Overview
| Generic Names: | CPIB; Chlorfenisate; Chlorphenisate; Clofibate; Clofibrato; Clofibratum; EPIB; Ethyl chlorophenoxyisobutyrate; Ethyl clofibrate; Ethyl p-chlorophenoxyisobutyrate; Ethyl para-chlorophenoxyisobutyrate |
|---|---|
| Trade Names: | Amotril; Amotril S; Angiokapsul; Anparton; Antilipid; Antilipide; Apolan; Arterioflexin; Arterosol; Artes; Artevil; Ateculon; Ateriosan; Athebrate; Atheromide; Atheropront; Athranid-Wirkstoff; Atrolen; Atromid; Atromid S; Atromid-S; Atromida; Atromidin; Atrovis; Azionyl; Bioscleran; Bresit; Cartagyl; Citiflus; Claripex; Claripex CPIB; Cloberat; Clobrat; Clobren-5F; Clobren-SF; Clofar; Clofibram; Clofibrat; Clofinit; Clofipront; Delipid; Deliva; Dura clofibrat; ELPI; Fibralem; Gerastop; Hyclorate; Klofibrat; Klofiran; Levatrom; Lipamid; Lipavil; Lipavlon; Lipide 500; Lipidsenker; Lipofacton; Lipomid; Liponorm; Liporeduct; Liporil; Liposid; Liprin; Liprinal; Lobetrin; Miscleron; Negalip; Neo-Atromid; Normalip; Normat; Normolipol; Novofibrate; Oxan 600; Persantinat; Regardin; Regelan; Regelan N; Robigram; Scrobin; Serofinex; Serotinex; Skerolip; Sklerepmexe; Sklero; Sklero-Tablinen; Sklero-tablinene; Sklero-tabuls; Sklerolip; Skleromex; Skleromexe; Tetrasipton; Thillate; Thiosan; Ticlobran; Vincamin compositum; Xyduril; Yoclo; neo-Atomid |
| PharmGKB Accession Id: | PA449045 |
Description
A fibric acid derivative used in the treatment of hyperlipoproteinemia type III and severe hypertriglyceridemia. (From Martindale, The Extra Pharmacopoeia, 30th ed, p986) (source: Drug Bank)
Indication
For Primary Dysbetalipoproteinemia (Type III hyperlipidemia) that does not respond adequately to diet. (source: Drug Bank)
ATC Therapeutic Category
- C10AB:Fibrates
Pharmacology, Interactions, and Contraindications
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 the synthesis and increases the clearance of apolipoprotein B, a carrier molecule for VLDL. (source: Drug Bank)
Pharmacology
Clofibrate is an antilipidemic agent similar to gemfibrozil. It acts to lower elevated serum lipids by reducing the very low-density lipoprotein fraction (S<sub>f</sub> 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 hyperlipoproteinemia. Several investigators have observed in their studies that clofibrate may produce a decrease in cholesterol linoleate but an increase in palmitoleate and oleate, the latter being considered atherogenic in experimental animals. The significance of this finding is unknown at this time. Reduction of triglycerides in some patients treated with clofibrate or certain of its chemically and clinically similar analogs may be associated with an increase in LDL cholesterol. Increase in LDL cholesterol has been observed in patients whose cholesterol is initially normal. Animal studies suggest that clofibrate interrupts cholesterol biosynthesis prior to mevalonate formation. (source: Drug Bank)
Food Interactions
Take with food, since it may reduce gastric irritation. (source: Drug Bank)
Absorption, Distribution, Metabolism, Elimination & Toxicity
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). (source: Drug Bank)
Protein Binding
Highly protein-bound (95% to 97%). (source: Drug Bank)
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. (source: Drug Bank)
Toxicity
Oral, mouse: LD<sub>50</sub> = 1220 mg/kg; Oral, rabbit: LD<sub>50</sub> = 1370 mg/kg; Oral, rat: LD<sub>50</sub> = 940 mg/kg. No reported case of overdosage in humans. (source: Drug Bank)
Isomeric SMILES Code:
CCOC(=O)C(C)(C)Oc1ccc(cc1)Cl (source: Drug Bank)
A list of non-curated publications that mention this drug along with other genes is available.
Drug Targets
| Gene | Description | |
|---|---|---|
| LPL |
|
(source: Drug Bank) |
| PPARA |
|
(source: Drug Bank) |
A list of non-curated publications that mention this drug along with other drugs is available.
Drug Interactions
| Drug | Description | |
|---|---|---|
| acenocoumarol |
|
The fibrate increases the anticoagulant effect (source: Drug Bank) |
| chlorpropamide |
|
The agent increases the effect of sulfonylurea (source: Drug Bank) |
| dicumarol |
|
The fibrate increases the anticoagulant effect (source: Drug Bank) |
| glibenclamide |
|
The agent increases the effect of sulfonylurea (source: Drug Bank) |
| gliclazide |
|
The agent increases the effect of sulfonylurea (source: Drug Bank) |
| glipizide |
|
The agent increases the effect of sulfonylurea (source: Drug Bank) |
| insulin-glargine |
|
Increases the effect of insulin (source: Drug Bank) |
| tolbutamide |
|
The agent increases the effect of sulfonylurea (source: Drug Bank) |
| ursodeoxycholic acid |
|
The fibric acid derivative decreases the effect of ursodiol (source: Drug Bank) |
| warfarin |
|
The fibrate increases the anticoagulant effect (source: Drug Bank) |
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
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Non-Curated Publications
A list of non-curated publications that mention this drug is available.