Bezafibrate is a medication that belongs to a class of drugs known as fibrates. It's primarily used to lower lipid levels in the blood, particularly triglycerides and cholesterol. By doing so, it can help reduce the risk of cardiovascular events like heart attacks and strokes.

Bezafibrate works by activating a receptor called PPAR-alpha (peroxisome proliferator-activated receptor alpha), which regulates the expression of genes involved in lipid metabolism. This activation leads to increased breakdown of triglycerides and increased production of "good" HDL cholesterol.

Bezafibrate (Bezalip) is a fibrate drug that reduces the synthesis of triglycerides and cholesterol. It is used as an adjunct to diet and exercise for the treatment of Type IIa and IIb mixed hyperlipidemia. It regulates the lipids and apoprotein levels by reducing serum triglyceride levels, LDL cholesterol levels, apolipoprotein A and B levels, and increases HDL levels. It is used to treat high levels of triglycerides, especially who are at risk of developing complications from dyslipidemias.

Bezafibrate Dose in Adult

Bezafibrate Use in the treatment of Dyslipidemia:  

• Usually recommend taking 400 mg of bezafibrate by mouth once a day.
• It helps by lowering the levels of bad fats like triglycerides and cholesterol, which can reduce the risk of heart problems like heart attacks and strokes.

Bezafibrate Dose in Children

Bezafibrate Dose in the treatment of Dyslipidemia:

Children and Adolescents:

• The typical dosage is between 10 to 20 mg per kilogram of body weight per day, up to a maximum of 400 mg daily.

Note: It's important to note that there's limited experience with bezafibrate in this age group, so caution is advised. Additionally, the manufacturer recommends giving the sustained-release tablet whole, which might make dosing challenging based on the child's weight.

Pegnancy Risk Factor: X

• Bezafibrate has shown negative effects on animals during pregnancy in studies.
• So, it's not safe for pregnant women to use.
• If a woman becomes pregnant while using bezafibrate, she should stop taking it right away.
• Women who plan to get pregnant should stop taking bezafibrate a few months before trying to conceive, and those who could get pregnant should use reliable birth control while taking bezafibrate.

Bezafibrate use during breastfeeding:

• We're not sure if bezafibrate passes into breast milk. Because of this uncertainty, it's not recommended for breastfeeding women to use bezafibrate.

Bezafibrate dose in kidney disease:

• If patient creatinine clearance (CrCl) is equal to or more than 60 mL per minute, no change in the dosage of bezafibrate is needed.
• If patient CrCl is less than 60 mL per minute or your serum creatinine level is greater than 1.5 mg/dL (or more than 135 micromol/L), using bezafibrate is not recommended.
• Also, if patient on dialysis, using bezafibrate is not recommended either.

Bezafibrate Dose in Liver Disease:

• If you have liver problems, using bezafibrate is not recommended.

Frequency not defined.

• Central Nervous System:
  • Headache
  • Dizziness
  • Insomnia
  • Migraine
  • Pain
• Dermatologic:
  • Pruritus
  • Eczema
  • Erythema
  • Urticaria
• Gastrointestinal:
  • Gastritis
  • Flatulence
  • Dyspepsia
  • Constipation
  • Diarrhea
  • Epigastric Distress
  • Nausea
• Hematologic & Oncologic:
  • Anemia
• Hepatic:
  • Increased Serum ALT
  • Increased Serum AST
• Hypersensitivity:
  • Hypersensitivity Reaction
• Neuromuscular & Skeletal:
  • Increased Creatine Phosphokinase
• Respiratory:
  • Bronchitis
  • Pharyngitis

Contraindication to Bezafibrate Include:

• Bezafibrate should not be used if you have hypersensitivity to bezafibrate, fibrates, or any ingredient in the medication, if you've experienced photoallergic or phototoxic reactions to fibrates, or if you have liver problems like hepatic impairment or primary biliary cirrhosis.
• It's also not recommended if you have kidney issues (indicated by serum creatinine greater than 1.5 mg/dL, CrCl less than 60 mL/minute, or if you're undergoing dialysis), pre-existing gallbladder disease, or if you're taking HMG CoA reductase inhibitors (statins) and are prone to myopathy (muscle problems).
• Pregnant or breastfeeding individuals should also avoid bezafibrate.
• Additionally, it's not meant for treating type I hyperlipoproteinemia.

