Clofibrato

Clofibrato Uses, Dosage, Side Effects, Food Interaction and all others data.

A fibric acid derivative used in the treatment of hyperlipoproteinemia type III and severe hypertriglyceridemia. (From Martindale, The Extra Pharmacopoeia, 30th ed, p986)

Clofibrato 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 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.

Trade Name Clofibrato
Availability Discontinued
Generic Clofibrate
Clofibrate Other Names Clofibrate, Clofibrato, Clofibratum, EPIB, Ethyl chlorophenoxyisobutyrate, Ethyl clofibrate, Liprin
Related Drugs Zetia, Praluent, Repatha, atorvastatin, simvastatin, rosuvastatin, Lipitor, ezetimibe, Crestor
Type
Formula C12H15ClO3
Weight Average: 242.699
Monoisotopic: 242.070972053
Protein binding

Highly protein-bound (95% to 97%).

Groups Approved, Investigational
Therapeutic Class
Manufacturer
Available Country
Last Updated: September 19, 2023 at 7:00 am
Clofibrato
Clofibrato

Uses

Clofibrato is a fibric acid derivative used to treat hypertriglyceridemia and high cholesterol.

For Primary Dysbetalipoproteinemia (Type III hyperlipidemia) that does not respond adequately to diet. This helps control high cholesterol and high triglyceride levels.

How Clofibrato works

Clofibrato 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. Clofibrato also inhibits the synthesis and increases the clearance of apolipoprotein B, a carrier molecule for VLDL. Also, as a fibrate, Clofibrato is an agonist of the PPAR-α receptor[4] in muscle, liver, and other tissues. This agonism ultimately leads to modification in gene expression resulting in increased beta-oxidation, decreased triglyceride secretion, increased HDL, increased lipoprotein lipase activity.

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.

Food Interaction

  • Take with food. Food decreases the risk of GI side effects.

Elimination Route

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.

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.

Innovators Monograph

You find simplified version here Clofibrato

*** Taking medicines without doctor's advice can cause long-term problems.
Share