Source: Υπουργείο Υγείας (CY) Revision Year: 2018 Publisher: Remedica Ltd, Aharnon Street, Limassol Industrial Estate, 3056 Limassol, Cyprus
Pharmacotherapeutic group: Lipid modifying agents, Lipid modifying agents, Plain
ATC code: C10AB02
Bezafibrate lowers elevated levels of serum cholesterol and triglycerides (i.e. lowers elevated low density lipoprotein and very low density lipoprotein levels, and raises lowered high density lipoprotein levels) by stimulating lipoprotein lipase and hepatic lipase, and by suppressing the activity of 3 HMGCo-A reductase resulting in stimulation of low density lipoprotein receptors on the cell surface.
Studies have shown Bezafibrate to be effective in treating hyperlipidaemia in patients with diabetes mellitus. Some cases showed a beneficial reduction in fasting blood glucose.
Significant reductions in serum fibrinogen levels have been observed in hyperfibrinogenaemic patients treated with Bezafibrate.
There is evidence that treatment with fibrates may reduce coronary heart disease events but have not been shown to decrease all-cause mortality in the primary or secondary prevention of cardiovascular disease.
Maximum concentrations of Bezafibrate appear around 2 hours after ingestion of Lacromid tablets. The protein binding of Bezafibrate in serum is approximately 95%. The elimination half-life is in the order of 2,1 hours although elimination is markedly slowed in the presence of limited renal function. Elimination may be increased in forced diuresis. The drug substance is non-dialysable (cuprophane filter).
Pharmacokinetic investigations in the elderly suggest that elimination may be delayed in cases of impaired liver function. Liver disease (except fatty liver) is a contraindication for the use of bezafibrate (see 4.3 Contraindications).
In elderly patients, there is a physiological reduction of the renal function with age. Bezafibrate dosage should be adjusted based on the serum creatinine and creatinine clearance values as indicated in the above table.
The elimination of bezafibrate is reduced in patients with impaired renal function and dosage adjustments are necessary to prevent drug accumulation and toxic effects.
Not surprisingly there is a correlation between creatinine clearance and the elimination half-life of bezafibrate; with decreasing creatinine clearance the elimination half-life is increasing.
Because of its high protein binding, bezafibrate cannot be dialysed (cuprophane filter). The use of bezafibrate is contraindicated in dialysis patients.
The chronic administration of a high dose of Bezafibrate to rats was associated with hepatic tumour formation in females. This dosage was in the order of 30 to 40 times the human dosage. No such effect was apparent at reduced intake levels approximating more closely to the lipid-lowering dosage in humans.
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