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QuickView for Clofibrate (compound)

Name: Clofibrate
PubChem Compound ID: 254788
Description: A fibric acid derivative used in the treatment of HYPERLIPOPROTEINEMIA TYPE III and severe HYPERTRIGLYCERIDEMIA. (From Martindale, The Extra Pharmacopoeia, 30th ed, p986)
Molecular formula: C31H45ClO5
Molecular weight: 533.139 g/mol
8075-95-4; Atromid; 3-.alpha.-hydroxy-5-.alpha.-androstan-17-one, mixture with ethyl 2- (4-chlorophenoxy)-2-methylpropanoate; Atromid (Ayerst 647); 5.alpha.-Androstan-17-one, 3.alpha.-hydroxy-, compd. with propionic acid, 2-(p-chlorophenoxy)-2-methyl-, ethyl ester; NSC79390
Name: Clofibrate
Name (isomeric): DB00636
Drug Type: small molecule
Description: A fibric acid derivative used in the treatment of HYPERLIPOPROTEINEMIA TYPE III and severe HYPERTRIGLYCERIDEMIA. (From Martindale, The Extra Pharmacopoeia, 30th ed, p986)
Ethyl para-chlorophenoxyisobutyrate; Chlorfenisate; EPIB; Chlorphenisate; Ethyl p-chlorophenoxyisobutyrate; Clofibate; CPIB; Ethyl clofibrate; Clofibratum; Ethyl chlorophenoxyisobutyrate.
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Brand: Dura clofibrat, Angiokapsul, Clobrat, Clobren-SF, Atheropront, Miscleron, Sklerepmexe, Skleromex, Clofibrat, Sklero-Tablinen, Clofibram, Yoclo, Levatrom, Lipidsenker, Lipide 500, Delipid, Arterosol, Hyclorate, Liposid, Ticlobran, Sklero-tablinene, Claripex, Lipomid, Liprinal, Liporil, Arterioflexin, Claripex CPIB, Xyduril, Cartagyl, Lipofacton, Atheromide, neo-Atomid, Atrovis, Scrobin, Amotril S, Athranid-Wirkstoff, Negalip, Antilipide, Regelan, Tetrasipton, Anparton, Regelan N, Atromid-S, Klofiran, Atromida, Citiflus, Bioscleran, Ateriosan, Serofinex, Clofipront, Liponorm, Normat, Vincamin compositum, Atromidin, Liporeduct, Antilipid, Thiosan, Fibralem, Athebrate, Clofinit, Normalip, Clofar, Apolan, ELPI, Artevil, Azionyl, Artes, Novofibrate, Lipavlon, Lipamid, Lipavil, Sklerolip, Atromid, Gerastop, Serotinex, Robigram, Sklero, Persantinat, Klofibrat, Skerolip, Deliva, Oxan 600, Neo-Atromid, Sklero-tabuls, Liprin, Atrolen, Regardin, Clobren-5F, Thillate, Ateculon, Bresit, Skleromexe, Atromid S, Normolipol, Cloberat, Lobetrin, Amotril
Category: Antilipemic Agents, Anticholesteremic Agents
CAS number: 637-07-0
Indication: For Primary Dysbetalipoproteinemia (Type III hyperlipidemia) that does not respond adequately to diet. This helps control high cholesterol and high triglyceride levels.
Clofibrate is an antilipidemic agent similar to gemfibrozil. It acts to lower elevated serum lipids by reducing the very low-density lipoprotein fraction (Sf 20-400) rich in triglycerides. Serum cholesterol may be decreased, particularly in those patients whose cholesterol elevation is due to the presence of IDL as a result of Type III h...
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Mechanism of Action:
Clofibrate 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. Clofibrate also inhibits ...
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Absorption: Completely but slowly absorbed from the intestine. Between 95% and 99% of an oral dose of clofibrate is excreted in the urine as free and conjugated clofibric acid; thus, the absorption of clofibrate is virtually complete.
Protein binding: Highly protein-bound (95% to 97%).
Biotransformation: Hepatic and gastrointestinal: rapid de-esterification occurs in the gastrointestinal tract and/or on first-pass metabolism to produce the active form, clofibric acid (chlorophenoxy isobutyric acid [CPIB]).
Half Life: Half-life in normal volunteers averages 18 to 22 hours (range 14 to 35 hours) but can vary by up to 7 hours in the same subject at different times.
Toxicity: Oral, mouse: LD50 = 1220 mg/kg; Oral, rabbit: LD50 = 1370 mg/kg; Oral, rat: LD50 = 940 mg/kg. No reported case of overdosage in humans.
Affected organisms: Humans and other mammals
Food interaction:
Take with food, since it may reduce gastric irritation.
Drug interaction:
AcetohexamideClofibrate may increase the effect of sulfonylurea, acetohexamide.
Insulin AspartIncreases the effect of insulin
GliclazideClofibrate may increase the effect of sulfonylurea, gliclazide.
TolazamideClofibrate may increase the effect of sulfonylurea, tolazamide.
Insulin DetemirIncreases the effect of insulin
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