Bezafibrate

Indications

Bezafibrate is used for: Hyperlipidaemias

Adult Dose

Oral Hyperlipidaemias Adult: As conventional tab: 200 mg tid, may increase dose gradually, to avoid GI symptoms, over 5-7 days. Maintenance: 200 mg bid. As modified-release tab: 400 mg once daily. Hepatic impairment: Severe: Contraindicated.

Child Dose

Renal Dose

Renal impairment: Dialysis patients: Contraindicated. CrCl (ml/min) Dosage Recommendation <15 As conventional tab: Contraindicated. 15-40 As conventional tab: 200 mg daily or on alternate days. >40-60 As conventional tab: 400 mg daily. <60 As modified-release tab: Contraindicated.

Administration

Should be taken with food.

Contra Indications

Gallbladder disorder, hypoalbuminaemia (e.g. nephrotic syndrome). Severe hepatic or renal impairment [CrCl <15 mL/min (conventional tab); CrCl <60 mL/min (modified-release tab)], patients undergoing dialysis. Pregnancy and lactation. Concomitant use of HMG-CoA reductase inhibitors (in patients w/ risk factors for myopathy), perhexiline maleate and MAOIs.

Precautions

Renal impairment [(CrCl ≥15 mL/min (conventional tab)]. Patient Counselling This drug may cause dizziness, if affected, do not drive or operate machinery. Monitoring Parameters Perform serum lipids, cholesterol and triglyceride tests, fasting glucose, creatinine, and CBC periodically, and LFT after 3-6 mth.

Pregnancy-Lactation

Interactions

Anion-exchange resins (e.g. cholestyramine) inhibit bezafibrate absorption, take at least 2 hr apart. May increase serum concentration of anticoagulants. Increased risk of renal impairment when used w/ immunosuppressants. May potentiate the therapeutic effect of sulfonylureas and insulin. Estrogens may increase lipid levels, dosing should be individualised in patients taking estrogen-containing contraceptives. Potentially Fatal: Potential hepatotoxic effect when used w/ perhexiline maleate or MAOIs. Increased risk of myopathy in predisposed patients who are taking HMG-CoA reductase inhibitors.

Adverse Effects

Side effects of Bezafibrate : Anorexia, nausea, GI upset, headache, dizziness, vertigo, fatigue, skin rashes, pruritus, urticaria, photosensitivity, alopecia, impotence, anaemia, leucopoenia, thrombocytopenia, pancytopenia, decreased appetite, peripheral neuropathy, paraesthesia, depression, insomnia, abdominal pain, constipation, dyspepsia, diarrhoea, abdominal distension, pancreatitis, cholestasis, cholelithiasis, Stevens-Johnsons syndrome, toxic epidermal necrolysis, myalgia, myopathy, myositis, erectile dysfunction, interstitial lung disease, acute renal failure. Rarely, rhabdomyolysis.

Mechanism of Action

Bezafibrate, a fibric acid derivative, reduces VLDL and LDL while increasing HDL levels. It increases the activity of triglyceride lipases involved in the catabolism of triglyceride-rich lipoproteins and inhibits hepatic acetyl co-enzyme A carboxylase synthesis.