Clofibrate

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Clofibrate
Clofibrate.svg
Clinical data
AHFS/Drugs.com Micromedex Detailed Consumer Information
Pregnancy
category
  • AU: B1
  • US: C (Risk not ruled out)
Routes of
administration
Oral
ATC code
Legal status
Legal status
  • US: Discontinued
Pharmacokinetic data
Protein binding Variable, 92–97% at therapeutic concentrations
Metabolism Hydrolyzed to clofibric acid; hepatic glucuronidation
Biological half-life Highly variable; average 18–22 hours. Prolonged in renal failure
Excretion Renal, 95 to 99%
Identifiers
CAS Number
PubChem CID
IUPHAR/BPS
DrugBank
ChemSpider
UNII
KEGG
ChEBI
ChEMBL
ECHA InfoCard 100.010.253
Chemical and physical data
Formula C12H15ClO3
Molar mass 242.698 g/mol
3D model (Jmol)
Boiling point 148 °C (298 °F)
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Clofibrate (tradename Atromid-S) is an organic compound. It is marketed as a fibrate. It is a lipid-lowering agent used for controlling the high cholesterol and triacylglyceride level in the blood. It increases lipoprotein lipase activity to promote the conversion of VLDL to LDL, and hence reduce the level of VLDL. It can increase the level of HDL as well.

Complications and controversies[edit]

It can induce SIADH, syndrome of inappropriate secretion of antidiuretic hormone ADH (vasopressin). Clofibrate can also result in formation of cholesterol stones in the gallbladder.

The World Health Organization Cooperative Trial on Primary Prevention of Ischaemic Heart Disease using clofibrate to lower serum cholesterol observed excess mortality in the clofibrate-treated group despite successful cholesterol lowering (47% more deaths during treatment with clofibrate and 5% after treatment with clofibrate) than the non-treated high cholesterol group. These deaths were due to a wide variety of causes other than heart disease, and remain "unexplained".[1]

Clofibrate was discontinued in 2002 due to adverse effects.

References[edit]

  1. ^ "WHO cooperative trial on primary prevention of ischaemic heart disease with clofibrate to lower serum cholesterol: final mortality follow-up. Report of the Committee of Principal Investigators". Lancet. 2 (8403): 600–4. September 1984. PMID 6147641. doi:10.1016/s0140-6736(84)90595-6.