4864 Gemfibrozil 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. 25812-30-0 3463 C15H22O3 White powder. 62°C 158.5°C at 2.00E-02 mm Hg 10 mg/mL (in base) Well absorbed from gastrointestinal tract (within 1-2 hours). Gemfibrozil increases the activity of extrahepatic lipoprotein lipase (LL), thereby increasing lipoprotein triglyceride lipolysis. It does so by activating Peroxisome proliferator-activated receptor-alpha (PPAR‘±) '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 of apolipoprotein B, a carrier molecule for VLDL. 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 Oral, mouse: LD₅₀ = 3162 mg/kg. 3, not classifiable as to its carcinogenicity to humans. (L135) 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. Symptoms of overdose include abdominal cramps, diarrhea, joint and muscle pain, nausea, and vomiting. 2014-09-11T05:17:33Z 2014-12-24T20:26:57Z Gemfibrozil C07020 5296 D015248 DB01241 true CC1=CC(OCCCC(C)(C)C(O)=O)=C(C)C=C1 C15H22O3 InChI=1S/C15H22O3/c1-11-6-7-12(2)13(10-11)18-9-5-8-15(3,4)14(16)17/h6-7,10H,5,8-9H2,1-4H3,(H,16,17) InChIKey=HEMJJKBWTPKOJG-UHFFFAOYSA-N 250.3334 250.15689457 Exogenous Solid 3.4 HMDB15371 CHEMBL457 3345 <p>Gianfranco Piccoli, Antonio Tarquini, Giovanni Frare, &#8220;Process for the preparation of gemfibrozil.&#8221; U.S. Patent US5654476, issued May, 1980.</p>