (source: Drug Bank) |
| pravastatin |
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Increased risk of myopathy/rhabdomyolysis (source: Drug Bank) |
| repaglinide |
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Increases the effect and toxicity of repaglinide (source: Drug Bank) |
| rosiglitazone |
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Increases the effect and toxicity of rosiglitazone/pioglitazone (source: Drug Bank) |
| rosuvastatin |
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Rosuvastatin possibly increases the effect of the fibrate (source: Drug Bank) |
| simvastatin |
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Increased risk of myopathy/rhabdomyolysis (source: Drug Bank) |
| ursodeoxycholic acid |
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The fibric acid derivative decreases the effect of ursodiol (source: Drug Bank) |
| warfarin |
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Gemfibrozil increases the anticoagulant effect (source: Drug Bank) |
Curated Information
The following diseases are in curated knowledge about this drug.
| Disease | Relationship | Evidence | |
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Cardiomyopathy, Dilated |
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Carotid Artery Diseases |
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Obesity |
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Rhabdomyolysis |
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visceral obesity |
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Non-Curated Information
A list of non-curated publications that mention this drug along with other diseases is available.
Additional Datasets
These datasets are minimally curated and are sorted alphabetically by title.
LinkOuts
Common Searches
Search PubMed
Search Medline Plus
Search PubChem
Search CTD
Non-Curated Publications
A list of non-curated publications that mention this drug is available.
