Adult: As adjunct to diet and other therapeutic measures for the management of Fredrickson classification types IIa, IIb, III, IV, and V: As conventional tab: 200 mg tid; to minimise gastrointestinal effects, dose may be gradually increased over 5-7 days. As prolonged-release or sustained-release tab: 400 mg once daily. Discontinue therapy if adequate response is not achieved within 3-4 months. Treatment recommendations may vary between countries and among individual products (refer to specific local product guidelines).
What are the brands available for Bezafibrate in Hong Kong?
Patients undergoing dialysis: As conventional or prolonged-release/sustained-release tab: Contraindicated.
CrCl (mL/min)
Dosage
<15
As conventional tab: Contraindicated.
15-<40
As conventional tab: 200 mg once every 24 or 48 hours.
40-60
As conventional tab: 200 mg bid.
<60
As prolonged-release/sustained-release tab: Contraindicated.
Hepatic Impairment
Contraindicated.
Administration
Bezafibrate Should be taken with food.
Contraindications
Known photoallergic or phototoxic reactions with fibrates. Gallbladder diseases (with or without cholelithiasis), hypoalbuminaemia, nephrotic syndrome. Hepatic impairment (except fatty liver disease which frequently occurs in patients with hypertriglyceridaemia). Renal impairment (CrCl <15 mL/min [conventional tab] and CrCl <60 mL/min [prolonged-release/sustained-release tab]) and patients undergoing dialysis. Pregnancy and lactation. Concomitant use of HMG-CoA reductase inhibitors in patients with risk factors for myopathy (e.g. electrolyte or hormonal imbalance, pre-existing renal impairment, severe infection, trauma, surgery).
Special Precautions
Patient with history of jaundice or hepatic disorder. Renal impairment (conventional tab). Elderly.
Adverse Reactions
Significant: Hepatotoxicity (e.g. abnormal LFTs), cholelithiasis; haematologic effects (including mild reduction in Hb, WBCs, and platelets); myopathy or rhabdomyolysis (usually with renal impairment). Gastrointestinal disorders: Diarrhoea, dyspepsia, flatulence, nausea, abdominal pain, constipation, abdominal distention, gastritis. Immune system disorders: Hypersensitivity reactions. Investigations: Increased creatine phosphokinase (CPK), blood creatinine, and alkaline phosphatase. Metabolism and nutrition disorders: Decreased appetite. Musculoskeletal and connective tissue disorders: Myalgia, muscular weakness, muscle cramps. Nervous system disorders: Headache, dizziness. Renal and urinary disorders: Acute renal failure. Skin and subcutaneous tissue disorders: Pruritus, urticaria, alopecia, rash, photosensitivity reaction.
Patient Counseling Information
Women of childbearing potential must use proven birth control methods during therapy.
Monitoring Parameters
Rule out the secondary causes of hyperlipidaemia before treatment. Obtain serum lipids, cholesterol, and triglycerides periodically (especially in the 1st few months of treatment). Monitor LFTs after 3-6 months, then at least annually; CBC regularly during the 1st 12 months of treatment; fasting glucose, serum creatinine and CPK levels periodically. Closely monitor for signs and symptoms of myotoxicity and cholelithiasis.
Overdosage
Symptom: Rhabdomyolysis. Management: Symptomatic treatment. In case of rhabdomyolysis, discontinue treatment and carefully monitor renal function.
Drug Interactions
Increased incidence and severity of myopathy with HMG-CoA reductase inhibitors. May potentiate the anticoagulant effects of coumarin-type anticoagulants (e.g. warfarin). May improve glucose utilisation of antidiabetic agents (e.g. insulin, sulfonylureas). Absorption may be impaired with anion-exchange resins (e.g. colestyramine); separate the doses by at least 2 hours between intake. May result in renal impairment with immunosuppressants (particularly in organ transplant patients). May enhance adverse effects with MAOIs.
Action
Description: Mechanism of Action: Bezafibrate is a fibric acid-derived lipid regulating agent. Its mechanism of action is not definitely established; however, it may elevate very low-density lipoprotein (VLDL) catabolism by increasing lipoprotein and hepatic triglyceride lipase action, attenuate triglyceride biosynthesis by inhibiting acetyl-coenzyme A carboxylase, and reduce cholesterol biosynthesis by preventing 3-hydroxy-3-methylglutaryl-coenzyme A reductase. Pharmacokinetics: Absorption: Rapidly and almost completely absorbed from the gastrointestinal tract (conventional tab). Time to peak plasma concentration: 1-2 hours (conventional tab); approx 4 hours (prolonged-release/sustained-release tab). Distribution: Volume of distribution: 17 L. Plasma protein binding: 94-96%. Excretion: Via urine (95%; approx 50% as unchanged drug, 20% as glucuronides); faeces (3%). Elimination half-life: 1-2 hours (conventional tab); 2-4 hours (prolonged-release/sustained-release tab).
Chemical Structure
Bezafibrate Source: National Center for Biotechnology Information. PubChem Compound Summary for CID 39042, Bezafibrate. https://pubchem.ncbi.nlm.nih.gov/compound/Bezafibrate. Accessed Apr. 29, 2024.
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