Source: Υπουργείο Υγείας (CY) Revision Year: 2011 Publisher: Medochemie Ltd, p.o box 51409, Limassol, Cyprus
Bezafibrate lowers elevated serum cholesterol levels and triglycerides, lowering elevated low density lipoprotein (LDLP) and very low density lipoprotein (VLDLP), and elevating depressed levels of high density lipoprotein (HDLP). These effects are mediated by stimulation of hepatic lipase and lipoprotein lipase, and suppression of 3–HMGCo–A reductase, with consequent stimulation of cell surface LDLP receptors.
Bezafibrate has been demonstrated to be effective in therapy of hyperlipidaemia in diabetes mellitus patients, in some instances resulting in a reduction of fasting blood glucose levels.
Bezafibrate therapy has resulted in significant decreases of serum fibrinogen levels in hyperfibrinogenaemic patients.
There is evidence that treatment with fibrates may reduce coronary heart disease events but they have not been shown to decrease all cause mortality in the primary or secondary prevention of cardiovascular disease.
Bezafibrate is well absorbed following oral administration with an absolute bioavailability of 100%; with peak serum levels occurring approximately two hours post dosing. Bezafibrate is approximately 95% plasma protein bound, with a volume of distribution of about 17 litres.
Bezafibrate undergoes some hepatic metabolism, the exact extent of which is unknown, metabolism occurs via hydroxylation and glucuronidation; hydrolytic cleavage by microsomal mixed-function oxidases may also be involved. The activity of the known metabolites, glucuronides and hydroxy derivatives, is unknown.
Elimination half life is about two hours, this is prolonged in the presence of impaired renal function, and may be prolonged in the elderly. Bezafibrate is none dialyzable, forced diuresis may result in increased elimination.
The majority of the dose is excreted in the urine, about 95% over 24 hours, approximately 40% as the unchanged drug and the remainder as metabolites, principally the glucuronide conjugate. Renal clearance is about 4 L/hour, plasma clearance is approximately 7 L/hour. A small proportion, <2%, of the dose is excreted in the faeces. It is unknown if bezafibrate is excreted in breast milk.
Long term administration of high doses of bezafibrate, at levels some 30-40 times the recommended dose in man, resulted in associated hepatic tumour formation in female rats. This effect did not manifest itself at lower dosage levels more closely approximating the recommended lipid lowering dosage in man.
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