Clofibrate

Systematic (IUPAC) name
ethyl 2-(4-chlorophenoxy)-2-methylpropanoate
Identifiers
CAS number	637-07-0
ATC code	C10AB01
PubChem	2796
DrugBank	APRD00879
ChemSpider	2694
Chemical data
Formula	C12H15ClO3
Mol. mass	242.698 g/mol
SMILES	eMolecules & PubChem
Physical data
Boiling point	148 °C (298 °F)
Pharmacokinetic data
Bioavailability	?
Protein binding	Variable, 92–97% at therapeutic concentrations
Metabolism	Hydrolyzed to clofibric acid; hepatic glucuronidation
Half life	Highly variable; average 18–22 hours. Prolonged in renal failure
Excretion	Renal, 95 to 99%
Therapeutic considerations
Pregnancy cat.	B1(AU) C(US)
Legal status	℞-only(US)
Routes	Oral
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Clofibrate (tradename Atromid-S) is 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 is proved that it can increase the level of HDL as well.

Can induce SIADH (syndrome of inappropriate secretion of antidiuretic hormone ADH or otherwise called vasopressin)

The World Health Organization Cooperative Trial on Primary Prevention of Ischaemic Heart Disease using Clofibrate to lower serum cholesterol observed that there was 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]

[edit] References

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. 

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