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QuickView for Gemfibrozil (compound)


PubChem
Name: Gemfibrozil
PubChem Compound ID: 3463
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.
Molecular formula: C15H22O3
Molecular weight: 250.333 g/mol
Synonyms:
Lifibron; Taborcil; Gemfibrozil (JAN/USP); Elmogan; Renabrazin; Synbrozil; AIDS-121781; Gozid; Gemfibrozil [USAN:BAN:INN]; Lipizyl.
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DrugBank
Identification
Name: Gemfibrozil
Name (isomeric): DB01241
Drug Type: small molecule
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.
Brand: Decrelip, Novo-Gemfibrozil, Lopid, Fibratol, Gemlipid, Genlip, Jezil, Lipur, Apo-Gemfibrozil, Cholespid, Gemfibril, Gen-Fibro, Lipozid, Gemfibromax, Bolutol, Fibrocit, Gevilon, Hipolixan, Nu-Gemfibrozil
Category: Fribic Acid Derivatives, Antilipemic Agents
CAS number: 25812-30-0
Pharmacology
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.
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).
Mechanism of Action:
Gemfibrozil increases the activity of extrahepatic lipoprotein lipase (LL), thereby increasing lipoprotein triglyceride lipolysis. It does so by activating Peroxisome proliferator-activated receptor-alpha (PPARĪ±) 'transcription factor ligand', a receptor that is involved in metabolism of carbohydrates and fats, as well as adipose tissue differentia...
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Absorption: Well absorbed from gastrointestinal tract (within 1-2 hours).
Protein binding: 95%
Biotransformation: Hepatic. Gemfibrozil mainly undergoes oxidation of a ring methyl group to successively form a hydroxymethyl and a carboxyl metabolite.
Route of elimination: Approximately seventy percent of the administered human dose is excreted in the urine, mostly as the glucuronide conjugate, with less than 2% excreted as unchanged gemfibrozil.
Half Life: 1.5 hours
Toxicity: Oral, mouse: LD50 = 3162 mg/kg. Symptoms of overdose include abdominal cramps, diarrhea, joint and muscle pain, nausea, and vomiting.
Affected organisms: Humans and other mammals
Interactions
Food interaction:
Take 30 minutes before meals.
Drug interaction:
DicumarolGemfibrozil may increase the anticoagulant effect of dicumarol.
CerivastatinIncreased risk of myopathy/rhabdomyolysis
TrimipramineThe strong CYP2C19 inhibitor, Gemfibrozil, may decrease the metabolism and clearance of Trimipramine, a CYP2C19 substrate. Consider alternate therapy or monitor for changes in therapeutic and adverse effects of Trimipramine if Gemfibrozil is initiated, discontinued or dose changed.
TolbutamideGemfibrozil, a strong CYP2C9 inhibitor, may decrease the metabolism and clearance of Tolbutamide, a CYP2C9 substrate. Consider alternate therapy or monitor for changes in Tolbutamide therapeutic and adverse effects if Gemfibrozil is initiated, discontinued or dose changed.
RepaglinideGemfibrozil may increase the effect and toxicity of repaglinide.
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