Warnings and Precautions

Hematologic effects

• When starting bezafibrate therapy, mild decreases in white blood cells (WBCs), platelets, and hemoglobin may occur, but these levels typically stabilize with continued use.

Hepatic effects

• Bezafibrate has the potential to harm the liver (hepatotoxicity), so if there's no significant improvement in symptoms within three months of starting therapy, it's advised to stop using it.
• People with a history of jaundice or liver disorders should use bezafibrate cautiously.
• If abnormal liver function test results are observed, treatment should be discontinued, as these abnormalities usually reverse once the medication is stopped.
• There's also a risk of developing gallstones (cholelithiasis) while on bezafibrate, so if diagnosed with gallstones, the medication should be stopped.

Myopathy and rhabdomyolysis

• Bezafibrate has been linked to rare cases of myositis or rhabdomyolysis, especially in individuals with kidney problems.
• It's crucial to monitor patients closely for any signs of muscle issues.
• Patients should be instructed to report any unexplained muscle pain, tenderness, weakness, or dark-colored urine.
• If signs of myotoxicity are present, such as elevated creatine phosphokinase (CPK) levels, therapy should be discontinued, especially if CPK levels are significantly elevated (10 times the upper limit of normal) or if myopathy is diagnosed.

Monitoring Parameters:

• Serum Lipids Evaluation:
  • Check levels of cholesterol and triglycerides regularly, especially during the initial months of treatment.
• Liver Function Tests (LFTs):
  • Perform LFTs 3-6 months after starting therapy, then at least once a year thereafter.
• Complete Blood Count (CBC):
  • Monitor CBC periodically during the first year of treatment.
• Fasting Glucose, Creatinine, and CPK:
  • Periodically assess fasting glucose levels, creatinine levels, and creatine phosphokinase (CPK) levels.

How to take Bezafibrate?

Administration Instructions for Bezafibrate Tablets

• Swallow Whole:
  • Do not crush or chew the tablet.
  • Take the tablet whole with enough fluid to help it go down.
• Timing with Meals:
  • Administer the tablet in the morning or evening.
  • Take it with or after meals.

Mechanism of action of Bezafibrate:

• The exact way bezafibrate works isn't entirely clear, but it likely boosts the breakdown of VLDL (very low-density lipoprotein) by increasing the activity of certain enzymes involved in breaking down fats in the liver.
• It also seems to reduce the production of triglycerides and cholesterol by blocking certain enzymes involved in their production, like acetylCoA carboxylase and 3-hydroxy-3-methylglutaryl-coenzyme A reductase.

Distribution:

• Volume of distribution is approximately 17 liters.

Protein Binding:

• Bezafibrate binds to proteins in the blood, with a binding range of 94% to 96%.

Half-life Elimination:

• The half-life of elimination ranges from 1 to 2 hours.

Time to Peak Serum Concentration:

• Bezafibrate reaches peak serum concentration in about 3 to 4 hours after administration.

Excretion:

• The primary route of excretion is through the urine, accounting for about 95% of elimination.
• A small portion is excreted in feces, approximately 3%.

International Brands of Bezafibrate:

• Bezalip SR
• JAMP-Bezafibrate SR
• PMS-Bezafibrate
• Befibrat
• Befizal
• Bezacur
• Bezafibrat
• Bezalip
• Bezalip PR
• Bezalip Rwetard
• Bezamil
• Bezastad
• Bezatol SR
• Cedur
• Clofibral
• Decrilip
• Difaterol
• Elpilip
• Etifibrat
• Eulip
• Lacromid
• Lipitrol
• Lipocin
• Lipocor
• Nimus
• Norlip
• Oralipin
• Oralipin Retard
• Polyzalip
• Regadrin B
• Zafibral
• Zafular

Bezafibrate brands in Pakistan: