Befizal - General Information
Antilipemic agent that lowers cholesterol and triglycerides. It decreases low density lipoproteins and increases high density lipoproteins.
Pharmacology of Befizal
Befizal is an antilipemic agent that lowers cholesterol and triglycerides. It decreases low density lipoproteins and increases high density lipoproteins. Befizal lowers elevated blood lipids (triglycerides and cholesterol). Elevated VLDL and LDL are reduced by treatment with bezafibrate, whilst HDL-levels are increased. The activity of triglyceride lipases (lipoprotein lipase and hepatic lipoproteinlipase) involved in the catabolism of triglyceride-rich lipoproteins is increased by bezafibrate. In the course of the intensified degradation of triglyceride-rich lipoproteins (chylomicrons, VLDL) precursors for the formation of HDL are formed which explains an increase in HDL. Furthermore, cholesterol biosynthesis is reduced by bezafibrate, which is accompanied by a stimulation of the LDL-receptor-mediated lipoprotein catabolism. Elevated fibrinogen appears to be an important risk-factor, alongside the lipids, smoking and hypertension, in the development of atheroma. Fibrinogen plays an important role in viscosity, and therefore blood flow, and also appears to play an important role in thrombus development and lysability. Befizal exerts an effect on thrombogenic factors. A significant decrease in elevated plasma fibrinogen levels can be achieved. This may lead, amongst other things, to a reduction in both blood and plasma viscosity. Inhibition of platelet aggregation has also been observed. A reduction in blood glucose concentration due to an increase in glucose tolerance has been reported in diabetic patients. In the same patients, the concentration of fasting and postprandial free fatty acids was reduced by bezafibrate.
Befizal for patients
When Bezalip or Bezalip retard is used at the same time as other medicines or substances the following interactions must be taken into account:
- Bezalip and Bezalip retard may enhance the action of anticoagulants of the coumarin type. For this reason, the dose of the anticoagulant should be reduced by 30 - 50% at the start of treatment with Bezalip or Bezalip retard and then titrated according to the blood clotting parameters.
- The action of sulphonylureas and insulin may be enhanced by Bezalip or Bezalip retard. This may be due to an improved glucose utilization with simultaneous reduction in insulin requirement.
- In isolated cases, a pronounced though reversible, impairment of renal function (accompanied by a corresponding increase in the serum creatinine level) has been reported in organ transplant patients receiving immuno-suppressant therapy and concomitant bezafibrate. Accordingly, renal function should be closely monitored in these patients and, in the event of relevant significant changes in laboratory parameters, bezafibrate should, if necessary, be discontinued .
- When Bezalip or Bezalip retard is used concurrently with anion-exchange resins (e.g. cholestryramine), an interval of at least 2 hours should be maintained between the two medicines, since the absorption of Bezalip or Bezalip retard is impaired.
- Perhexiline hydrogen maleate or MAO-inhibitors (with hepatotoxic potential) must not be administered together with Bezalip or Bezalip retard.
Bezafibrate must not be used in:
- liver disease (with the exception of fatty liver which is a frequent accompaniment to hypertriglyceridaemia)
- gall-bladder diseases with or without cholelithiasis (as a possible liver involvement cannot be excluded)
- Bezafibrate 200 mg: Patients with severe renal impairment presenting serum creatinine levels > 6 mg / 100 ml or creatinine clearance < 15 ml / min
- Bezafibrate retard 400 mg: in patients with renal impairment presenting serum creatinine levels > 1.5mg/100ml (>135 micromol/l) or creatinine clearance < 60 ml/min or in patients undergoing dialysis.
- known hypersensitivity to bezafibrate, to any component of the product or to other fibrates.
- known photoallergic or phototoxic reactions to fibrates
- during pregnancy and lactation
Additional information about Befizal
Befizal Indication: For the treatment of primary hyperlipidaemia types IIa, IIb, III, IV and V (Fredrickson classification) corresponding to groups I, II and III of the European Atherosclerosis Society guidelines - when diet alone or improvements in lifestyle such as increased exercise or weight reduction do not lead to an adequate response. Also for the treatment of secondary hyperlipidaemias, e.g. severe hypertriglyceridemias, when sufficient improvement does not occur after correction of the underlying disorder (e.g. diabetes mellitus).
Mechanism Of Action: Like the other fibrates, bezafibrate is an agonist of PPARα; some studies suggest it may have some activity on PPARγ and PPARδ as well.
Drug Interactions: Not Available
Food Interactions: Not Available
Generic Name: Bezafibrate
Synonyms: Bezafibrat; Bezafibratum [inn-latin]; Bezafibrato [inn-spanish]
Drug Category: Antilipemic Agents
Drug Type: Small Molecule; Approved
Other Brand Names containing Bezafibrate: Bezalip; Bezalip retard; Bezatol; Bezatol SR; Cedur; Befizal;
Absorption: Bezafibrate is almost completely absorbed after oral administration. The relative bioavailability of bezafibrate retard compared to the standard form is about 70%.
Toxicity (Overdose): Not Available
Protein Binding: 94-96% of bezafibrate is bound to protein in human serum.
Half Life: 1-2 hours
Dosage Forms of Befizal: Tablet Oral
Tablet, film coated, extended release Oral
Tablet, extended release Oral
Chemical IUPAC Name: 2-[4-[2-[(4-chlorobenzoyl)amino]ethyl]phenoxy]-2-methylpropanoic acid
Chemical Formula: C19H20ClNO4
Bezafibrate on Wikipedia: http://en.wikipedia.org/wiki/Bezafibrate
Organisms Affected: Humans and other mammals