Clofibrate

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Clofibrate
Clofibrate.svg
Systematic (IUPAC) name
ethyl 2-(4-chlorophenoxy)-2-methylpropanoate
Clinical data
AHFS/Drugs.comMicromedex Detailed Consumer Information
Pregnancy cat.B1 (AU) C (US)
Legal statusDiscontinued (US)
RoutesOral
Pharmacokinetic data
Protein bindingVariable, 92–97% at therapeutic concentrations
MetabolismHydrolyzed to clofibric acid; hepatic glucuronidation
Half-lifeHighly variable; average 18–22 hours. Prolonged in renal failure
ExcretionRenal, 95 to 99%
Identifiers
CAS number637-07-0
ATC codeC10AB01
PubChemCID 2796
DrugBankDB00636
ChemSpider2694 YesY
UNIIHPN91K7FU3 YesY
KEGGD00279 YesY
ChEBICHEBI:3750 YesY
ChEMBLCHEMBL565 YesY
Chemical data
FormulaC12H15ClO3 
Mol. mass242.698 g/mol
Physical data
Boiling point148 °C (298 °F)
 YesY (what is this?)  (verify)
 
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Clofibrate
Clofibrate.svg
Systematic (IUPAC) name
ethyl 2-(4-chlorophenoxy)-2-methylpropanoate
Clinical data
AHFS/Drugs.comMicromedex Detailed Consumer Information
Pregnancy cat.B1 (AU) C (US)
Legal statusDiscontinued (US)
RoutesOral
Pharmacokinetic data
Protein bindingVariable, 92–97% at therapeutic concentrations
MetabolismHydrolyzed to clofibric acid; hepatic glucuronidation
Half-lifeHighly variable; average 18–22 hours. Prolonged in renal failure
ExcretionRenal, 95 to 99%
Identifiers
CAS number637-07-0
ATC codeC10AB01
PubChemCID 2796
DrugBankDB00636
ChemSpider2694 YesY
UNIIHPN91K7FU3 YesY
KEGGD00279 YesY
ChEBICHEBI:3750 YesY
ChEMBLCHEMBL565 YesY
Chemical data
FormulaC12H15ClO3 
Mol. mass242.698 g/mol
Physical data
Boiling point148 °C (298 °F)
 YesY (what is this?)  (verify)

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).

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 affects.

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.